TW200418452A - Benzofuran compounds, compositions and methods for treatment and prophylaxis of hepatitis C viral infections and associated diseases - Google Patents

Abstract

The present invention relates to novel benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.

Description

200418452 Description of the invention: [Technical field to which the invention belongs] The present invention relates to novel benzofuran derivatives and analogs, and compositions containing the same ingredients, and to the treatment or prevention of related viral infections and diseases Uses, especially those caused by hepatitis C virus and related diseases. [Prior art] Hepatitis C is a common infection that causes chronic hepatitis, cirrhosis, liver failure, and liver cancer. At least 85% of cases of hepatitis C virus (HCV) infection cause chronic hepatitis. It is the leading cause of liver transplantation in the United States and causes at least 10,000 deaths each year (Hepatology, 1997, 26 (Supplementary 1), 2S-10S). In the United States, physicians use interferon and interferon combined with ribavirin to treat liver cancer caused by HCV. These treatments have improved the serum enzyme response in some patients. The rest did not respond to treatment. For those who responded, sustained clinical improvement was seen in only a very small percentage of patients; most patients recovered after stopping. Therefore, the effectiveness of treatment for chronic hepatitis C varies widely, and the cure rate remains low. Moreover, treatment is often accompanied by considerable side effects. Clearly, we need new treatments and preventions for infections and diseases caused by hepatitis C virus (HCV). Hepatitis C virus is a member of the Flaviviridae family. The HCV genome is a single-stranded linear RNA with a forward strand (Hepatology, 1997, 26 (Supplementary Edition 1), 11S-14S). HCV exhibits a wide range of genetic heterogeneity, and at least 88828.doc 200418452 has identified 6 genotypes and more than 50 subtypes. After HCV infection, viral RNA is translated into polyproteins. This polyprotein of about 3,000 residues is subsequently digested into individual proteins by the host's peptidase and virus-encoded protein. The HCV genome encodes structural proteins (required for viral combinations) and non-structural proteins (required for replication). Some non-structural proteins include: NS2, NS3, NS4A, NS4B, NS5A, and NS5B (J. General Virology, 2000, 81, 163 1-1648). NS5B is an RNA-dependent RNA polymerase required for viral replication. In forward-strand RNA viruses such as HCV, RNA is the only genetic material. Since mammalian host cells generally lack RNA-dependent RNA polymerase activity, this forward-stranded RNA virus encodes a replicative polymerase (in the case of HCV, NS5B) necessary for the production of its own viral particle progeny. Thus, inhibition of NS5B activity provides an attractive target for HCV drug design. SUMMARY OF THE INVENTION According to one aspect, the present invention provides compounds and compositions for the treatment and prevention of viral infections and diseases related to viral infections in living hosts. The compounds of the invention have the following general formula:

among them:

Ri represents a group selected from the group consisting of hydrogen, an alkyl group, a prime element, and a cyano group, and R2 represents a group selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted 88828.doc 200418452 Oxy, hydroxy, cycloalkyl, cycloalkoxy, polyfluoroalkyl, polyfluoroalkoxy, iS element, amine, monoamine, diamine, cyano, substituted or unsubstituted A alkoxy group and a substituted or unsubstituted heterocyclic group, R3 represents a group selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, Alkenyl, halogen, hydroxy, polyfluoroalkyl, polyfluoroalkoxy, formamyl, carboxyl, alkylcarbonyl, alkoxycarbonyl, hydroxyalkylcarbonyl, amino, substituted or unsubstituted monoalkylamino, Dialkylamino, cyano, amido, alkoxyamido, substituted or unsubstituted heteroarylamino, ethylamino, amino, urea, lean amine, amino, Substituted amines, substituted or unsubstituted heterocyclic sulfosulfanyl, alkylthio, alkylthiosulfanyl, alkylsulfinyl, alkylsulfonic acid, and substituted or unsubstituted A group consisting of a cyclic group and -o (ch2) -c (= o) -r7, R4 represents a group selected from the group consisting of hydrogen, alkyl, halogen, and alkoxy, and R5 represents a group selected from Alkane (Ci-CO group and cycloalkyl group group, R6 represents a group selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl, R7 represents a group selected from the group consisting of a dialkylamino group, a substituted or unsubstituted arylamine group, a substituted or unsubstituted heteroarylamine group, and a substituted or unsubstituted aryl group, the Monoalkylamino substituents are one or more groups independently selected from the group consisting of cycloalkyl, hydroxyl, alkoxy, and substituted or unsubstituted heterocyclic groups. The arylamino substituent and the hetero The arylamine substituent is one or more groups independently selected from the group consisting of an alkyl group and an alkyloxy carboxyl group. 88828.doc -10- 200418452 The sulfonamide substituent is one or more groups independently selected from an alkenyl group and a cycloalkyl group. , Alkoxy, hydroxy, fluorene, polyfluoroalkyl, polyfluoroalkoxy, carboxyl, alkylcarbonyl, oxocarboxyl, fluorenamine, substituted or unsubstituted aryl groups, and A group of a group consisting of a substituted or unsubstituted heterocyclic group, the heterocyclic sulfonyl substituent is one or more groups independently selected from the group consisting of an alkoxy group and a hydroxyl group, and the alkyl group is substituted And the alkoxy substituent are independently selected from one or more of fluorenyl, amine, monoalkylamino, dialkylamino, alkoxy, cycloalkyl, hydroxy, alkyl, halogen, cyano, poly Fluorenyl, polyfluorinyloxy, ammonium, benzylamine, ammonium acid, carbonyl, oxocarbonyl, mirror group, benzo [1,3] dioxenyl, substituted or unsubstituted A group consisting of a substituted aryl group and a substituted or unsubstituted heterocyclic group, the heterocyclic group substituent being one or more independently selected from alkyl, amine, amido, and monoalkylamino , Cycloalkyl-alkylamino, dialkylamino, alkoxy, alkoxyalkyl, hydroxyl, hydroxyalkyl, cycloalkyl, carboxyl, carboxamidine, iS element, ialkyl, cyano, polyalkyl Fluoroalkyl, polyfluoroalkoxy, alkanesulfonyl, alkylcarbonyl, cycloalkylcarbonyl, alkoxycarbonyl, mercapto, oxy, substituted or unsubstituted aryl, aralkyl and substituted or unsubstituted A group of groups consisting of substituted heteroaryl groups, the heteroaryl substituents being one or more independently selected from alkyl, amine, alkoxy, alkoxyalkyl, hydroxyl, hydroxyalkyl, cycloalkyl , A carboxyl group, a carboxylic acid amine, a halogen, a polyfluoroalkyl group, a polyfluoroalkoxy group, an alkanesulfonyl group, a mercapto group, and an oxy group; the benzyloxy substituent is independently selected from one or more groups Alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, hydroxy, carboxyl, alkoxycarbonyl, i-prime, cyano 88828.doc -11-200418452, alkylsulfonyl and phenyl groups Group, the aryl substituent is one or more independently selected from the group consisting of alkyl, alkoxy, hydroxyl, halogen, polyfluoroalkyl, polyfluoroalkoxy, cyano, amine, monoalkylamino,- A group consisting of monoamine, amine, oxobutoxy, acid amine, donkey amine, renyl, hydrazone, carboxyl, oxonyl, weyl and heterocyclic groups And its pharmaceutically acceptable salts; the limitation is that the formula does not include compounds selected from the group consisting of: 5-methoxy-2-phenyl-benzo Acid-carboxylic acid and amine -3- several warp-2-phenyl - benzofuran-3-carboxylic acid A Amides. The present invention also relates to a person in the pharmaceutical group including an antiviral compound of formula I, a corresponding use method for treating and preventing infection caused by C virus of liver cancer, and an intermediate compound and a related method for preparing the antiviral compound described herein. [Embodiment] In one aspect, the invention provides a compound of formula I: 88828.doc

Ri, R2, R3, R4, 115 and ruler 6 are as defined above. In a second aspect, the invention provides a compound of the formula:

200418452 of which:

Ri represents a group selected from the group consisting of hydrogen, radical, halogen and cyano, and R2 represents a group selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, hydroxyl, cyclic Alkyl, cycloalkoxy, polyfluoroalkyl, polyfluoroalkoxy, halogen, amine, monoalkylamino, dialkylamino, cyano, substituted or unsubstituted benzyloxy and substituted Or a group of unsubstituted heterocyclic groups,

Rh represents a group selected from a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a fluorenyl group, a halogen, a hydroxy group, a polyfluoroalkyl group, a polyfluoroalkoxy group, a methylketyl group, a thiol group, Ranyl, oxocarbonyl, oxoalkyl, amine, substituted or unsubstituted monoalkylamino, dialkylamino, cyano, ethylamino, alkoxyamino, substituted or Unsubstituted heteroarylamino, ethylsulfonamido, ureido, carboxyamido, sulfa, substituted sulfa, substituted or unsubstituted heterocyclic sulfoamido, alkylthio, alkyl A group consisting of thionyl, alkylsulfonyl, alkylsulfonic acid, a substituted or unsubstituted heterocyclic group, and -0 (CH2) -C (= 0) -R7, JU stands for election A group selected from the group consisting of hydrogen, alkyl, halogen, and alkoxy, R5 represents a group selected from the group consisting of alkyl (C1-C 6) and cyclonyl, and R6 represents a group selected from substituted or R? Represents a group selected from the group consisting of an unsubstituted aryl group and a substituted or unsubstituted heteroaryl group, and R? Represents a group selected from a diamine group, a substituted or unsubstituted arylamine group, a substituted or unsubstituted Superseded A group consisting of an amine group and a substituted or unsubstituted aryl group, the monoalkylamino substituent is one or more independently selected from cycloalkyl, hydroxyl, B8828.doc -13- 200418452 alkoxy A group consisting of a substituted or unsubstituted heterocyclic group, the arylamino substituent and the heteroarylamino substituent are one or more independently selected from the group consisting of an alkyl group and an alkoxy group A group of groups, the continuous amine substituent is one or more independently selected from alkenyl, cycloalkyl, alkoxy, hydroxy, halogen, polyfluoroalkyl, polyfluoroalkoxy, carboxyl, alkylcarbonyl, and oxygen A radical of the group consisting of a phenyl group, a benzylamine, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocyclic group, the heterocyclic sulfonyl substituent is independently selected from one or more A group of alkoxy and hydroxy groups, the alkyl substituent and the alkoxy substituent are one or more independently selected from alkenyl, amine, monoalkylamino, dialkylamino, alkoxy Radical, cycloalkyl, mesityl, carboxyl, sulfonium, cyano, polyfluoroalkyl, polyfluoroalkoxy, sulfonamide, carboxysulfonamide, alkylsulfonyl Alkylcarbonyl, alkoxycarbonyl, sulfhydryl, benzo [1,3] dihydrocarbyl, substituted or unsubstituted aryl, and substituted or unsubstituted heterocyclic group, Heterocyclyl substituents are one or more independently selected from alkyl, amino, amido, monoalkylamino, cycloalkyl-alkylamino, dialkylamino, alkoxy, alkoxyalkyl, hydroxyl , Hydroxyalkyl, cycloalkyl, carboxyl, carboxamido, halogen, haloalkyl, cyano, polyfluoroalkyl, polyfluoroalkoxy, alkanesulfonyl, alkylcarbonyl, cycloalkylcarbonyl, alkoxycarbonyl , Fluorenyl, oxy, substituted or unsubstituted aryl, aralkyl and substituted or unsubstituted heteroaryl group, the heteroaryl substituent is one or more independent Selected from the group consisting of alkyl, amino, alkoxy, alkoxyalkyl, hydroxyl, hydroxyalkyl, cycloalkyl, carboxyl, carboxyamido, 88828.doc -14- 200418452 halogen, polyfluoroalkyl, polyfluorocarbon A group consisting of an oxy group, a succinyl group, a thiol group, and an oxy group, and the alkoxy substituent is one or more kinds independently selected from alkyl, alkoxy, polyfluoroalkyl, poly Alkoxy, hydroxyl, carboxyl, alkoxycarbonyl, functional group, cyano, fluorenyl, and phenyl groups; the aryl substituent is one or more independently selected from alkyl, alkoxy Base, hydroxyl, halogen, polyfluorenyl, polyfluorinated oxy, cyano, amine, monoamine, diamine, amine, oxyalkyl, st, si Base, carboxyl, alkanesulfonyl, alkylcarbonyl, alkoxycarbonyl, sulfo and heterocyclic groups, and pharmaceutically acceptable salts thereof. In a third aspect, the invention provides a compound of the formula:

Wherein: K represents a group selected from the group consisting of hydrogen, alkyl, halogen and cyano, and R2 represents a group selected from hydrogen, substituted or unsubstituted academic group, substituted or unsubstituted alkoxy group, Hydroxyl, cycloalkyl, cycloalkoxy, polyfluoroalkyl, polyfluoroalkoxy, iS element, amino, monoalkylamino, dialkylamino, cyano, substituted or unsubstituted benzyloxy A group consisting of a group and a substituted or unsubstituted heterocyclic group, R3 represents a group selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, alkenyl, Li, hydroxyl, polyfluoroalkyl, polyfluoroalkane 88828.doc -15-200418452 oxy, formamyl, carboxyl, alkylcarbonyl, alkoxycarbonyl, hydroxycarbonylcarbonyl, amino, substituted or unsubstituted Monoamine amine, di: fe amine, diyl, amine, alkoxy amine, substituted or unsubstituted heteroaryl amine, ethylammonium, ammonium, intestine, Donkey amines, amines, substituted ~ amine hydrazones, substituted or unsubstituted heterocyclic groups, thiol, thiosulfite, sulfamoyl, alkylsulfonic acid and substituted or An unsubstituted heterocyclic group and a group consisting of -0 (CH2) -C (= 0) -R7. FU represents a group selected from the group consisting of hydrogen, alkyl, halogen, and alkoxy. R5 represents a group selected from the group consisting of alkane (CrCd group and cycloalkyl group), R6a represents a group selected from the group consisting of substituted aryl group and substituted or unsubstituted heteroaryl group, R7 Represents a group selected from the group consisting of a dialkylamino group, a substituted or unsubstituted arylamine group, a substituted or unsubstituted heteroarylamine group, and a substituted or unsubstituted aryl group, the monomer Alkylamino substituents are one or more groups independently selected from the group consisting of cycloalkyl, hydroxyl, alkoxy and substituted or unsubstituted heterocyclic groups, the arylamino substituent and the heteroaryl The amine substituent is one or more groups independently selected from the group consisting of an alkyl group and an alkoxycarbonyl group, and the sulfonamide substituent is one or more groups independently selected from an alkenyl group, a cycloalkyl group, an alkyloxy group, a hydroxyl group, a functional group Element, polyfluoroalkyl, polyfluoroalkoxy, carboxyl, alkylcarbonyl, alkoxycarbonyl, carboxamido, substituted or unsubstituted aryl, and substituted or unselected A group of a heterocyclic group consisting of one or more substituents independently selected from the group consisting of an alkoxy group and an alkyl group, 88828.doc -16-200418452 the alkane group And one or more alkoxy substituents are independently selected from the group consisting of alkenyl, amine, monoalkylamino, dialkylamino, alkoxy, cycloalkyl, light, leptyl, ii, Cyano, polyfluorenyl, polyfluorinyloxy, fluorenamide, carboxamido, alkanesulfonyl, alkylcarbonyl, alkoxycarbonyl, fluorenyl, benzo [1,3] erakizaki, A group of a group consisting of a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group, wherein the heterocyclic group substituent is one or more independently selected from an alkyl group, an amine group, an amine group, Monoamine, cycloalkyl-cycloalkyl, dialkylamine, oxyalkyl, oxyalkyl, light, hydroxyalkyl, cycloalkyl, alkyl, ammonium, halogen, haloalkane Cyano, cyano, polyfluoroalkyl, polyfluoroalkoxy, alkanesulfonyl, alkylcarbonyl, cycloalkyl, alkoxymethyl, acid, oxy, substituted or unsubstituted aryl, Aralkyl and substituted A group of groups consisting of an unsubstituted heteroaryl group, the heteroaryl substituent is one or more independently selected from the group consisting of alkyl, amine, alkoxy, oxyalkyl, benzyl, technical, and cyclic Alkyl, alkyl, amine, halogen, polyfluoroalkyl, polyfluoroalkoxy, alkanesulfonyl, fluorenyl, and oxy; the benzyloxy substituent is one or A plurality of groups independently selected from the group consisting of alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, hydroxyl, carboxyl, alkoxycarbonyl, halogen, cyano, fluorenyl and phenyl The aryl substituent is one or more independently selected from the group consisting of alkyl, alkoxy, hydroxy, halogen, polyfluoroalkyl, polyfluoroalkoxy, cyano, amine, monoalkylamino, and dialkylamino. , Aminoalkyl, alkoxyalkoxy, amido, amidoalkyl, carboxyl, alkanesulfonyl, alkylcarbonyl, alkoxycarbonyl, mercapto and heterocyclic groups 88828.doc -17- 200418452 Group basis, and its pharmaceutically acceptable salts. In a fourth aspect, the invention provides a compound of the formula:

Where: Heart represents a group selected from the group consisting of hydrogen, methyl, and chloro, and R2 represents a group selected from hydrogen, methyl, ethyl, isopropyl, n-butyl, cyclopropyl, hydroxyl, and methylol. , Methoxymethyl, methoxy, trifluoromethoxy, difluoromethoxy, cyclopropylmethoxy, carboxymethoxy, cyanomethoxy, cyanomethylmethoxy, 1-hydroxyf -Cyclopropylmethoxy, amine formamyl methoxy, methylamine formamyl methoxy, diethylamine formamyl methoxy, (4-ethoxycarbonyl_phenylamine formamyl)- Methoxy, tert-butoxycarbonylmethoxy, ethoxy, 2-methoxyethoxy, 2-chloro-ethoxy, 2-carboxyethoxy, 2,2,2-trifluoro Ethoxy, Fluoro-phenyl) -ethoxy, 2- (4-fluoro-phenyl) -2-oxy-ethoxy, 2- (4-methoxy-phenyl) ) -2-oxy-ethoxy, propoxy, isopropoxy, oxy-propoxy, 2-¾yl-propoxy, 3- # imyl-propoxy, 2-quinyl 2-methyl_propoxy, 3-bromo-propoxy, 3-ethoxy_propoxy, butoxy, 2-hydroxy-2-methyl-butoxy, cyclopentyloxy , Fluorenyl propoxy, cyano, chloro, fluoro, methanesulfonate , Benzyloxy, 2-phenylfluorenyloxy, 2-difluoromethoxy-fluorenyloxy, 3-methoxy-fluorenyloxy, 3-methoxycarbonyl-benzyloxy, 3-carboxy-fluorenyl Oxy, 3-cyano-benzyloxy, 4-methoxy-fluorenyloxy, 'fluoro-benzyloxy, 4-cyano-benzyloxy, 4-methoxycarbonyl-benzyloxy, 4- Carboxy-benzyloxy, 4-carboxy 88828.doc -18- 200418452 -3-hydroxy-benzyloxy, 'methanesulfonyl-fluorenyloxy, 3,4-difluorobenzyloxy, 3,5 -Monomethoxy-benzyloxy, 2,2-dimethyl-4-oxy-4H-benzo [ι, 3] di, phen-5-ylmethoxy, 2,2-dimethyl -4-oxy-4H-benzo [1,3] difluorene-7-ylmethoxy, 2,2-dimethyl-4-oxy-4H-benzo [1,3] difluorene Cultylmethoxy, 3-chloromethyl_ [1,2,4] thiadiazol-5-yloxy, 5-chloro- [1,2,4] PSer 'Wow-3' " Ylmethoxy, 5-chloro- [1,2,3] xanthiene-4-ylmethoxy, 5-p-fluorenyl- [1,3,4] fluorenediazole-2- Methoxy, 5- (3,5-dimethyl-isofluoren-4-yl)-[1,2,4] fluoradiazol-3-ylmethoxy, 5- (cyclopropylmethyl- Amine)-[1,2,4] thiadiazol-3-ylmethoxy, 5-third-butyl- [1,2,4] pyridazol-3-ylmethoxy , 5- (4-methoxy-phenyl) _ [1,2,4] indion-3-ylmethoxy, 5-diethylamino- [1,2,4] thiadiazole -3-ylmethoxy, [1,3,4] thiadiazol-2-ylaminomethylmethylmethoxy, 3,5-dimethyl-isoxazol-4-yl, isoxazole- 3-ylmethoxy, 3,5-dimethyl-isoxazolylmethoxy, 5-methyl-isoazazol-3-ylmethoxy, pyrazol-2-ylmethoxy, thiazole 4-ylmethoxy, 2-methyl-pyrazol-4-ylmethoxy, 1-pyrazol_2-yl-ethoxy, pyrazolylaminomethylmethylmethoxy, (4,5 -Dimethyl-pyrazol-2-ylaminomethylmethyl) -methoxy, 4-chloro-1-methyl-1H-pyrazol-3-ylmethoxy, 2-pyrazole-1- Ethoxy-ethoxy, 2- (3,5-dimethyl-pyrazol-1-ylethoxy, ethoxyethoxycarbonyl, thiazolylmethoxy, 4-carboxy-pyrazol-2-yl Methoxy, 5-amino-4H- [1,2,4] tris (3-methylmethoxy), thien-2-yl, furan-2-yl, 2-morpholin-4-yl- Ethoxy, 3-hexahydropyridin-1-yl-propoxy, tetrahydro-furyl, 1-methyl-1H-tetrat-5-ylmethoxy, 1-methyl-1H-imidazole_ 2-ylmethoxy, 丨 _benzyl-1H_ Weijun-2-ylmethoxy, 3H-Weijun-4-ylmethoxy, leaf (: Bent-4-yl-methoxy, 6-bromomethyl4pyridin-2-ylmethoxy and 2- (4-cyano-hexahydropyridin-1-yl)-88828.doc -19- 200418452 a group of groups consisting of ethoxy groups, R3 represents a group selected from the group consisting of gas, methyl, methoxy, mesityl, mesityl; μ borrowed group_ethyl, 1-hydroxy-2-methyl-propyl Methyl group, methyl group, methyl group, methyl group, methyl group, urea group, vinyl group, bromo group, chloro group, cyano group, ethyl group, 2-hydroxy group. Amine, carboxylic acid amine, amine, methylamino, dimethylamino, ethylamino, diethylamino, isopropylamino, tertiary butylamino, ethyl-methyl Amino-amino, 2-methoxy-ethylamino, cyclopropylmethyl-amino, 2,3-dihydroxy-propylamino, methylamino-ethyl, dimethyl Aminomethyl, 1-amino-1-methyl_ethyl, 2-amino-1-hydroxy-1-methyl-ethyl, ethylamino, 1-ethylamino- 丨 _ Methyl-ethyl, (2-methoxy-ethyl) -methyl-amino, ethyl_ (2-methoxy_ethylfluorenyl) _amino, 3-chloro-propane-1- Sulfonylamino, methanesulfonylamino, ethyl-methanesulfonylamino Group, isopropyl-methanesulfonyl-amino group, isobutyl-methanesulfonyl-amino group, cyclobutyl-methanesulfonyl-amino group, cyclopentyl-methanesulfonyl-amino group, Cyclopropylmethyl-methanesulfonyl-amino group, (2-hydroxy-ethyl) -methanesulfonyl-amino group, (2-hydroxy-propyl) -methanesulfonyl-amino group, (2 -Fluoro-ethyl) _methanesulfonyl-amino, 2- (4-fluoro-phenyl) -2-hydroxy-ethyl] -methanesulfonyl-amino, (1-hydroxymethyl -Cyclopropylmethyl) -methanesulfonyl-amino group, (4-carboxy_benzyl) -methanesulfonyl-amino group, allyl-methanesulfonyl-amino group, ethenyl-methane Continued S-basic-amino, benzyl-methylsulfanyl-amino, carboxymethyl-methanesulfanyl-amino, methane-sulfanylamino-methyl, 1-methanesulfanylamino -1 -methyl-ethyl, methanesulfonyl-methyl-amino, 1- (methanesulfonyl-methyl-amino) -ethyl, methylsulfanyl-propyl-amino, methyl Achievement group_ (2_methoxy-ethyl) -amino group, methanesulfonyl group ((2,2,2_trifluoro-ethylamino group), 88828.doc -20- 200418452 -(2-oxy-propyl) _amino, methane Fluorenyl_ (2_trifluoromethoxy-ethyl) -amino group, methyl pentyl group- (4-methoxy-methyl group) _amino group, methylsulfonyl sulfonyl group- (4-methyl Oxycarbonyl-benzyl) _amino, methanesulfonyl-methoxymethyl-amine, methanesulfonyl-methylaminomethylmethyl-amino, (methanesulfonyl-methyl-amine ) -Methyl, amine sulfonyl, methylamine sulfonyl, dimethylamine sulfonyl, ethylamine sulfonyl, cyclopropylaminesulfonyl, cyclobutylaminesulfonyl, 3 -Methylfe% S-base-based, winter-based, 4-methylsulfonyl-phenyl, unyloxy, 1H-P than p--4-yl, 2H-p than p--3-yl, 1- Methyl-iH-p than Jun-3-yl, 2-methyl-2H-pyrazol-3-yl, 5-methyl-1H-pyrazol-4-yl, 5-methyl-2H-pyrazole -3-yl, 1,5-dimethyl-1H-pyrazol-3-yl, 2,5-dimethyl-2H-pyrazol-3-yl, 2,5-dimethyl-2H-methyl Fluoren-3-ylamino, 3,5-dimethyl-1H-P than jun-4-yl, 1,3,5-trimethyl-1H-p than fluoren-4-yl, isocrazy- 3-yl, 5-methyl-isotetra-3-yl, 3-cyclopropyl-isoxazol-5-yl, 5-cyclopropyl-isoxazol-3-yl, 3,5-di Methyl-isonizol-4-yl, 3,5-dimethyl-isopurazol-4-ylamino, 5-methoxymethyl -Isoxazol-3-yl, 5-ethoxymethyl-isisonazol-3-yl, 5-isopropoxymethyl-isoxazol-3-yl, 5-hydroxymethyl-isoamidine Azol-3-yl, 4- (2-hydroxy-ethyl) -isopurazol-3-yl, 3-methoxymethyl-5-methyl-isoxazol-4-yl, 5-methoxy Methylmethyl-3-methyl-isopropyl-4-yl, 5-cyclopropyl-3-methoxymethyl-isopropyl-4-yl, 3-cyclopropyl-5-methoxy Methylmethyl-isocrazy-4-yl, (3,5-dimethyl-isoxazol-4-ylmethyl) -methanesulfonyl-amino, 3-methoxymethyl-isofluorenyl Azol-5-yl, 3-methyl-isoxazol-5-yl, methanesulfonyl- (5-methyl-isoxazol-3-ylmethyl) -amino, thiazol-2-yl, Thiazol-5-yl, methanesulfonyl-thiazol-2-ylmethyl-amine, methanesulfonyl-thiazol-4-ylmethyl-amine, methanesulfonyl- (2-methyl-thiazole) 4-ylmethyl) -amino group, (4-carboxy-thiazol-2-ylmethyl)-88828.doc -21-200418452 formamyl-amino group, (4-ethoxycarbonyl ^ selazole_2 _Ylmethyl) _methanesulfonyl-amino, pyridin-3-yl, pyridin-'yl, pyridin-4-ylamino, 6_fluoroyl_pyridin-3-yl, methanesulfonyl_pyridine _4_methylmethyl_amino, (6_bromo Methyl_pyridin-2-ylmethyl) _methanesulfonyl_amino, pyrrolidin_1_yl, pyrrolidinyl, pyrrolidinsulfonyl, 3-hydroxy-pyrrolidin-1-yl, 3- Hydroxy-pyrrolidin-1-sulfonyl, 5-oxy_pyrrolidin_3-yl, ^ ethylsulfonyl_pyrrolidin-2-yl, 1-ethynyl-pyrrolidin-3-yl, 丨 ― Carbaminyl_pyrrolidine_2_yl, 丨 Methylcarbaminyl-pyrrolidine_2_yl, each methylaminomethaneoxy-pyrrolidyl group, 1-cyclopropanecarbonyl-pyrrolidine -2-yl, 1-methanesulfonyl_pyrrolidinyl, 1-methylsulfonium δM-yl-ehikolide-3 -yl, 3-amino-u-bihalidone_ 1 -Pyrrolidin-1-yl, 1Η_pyrrole_2_yl, m_pyridine_3_ are 3-cyano-4-hydroxy-2-oxy-2,5-dihydro-pyrrole-1-yl Methyl and furan are sulfan-3-yl, (cran-3-ylmethyl) -amino, tetrahydro-cranyl, (hydro-sulfan-2-ylmethyl) -amine, [ 1,3,4] slogans two-mouthed 2-yl, [1, 2, 4], azole-3-yl, 5-methyl- [U〆] pyridazol-3-yl, 5-methyl -啰 ~~ -2-yl, 5-trifluoromethyl- [1,2,4] $ dijun-3_yl, morpholin-4-yl, ___ world 2,6, monomethyl-? Fu Lin -4 -Base, 2-Morpho Phenyl-4 -yl-ethylamino, morphone S! Yl, methanesulfonyl- (2-morpholine_4-yl-ethyl) -amino, hardyl, lin-4_yl , Thiomorpholin_4_sulfonyl, 1_oxy_thiomorpholin ,,,, ^ earth, 1,1, monooxy-1λ6-isop graveyard sitting 2-yl, 2 -Oxyzaki-yodo-5-yl, 5-triazol ^ τ, 2, oxy-indazol-5-yl, humidaz-5-yl, 1-imidazol-4-yl, n Wenji, 2,5-dioxy-imidazolidin-4-yl, 4-methyl-2,5-dioxy-imidazolium, stilbene%, 4, yl, pyrimidin-5-yl, 2, 5-dimethyl-2Η- [1,2,4] triazol-3-yl, 9, -2Η- [1,2,4] triazol-3-yl, 4Η_ [1,2,4] tris Azol-3-yl, 5-methylformyl 4 2H. 88828.doc -22- 200418452 [1,2,4] triazol-3-yl, 1H-tetrazol-5-yl, 1-methyl-1H -Tetrazol-5-ylmethoxy, methanesulfonyl- (1-methyl-1H-tetrazol-5-ylmethyl) -amino, hexahydropyridin-1-yl, 4-fluoro -Hexahydrop-pyridian-1-yl, 4,4-difluoro-hexahydroeodo-1-yl, 3-pyridyl-hexahydrou-pyridine_1-yl, 4-light-based ? Biyodo-1-yl, 4-¾yl-hexahydropyridine-1-continyl, 4-aminomethylpyridyl-hexahydropyridine-1-yl, 4-methyl-hexahydropyridine-1- And 5-chloro- [1,2,4] pyrimidazol-3-ylmethyl, R4 represents a group selected from the group consisting of hydrogen and methyl,

Rs represents a group selected from the group consisting of methyl, ethyl, isopropyl, and cyclopropyl, and R6 represents a group selected from phenyl, 4-methyl-phenyl, 4-ethyl-phenyl, 4-methoxy-phenyl, 4-hydroxy-phenyl, 4-bromo-phenyl, 2-chloro-phenyl, 2-fluoro-phenyl, 4-fluoro-phenyl, 2, 4-difluoro-phenyl, 3,4-difluoro-phenyl, 4-bromo-3-fluoro-phenyl, 3-chloro-4-fluoro-phenyl, 4-chloro 3-fluoro-phenyl, 2,4,5-trifluoro-phenyl, 3-fluoro-4-fluorenyl-phenyl, 4-fluoro-3-methyl-phenyl, 4- Fluoro-3-hydroxy-phenyl, 2-ethoxy-4-fluoro-phenyl, 3-trifluoromethyl-phenyl, 4-trifluoromethyl-phenyl, 4-cyano-benzene Group, 4-amino group, private group, 4- (ethosylamino-methyl) _phenyl group, 4-morpholinol-phenyl group, 4-pyrrolidin-1-yl-phenyl group, furan- 2-yl, furan_3-yl, 3-methyl-furan_2_yl, thien-2-yl, 5-chloro-pyrimin-2-yl, pyridin-4-yl and pyridin-3-yl, The limitation is that the formula does not include compounds selected from the group consisting of 5methoxy-2-phenyl-benzofuran-3-carboxylic acid formamide and 5-hydroxyphenyl-benzofuran. Formamidine carboxylate . Preferred compounds of formula I include compounds in which 1 is _0 (^ 3 or _〇 (CH) (CH3) 2, -CHWH3 and 88.doc.-23- 200418452. Other preferred compounds of formula i include wherein Preferred aspects of the invention include compounds of formula I in which the aryl group represented by R6 is a substituted phenyl group, the phenyl substituent being one or more independently selected from the group consisting of fluoro, chloro, molyl, A group of methoxy and cyano groups. Another preferred aspect of the invention includes compounds of formula Ic:

Among them, Aik is a unitary radical and R !, R3, and R4 are as defined in the reference of Formula I above, and a pharmaceutically acceptable salt thereof. Preferred compounds of the present invention include 2- (4-fluoro-phenylmethoxy-6-morpholinol-benzofurancarboxylic acid formamidine, 2- (4-fluoro-phenyl) -5_ Isopropoxy-6-morpholin-4-yl-benzofuran-3-methanoic acid formamidine, 2- (4-fluoroyl-benzyl) -5-isopropoxymethanesulfonylamine -Benzofuran_3_carboxylic acid formamide, 2- (4 • fluoro-phenyl) -5-isopropoxy-6-[(2-methoxy-ethyl) _methyl_ Amine] -benzofuran-3-carboxylic acid formamidine, 5-methoxy ('fluoro group_phenyl) -6-morpholin-4-yl-benzofuran-3_carboxylic acid formamidine Amine and 2- (4-fluoro-phenyl) -6-[(crean-3-ylmethyl) -amino] isopropoxy-benzofurancarboxylic acid formamide, 6- (3, 5-dimethyl-isoxazol-4-yl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine, 5-cyclopropyl -2- (4-fluoro-phenyl) -6-[(2-hydroxy · ethyl) _methanesulfonyl-amino] _benzofuran_3_carboxylic acid carboxylic acid amine, 6_ (3,5 -Dimethyl-isoxazol | yl) _2- (4-fluoro group · phenyl) _5- (3 group-propoxy) _benzofuran-3-carboxylic acid formamidine, and its pharmacy Acceptable salt 88828.doc -24- 200418452 " acid The present invention provides a pharmaceutical composition comprising one or more compounds of formula i, which are " accessible carrier vehicles. Preferred pharmaceutical compositions include one or more of the compounds listed in Table 1 below, and pharmaceutically acceptable salts thereof. Incorporate a pharmaceutically acceptable carrier medium. According to yet another aspect, the present invention provides a live host, for example, a method of preventing or treating human < Fulet < " >, preventing or treating hepatitis C infection and diseases associated with such infection. , Including administering to a host susceptible to or suffering from the infection, a therapeutically effective amount of a compound of formula I. Another aspect of the present invention provides for the prevention or treatment of hepatitis C infection and the treatment of living monks, including human mammals, for example. Diseases related to such infections. This method includes administering to a host susceptible to or suffering from the infection, a therapeutically effective amount selected from 5-methoxy-2_phenyl_benzofuran_3_carboxy Compounds of the group consisting of formamidine acid and formamidine 5-hydroxy-2-phenyl-benzofurancarboxylate. The compounds of the above formula I, their isomers and pharmaceutically acceptable salts exhibit disease resistance. Activity. The present invention It is particularly effective against hepatitis C virus and can be used to prevent and / or treat host-associated infections and diseases with this virus. In vitro studies (cell-based and biochemical) performed have shown the compounds described herein as antiviral agents For example, human liver-derived cell lines containing HCV replicons are used to evaluate the antiviral activity of representative compounds. Furthermore, the antiviral activity is determined by RNA synthesis enzyme assays for the inhibitory activity of the compounds against viral RdRp. As used herein, the term "compounds of the invention" means a collection of compounds of formula I, their pharmaceutically acceptable salts and mixtures thereof. The compounds of the present invention 88828.doc -25-200418452 are identified herein by their chemical structure and / or chemical name. When referring to = chemical structure and chemical name, and t chemical name conflicts with chemical structure ', its chemical structure determines its identity. When used in this text, the term "carbon radical" refers to a linear or branched aliphatic aliphatic hydrocarbon group of up to 10 carbon atoms. The preferred is up to 6 carbon atoms, and the more preferred is " Carbon atom. Similarly, "fluorenyl, or a combination of any variation thereof, is used to name substituents such as alkoxy (4-alkyl), cycloalkyl, and square (-alkyl-aryl) ), Monofluorenylamino group (_NH_alkyl), amine alkyl group (f-NH2), alkylthio (_s_alkyl), alkylthiothio (_s (= 〇) _alkyl), alkyl Sequential group (-SWW group), alkanoic acid (_〇_s (〇) 2- alkynyl), or the like 'is also aimed at straight or branched chain lipids up to 1 () carbon atoms The aromatic hydrocarbon group is preferably 1 to 6 carbon atoms, and more preferably 1 carbon atom. In addition, in the structural formula of this article, "alk" represents a radical group, and if its bivalence is displayed, "xian" means ^ Ying Zhiyan group. In addition, "fluorene group (the term" w "has ^ carbon atoms Alkyl group. As used herein, the term "alkenyl" refers to an aliphatic hydrocarbon group containing 2 to 7 atomic hindering atoms containing at least one straight or branched double bond. The Λ-type alkenyl moiety may exist as E or Z Configurations, the compounds of the present invention include two configurations. The term "block group" as used herein refers to an aliphatic hydrocarbon group containing at least one straight or branched two to three carbon bond of 2-7 carbon atoms.

The term "phenyl" as used herein refers to the s group. The term "substituted < phenyl" refers to a phenyl substituted with the indicated substituent. As used herein, the term "aryl," when used as such, or, is 88828.doc -26- 200418452 combined forms such as "aralkyl," when used, for inclusions having 6-10 carbon atoms But not limited to the aromatic carbocyclyl group of 'phenyl and fluorenyl. The term `` 4aryl '', as used herein, means a 5- or 6-ring aromatic ring having at least one counter atom and one or more oxygen, nitrogen or sulfur atoms on the ring, such as e.g. p-secenyl, p-pyridyl, e-pyridyl, fluorenyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, 1,2,4-pyridine Diazolyl, ι, 2,3-triazolyl, ι, 2,4 · triazolyl, 1-3-oxadiasulfate, thiadiazolyl, tetrazolyl, and the like. As used herein, the term "cycloalkyl," refers to non-aromatic carbocyclic groups of 3-7 carbon atoms, such as, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and the like. When used As used herein, the term "cycloalkoxy" refers to a group or substituent of the formula -cycloalkyl, wherein the cycloalkyl is as defined above. As used herein, the term "polyfluoroalkyl," refers to a group or substituent having one or more fluoro substituents, and includes perfluoroalkyl. Examples include trimethyl and trifluoroethyl As used herein, the term "polyfluoroalkoxy" refers to fluorenyloxy having-or more fluoro substituents, and includes all gas alkoxy. Examples include trifluoromethoxy and trifluoromethoxy. Fluoroethoxy. As used herein, the term "heterocyclyl" refers to an aromatic or non-aromatic group having at least one carbon atom and one to four heteroatoms independently selected from oxygen, nitrogen, or sulfur atoms on its ring. Family ring base. The attachment point of the heterocyclic group can be via a carbon atom or via a heteroatom. Heterocyclyl is preferably 3 carbon atoms, and more preferably 4, 5, or 6 rings. Examples of heterocyclic groups include trimethylenepentaminyl, stilbene, tetrahydrosuccinyl, "sedenyl", "synthetic radicals, materials, genomics 88828.doc -27- 200418452, hexahydrogen ratio Dianji, hexahydropyridine, yoke bond, No. Junji, Yintu Dianji, far α sitting group, mitoyl, mibiting pding group, said. Sorryl, 2-P-pyridyl, isoxazolyl, isoxazolyl, morpholinyl, thiomorpholinyl, 1,2,3-humdiazolyl, 1,3,4-fluorene Diazolyl, 1,2,4-oxadiazolyl, 1,2,3-triazolyl, 1,2,4-tri-alpha phenyl, 1-3 -oxosulfate, ρ-dithiol , Tetrayl and its analogs. As used herein, the term "amido" refers to a group or substituent of the formula NR'fC (= 0) where R "and Rm independently represent hydrogen, alkyl, or cycloalkyl. Similarly, The term "amidoalkyl" as used herein refers to the formula -alkyl-NR "C (= 0) Rm group or substituent, where R" and Rf "are as previously defined." Alkoxy " The term "amino", as used herein, refers to a group or substituent of the formula -NR'fC (= 0) -alkyl-alkoxy, wherein R ", alkyl and alkoxy are as previously defined . The term "carboxamide", as used herein, refers to a group or substituent of the formula C (= 0) -NR "R'n, where Rn and R '" are as previously defined. "Ureido" The term, when used herein, refers to a group or substituent of the formula -NR'C (= 0) -NRnRm, where 11 "and 11 '" are as previously defined, and Rf represents hydrogen or alkyl. The term "sulfonamide", as used herein, refers to a group or substituent of the formula -S02NRnR '" or NRn-S02Rm, where Rn and R'n are as previously defined. The term substituted sulfonamide, as used herein, refers to a group or substituent of the formula -N (alkyl) -S02 (alkyl) in which at least one alkyl group is further substituted with the indicated substituent. The term "acetamidinesulfonylamino", as used herein, is directed to the formula -N (S02-R " HC (= 0) CH3), where R "is as previously defined. 88828.doc -28- 200418452 The term "heterocyclic sulfonyl", as used herein, refers to a group or substituent of the formula -so2-het, in which HET is a heterocyclic group as described above. Preferred heterocyclic groups include t Dydonyl, hexahydrop-doped Si, morpholinyl, stilbene blue, and thiomorphoyl sulfonic acid. When used herein, the term "arylamino" refers to formula -N (Rf ')-an aryl group or substituent, wherein R "and aryl are as previously defined. A substituted arylamine group, as used herein, is directed to a substituent in which the aryl group is further indicated. Substituted arylamino or arylamine substituents. The term "heteroarylamino", as used herein, refers to a group or substituent of the formula -N (R ")-heteroaryl, where R '' and hetero Aryl is as previously defined. A substituted heteroarylamino group, when used herein, is directed to a heteroarylamino group in which the heteroaryl group is further substituted with a indicated substituent or Aromatic amine substituents. A substituted monoalkylamino group, as used herein, is directed to a monoalkylamino group or substituent as defined above, wherein the alkyl group is further substituted with the indicated substituent. Similarly, The term "cycloalkyl-alkylamino", as used herein, refers to a monoalkylamine group or substituent as defined above, wherein the alkyl group is further substituted with a cycloalkyl group as described above. When used herein, it refers to a group or substituent of the formula -C (= 0) OH. The term "carbonyl", whether used alone or in conjunction with other terms, such as "alkoxycarbonyl", means -C (= 0)-. The term "alkylcarbonyl", as used herein, refers to a group or substituent of an alkyl group of the formula -C (= 0); and includes, for example, methylcarbonyl, ethylcarbonyl, propylcarbonyl, butyl Carbonyl and pentylcarbonyl. Similarly, the term "cycloalkylcarbonyl", when 88828.doc -29-200418452 is used herein, refers to a group or substituent of the formula -c (= o) -cycloalkyl. The term "burning carboxyl", as used herein, refers to a compound of formula -C (= 0) -Cyno-OH. "Alkane The term "carbonyl," as used herein, refers to a group or substituent of the formula -C (= 0) -0-alkyl; and includes, for example, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, butoxycarbonyl, and pentyl. Oxycarbonyl. The term "formamyl", when used herein, refers to a group or substituent of the formula -C (= 0) -H. The term "thio", when used herein, refers to the formula -SH. Group or substituent. The term "benzyloxy", as used herein, refers to a group or substituent of the formula -OCH2-phenyl. A substituted benzyloxy is a substituent in which the phenyl is further indicated. Substituted benzyloxy. A substituted monoalkylamine, as used herein, is directed to a group or substituent of the formula -NH-alkyl; wherein the alkyl group is further substituted with the indicated substituent. The term "hexane", as used herein, is directed to a mixture of linear and branched hexane hydrocarbon solvents, where the solvent mixture mostly contains n-Hexanol and a small amount of branched hexane. The term "halogen", as used herein, refers to a group or substituent selected from the group consisting of chlorine, bromine, iodine and fluorine. The term "haloalkyl", as used herein, refers to an alkyl group, as defined above, further substituted with a prime as defined above. The term "psig" refers to gauge pressure in pounds per square inch. The term "HPLC", as used herein, refers to the HPLC chromatography 88828.doc -30- 200418452 analysis. The term "TLC" when used in this article "exhibits each other clearly, and makes use of the arm + analysis method. The structure type, the term, when used in this article, the shape of the atomic movement,-士 夕 # For the reason that y becomes one or more isomers. The term "amino group" when used herein is directed to the .2-group. The term "benzo" is called "two-well-based".

Radical or substituent of X. = Host, the term ', when used herein, is directed against living and capable of π sunny fire C virus "virus-infected organisms, such as mammals, including class 0 compounds of the present invention and their isoforms and their pharmaceutically acceptable Accepted salts, f can be used for the treatment and prevention of viral infections, especially hepatitis C virus, when combined with or other diseases, or other biologically active substances; including but not limited to the composition selected from the following Group of people: interferon, polyethylene glycol interferon, rabavirin, protease inhibitors, polymerase inhibitors, small interfering RNA compounds, antisense compounds, nucleotide analogs, nucleosides Analogs, immunoglobulins, immunomodulators, hepatoprotective agents, anti-inflammatory agents, antibiotics, antivirals and anti-infective compounds. Such combination therapies also include the simultaneous or sequential provision of a compound of the invention with other pharmaceutical agents or extenders, such as aCyclvir, famicyclovir, Fagancyclovir Vaigancycivir and related compounds' rebavirin and related compounds, amantadine and related compounds, different 88828.doc • 31-200418452 interferons such as, for example, Trichomon interferon_α, interferon_β, Interferon substances, as well as interfering with Kuai Fu & 丄 τ and its members. In addition, for example, when two rhodium is combined from interferon and two interferon and interferon, a compound can be invented as a combination of another ice, evening, and earthworm, which is a combination of another < evening sun combined therapy . = The combined silk can be sequential, that is, the treatment of one agent first, the two agents (for example, the individual treatment includes a different one of the invention or /, the Chinese medicine treatment includes the compound of the invention, and the other- (Including one or a kind of biologically active muscarinic agent), or it can be treated with two agents at the same time (same: ground) < clothes order therapy may be reasonable after the first treatment is completed and the second therapy may be started in time. Treatment with two agents at the same time4 can be the same daily dose or separate doses. The dosage of two concurrent or sequential combination therapies will depend on the absorption, distribution, metabolism: and excretion rate of the components of the combination therapy, and other factors known to those skilled in the art. The dose value also depends on the severity of the condition to be reduced. It should be further understood that, for any particular patient, the specific dose therapy, and progress can be adjusted at any time according to the patient (needs and professional judgment of the person who administers or supervises the combined therapy. Specific implementation examples in step ^ The compounds of the present invention can be used in combination therapy with other hcv polymerase inhibitors in the treatment of human HCV.

In a further specific embodiment, the compound of the present invention can be used in combination with other HCV life cycle inhibitors in a combination therapy mode for treating human HCV.

Examples include, for example, inhibitors of HCV cell attachment or viral entry, HCV translation, HCV RNA transcription or replication, HCV maturation, combination or virus release, or inhibitors of HCV enzyme activity, such as HCV nucleotide transferase , Helicase, protease or polymerase. 88828.doc -32- 200418452 As long as the combination does not diminish the antiviral activity of a compound of the group of the invention, or the antiviral activity of a pharmaceutical composition thereof, the combination therapy of the invention is intended to include any compound of the group of the invention and Chemically compatible combination of other compounds of the group of the invention. The term "interferon-α", as used herein, means a family of highly specific species-specific proteins that inhibit virus replication and cell proliferation and regulate the immune response. Typical suitable interferons include, but are not limited to, recombinant interferon a-2b such as INTRON-A INTERFERON purchased from Schering Corporation, Kenilworth, NJ; recombinant interferon a-2a such as purchased from 11 (^ 111 & 11- 1 ^ foot 〇〇1 ^, &gt; 1111: 16 ah, 1 ^ of 11 (^ 61 &gt; 〇11 interferon; recombinant interferon a-2c, such as purchased from Boehringer Ingelheim Pharmaceutical, Inc., Ridgefield, Conn. BEROFOR ALPHA 2 INTERFERON; interferon alpha-nl, such as a mixture of purified natural alpha interferon purchased from Sumitomo, Japan by SUMIFERON; or Wellferon interferon a- purchased from Glaxo-Wellcome Ltd., London, Great Britain nl (INS); or a consensus "interferon such as described in U.S. Patent Nos. 4,897,471 and 4,695,623 (the contents of which are incorporated herein by reference in their entirety, and in particular Examples 7, 8 or 9); and purchased from Amgen, Inc., Newbury Park, Calif., A specific product, or interferon α-η3, manufactured by Interferon Sciences and purchased from Purdue Frederick Co., Norwalk, Conn., A natural interferon mixture with the trademark ALFERON. Use interferon or a-2b Better. Because interferon a-2b is among all the interferons and is the world's largest accredited interferon for the treatment of chronic hepatitis C infection. There are instructions for the manufacture of interferon a-2b in US Patent 4,503,901. 88828. doc -33-200418452 '' Polyglycolized interferon, the term, when used herein, means a polyethylene glycol-modified conjugate of interferon, interferon and interferon a-2b Better. The preferred conjugate of polyethylene glycol_interferon a_2b is PEG.sub.12000.-f ^ a-2b〇uPEG.sub. 12000-IFN aji] 1η When used herein, it means co- The conjugate is prepared, for example, according to the method of international application number WO95 / 13G9G, and contains interferon α · 2 linked by urea and vinegar between _2b amine groups, and the average molecular weight of polyethylene glycol is 12 Å. The compounds described can also infect or resolve viral infections in cell, tissue or organ culture and other in vitro applications. For example, if the compounds of the present invention are included as supplements for growth culture fluids of cells or tissue cultures, and cells or tissues Cultivation becomes public, and ... I is not the first anti-virus infection by the virus or culture of; loss of dye. The above-mentioned compounds can also be used to reduce cultures or other biological materials that are affected by viruses, bacteria, heart, or blood, after any number of treatment conditions determined by skilled technicians during the treatment period. (Eg blood). The compound of the present invention can be used with inorganic and organic acids such as hydrochloro-L lactate and hydrazone, acetic acid, lactic acid or the like; /, ^ /, such as sodium or potassium lice, hexapyridine, ammonium hydroxide, Or its analogs without _ flying dagger salt. The medicine of the compound of formula I can be used as a formula, to form a useful method, according to the person familiar with the art in ethanol, and to add about U equivalent days to make lice lice sodium or wind potassium, Allow shape ". Examples of pharmaceutically acceptable salts are listed in Table 3 below. The isomers of the compounds of the present invention are heterocyclic, which may include <%% substituents and different isomers. Let us also draw the chemical structure and therefore the compounds of the present invention 88828.doc -34- 200418452, also covering all these corresponding possible tautomeric forms. Such tautomers may, in some instances, be resolved into individual compounds by methods known to those skilled in the art. The compounds of the present invention can be used to treat living hosts, such as human mammalian HCV. When administered to a living host, the compound can be used alone or as a pharmaceutical composition. A pharmaceutical composition comprising a compound of the present invention, whether alone or in combination with each other, to provide a treatment against hepatitis C infection. The antiviral pharmaceutical composition of the present invention comprises, as an active ingredient, one or more compounds of the above formula I, combined with a pharmaceutically acceptable carrier vehicle or auxiliary agent. The composition can be prepared in different administration forms including lozenges, film-coated tablets, pills, or sugar-coated pills, or can be filled into a suitable container such as a capsule, or in the case of a suspension, filled into a bottle. As used herein, a "pharmaceutically acceptable carrier medium" may include any and all solvents, diluents, or other liquid carriers, dispersions or suspension aids, and surfactants, as long as they are suitable for the particular dosage form required. , Isotonic agents, thickening or emulsifying agents, preservatives, solid adhesives, lubricants and the like. Remington's Pharmaceutical Sciences, 20th edition, A. R. Gennaro (William &amp; Wilkins, Baltimore, MD, 2000) discloses different carriers for formulating pharmaceutical compositions and their known preparation techniques. To date, all traditional carrier media have been used except for the production of any unnecessary biological effects, or any incompatible with the antiviral compounds of the present invention in a destructive manner with any other component of the pharmaceutical composition Covered by the scope of the present invention. In the pharmaceutical composition of the present invention, based on the total weight of the composition, the active 88828.doc -35-200418452 is present in an amount by weight that may be at least 0.5%, and usually not more than 90%, including any Carrier vehicle and / or adjuvant. Preferably, the proportion of the active agent varies with the weight of the composition, and it varies from 5 to 50% of the composition. The composition can be formulated using organic or inorganic solid or liquid carrier vehicles suitable for parenteral or parenteral administration. Gelatin, lactose, starch, magnesium stearate, talc, vegetable and animal fats and oils, gums, polyglycols, or other known pharmaceutical ingredients may be suitable for use as carrier media or excipients. The compounds of the present invention can be administered in any amount and route effective to reduce viral infectivity. Therefore, when used herein, the expression "amount effective to reduce viral infectivity" refers to a non-toxic but sufficient amount of anti-virus to provide the necessary prevention and / or treatment of viral infection. The exact amount required will depend on the species of the individual patient, the age and general condition of the patient, the severity of the infection, the specific antiviral agent, the mode of administration, and the like. The antiviral compound is preferably formulated in a dosage unit form to facilitate administration and maintain dosage consistency. As used herein, a "dosage unit type" refers to a physically separate amount of an antiviral agent suitable for the patient being treated. Each dose should contain the amount of active substance calculated to produce the desired therapeutic effect, or a combination of any selected pharmaceutical carrier and or supplementary active agent. Typically, the unit dose of an antiviral compound of the present invention comprises an antiviral agent having a composition weight of from about 2 mg to about 7000 mg, preferably in a range from about 10 mg to about 2000 mg. When administering this compound, taking into account the nature and severity of the infection to be treated, it can be administered orally, rectally, such as by intramuscular injection, subcutaneous injection, intravenous immersion 88828.doc -36- 200418452 or similar parenteral Intracranial, intravaginal, intraperitoneal, bureau 4 and other paths, and can be used such as powder, ointment, or drops or the like; or by inhalation such as aerosol or similar. Depending on the route of administration, the compound of the present invention is administered at a dose of about 0.05 to about 100 mg / kg of the patient's body weight one or more times a day to achieve the desired therapeutic effect. The compounds of the invention can typically be administered from 1 to 4 times per day to deliver the aforementioned agents: r ° However, the proper administration of the compounds and compositions described herein will depend on the needs of the individual host or patient being treated , The therapeutic grievance administered and the judgment of the participating healthcare professionals. Concentrating on the effect of inhibiting viral RNA synthesis produced by this compound, we expect that these compounds can be used not only to treat viral infections, but also to prevent viral infections. Whether treating or preventing a viral infection, the dose may be substantially the same. The following examples are provided to further illustrate the invention. These examples illustrate suitable synthetic methods for representative compounds of the present invention. However, the synthetic method is intended to be illustrative, and not limited to the following examples. The starting materials for preparing the compounds of the present invention can be conveniently prepared, if not commercially available, according to one of the following examples or by using known chemical methods. Preparation of 2-amidan-3-yl-5-methoxy-benzofuran-carboxylic acid formamide (aK2- ^ an-3-yl-5-hydroxy-benzofurancarboxylic acid ethyl ester).

88828.doc -37- 200418452 In a 25 ml three-necked flask under oven-dried argon pressure, ethyl β-oxyfuranpropionate (2.22 g, 12.2 mmol) was dissolved in absolute ethanol (4 ml). At the same time the porcelain sticks are stirred. Zinc chloride (anhydrous, 1.66 g, 12.2 mmol) was added and the reaction was stirred with a magnetic bar until homogeneous (20 minutes). Put solid 1, benzene (1.32 grams, 12.2 millimoles) in the reaction flask and add 指 "glass wool insulated arm addition funnel (using cotton plug). The reaction in oil was heated under mild reflux, slowly dissolved with hot ethanol, and M-benzene was dropped into the pot over 18 hours. The reaction was cooled to room temperature and treated with water (about 1 ⑻mL). After extraction with ethyl acetate (3 × 75 ml), the organic layers were combined, dehydrated and evaporated. The resulting oil was purified by HPLC (silica gel, ethyl acetate / hexane) to provide 1.42 g (43%) of the product as pale yellow crystals. Compound l (b) (2-crean-3-yl-5-methoxy-benzofuran-3-carboxylic acid ethyl ester).

Combine oven 1 (a) (1.42 g, 5.21 mmol), potassium carbonate (ground, 2.16 g, 15.6 mmol) and anhydrous acetonitrile (20 mL) in a 50 mL flask under oven-dried argon ). Decombustion (3.25 ml, 52.2 mmol) was added to this mixture, and the reaction was heated at reflux for 18 hours. The reaction was cooled to room temperature and filtered through a CeliteTM 503 (Secondary Celite) sheet before the solvent was evaporated. The resulting solid was purified by HPLC (silica gel, ethyl acetate / hexane) to provide 1.37 g (92%) of the desired product as pale yellow crystals. c. Preparation of compound l (c-1 (2-crean-3-yl-5 -methoxy-benzofuran-3) to 88828.doc -38-200418452

In a 50 ml flask, compound 1 (b) (1.37 g, 4.78 mmol) was combined with 4-methyl oxychloride (0.4 g, 713 mmol) in a 50% ethanol aqueous solution (3 5 4 Rise). The mixture was refluxed overnight and cooled to room temperature. Evaporation-semi-solvent 'and acidified at 3 moles HC1, the white precipitate produced by filtration, washed with water' and mixed at 60 ° C. O Vacuum drying provided 1.21 g (97%) of the desired product. d. 5-Methanyl-benzyl-pyrano-uranyl formate amine. Compound l (c) (0.05 g, 019 mmol) was dissolved in an oven-dried chloroform at 10 Anhydrous tetrahydrofuran (THF) (3 ml) in a ml flask. 15 l, -carbonyldiimidazole (0.05 g, 0.31 mmol) was added with stirring by a magnetic bar, and the resulting mixture was gently heated to about 50 ° C for 30 minutes to drive off C02. An excess of methylamine (a 2.0 mol THF solution, 2 ml) was added, and the addition was continued for 4 hours. The reaction was cooled to room temperature and the solvent was evaporated to give an oil, which was purified by HPLC (reverse phase C18, ethyl acetate / water). After lyophilization, 021 g (39%) of the desired product was isolated as a white solid. Example 2 Preparation of Dimethyl-5_trifluoromethylfluorenyl-benzylpyridine_3_rabbitamine amine a.Ul Compound 2 (a) _ (5-Epi-2-phenyl-benzofuran _3-carboxylic acid ethyl ester).

2 (a) 88828.doc -39- 200418452 The intermediate compound is essentially prepared according to the general method of Example 1 and step 骡 a above, but β-oxy-3-furanpropionic acid is replaced with ethyl ethyl fluorenyl Ethyl ester. b. Preparation of compound 2 (b) (5-thiomethylthiocarbonyloxy-2-phenyl-benzofuran-3-carboxylic acid ethyl ester).

In a 25 ml flask opened at atmospheric pressure, add tetrabutylammonium hydrogen sulfate (0.06 g, 0.177 mmol) to 12 mole sodium hydroxide (5 ml) and carbon disulfide (5 ml), while magnetically stirring . Compound 2 (a) (0.5 g, 1.77 mmol) and potassium iodide (0.12 ml, 1.93 mmol) were added, and the mixture was stirred vigorously at room temperature for 1 hour. The reaction mixture was poured into a separatory funnel, the organic layer was collected, and the aqueous layer was washed with carbon disulfide (3 × 10 ml). The organic layers were combined, dehydrated over sodium sulfate, and the solvent was evaporated to produce a color-shifting oil, which was purified by HPLC (silica gel, ethyl acetate / hexane) to provide 0.42 g (63%) of the desired product as a clear oil. c. Preparation of the compound phenyl-5-trifluoromethoxy-benzofuran-3-ethylacetate).

In a 25 ml flask under argon pressure, HF / pyridine (70%, 2.56 88828.doc -40-200418452 ml) was added to -781: 1,3-dibromo-5,5-dimethylinner A suspension of urea (0.96 g, 3.36 mmol) and compound 2 (b) (0.42 g, M3 mmol) in dichloromethane (10 ml). Once the addition was complete (20 minutes), the reaction was transferred to an ice bath and magnetically stirred at 0 ° C for 1 hour. The reaction mixture was then poured into a 50:50 saturated aqueous solution of NaHCCVNaHSCMIO (100 ml) and extracted with ether (3 x 40 ml). The organic layer was dehydrated over sodium sulfate and the solvent was evaporated. The crude product was purified by HPLC (reverse phase C18, acetonitrile / water) to provide 0.12 g (30%) of the desired product as a yellow oil. d. 2 ^ _phenyl-5-trifluoromethoxy-benzofuran-3- # acid formamide monument. The title compound was essentially prepared according to Example 1 above, steps 骡 ^ and ^; however, compound 2 (c) was used instead of compound 1 (b) in step 骡 c. Example 3 Preparation of Difluoro-Arytyl) -5_methoxy · benzofuran_3_methanesulfonic acid formamidine a • Preparation of compound H (3_ (3,4-difluoroyl-phenyl) -3 -Oxy-ethyl propionate).

Let methyl malonate 4 methyl salt (7.46 g, 43.8 mmol mMgCl2 (314 g, 33.0 mmol)) be mixed in anhydrous THF (36 ml) and refluxed for 々 hours. 3,4 monofluoro To a solution of acetic acid (5.22 g, 33 mmol) in anhydrous ml) was added u, -carbonyldiimidazole (629 g, 38.8 mmol) in one portion, and the mixture was heated for another 30 minutes. Then, the second solution was added to the MgCh solution at room temperature. The reaction mixture was allowed to stir at room temperature overnight (16 hours). -41-88828.doc 200418452 2 The reaction flask was cooled in an ice bath, and a solution of HC1 (10 ml of concentrated HO and 20 mL) was added. The resulting mixture was allowed to stir at room temperature for i hours. Ethyl acetate was added to extract the product, and the combined organic layers were washed with saline and water, dehydrated over Na 2 SO 4, and concentrated to form an oil residue. The crude product was purified on a short flash column (silica gel, 10:90 ethyl acetate / hexane) to provide 70 g (93%) of the desired product as an off-white oil. Than 1 ^^^ (2_ (3,4_difluoroyl_phenyl) _5_hydroxy_benzofuran-3-ethyl ethyl acetate). ,

Absolute ethanol (10 ml) was added to an oven-dried argon flask containing anhydrous ZnC12 (2.98 g, 21.9 mmol, pre-dried in the oven for 1 hour). Then, compound 3 (a) (5.0 g, 21.9 mmol) was added to the above-mentioned clear solution. Put 1,4-benzoquinone (2.37 g, 21.9 mmol) into an added boiled tile (with a piece of glass wool on the bottom of the flask) with arms, and install a condenser on the addition flask into the flask The reaction mixture was heated to 1 in an oil bath. 〇. Let the ethanol slowly I * return to the sludge and pass through the arms of the addition flask (covered with glass wool and aluminum mesh); then, slowly wash away the 1,4-benzoquinone through the barrier (18 hours). The reaction mixture was cooled to room temperature, diluted with ethyl acetate, washed with brine and water, and dehydrated with Na 2 SO 4. After concentration, the residue was purified by flash column chromatography (silica gel, 10% ethyl acetate in hexane) to provide 3.60 g (52%) of the desired product as a pale yellow oil. c. Preparation 3 (common (2- (3,4-difluoro-phenyl) _5_methoxy-benzofuran_3 -acetic acid ethyl acetate). 88828.doc -42-

200418452 Potassium carbonate (276 mg, 2.0 mmol) was added to a solution of compound 3 (b) (255 mg, 0.8 mmol) in acetonitrile (5 ml). The mixture was heated at reflux for 30 minutes, and then cooled to room temperature. Methane iodide (249 µl, 4.0 mmol) was added 'and the reaction mixture was stirred: stir overnight. The mixture was diluted with water and extracted with ethyl acetate. The organic layer was washed with a saline solution and dehydrated. The crude product was purified by column chromatography (silica gel, 5:95 ethyl acetate / hexane) to provide 235 mg (88%) of the desired product as a white solid. d. Compound JlL · Compound 3 (dl (2- (3,4-difluoro-phenyl) -5-methoxy-benzofuran-3-metanoic acid).

3 (d) Sodium hydroxide (10 ° C, 0.5 ° L) was added to a hot solution of compound 3 (c) (23 mg, 0.69 mmol) in absolute ethanol (8 ml). The reaction mixture was heated to 90 ° C and stirred for 2 hours. After cooling to room temperature, the mixture was acidified to pH 2 with 10% HCl. The resulting suspension was extracted with ethyl acetate, NadCU was dehydrated, and concentrated to provide a quantitative white solid (20 mg). The product was carried on to the next step without further purification. e. Preparation of 2- (3,4-dioxo-phenylammonium methanoate. 88828.doc -43- 200418452) Methylamine (0.45 ml, 2.0 mole concentration thF solution) was added to compound 3 ) (91 * g, 0.30 * mol) in anhydrous N, N-dimethylformamide (DMF) (5 pens) solution, followed by addition of benzotriazolyloxypyrrolidinyl rust Hexafluorolite (PyBOP) (156 * grams, 0.30 millimoles). The resulting reaction mixture was stirred at room temperature for 2 hours, diluted with water, extracted with ethyl acetate, dehydrated and dried. The crude product was purified by chromatography (Shijiao gum, 1 ·· 90 ethyl acetate / hexane). 72 mg (76%) of the product was provided as a white solid. Example 4 (Amidinoamino-methyl)- Phenylisopropoxyl-benzylpyran-3_carboxamidine_formamidine Preparation a • Compound 4 (a) (3- (4-Bromo-phenyl) -3-oxy · propane Acid ethyl ester).

Ethyl malonate potassium salt (5.63 g, 33.08 mmol) and magnesium chloride (2.37 g, 24.87 mmol) were refluxed under argon pressure in THF (60 ml) for 4 hours. In a second reaction vessel, 1,1 carbonyldiimidazole (4.76 g, 29.35 mmol) was added to 4-bromoarsinic acid (5.0 g, 24.87 mmol) in THF (30 ml) under argon. Solution, and gently reflux the solution for 30 minutes. Both reactions were cooled to room temperature, and the second solution was added dropwise to the ethyl malonate / magnesium chloride mixture. The reaction mixture was allowed to stir at room temperature for 16 hours. Concentrated hydrochloric acid (10 ml) and water (20 ml) were mixed in an addition funnel and added dropwise to the reaction mixture over a period of 15 minutes. The organic solvent was removed by rotary evaporation, and the product was extracted several times with ethyl acetate. The organic layers were combined, washed with brine and concentrated. The product 88828.doc -44- 200418452 was purified by flash analysis (stone gum, ethyl acetate / hexane gradient) to provide 6.07 g of the desired product as an orange oil. · Bromo_phenyl) _5_hydroxy_benzofuran_3_carboxylic acid ethyl ester).

The addition funnel, flask, stir bar and zinc chloride (3.02 g, 22.13 mmol) were dried in the baking phase for 1 hour and cooled under argon. Compound 4 (a) (60 g, 22.13 mmol) was dissolved in ethanol (ml) and added to a flask containing chloride. I 添加 —benzoquinone (2.39 g, 22 · 13 mmol) was added through an addition funnel (covering glass wool and aluminum foil and using a cotton plug). The reaction was heated in an oil bath to 105; ^, and the amount of ethanol condensed into the addition funnel was adjusted to promote the "hourly" addition of benzoquinone. When the i, 4-benzene was consumed, the reaction was cooled At room temperature, ethyl acetate was added, and the crude product was washed with brine. The aqueous layer was washed several times with ethyl acetate, and the organic layers were combined and concentrated. The product was purified by flash chromatography (silica gel, gradient) and contacted with acetic acid. Ultrasonic in ethyl acetate's hexane solution = 2.24 g (28%) of the desired product as an orange solid. Bromo-phenyl) -5_isopropoxy-benzofuran-3-carboxylic acid ethyl ester).

Compound 4 (b) (10.59 grams, 29.32 millimoles) and ethidium chloride (ml) were added 88828.doc -45- 200418452 to a solution containing anhydrous potassium carbonate (10.3 grams, 73.30 millimoles). Oven-dried flask. The mixture was heated at reflux for 1 hour and then cooled to room temperature. 2-Decomposed propane (8.78 ml, 87.96 mmol) was added and the reaction mixture was heated at reflux for 16 hours. The reaction mixture was allowed to cool to room temperature, concentrated, dissolved in ethyl acetate and filtered. The filtrate was concentrated in vacuo, and the crude product was recrystallized (ethyl acetate and hexane) to provide 9.38 g (79%) of the desired product as a brown solid. d-Preparation of compound 4 (d) (2- (4--> Styrolyl- winteryl) -5 -isopropoxy-benzoanan-3 -chitoic acid).

Potassium hydroxide particles (1.0 g, 17.82 mmol) were added to a suspension of compound 4 (c) (2.02 g, 5.01 mmol) in 1: 1 ethanol / water (25 ml / 25 ml). The reaction mixture was heated at reflux for 2 hours. The reaction mixture was cooled to room temperature and concentrated in vacuo. The crude product was extracted into ethyl acetate without acidification. The organic layer was concentrated and the solid was recrystallized (ethyl acetate and hexane) to provide ^ "g (99%) of the desired product as an orange solid. Bromo-phenyl) -5-isopropoxy-benzofuran -3-carboxylic acid formamidine).

4 (e) 1- (3-Dimethylaminopropyl) -3-ethylcarbonyldiimide (1.40 g, 7.32 mol), 1- # is benzotriazole (0 99 g , 7.32 millimoles) and methylamine (4.88 88828.doc -46- 200418452 pen liters, 2.0 Molar concentration of THF solution, 9.75 millimoles) was added to compound 4 (d) (1.83 grams, 4.88 millimoles). Mol) in dichloromethane (35 ml). The reaction mixture was allowed to stir at room temperature for 16 hours, then concentrated, dissolved in ethyl acetate and washed with water. The organic layer was concentrated in vacuo and the crude product was purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 24 g (66%) of the desired product as a yellow solid. f. "Hui" compound 4 (f) (2- (4-cyano-phenyl) -5-isopropoxy-benzoanan-3-carboxylic acid formamidine).

Copper cyanide (1.95 g, 21.81 mmol) was added to a solution of compound 4 (e) (121 g, 3.12 mmol) in 1-methyl · 2-pyrrolidone ... (ii) (ml). The reaction mixture was heated to 170 ° C in an oil bath. The reaction was cooled to room temperature, diluted with water and ethyl acetate, and filtered through a CeliteTM plug, and wet with ethyl acetate and water. The layers were separated and the organic layer was concentrated in vacuo. The crude product was purified by flash chromatography (silica gel, ethyl acetate / hexanes gradient) to provide 0.68 g (65%) of the desired product. Compound 4 (g) (2- (4-aminomethyl-phenyl) -5-isopropoxy-benzo-anthran-3-carboxylic acid formamidine, HC1 salt).

10% Pd / C (0.10 g) was mixed with water and concentrated hydrochloric acid (0.5 ml), and the solution containing compound 4 (f) (0.68 g, 2.03 mmol) in methanol (15 ml) was added 88828. doc -47- 200418452 should be flask. The reaction flask was shaken on a Parr shaker under 55 psig of hydrogen for 16 hours. The reaction mixture was filtered through CeliteTM and wet with ethanol. The filtrate was concentrated in vacuo and the crude product was recrystallized (ethyl acetate) to provide 0 65 g (86%) of the desired product as a dark yellow solid. h.ijf. 4 (h) (2- [4- (Ethylamido-methyl) -phenyl] isopropoxy-benzo-anan-3 -metamate).

4) Triethylamine (0.037 ml, 0.267 mmol) was added to a dichloromethane (10 ml) solution containing compound 4 (g) (50 mg, 0.133 mmol). Acetic anhydride (0.015? Liter, 0.160 ¾ mole) was added to the solution, and the reaction was stirred at room temperature. After 16 hours, digas methane (10 ml) and water (15 ml) were added to the mixture 'to separate the layers. The organic layer was concentrated in vacuo and the crude product was purified by flash chromatography (silica gel, ethanol / ethyl acetate) to provide 50 mg (96%) of the desired product as an off-white solid. Example 5 Preparation of light-phenyl-isopropyl gas cap-benzofuran-3- # formamidine .

-48- 88828.doc 200418452 reflux ethyl potassium malonate (9.92 g, 58.27 mmol) and magnesium chloride (4.17 g, 43.81 mmol) in THF (100 ml) for 4 hours under argon . In the second reaction vessel, will! ,! Carbonyl diimidazole (〇1) 1) (8.38 g, 51.7 mmol) was added with THF (10 ml, 43.81 mmol) in THF (60 ml) under argon. Solution. The solution was allowed to reflux gently for 30 minutes. Both reactions were cooled to room temperature, and the second solution was added dropwise to the ethyl malonate / magnesium chloride mixture. The reaction mixture was allowed to stir at room temperature overnight. After 16 hours', a hydrochloric acid solution (20 ml of concentrated HC1 and 40 ml of water) was added to the reaction mixture. The organic solvent was removed under vacuum and the product was extracted several times with ethyl acetate. The organic layers were combined, washed with brine and concentrated. The product was purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 10 g (77%) of the desired product as a pale yellow solid. 5 (b) (2- (4-Ethoxy-phenyl) -5-hydroxy-benzofuran-3-carboxylic acid ethyl ester).

Compound 5 (a) (10.0 g, 33.52 mmol) was dissolved in ethanol (15 ml), and oven dried with zinc chloride (oven dried, 4.57 g, 33.52 mmol) was added. Flask. Put grams, 33.52 millimoles) into the addition funnel (cover the glass wool with Ming Ming and use a cotton plug). The reaction was heated in Yolo to 100 ° C, and the amount of ethanol condensed into the addition funnel was adjusted to promote the addition of 1, anthraquinone for 18 hours. When 1,4-benzoquinone is consumed, cool the mixture to ^

HO 88828.doc -49- 200418452 warm, add ethyl acetate, and wash the crude product with saline. The aqueous layer was washed several times with ethyl acetate, and the organic layers were combined and concentrated in vacuo. The product was purified by flash chromatography (silica gel's ethyl acetate / hexanes gradient) and super-first-waved in a 15% ethyl acetate-fired solution to provide 4.08 g (31%) of the desired product as a solid. c. Rabbit preparation_complex 5 (, g) _ (2- (4 -fluorenyl-phenyl) -5 -isopropoxy-benzohuffan-3-ethyl behenate).

Compound 5 (b) (4.07 g, 10.48 mmol) and acetonitrile (60 ml) were added to an oven-dried flask containing potassium carbonate (oven dried, 3.62 g, 26.20 mmol). The mixture was heated at reflux for 1 hour and then cooled to room temperature. Propane iodide (3.14 ml, 31.43 mmol) was added and the reaction mixture was heated under reflux again. After 16 hours, the reaction mixture was cooled to room temperature, concentrated, and washed with ethyl acetate. The organic layer was concentrated in vacuo and purified by flash chromatography (Shi Xi $, ethyl acetate / hexane gradient) to provide 4.07 g (90%) of the product as a yellow solid.

Ran-3-a few acids).

88828.doc -50- 200418452 Add potassium hydroxide particles (0.5 g, 891 mmol) to compound 5 (c) (i g, 2.32 «mol) in 1: 1 ethanol / water (20 ml / 20 ml) suspension. The reaction mixture was heated at reflux for 2 hours and then cooled to room temperature. Mortar-concentrated hydrochloric acid 'was added to remove the precipitate and dried to provide 0.92 g (99%) of the product as a white solid. Benzyloxy_phenyl) _5-isopropoxy_benzobenzopyran-3-carboxylic acid formamidine) '.

Compound 5 (d) (0.92 grams, 2.48 millimoles) and benzotriazole_1_yl_oxy-shen-saw-Hanayl-phosphonium hexafluorophosphate (129 grams, 2.48 millimoles) Mix under argon and treat with methylamine (20 ml, 2.0 Molar THF solution). The falling liquid was stirred at room temperature for 3 hours. The reaction mixture was concentrated, dissolved in ethyl acetate and washed with water. The organic layer was concentrated and purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 0.78 g (76%) of the desired product as a white solid. f. UL1 dagger compound 5 (fluorene (2- (4-hydroxy-phenyl) -5-isopropoxy-benzoanan-3-carboxylic acid formamidine).

5 (f) A 10% Pd / C (0.10 g) water mixture was added to ethanol / ethyl acetate (20 ml / 10 ml) containing compound 5 (θ (0 78 g, 1.88 ¾ mole)). Solution. Let 88828.doc -51-200418452 shake the reaction mixture on a Parr shaker at 55 psig of hydrogen for 6 hours. Filter the reaction mixture through CeliteTM, wet with ethyl acetate and ethanol. Concentrate the filtrate and recrystallize the crude product ( Ethyl acetate and hexane) to provide 0.57 g (93%) of the desired product as an off-white solid. Example 6 2- (4-Fluoro-phenyl) -5-isopropoxy-6-say Preparation of 1-yl-benzyl-3-alanine methaneamine a. Preparation of compound 6 (aV3-(; 4-fluoro-phenyl) -3-oxy-propionic acid ethyl ester ).

THF (1 liter) of 4-fluorobenzoic acid (275 g, 1.96 mol) was added to a solution of 1,1'-carbonyldiimidazole (CDI) (381 g, 2.36 mol) in THF (1 liter) over 1 hour. . The reaction mixture was stirred at 30 ° C. for 1 hour and then at room temperature overnight. Magnesium chloride: (186 g, 1.96 moles) was added over 5 minutes to a second mixture of potassium ethyl malonate (435 g, 2.56 moles) in THF (2 liters). The resulting mixture was allowed to stir overnight in a closed device. The first mixture was added to the malonic acid mixture over a period of 11/2 hours. The reaction mixture was allowed to stir at room temperature for several hours, and then warmed to 30 ° C for several hours. The reaction mixture was treated with 4 equivalents of HC1 (1.0 liter) and the layers were separated. The aqueous layer was diluted with water (1 liter), reduced to about pjj 1 with Hci (250 ml), and washed with ethyl acetate (1 liter). The organic layer was concentrated to provide 65 g of crude product. The original organic layer was concentrated to remove thf, diluted with ethyl acetate (1 liter), and wet with water (1 liter). The organic layers were combined with 65 g of crude product and concentrated to an oil. The oil was diluted with ethyl acetate (1 liter) and the crude product was vacuum distilled over 50 / 〇 88828.doc -52- 200418452 to provide

NaHC03 (1 liter) wets. The organic layer was concentrated 322 g (78%) of the desired product. b. Preparation of compound Ethyl Acetate). -Benzyl) -5-hydroxy-benzofuran-3-

Compound 6 (a) (157 g, 0.75 mol) was added to a flask containing chloride (100 g, 074 mol) and ethanol (250 ml), and another ethanol (about 50 ml) was added. Wash in. Mix M-Benzene (80 g, 0.74 mol) with CeliteTM (4 (^), put the light stopper into the glass funnel to add the funnel. Heat the reaction mixture to 95τ, and at a rate of about 4 ml / min Add 4-benzoquinone. When the benzoquinone is consumed, cool the mixture to room temperature, add ethyl acetate (2 liters), and wash the crude product with water (1 liter) and brine. Remove The insoluble impurities are concentrated. The filtrate is concentrated. The resulting solid is stirred in dichloromethane (500 ml) and cooled to _20τ. The other impurities are removed. The mash is concentrated and mixed with dichloromethane (400 ml). The crude product was cooled to -20 ° C and filtered. The separated solid was wetted with dichloromethane and air-dried to provide 71.8 g (32.3%) of the desired product. Compound 6 (c_i (2- (4-fluoro -Phenyl) -5-isopropoxy-benzoanan-3-carboxylic acid ethyl ester).

88828.doc -53-200418452 Cesium carbonate (111.6 g, 343 mmol) was added to 1-methyl-2-pyrrolidone (250 ml) of compound 6 (b) (73.5 g, 245 mmol) ). The reaction mixture was heated in an oil bath to 5 ° C. for 16 hours, and then cooled to room temperature. The solids were removed by filtration, and the mash was diluted with a salt solution and a third butyl methyl ether. Tributyl methyl ether wets the water layer several times. The organic layers are combined and concentrated. The solid formed overnight is filtered and wetted with hexane to provide about 28 g of the desired product. Column chromatography (silica gel, ethyl acetate) / Hexane gradient) to purify the filtrate to provide an additional 47.2 g of the desired product. D.ij compound 6 (d) (6-bromo-2- (4-fluoro-phenyl) _5_isopropoxy_ Benzofuran-3 · ethyl carboxylate).

A solution of bromine (0.75 ml, 0.014 mol) in anhydrous dioxane (20 ml) was added over 1 hour to an anhydrous dioxane (50 ml) compound 6 (0 (4.59 g, 0.014 mmol). The reaction mixture was stirred at 300 watt-lamp under room temperature argon for 1 hour. Add another 3 drops of bromine and stir the reaction overnight. The reaction mixture was concentrated to 1/2 volume Diluted with water, extracted with red acetate MgS04 after dehydration with ethyl acetate and dehydrated and concentrated. The crude product was purified by Ηρχ (reverse phase, acetonitrile / water gradient) to provide the desired product as a white solid. E.im 6 (red (2 -(4-fluoro-phenyl) -5-isopropoxy-6-pyrrolidin-1-yl-benzoanan-3-acetic acid). 88828.doc -54- 200418452

An oven-dried flask containing cesium carbonate (dry, 0.217 g) was placed in a dry bag under argon pressure, and compound 6 (magnesium (0,250 g, 0594 mmol), ginseng (diphenylene) was added. Methylacetone) dipalladium (0) (0.016 g, 0.00178 mmol) and rac-2,2-bis (diphenylphosphino) _u, _diamidino (racemic mixture, 〇〇 ιg, 0.0177¾ mole). Remove the flask from the dry bag, wash it, and fill it with argon to make it vacuum (3x). Add anhydrous toluene (10 ml) to the flask, followed by pyrrolidine (0.059 ml). The reaction mixture was heated to 95 overnight in an oil bath, then cooled to room temperature, diluted with ether, filtered through CeHteTM tablets and washed with ether. The solvents were evaporated and flash chromatography (silica gel, ethyl acetate) / Hexane) The crude product was purified to provide 0.117 g (49%) of the desired product as a yellow oil. Compound 6 (Γ) · (2- (4-fluoro-phenyl) _5_isopropoxy -6-pyrrolidin-1-yl-benzofuran-3-carboxylic acid).

It is known that potassium hydroxide (one grain) was added with a compound 6 (e) (On4 g, 0.277 mmol) &lt; 2: 1 ethanol / water (2.0 ml / 10 ml) solution. The reaction mixture was heated at reflux for more than 2 hours and then stirred at room temperature overnight. The ethanol was removed from the mixture by evaporation. The remaining oil was dissolved in water and diluted with 3 equivalents of hydrochloric acid to 88828.doc '55-200418452. A solid formed (about pH 7.5). The yellow solid was filtered to provide 0.9 g (85%) of the desired product. g · Preparation of compound 6 (g) (2- (4-fluoro-phenyl) -5-isopropoxypyrrolidin-1-yl-benzofuran-3-carboxylic acid formamidine).

Xylidene-1-yl-oxy-shen-erodolide-squadenahexafluoroscale salt (1 g, 0.183 mmol) was added to compound 6 (f) SBE-0628-198 (79.0 mg, 0.206 mmol) of methylamine (3.0 ml, 2.0 mol THF solution) in an oven-dried flask under direct air. The reaction mixture was allowed to stir at room temperature for 6 hours and then concentrated in vacuo. Purification of the resulting oil by flash chromatography (silica gel, ethyl acetate / hexane) provided 0.045 g (63%) of the product as a yellow solid. Example 7 — Preparation of a mono-gas methoxy-2- (4-fluoro-benzyl) -benzyl-3-anthamic acid methylamino amine digas methoxy-2- (4-fluoro- Phenyl) _benzofuran-3-ethyl acetate).

And potassium potassium (28 mg, 0.167 mmol) and potassium carbonate (0.69 g, 5.00 88828.doc -56- di :), compound 6 (b) (0.50 g, 1.67) which can be prepared according to Example 6 2 — A), 2 methyl ethyl ketone solution. The reaction mixture was allowed to stir at room temperature for 10 minutes. : = Ethyl chlorodifluoroacetate (0.32 ml, 2.50 mmol), and the reaction was allowed to take place:] hr. The reaction was allowed to cool to the chamber and concentrated in vacuo. The crude product was dissolved in ethyl acetate and washed with water and 1 molar hydrochloric acid. The product was concentrated and purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide mg (22%) of the desired product as a white solid. Difluoromethoxy_2_ (4-fluoroyl_phenyl) _benzofuran-3-carboxylic acid). ^ 7 (b) potassium hydroxide particles (0.50 g, 891 mmol) were added to compound 7 (magic (0.13 g, 0.371 mmol)) in 1: 1 ethanol / water (7 ml / 7 ml ) Suspension. The reaction mixture was heated at reflux for 5 hours. The reaction mixture was cooled to room temperature and cooled down. Add 1 molar hydrogen acid until the solution became acidic, forming a precipitate. Filter the solid and dry to provide 120 mg ( 100/0) The desired product as a white solid. Meeting 7 (Red (5-difluoromethoxy-2- (4-fluoro-phenyl) -benzylfuran-3-carboxylic acid formamidine amine).

Add 1- (3-Dimethylaminopropyl) -3 -ethyl-diimide hydrochloride (0.08 g 88828.doc -57- 200418452 0.558 mmol) and methyl 0.745 mmol) Add, 0.558¾ mole), 1-light benzotrisalyl (i.e. mg, amine (2.0 Molar concentration in THF solution, 0.37 ml, compound 7⑻ (0.12 g, 0.372 mmol) dichloro) Formaldehyde solution). The reaction mixture was stirred at room temperature for 16 hours, then concentrated, dissolved in ethyl acetate and washed with water. The organic layer was concentrated and purified by flash chromatography (silica gel, ethyl acetate / hexane gradient). The crude product provided 87 mg (70%) of the desired product as a white solid. A M4-Fluoro-phenyl V5_Wusheng Aildl Acid Formamidine The title compound (0.038 g, yellow solid) was essentially based on It was prepared by the general method described in Example 6 above, however, in step 骡 e, a dry bag was not used and pyrrolidine was replaced with 2-methoxyethylamine. Moreover, the title compound was subjected to reversed phase HpLc using 60% to 90 % Of acetonitrile in water was purified by gradient. Was 9X ^ (3- methoxy-6-methyl-phenyl flavyiium -2_ chloride).

Anhydrous HC1 was ventilated through 0 ° C of 2-hydroxy-5-methylbenzaldehyde (20 g, 14.69¾ mole) and 2-methoxyacetophenone (2 ml, 1451 mmol). A solution of ethyl acetate (28 ¾ liters) and ethanol (7 ml) was allowed to stand for 1 hour. The reaction was then 88828.doc -58- 200418452 filtered to separate the solid lid and placed in the refrigerator for 56 hours. Add ether to settle to provide 3.73 g (88%) of the desired salt. -Methyl benzofuran-3-carboxylic acid). b. Complex compound methyl-2-phenyl

Hydrogen peroxide (7.5 ml, 72.8 millimoles) was added to compound 9⑷ (3.5 g. Molole) in 50% methanol in water (72 ml). The reaction mixture was allowed to warm overnight, cooled to room temperature and diluted with ether. The layers were separated and the aqueous layer was taken with ether (2x). The organic layers were combined, washed with saline, dehydrated (MgS04) and evaporated. Purified by gel column chromatography, Lishe hexane / acetic acid was used as the eluent to provide 736 mg (22 6%) of the desired compound as a white solid. Methyl | phenyl-benzoanuronic acid).

An aqueous potassium hydroxide solution (4 equivalents, 12 ml) was added to a methanol (15 ml) suspension of compound 9 (b) (6 pen grams, 2.46 mmol). Make the response high. The mixture was allowed to cool to room temperature and acidified to pH 2 with i-equivalent hydrochloric acid. The precipitate was collected by suction filtration, washed with water and dried to yield 471 mg (76%) of the desired carboxylic acid. 88828.doc -59- 200418452

Methylamine (0.495 ml of a 2 molar solution in THF, 0.99 mmol), 1- [3- (dimethylamino) propyl] -3_ethylcarbonyldiimine hydrochloride ( 142 mg, 0.742 mmol) and hydroxybenzotriazole (100 mg, 0.742 mmol) were added to compound 9 (c) (125cs g, 0.495¾ Mol) in anhydrous dichloromethane (2 mL ) Solution. The reaction was allowed to stir overnight at room temperature under argon, the equivalent concentration of hydrochloric acid was added to stop the heat and extracted with dichloromethane. The organic layer was washed with saline, dehydrated (MgS04) and evaporated. Purified by column chromatography on silica gel using dichloromethane as the eluent &apos; to provide 49 mg (37%) of the title product as a white solid. Example 10 Methyl_2_ (4: fluoro-phenylbenzene sulfonate-bitan_3. Miao succinimidine depletion by a ... Preparation ... Compound 9 (a) (1- ( Fluoro-phenyl) · 2-methoxy-ethanone).

A solution of 4-fluorobenzylhydrazone gas (25.6 g, 161 mmol) in acetonitrile (60 ml) was added dropwise to 0 ° C trimethylsilane diazomethane (96 ml of a 2 molar solution) , 193.2 mmoles) and triethylamine (27 ml, 193.2 mmoles) in anhydrous acetonitrile (250 ml). The reaction was allowed to stir at 0 ° C for 2 hours, then was capped and left in the refrigerator overnight. The solvent was removed by rotary evaporation, and the residue was dissolved in a saturated sodium bicarbonate solution and extracted with ethyl acetate. The organics were washed with water and saline, dehydrated (MgS04) and evaporated to yield 25.16 g of a yellow solid. The solid was dissolved in anhydrous methanol (200¾ liters) 'and tri-emulsified boride (19.4 ml, 161 mmol) was added. The reaction was allowed to stir at room temperature for 2 hours, and 88828.doc -60-200418452 scavenger was removed by rotary evaporation. The residue was dissolved in diethyl ether, washed with water and saline, dehydrated (MgS04) and prepared. Purification using 5: 1 hexane / ethyl acetate silica gel column chromatography provided 18.77 g (69%) of the desired product as an orange solid. The title compound made from fluoro-phenylammoniummidine is essentially prepared according to Example 9, Step 骡 ab, however, in step a, 2-methoxy-4'-fluorophenylethyl g is the same as Substitute 2-methoxyacetophenone and replace 2-methoxyacetophenone with compound 10 (a).

Example Preparation of U-based-5_ (2,2,2-trifluoropyrano-3_le_formamidine — aH compound 11⑷ (5_hydroxy_2_phenylbenzofuran_3_carboxylic acid) 88828.doc

Compound 11 (a) was prepared according to the general method of Example 3 and Step d in the above. However, Compound 2 (a) was used instead of Compound 3 (c). b. Preparation of resin 11 (b).

Let 4-methylmethyl-3-methoxyphenoxymethyl functionalized styrene grease-61- 200418452 vinylbenzene copolymer (2 g, Aidrich, 0.9 mmol / g) in acetic acid One of them was swollen in K (20 μl) and then dried. Add 1% dichloromethane in acetic acid (20 ml) followed by methylamine (2 mole concentration thf, 4 ml) and allow the mixture to sonicate for 20 minutes. Then, the resin mixture was allowed to stand at room temperature for 16 hours. A 1% suspension of 1% acetic acid in dichloroethane (5 ml) of sodium ethoxyborohydride (422 pens, 2¾ mol), which was sonicated, was added, followed by gentle stirring at room temperature for 16 hours. Methanol (5 ml) was added and the solvent was drained. Then wash the resin thoroughly with methanol and chloroform. Repeated reactions ensure complete consumption of the aldehyde bound to the resin. It is not necessary to specify the characteristics and let the dried resin go to the next step. c.ldlL # 子 脂 lUc.

Resin 11 (b) was swelled in DMF (6 ml), then compound 11 (a) (325 mg, 1.5 mmol) was added, followed by benzotriazole-; 1-yl-oxy_- Pyrrolidine-squarehexafluorophosphate (78 mg, 15 mmol,

NovaBiochem), diisopropylethylamine (0.523 ml, 3 mmol) and DMF (4 ml). The reaction mixture was stirred gently under nitrogen for 4 hours and then drained. The resin was thoroughly washed in DMF (6X10 * L), methanol (6X10ml) and digas methane (6x10 * L), and dried under vacuum. Let the dried resin continue to step d. 88828.doc 62- 200418452 A small sample was treated with 25% trifluoroacetic acid (TFA) in dichloromethane (CH2C12) to qualitatively evaluate the resin load. After 30 minutes, the TFA-CH2C12 mixture was filtered off, and the filtrate was evaporated to dryness. Characterization of the dried product from TFA treatment by LC-MS and NMR showed successful resin loading. d · Preparation of 2-benzyl-542.2,2-trifluoro-ethanylbenzovanan-3-boron_methyldonamine. Mix cesium carbonate (325 mg, 1 mmol) with DMF (2 ml) And heated to 75 ° C for 10 minutes. Resin ll (c) (150 mg, about 0.135 mmol) was added as a solid, followed by the addition of 2,2,2-trifluoroethyl ester (2 10 mg, 1 mmol) and DMF (2 Ml). The reaction mixture was heated under nitrogen at 75 ° C for 18 hours. Then, the resin was allowed to cool to room temperature, washed thoroughly with DMF (6 × 10 ml), methanol (6 × 10 ml), and dichloromethane (CH2C12) (6 × 10 ml), and dried under vacuum. The dried resin was treated with 25% TFA in CH2C12 for 60 minutes. The tfa-chW2 mixture 'was filtered off and the filtrate was evaporated to dryness. It was then purified by reverse-phase HPLC on a Gilson HPLC-MS semi-preparative system (acetonitrile / water dissociation with 0. 0/0 acetic acid) to provide 12.7¾ (27 ° / 0) of the desired product. Example 12 Preparation of m-like group: phenyl) -5-^^ _ benzopyran_3_methanoic acid melanidine Preparation of compound 12 (&amp; 1〇) ^ Compound 12iaVin (2-gas 4-fluoro group -Phenyl) -5-hydroxy-benzofuran-3-carboxylic acid methyl ester and 2- (4-fluoro-phenylphenyl 5-hydroxy-benzofuran-3-carboxylic acid ethyl ester).

88828.doc -63- 200418452 Put 4-fluorofluoroacetic acid f-ester (4.0 g, 20.4 mmol), zinc chloride (anhydrous, 2.73 Grams, 204 millimoles), and babar on ethanol (8 liters) while magnetic stirring. The solid, 4-benzoquinone (2.21 g, 20.4 mmol) was placed in an addition funnel on the reaction flask. The reaction was heated under gentle reflux in an oil bath, slowly dissolved in hot ethanol and 1,4-benzoquinone was dropped into the pot over 18 hours. The reaction was cooled to room temperature and then diluted with ethyl acetate (40 mL) and water. After extraction with ethyl acetate (2x), the organic layers were combined, dehydrated over NaJCU, filtered through silica gel and evaporated to dryness. The resulting residue was filtered, and then purified by HPLC (Shi Xijiao, 40% ethyl acetate / hexane), and the crude product was further purified from hot ethyl acetate / hexane by crystallization to provide 209 g (36%) of the compound. A mixture of 12 (a) fluorene and compound i2 (a) (ii). 12 (b) 〇l compliance compound 12fbVin (2- (4-fluoro-phenyl) -5-methoxy-benzofuran 3-carboxylic acid methyl ester and 2- (4-fluoro-phenyl) _5_methoxy-benzofuran-3-carboxylic acid ethyl ester).

12 (b) (1) 12 (b) (ii) Methane iodide (0.43 ml, 6.99 mmol) was added to compound 12 (a) ⑴ and compound I2 (a) (ii) ( h00 g, 3.49 mmoles), potassium carbonate (milled, 1.21 g, 8.73 mmoles), and anhydrous acetonitrile (15 ml). The reaction mixture was heated at reflux under argon for 18 hours, then, cooled to room temperature and stirred for 24 hours. The mixture was diluted with acetonitrile (10 ml) and filtered, and the solvent was evaporated to dryness. The crude solid was diluted with 60:40 ethyl acetate / hexane, filtered, and purified by HpLc (Shi Xi 88828.doc -64- 200418452 gum, ethyl acetate / hexane) to provide 0.85 g (78%) of Desired product. Compound 12 (cK2- (4-fluoro-phenyl V5-methoxy-benzosulfan-3-carboxylic acid).

Compound mixture 12 (b) (0.85 g, 2.70 mmol) was combined with hydrated pellets (0.23 g, 4.06 mmol) in ethanol (24 mL) and water (4 mL). The mixture was allowed to reflux gently overnight and cooled to room temperature. Rotary evaporation removes the solvent and dissolves the remaining solids in water. The solid was acidified by HC1 at a concentration of 3 moles, and the solid was precipitated, filtered, washed with water and burned, and partially dried under vacuum to provide 0.84 g of the desired product. d. Preparation of the substance 12 (d) (2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine).

1,1'-carbonyldiimidazole (42 mg, 0.262 mmol) was added to a solution of compound 12 (c) (50 mg, ca. 175 mmol) in anhydrous THF (3 ml) under argon. The reaction mixture was heated gently for 30 minutes to drive off C02, after which 1 ethylamine (40 wt. F% aqueous solution, 1 ml) was added. The reaction mixture was allowed to stir overnight at room temperature. The dried product was purified by HPLC (reverse phase C18, 1 ml of dimethylacetone in acetonitrile / water, 2x). The acetonitrile was removed by rotary evaporation, and 88828.doc -65- 200418452 was isolated by filtration. The solid was washed with water and hexane to provide 14.3 mg (28%) of the desired product. Example 13 Fluoro-phenyl) -5-methoxydi ^ carboxylic acid formamidine ^ Preparation a. Compound i- Compound 13 (a) (6-bromo-2- (4-fluoro-phenyl) _5_methoxy-benzoanan-3 -ethyl metaboate).

A solution of bromine (127 mg, 0.795 mmol) in anhydrous dioxane (1 ml) was added dropwise over 20 minutes to compound 12 (b) (ii) (250 mg, 0. 795 mmol) in anhydrous diuridine (3 ml). The reaction was allowed to stir in a 300-watt bulb under room temperature argon for 3 hours. The reaction mixture was diluted with water, the solid was filtered off, washed with water and hexane, and dried in a vacuum baking phase. The crude product was purified by HPLC (reverse phase, acetonitrile / water gradient) to provide 47 mg (15/0) of the desired product as a white solid. b. ^ Dioxy-benzofuran I system. The title compound was essentially prepared according to the usual method described in Example 1, Steps 骡 c and d, however, in step c, Compound 13 (&amp;) was substituted for Compound i (b). f Example 14 Benzofuran-3-carboxylic acid formamide &lt; ^^ 14 (a) (ii) (5 ^ 1 group-6_methyl_2_ 88828.doc 200418452 phenylbenzofurancarboxylic acid ethyl ester with 5 -Hydroxy-7-methyl-2-phenyl-benzofuran-3-acetic acid ethyl ester).

X. Bar-to-ethanol (30 ¾ liters) and ethyl benzylacetate (9.9 ml, 57.3 mmol) were added to anhydrous ZnCh under argon (7-8 g, 57.3 mmol, pre-dried in the oven for 1 hour). Oven-dried flask. Put methyl_, 4-benzoquinone (0 g, 57.3 * mol) into an addition funnel (with a glass wool sheet at the bottom of the funnel) with an arm and configure a condenser on the addition funnel. The reaction mixture in the flask was slowly heated in an oil bath. The ethanol was refluxed through the arm of the addition funnel (covered with glass wool and aluminum foil), and then methyl 4 + benzoquinone was slowly washed off overnight (8 hours). The reaction mixture was allowed to cool to room temperature, diluted with ethyl acetate (about 200 ml), washed with water (2 x 300 ml) and dehydrated with NαΑ04. After concentration, the residue was purified by column chromatography (anhydrous loading on silica gel, ethyl acetate / hexane solvent gradient), and crystallized in 2 batches to produce compound i4 (a) (i). The mixture with chemical characters 14 (a) (ii), which proceeded to the next step without further purification. B. Preparation of chemical compounds 1 into 14 (bKO and compound 14ibVn \ ri A is ~ methyl-2-phenyl- Ethyl benzofuran-3-carboxylic acid and 5-methoxy-7-methyl-2-benzo-2-benzofuran-3-carboxylic acid ethyl ester).

14 (b) (i)

14 (b) (ii) 88828.doc -67- 200418452 Compound mixture 14 (a) (1.0 g, 3.37 mmol), potassium carbonate (milled, 1.16 g, 8.42 mmol) Combine with anhydrous acetonitrile (20 ml) in an oven-dried 50 ml flask under argon. Methyl iodide (0.42 ml, 6.75 mmol) was added to the mixture and the reaction was heated under reflux for 3 hours under argon. Then, the reaction mixture was cooled to room temperature, and the rotary sword was removed by rotary evaporation. The residue was diluted with ethyl acetate and filtered, followed by evaporation of the solvent. The resulting oil was diluted with hexane and the solid was isolated by filtration. The crude product was purified by HPLc (silica gel 'ethyl acetate / hexane) to provide 0.135 g of compound 14⑼⑴ and 0.432 g of compound 14 (b) (ii). The preparation of methy-2dibenzopyran_3_methanepyrene acetic acid is essentially made according to the method described in Example 12, Steps 0 and d above, however, in step 骡 c Substitute compound 14 (1)) (1) for compound 12 (b). Example 15 Diphenyl) -5-isodioxo-2,3-yl-benzyl) -5-isobutyramide _

-Butoxychitylamino-p-pyrrozoosis-1 -yl)

88828.doc 200418452 Anhydrous cesium carbonate (270 mg, 0.830 mmol), bis (diphenylmethyleneacetone) dipalladium (0) (11 mg, 0.00119 mmol), rac-2,2 -Bis (diphenylphosphino dinaphthyl) (11 mg, 0.00178 mmol), 3- (third) -butoxycarbonylamino) pyrrolidine (0.132 g, 0.712 mmol) and according to examples Compound 6 (d) (250 mg, 0.593 mmol) prepared in 6 was placed in an oven-dried two-necked flask that was degassed and washed several times with argon. Anhydrous toluene (2 ml) was injected into the reaction mixture, and the reaction flask was purged with argon. The reaction was allowed to stir at 8 crc under argon for 18 hours, then cooled to room temperature, diluted with ether (8 ml), and filtered through a silicone sheet. The solvent was evaporated and the resulting oil was purified by HPLC (reverse phase, acetonitrile / water gradient) to provide the desired product. b.HJL house 15 (b) (6- (3-Amino-pyrrolidin-1_yl) -2- (4-fluoro_phenyl) -5-isopropoxy-benzofuran_3 _ A few sour).

Known compound 15 (a) and 3 potassium hydroxide particles (about 0.4 g) in ethanol (30 mmol)

The reaction was treated with 6 mol of acetic acid to about pH until a precipitate formed. The solid was filtered off and the meal provided 86 mg of the desired product. Amino-pyrrolovenyl-Ceisopropylhydrogen Preparation. Fluorophosphate (PyBOP) Benzotriazol-1-yloxy ginsyl pyrrolidine hexafluorophosphate 08888.doc 200418452 (123 mg, 0.216 mmol) methylamine (10 ml, A 20% molar solution of THF) and a typical water DMF mixture of compound I5 (b) (86 mg, 0.216 mmol). The resulting reaction mixture was allowed to shake at room temperature for 30 minutes' and concentrated on a rotary evaporator. The crude solid was sonicated and dissolved in ethyl acetate. The solution was washed with water, dehydrated and concentrated. The crude product was purified by preparative hPLC (reverse phase C18, B / water, plus 4 drops of dimethylformamide to stabilize the product) to provide 20 mg of the title compound. Example 16 Preparation of phenyl) -5-isopropenyl-benzylpyran-3-methane ^ formamidine amine Preparation of fluoro-phenyl) -5-isopropoxy-benzocran-3- carboxylic acid).

Compound 6 (c) (18.5 g, 5.4 moles) prepared according to Example 6 was added to potassium hydroxide (9.1 g, 0.612 moles) in 1: 1 ethanol / water (200 ml). Stir the solution. After stirring at reflux temperature for 12 hours, the solvent was removed and the remaining slurry was dissolved in water and extracted with second butyl methyl ether. The organic layer was discarded, and the aqueous layer was acidified with 3 equivalents of hydrochloric acid. The solid was isolated by centrifugation, wet with water and hexane, and dried in a 60 ° C oven to provide 150 g (88%) of the desired product. Fluoro_phenyl) _5_isopropoxynitro_benzocran-3-acid acid). 88828.doc -70-

16 (b) 200418452 Pour a mixture of (4: 1) concentrated (70%) nitric acid (200 ml) and glacial acetic acid (50 ml) into an assembly thermometer, mechanical stir bar and solid addition funnel. One milliliter of chanterelles. The solution was cooled to 10 ° C in an ethanol / dry ice bath. through. Minutes, compound 16 (a) (100 g, 318 moles) prepared according to the previous step was added in portions. The reaction was allowed to stir at -10 ° C for 1 hour and then allowed to warm to 10 ° C over another 4 hours. The suspension was carefully poured into ice-cold water, and the precipitate was collected by filtration, washed thoroughly with water, and then air-dried. The yellow powder was a mixture of 16:84 with the 6-nitro isomer. The isomer was separated by recrystallization (150 ml of ethyl acetate plus 2 ml of hexane dropwise until clouded) to provide 8.2 g (72%) of the desired product as a yellow powder. c. 篁 AiL gold 16 (cK2- (4-fluoro-phenyl V5-isopropoxy-6-nitro-benzofuran-3-carboxylic acid formamide)).

Add 1-light benzotriazole (98% purity, 2.82 g, 20.9 mmol) followed by anhydrous dichloromethane (70 mL) to compound 16 in a 100 mL dry flask under dry argon (b) (5 grams, 13.9 mol). Then, 1- (3-dimethylaminopropyl) -3-ethylcarbonyldiimide hydrochloride (4 g, 20.9 mmol) was introduced. Finally, 88828.doc -71-200418452 methylamine solution (a THF solution with a concentration of 2 moles, 13.9 ml, 27.8 moles) was added to the slurry and stirred vigorously. The reaction mixture was allowed to stir at room temperature overnight. The reaction mixture was diluted with dichloromethane (120 ml) and washed with water (3x) and saline (3x). The organic layer was separated, dehydrated over magnesium sulfate, and filtered through a silicone pad, and wet with ethyl acetate. The organic layer was concentrated to provide 5.01 g (97%) of the desired product. d. Preparation of stealing compound 16idV6-amino-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine).

Ultrasonically add activated 10% Pd / c (200 mg, 10% by weight) to ethyl acetate (125 ml) of compound 16 (c) (2.0 g, 10.7 mmol) prepared according to step c above. Shaking suspension. The mixture was allowed to stir overnight in a Pair shaker at 50 psig hydrogen pressure. The reaction was then filtered through a CeliteTM tablet and wet with a 9: 1 ethyl acetate / methanol mixture. The filtrate was concentrated to provide 178 g (97%) of the pure expected product. Spring Example 17 Preparation of 6-Amino- 2- (4-fluoro-benzum) -5 -methoxy-benzylamine-flavor-3-methylsulfanilate a. Preparation of Chemical Society_ 物 17j ^ ( 2- (4-fluoro-phenyl) -5-methoxy-6-nitro-benzofuran-3-carboxylic acid).

88828.doc -72- 200418452 Intermediate compounds are essentially prepared according to the general method of Example 16, Step 骡 b, described above, 'but' instead of compound I6 (a) with compound 12 (c). Fluoro-phenyl) -5-methoxynitro-benzyl-3-benzylformamide).

To a suspension of compound 17 (a) (2.0 g, 6.04 mmol) in anhydrous dichloromethane (50¾ liter) was added methylamine (6¾ liter, 2 mol concentration thF solution), 1- [3 -(-Methylamino) propyl] -3 -ethyl dianimine hydrochloride (edci) (1.74 g, 9.06 ¾ mole) and rollylbenzotrimethylene (1 22 g, 9 · 〇 6 millimoles). The mixture was allowed to stir overnight. The reaction was quenched by the addition of water (100 ml) and diluted with monochloromethane (50¾ liters). The layers were separated and the aqueous layer was extracted with dichloromethane (3x). The combined organic layers were washed with water and saline, dehydrated with magnesium sulfate, and dried. The oil was triturated with Jijian / acetic acid (3: 1) to provide a yellow solid, which was filtered and air-dried. This reaction yielded 2.0 g (97%) of the expected compound. Preparation of D'yl (2- (41-yl-phenyl) -5-methyl-methyl-3-methylcarboxylate). The title compound is substantially prepared according to the general method of Example 16 and Step d described above, however, Compound 16 (c) is replaced by Compound 17 (b). Example 18 Fluoro-phenyl) -5diran_3_ borrowed from formamidine 88828.doc -73- 200418452 Diisopropylethylamine (83 · 2 μl, 477 μmol) was followed by To liver acetate (239 μmol) was added 6-amino-2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine prepared according to Example 17 (75 mg, 239 μmol) in anhydrous chloroform (3 ml). After 1 hour, the reaction was quenched with water (3 ml). After concentrating to dryness, the crude oil was purified by HPLC (reverse phase, C18, acetonitrile / water plus 0.1% acetic acid) to provide 73 mg (87%) of the title compound. Example 19 Preparation of 1- (4-Fluoro-Mosyl) -5-isopropoxy-6-methylamino-fluorene ## Succinimidine A 6-amino-2 to be prepared according to Example 16 -(4-Fluoro-phenylisopropoxy-benzofuran-3-carboxylic acid formamide (55 mg, 161 μmol) was dissolved in anhydrous acetic acid (2 mL). Triethylamine (25 μ Liters, 193 micromoles) was added to the reaction mixture, followed by the slow addition of dimethyl sulfate (17 microliters, 177 micromoles). After 2 hours, water (1 mL) was added. The reaction was concentrated to dryness and subjected to HPLC (reaction). Phase) Purified crude product 'provided 32 mg (56%) of the pure product. Example 20 A fluoro-phenylisopropylammonium-benzofuran-3 methanomethoxamine was borrowed from the title compound (35 mg , 59%) was essentially prepared according to the general method of Example 19, however, the equivalents of triethylamine and dimethyl sulfate were doubled. Example 21 Isopropoxy-6-methylij Lingolinaminodibenzo 6-Amino-2- (4-fluoro-phenyl) _5_isopropoxy88828.doc 200418452-Dongfuran-3 -Formamidine carboxylate (100 mg, 292 μmol) Anhydrous dihydrate dissolved in argon Methyl chloride (3 ml). Allow the reaction to cool to 0 ° C in an ice bath (: .pyridine (16.83 μl, 321 μmol) and sulfonyl chloride (22.61 μl, 292 μl under argon). Mol), and then added dropwise to the first aniline solution. The reaction mixture was allowed to warm to room temperature for 1 hour. The reaction mixture was diluted with water (20 mL) and extracted with dichloromethane (3 × 10 mL). The combined organic layers were washed with i-equivalent concentration HC1, water, saturated sodium bicarbonate aqueous solution and saline solution, and concentrated in vacuo. The crude product was subjected to column chromatography (silica gel, 20-50% ethyl acetate / hexane). Gradient) purification provided 68 mg (56%) of the product. 2- (4-Fluoro-phenyl) -5-isopropoxy-6-methanesulfonylamino-benzofuran-3-carboxylic acid The alternative preparation method of formamidine is as follows: a. Preparation. Compound 2l (a> l (3- (4-fluoro group_phenyl) _3_oxy. Ethyl propionate).

The thf (8.0 liters) of the unsalted salt (U8 kg, 9.28 mol) of the sulphuric acid was treated with magnesium chloride (0.68 kg, 7.14 mol) in a single treatment. The exothermic reaction was allowed to stir at 65 to 70 ° C for 6 hours and then overnight at room temperature. At the same time, a THF (3.7 liter) solution of fluoxamic acid (1.00 kg, 7.14 moles) was slowly added to a THF (37 #) mixture of carbonyldiimidazole (1.39 kg, 8.56 moles), and the mixture was added at 3 (TC Stir for 2 hours. Let the solution be mixed with 20 to 30 ° C of ethyl malonate over 1/4 hour and stir overnight at 30 ° C. Allow the mixture to cool to 20 ° C and dilute HC1 ( 4 equivalent concentration, 70 liters) and neutralized, and the water layer was removed. The solution was concentrated, and the product was collected by high vacuum distillation. 88828.doc -75-200418452 The resulting solution was dissolved in ethyl acetate and subjected to 5% hydrogen hydrogen Wet. Concentrate the organic layer and collect the desired product of 36 kg of colorless oil by distillation. Compound 21 (a) can also be prepared according to the following method: Toluene (7.20 g; Tributyl oxide (kg, 23.17 moles) flask. Stir the mixture, then add diethyl carbonate (6.61 kg, 55.96 moles) over 20 minutes. Let the reaction heat to> 7yc for more than! Hours. Let the reaction cool To the stolen, and add qi acetophenone (2.00 kg, 14.91 mole) over i hours Benzene (03 kg) wets. Makes the reaction

Stir at about 70 ~~ for another hour. The reaction was cooled to room temperature and stirred overnight. Add solution of hydrochloric acid and water (3.3 liters of 87 kg of concentrated sulfuric acid in water)

And let the reaction mix for 10 minutes. The layers were separated and the aqueous layer was wetted with water (20 liters) pan W sodium bicarbonate. The product was isolated by vacuum evaporation to provide 2.44 kg (80%) of the desired product. b. fluorofluoro_phenyl) _5_isopropyl-benzofuran_3_carboxylic acid ethyl ester).

/ P-phenylbenzidine (617 g, 5.7 mol) (3.6 liters) over a period of 6 hours / The mixture is added with 105C zinc chloride (778 ~ 81 g, about 5.7 mol) Ear) and compound 21 (a) (1200 g, 5.71 mol) in ethanol liters) solution, steaming thf 4 to maintain this temperature. After 1 hour 'the reaction was quenched with water / ethyl acetate (6 L / 8 L). Remove insoluble materials in an oven and wash the organic layer with water (3 liters) and concentrate to dryness. The solids were slurried in dichloromethane (2 liters) and filtered. 88828.doc -76- 200418452

1012 g of the desired product were obtained as a white solid. lR NMR m CDC13 (300 MHz): 8.02 (m5 2H); 7.51 (d5 iH J = 2.90 Hz); 7.38 (d, 1H); 7.16 (m, 2H); 6.88 (dd, 1H, J = 8 / 7〇 '2.79); 5.09 (s? IH); 4.40 (q? 2H5 J = 7.2 Hz); 1.40 (t? 3H? J.7 &gt; 2〇Hz) 0 Mass Spec: (M + l) = 301 . c. Disk making: Compound 21 (c). (2- (4-fluoro-phenyl) _5-isopropoxy_benzo-3-anthanoic acid ethyl ester).

A solution of compound 21 (b) (2.35 kg, 7.83 moles) in 1-methyl-2-pyrrolidone (8.3 liters) was treated with cesium carbonate (5.10 kg, 15.65 moles) for 10 minutes. Add 2-bromopropane (2.98 kg, 24.26 moles) and allow the reaction mixture to heat at 50 ^ overnight. The reaction was added with dilute ammonium hydroxide (18 liters) and stirred for 30 minutes. The mixture was diluted with water (11.8 liters) and extracted with heptane (14.7 liters). The layers were separated and the organic layer was wetted with water. Concentration by rotary evaporation provided a product that would solidify and produce quantitative yields. NMR in CDCI3 (300 MHz): 8.02 (m? 2H); 7.56 (d5 1H? J = 2.34 Hz); 7.40 (d? 1H? J = 8.79 Hz); 7.16 (t? 2H5 J = 8.79 Hz); 6.95 (dd5 1H, J = 8.79 Hz); 4.59 (m? 1H); 4.41 (q? 2H? J = 7.03) and 1.39 (m, 9H). Mass Spec: (M + l) = 343. d. Compound 21 (d) (2- (4 • fluoro-phenyl) -5-isopropoxy-6-nitro-benzofuran-3-carboxylic acid ethyl ester).

88828.doc -77- 200418452 At approximately 20 ° C, slowly add a solution of compound 21 (c) (2.68 kg, 7.83 moles) in chloroform to a mixture of cold chloroform (13.4 kg) and 70% nitric acid (6.7 kg). . After 1 hour, the reaction mixture was cooled to room temperature and diluted with water (8.6 liters). The organic layer was separated, washed and concentrated to a solid. The crude product was mixed with tributyl methyl ether and stirred for 1 hour. The solid was collected by filtration, wetted with heptane, and dried to provide 2.43 g (80%) of the desired product. lR NMR in CDC13 (300 MHz): 8.05 (m5 2H); 8.00 (s? 1H)

7.76 (s, 1H); 7.20 (m, 2H); 4.71 (septuplet, 1H, J = 6.00 Hz); 4.42 (q, 2H, J = 7.20 Hz); 1.45 (d, 6H, J = 6.00 Hz); 1.41 (t, 3H J = 7.20 Hz) 0 Mass Spec: (M + l) = 388 0 e. Preparation of compound 21 (ei (6-amino-2- (4-fluoro-molyboxypropyl) _ Benzofuran-3-carboxylic acid ethyl ester).

Compound 21 (d) (285.10 g, 0.736 mol) was combined with isopropyl acetate (1 liter) in a thick-walled Parr tube. 10% Pd / C (16.51 g) was carefully moistened with isopropyl acetate (1200 ml) and washed into a Parr tube. The reaction mixture was hydrogenated in a Parr shaker with 0-50 psig hydrogen pressure until hydrogen absorption ceased. The mixture was filtered through CeliteTM and moistened with isopropyl acetate (1 liter). The filtrate was concentrated by rotary evaporation and the remaining wet solids were separated. The above reaction was repeated using 287.52 g (0.74 mole) of compound 21 (d), 16.67 g of 10% Pd / C and 1200 ml of isopropyl acetate. The products were combined and used directly in the next step 88828.doc -78- 200418452. Alas. f. Preparation of compound 2-1. (f) (2- (4-fluoro-phenyl-isopropoxy-6-methanesulfonamido-benzofuran-3-carboxylic acid ethyl acetate).

Compound 21 (e) (about 1.48 moles) was dissolved in dichloromethane (5.6 liters) and cooled in an ice / ethanol bath. Methanesulfonyl chloride (186 · 27 g, 1.63 moles) was added in one portion 'followed by diisopropylethylamine (2,016 g, 1.63 moles) dropwise over 25 minutes. The final reaction was allowed to warm to room temperature and was stirred under nitrogen for about 36 hours. The reaction was distinguished between water (2 liters), the layers were separated, and the organic layer was wetted with water (3 X 2 liters). The combined aqueous layers were back-extracted with dichloromethane (500 ml), and the organic layers were combined. The organic layer was concentrated by rotary evaporation. During the concentration period, after the product started to form a precipitate, ethanol was slowly added. After the dichloromethane was removed, the mixture was diluted with tert-butyl methyl ether (500 ml). The product was isolated by filtration and air-dried to provide a mixture of 603.1 g of product (90,8%) and disubstituted amine (8.9%). ! H NMR in DMSO (300 MHz): 9.00 (s, 1H); 8.05 (m? 3H); 7.60 (s? 1H); 7.53 (s? 1H); 7.39 (dd? J = 8.8 &amp; 8.8 Hz? 2H); 4.73 (septet, J = 5.9 Hz, 1H); 4.32 (q, j = 7 〇hz, 2H); 3.00 (s, 3H); 1.37 (d, J = 5.9 Hz, 6H); 1.32 (t, J = 7.0 Hz, 3H). g. Preparation of compound 2irgV2-r4-i [fluorene-ynon) 5 $ propoxy-6-methane (continuous amino-benzo-benzoan-3-acid). 88828.doc -79- 200418452

Compound 21 (f) (570 g) was added with a solution of ethanol (6 liters) and i-equivalent concentration of 0.001 (6 liters). This solution was slowly heated to Naida for several hours. The heat source was then removed and when the mixture reached approximately 50 ° C, a 6 equivalent concentration was added] to approximately pH 2. The mixture was allowed to stir for about 15 minutes, and the solid was quickly separated by filtration, and wetted with 50/50 ethanol / water (500 mL), then water (500 mL). The solid was dried in a vacuum oven to provide 513 grams of the desired product. H NMR m DMSO (300 MHz) Compound 21 (g), substantially as described above: 8.97 (s, 1H); 8.05 (m, 2H); 7.58 (s, 1H); 7.54 (s, 1H); 7. · 38 (dd, J = 8.8 &amp; 8.8 Hz, 2H); 4.69 (septet, J = 5.9 Hz, 1H); 2.99 (s, 3H); 1.35 (d, J = 5.9 Hz, 6H). h.l_ 备 化 _ Compound 21 (M (2_ (4-fluoro-phenyl) _5_isopropoxy-6-methanesulfonylamino-benzofuran-3-3-methanomethamine ). Should

21 (h) Compound 21 (g) (440.7 g, 1.082 mol) was mixed with dichloromethane (4.4 liter) 'and stirred under argon. Add carbonyldiimidazole (236 8 g, 1.46 mol) in one portion. Allow the mixture to stir for 2 hours, then cool in an ice / ethanol bath. In 15 minutes, 88828.doc -80-THF of methylamine mole concentration precooled in an ice / ethanol bath; each solution (705.2 g, 1.6 mole) was added to the reaction. Allow the reaction to stir at room temperature. The reaction was cooled by ice (500 grams) and water (2 liters). Next, add HC1 until pH 2. The layers were separated and the organic layer was washed with water (2 x 2 liters). The combined aqueous layers were extracted with monochloromethane. The organic layers were combined and evaporated to remove volatiles. Ethanol (1 liter) was added after solids started to form. When the crystallization started, a 5% water (1 liter) solution was added. The mixture was cooled to room temperature and stirred overnight. The solid was isolated by centrifugation, wet with 20% water in ethanol (1 liter), and dried to provide 380.75 g of the desired product. Example 22 Meeting Example 23 6-Ethylamino-2- (4-fluoro-phenyl) _5-isopropoxy_benzofurancarboxylic acid formamidine and 6-ethylethyl-2- Preparation of (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine mono-aryl propylethylamine (407 μl, 2.34 mmol) and chihua Ethyl alcohol (187 liters, 2.34¾ moles) was added to the amino-2- (4-fluoro-phenyl) -5-isopropoxy-benzofurancarboxylic acid formamidine (made in Example μ) 200 mg, 584 μmol) of anhydrous acetonitrile (8 ml). The reaction was detected by analytical LC / MS conditions, and water (4 ml) was added to stop the heat. After concentrating to dryness, the crude product was purified by preparative hplc (reverse phase C18, acetonitrile / water plus 0.1% acetic acid) to provide 97 mg (45%) of 6-ethylamino-2- (4-fluoro group) -Phenyl) -5-isopropoxy-benzocran_3-methanemetamide and 63 mg (27%) of 6-diethylamino-2- (4-fluoro-phenyl) ) -5-isopropoxy-benzoanan-3-methanoic acid total amine. Example 24 Preparation of 2- (4-fluoroyl-phenyl) -5-isopropoxy-6-morpholin-4-yl-benzofuran_3-acid methylformamide 88828.doc -81 -200418452 a. Compound A-compound bromo-2- (4-fluoro-benzene grave) -5-isopropoxy-benzofuran-3-polyacid).

Bromine (pure, 1.1 ml, 20.70 mmol) was added dropwise over 30 minutes to 30-watt compound 16 (a) (5.0 g, 0.016 mole) of 1,4-dioxane ( 160 ml) of stirred solution. After stirring for an additional 20 minutes, the reaction mixture was mixed with water and extracted with ethyl acetate. The organic phase 'was washed with water and brine, dried over MgS04, and concentrated under reduced pressure to give a yellow solid. The product was developed by sintering with 30% ethyl acetate and yielded 4.1 g (66%) of the desired product as a white solid. b. Compound 24 (b) (6-bromo-2- (4-fluoro-phenylisopropoxy-benzofuran-3-carboxylic acid formamidine).

Benzotrifluoren-1-yloxysamidine pilolidene hexafluoroscale salt (10.79 g, 20.76 mmol) and methylamine (43.0 ml, 86 mmol) (200 mmol) Ear; Chendu's THF solution) was added to the DMF (10.0 ml) solution of the character 24 (a) (6.8 g, 17.3 mmol) in the gas prepared according to the previous steps. After stirring at room temperature for 12 hours, the reaction mixture was treated with water and extracted with ethyl acetate 88828.doc -82- 200418452. The organic layer was washed with water and saline, dehydrated with MgSO and concentrated under reduced pressure. The crude product was purified by column chromatography (silica gel, 50 to 100% ethyl acetate / hexane) to give 6.5 g (92%) of the desired product as a white solid. c. 2_z £ 4-Fluoro-benzene V5-isomorpholine_4-yl-benzowazine-3-methanoic acid formamidine. Compound 24 (b) (120 mg, 0.30 Millimoles), ginseng (diphenylmethyleneacetone) dipalladium (54 mg, 0.0059 millimoles) and (2-dicyclohexylphosphine_2, _ν, ν_dimethylamino) -diphenyl Base (3.0 mg, 2.4 mole%) was added to an oven-dried 100-pen round bottom flask. The flask was sealed with a rubber compartment, degassed and purged with argon. Morpholine (31 microliters, 0.35 millimoles) and lithium bis (trimethylsilylfluorenamine) (650 microliters, 0.65 millimoles, τΗρ solution in molarity) were added to the reaction mixture. Quickly remove the compartment and place the reflux condenser in the flask. The reaction flask was degassed again and washed with argon. The reaction mixture was then heated to 65 ° C for 12 hours and cooled to room temperature. Add molar concentration of hydrochloric acid (600 μl) and stir the reaction mixture for 5 minutes before passing through small pieces of CeliteTM. The filtrate was diluted with water and extracted with ethyl acetate. The organic layer was washed with water and saline, dehydrated with MgSO and concentrated under reduced pressure. The crude product was purified by column chromatography (silica gel, 20-40% ethyl acetate in hexane) to provide 70 mg (57%) of the desired product as a white solid. Example 25 Mr. Oxy-4-methyl-2-phenyl-benzoylamine compound 25 (a) (4-Ao-5-hydroxy-2-phenyl-benzofuran_3_carboxyl Acid ethyl ester). 88828.doc »83-

200418452 A mixture of CS2: CH3CN (3: 1) (8,0 ml) in argon was dissolved in compound 2 (a) (450 mg, 1.595 mmol) prepared according to Example 2. The solution was cooled to 0 ° C and N-bromosuccinimide (312 mg, 1.755 mmol) was added in one portion. The reaction was allowed to stir at 0 ° C for 4 hours and then cooled to room temperature. The solvent was evaporated, and the residue was dissolved in ethyl acetate, washed with water and a saline solution, dried over MgS04, and concentrated under reduced pressure. The crude product was purified by HPLC (silica gel, dissolved with 10-100% ethyl acetate in hexane) to provide 396 mg (69%) of the desired product. b. Preparation of compound 25 (bK4-bromo-5-methoxy-2-phenyl-benzofuran-3-carboxylic acid ethyl ester).

Under argon, potassium carbonate (3 65 mg, 2.638 mmol) and potassium iodide (1.3 ml, 21.1 mmol) were added to compound 25 (a) (380 mg, 1.055 mmol) in acetonitrile ( 5.0 ml) solution. After stirring for 4 hours under reflux, the reaction mixture was cooled to room temperature, diluted with water and extracted with ethyl acetate. The organic layer was washed with water and saline, dehydrated with MgS04, and concentrated under reduced pressure to provide 385 mg (98%) of the desired product. c. Preparation of gold compound 25 (5-methoxy-4-methyl-2-phenyl-benzofuran-3-88828.doc -84- 200418452 ethyl carboxylate).

Under argon, compound 25 (b) (30 mg, 0.082 mmol) and Ag20 (46.5 mg, 0.201 mmol), methyl W acid (6.0 mg, 0.0884 mmol), K2C03 ( 34.0 mg, 0.246 mmol), 1,1-bis (diphenylphosphineferrocene) dichloropalladium (II) and dichloromethane complex (1: 1) (Pd (dppf) Cl2) (6.0 Mg, 10 mole%) and THF (degassed, 1.0 ml) in a tube. The pressure tube was sealed, and the reaction mixture was stirred at 80 ° C for 12 hours, cooled to room temperature, and cooled with a mixture of 30% H202 (5 ml) and 10% NaOH. The reaction mixture was diluted with water and extracted with ethyl acetate. The organic phase was washed with water and saline, dried over MgS04, and concentrated under reduced pressure. The crude product was purified by reverse phase HPLC to provide 16.9 mg (64%) of the desired product. d. Preparation of compound 25 (dK5-methoxy-4-methyl-2-phenyl-benzofuran-3-carboxylic acid).

25 (d) Compound 25 (c) (16.9 mg, 0.0545 millimoles) was dissolved in ethanol (2.0 milliliters) and 12 mol NaOH (200 microliters) was added. The reaction was heated to 100 ° C for 6 hours and cooled to room temperature. The solvent was evaporated under reduced pressure. The residue was checked in water, acidified with 10% HC1 aqueous solution, and extracted with ethyl acetate. The organic layer was washed with water and 88828.doc -85- 200418452 salt solution, dehydrated with MgS04, and concentrated under reduced pressure to provide 13.5 mg (87%) of the desired product. Of 4-methylmethylformamide carboxylate

A solution of bromo-ginsyl-pyrrolidinyl-quat hexafluorophosphate (PyBrOp) (25 (mg), 0.1 (26 mol) and methylamine (0.5 ml, 2.0 mol concentration of TMP) ) Add the compound 25 (d) (13.5 mg, 0.479 mmol) in DMF (1.0 pen liters)) argon under argon. After stirring at room temperature for 2 hours, the reaction mixture was treated with water and extracted with ethyl acetate. The organic layer was washed with water and saline, dehydrated with MgS04, and concentrated under reduced pressure. The crude product was purified by column chromatography (silica gel, ethyl acetate / hexane) to provide 9.0 mg (64%) of the title compound. Example 26 1xyl ij ·-, dynyl · benzyl _3 _ read chloridamine Ningbei L gas pass ― compound 26 (a) (acetic acid 4-cyano-2-phenylethynyl- Phenyl ester).

Add 1,4-dioxane (2.5 ml, anhydrous) to Cul (8.0¾: g, 2 mole%) and dichlorobis (benzonitrile) (n) ( 24 mg, 3 mole%) of the stirred suspension, and often washed with argon. In a syringe, tris-tertiary-butylphosphine (542 μl, 0.25 mol concentration of 4-dioxane solution), diisopropylamine (350 μl, 4.17 mmol), bromoacetate The cyano-phenyl ester (500 mg, 2.08 mmol) and phenylacetylene (254 mg, 2.71 mmol) were added to the stirred reaction mixture. The reaction mixture was allowed to stir for 6 hours, then diluted with ethyl acetate 88828.doc • 86-200418452 and passed through a small piece of silicone. The filtrate was concentrated and the crude product was purified by column chromatography (silica gel, dissolved with 5-20% ethyl acetate in hexane) to provide 390 mg (72%) of the desired product. b. Preparation of compound 26 (b) (4-hydroxy-3-jasmine ethynyl-benzonitrile).

Potassium carbonate (309 mg, 2.24 mmol) was added to a solution of compound 26 (&amp;) (390 mg, 1.49 mmol) in methanol (10.0 ml). The reaction mixture was stirred at room temperature overnight, and then the solvent was evaporated to dryness under reduced pressure. The residue was treated with water and extracted with ethyl acetate. The organic layer was washed with water and saline, dehydrated with MgS04, and concentrated under reduced pressure. The crude product was purified by column chromatography (silica gel, dissolved in 5 to 25% ethyl acetate in hexane) to provide 180 mg (55%) of the desired product. c. Preparation of compound 26 (cV5-cyano-2-benzyljamopyran-3-boronic acid methyl ester).

Let compound 26 (b) (100 mg, 0.4566 mmol) be mixed with thiourea (2.0 mg, 5 mole%), CBr4 (378.5 mg, 1.141 mmol), cesium carbonate (445 mg, 1.3 67 millimoles), tritium 412 (8.2 mg, 5 mole%) and methanol (2 mL). The reaction mixture was treated with a stream of carbon monoxide at room temperature for 5 minutes and 45 ° C for 10 minutes. Continue stirring at 45 ° C under carbon monoxide pressure (balloon) overnight. The reaction mixture was then passed through small pieces of silicone and moistened with ethyl acetate 88828.doc -87- 200418452. The filtrate was concentrated and the crude product was purified by column chromatography (hard gum, dissolved with 5 to 10% ethyl acetate in hexane) to provide 74 mg of 60:40 compound 26 (c) and 2-phenyl- A mixture of benzofuran-5-carbonitrile. d. Preparation of Compound 26 (d) (5-Amino-2-Deryl-Deropentosulfuric Acid).

26 (d) A mixture of the above compound 26 (c) and 2-phenyl-benzocystan-5_carbonylnitrile (74 mg) was dissolved in ethanol (2.0 ml) and subjected to a concentration of 12 mol NaOH (2 〇〇μΙ) for processing. The reaction was heated to 50 ° C for 6 hours, then cooled to room temperature, and the solvent was concentrated under reduced pressure. The residue was dissolved in water, acidified with 10% HC1 aqueous solution, and extracted with ethyl acetate. The organic layer was washed with water and saline, dehydrated with MgS04, and concentrated under reduced pressure. The crude product was purified by column chromatography (silica gel, eluting with 30-40% ethyl acetate / hexane) to yield 30 mg (25% yield from step c_d) of the desired product. e. The target product (16.G mg, 51%) of Olyl-2-benzyl-benzofuramine was essentially made according to the method of Example 25 and the procedure 'However', the compound 25 was substituted for the compound 25 '& lt ^ 1127 A plate of pyridin-4-yl-methyl methanoate prepared with isopropyloxy). h3ct

OH

XX 27 (a) 88828.doc -88- 200418452 Add 2-iodopropane (27.22 ml, 0.27 mole) to terephthalic acid (30 g, 0.27 mole) in ethanol (30 Ml), and the reaction mixture was heated to 60 ° C. Dissolve potassium hydroxide (15.3 g, 0.27 mole) in water (50 ml) 'and add the reaction mixture dropwise over 1 hour. After it was stirred at 60 ° C for 5 hours, the mixture was cooled to room temperature, and the solvent was removed under reduced pressure. The residue was acidified with 6 equivalents of HC1 and extracted with ethyl acetate. The organic layer was washed with water and saline, dehydrated with MgSO and concentrated. The crude product was purified by column chromatography (crushed gel, dissolved in ethyl acetate / hexane of 10 to 3) to yield 20.3 g (49%) of the desired product. b. Preparation of compound 27 (b) i2-bromo-4-isopropoxy-phenol).

1 Bromosuccinimide (5.85 g, 0.033 mole) was added to a stirred solution of compound 27 (a) (5.0 g, 0.033 mole) in carbon disulfide (132 ml). The reaction mixture was allowed to stir at room temperature for 2 hours, and then the solvent was evaporated to dryness under reduced pressure. The residue was treated with water and extracted with ethyl acetate. The organic layer was washed with water and saline, dried over MgSO and concentrated. The crude product was purified by column chromatography (silica gel, eluting with ethyl acetate / hexane at 5-10%) to yield 4.65 g (61%) of the desired product. c. Preparation of compound 27 (c) 2-bromo-4-isopropoxy-phenylacetate acetate).

27 (c) 〇-89-88828.doc 200418452 Add 4-dimethylaminopyridine (catalytic) and triethylamine (69 ml, 0.050 mole) to compound 27 (b) (4.6 g , 0.02 mmol of methylene chloride (20 ml). The reaction mixture was allowed to stir for 10 minutes, and then acetic anhydride (4.5 pen liters, 0.48 moles) was added. After stirring for 4 hours, water was added to the reaction mixture. The mixture was extracted with ethyl acetate, and the organic layer was washed with water and brine, dried over MgS04 and concentrated. The crude product was purified by column chromatography (silica gel, eluting with 0 to 10% ethyl acetate / hexane) to yield 4.75 g (87%) of the desired product. Ken "27 (d) (4-trimethylsilylethyl-pyridine).

JH3 H3C Si CHj-

27 (d)

Compound 27 (d) (2.4 g, 53%) was substantially prepared according to the general method described in Example 26, Step 骡 a. However, 4-bromoanedian hydrochloride and (trimethylsilyl) were used. Acetylene replaces 2-bromo-4-cyano-phenyl acetate and phenylacetylene. Preparation of gA compound 27 (e) (4-ethynyl-pyridine).

27 (e) Potassium hydroxide (21.0 mg, 3.0 mole%) was added to a solution of compound 27 (d) (2.2 g 0.0126 mmol) in degassed methanol (80 ml). After stirring for 30 minutes, water was added and the mixture was extracted with dichloromethane. The organic layer was washed with water and saline 88828.doc -90- 200418452, dehydrated with MgSO4, and concentrated to give 640 mg (53%) of the desired product. f. Preparation of compound 27 (f) (isopropyloxy-2-pyridylethylethyl-phenylphenyl).

27 (f) δ Compound 27 (f) (564 mg, 61%) is substantially prepared according to the general method described in Example 26, Step 骡 a, however, Compound 27 (c) and Compound 27 (e) are substituted 2-bromo-4-cyano-phenyl ester and phenylacetylene. g. Preparation of compound 27 (g) (4-isopropoxy-2-pyridin-4-ylethoxy-phenol).

Hydrazine (9.5 ml, 0.5 mole solution in THF) was added to a stirred solution of compound 27 (f) (564 mg, 1.91 mmol) in THF (3.0 ml). Stir: After 30 minutes, add water and extract the product with ethyl acetate. The organic layer was washed with water (3 x 100 ¾ liters) and brine ', dehydrated with MgSO and concentrated to provide 470 mg (97%) of the desired product as a white solid. h. Preparation of compound 27 (h) (5-isopropoxy-2-p ratio yodo-4-yl-benzofuran-3-carboxylic acid methyl ester).

88828.doc -91-200418452 Intermediate compound (430 mg, 74%) is essentially prepared according to the general method described in Example 26, step • flc, however, compound 27 (g) is substituted for compound 26 (b) . Oxygen-benzylfuran-3- # acid formamidine production 0. Bell hydroxide (540 mg) and water (ι · mL) were added to compound 27 (g) dissolved in dioxane (200 mg, 0.644 mmol). The reaction mixture was allowed to stir at 80 C for 12 hours. The mixture was cooled to room temperature, and the solvent was concentrated under reduced pressure. The residue was dissolved in water, brought to pH 7.0 with 10% HC1, and extracted with ethyl acetate. The organic layer was washed with water and saline, dehydrated with MgSO and concentrated under reduced pressure to provide 130 mg (68%) of the acid. The above-mentioned acid (65 mg, 0.22 mmol), benzotriazol-1-yloxy, and hexafluorophosphate (PyBOP) (148 mg, 0.284 mmol) were dissolved in DMF (0.5 ml) and methylamine (2.2 ml, 2.0 Molar THF solution). After stirring for 12 hours, water was added and the crude product was extracted with ethyl acetate. The organic layer was washed with water and saline, dehydrated with MgSCU and concentrated. The crude product was purified by column chromatography (silica gel, dissolved in 0 to 5% methanol / ethyl acetate) to provide 65 mg (96%) of the title compound. Example 28 6- (3,5-Dimethyl-isopent-4-yl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine Preparation of amines a. Prepare compound 28 (a) (2- (4-fluorophenyl) -5-methoxymethoxybenzo-3-carboxylic acid ethyl ester).

88828.doc -92- 200418452 Compound 21 (b) (50.0 g, 0.167 mol, prepared according to the general method described in Example 21) Anhydrous 1-methyl-2-pyrrolidine under argon Ketone (176 ml) while mechanically stirring. Once homogenized, cesium gallate (108.8 g, 0.334 mol) was added in portions over 5 minutes. Methane iodide (32.2 pen liters, 0.516 mol) was added over 5 minutes. The reaction was heated to 50. 〇 reached 1 $ hours, then chrysanthemum 1 temperature to concentrated ammonium hydroxide (39 ml), and stirred for 30 minutes. The mixture was diluted with heptane (1000 ¾ liters) and washed with water (3 x 1000 ml). The combined organics were dehydrated over magnesium sulfate and evaporated to dryness. The resulting solid was stirred in hexane for 18 hours, filtered and dried. Because the reaction was not complete (known by the proton nmr), the separated solid was treated with anhydrous ^^-: pyrrolidone (176 ml). Once homogenized, cesium carbonate (400 g, 0123 mol) and methane iodide (20.0¾ liter, 0.321 mol) were added. The reaction was reheated to utah for u hours, cooled to room temperature, diluted with ammonium hydroxide (24 mL), and disturbed for% minutes. The mixture was diluted with water (1-mL) and extracted with tert-butyl methyl acid (3X3GGU). The combined organics were washed with water (3 ml) and dehydrated over magnesium sulfate. After evaporation of the solvent, the product was crystallized from hot heptane to provide M "g (61%) of the desired product as a brown solid. b. Lifluorophenylmethoxybenzofuran-3.carboxylic acid).

0.112 Compound 28⑷ (32 g, (U02 Molar) and 4 oxidized (63 g 88828.doc -93- 200418452 Molar) was combined in ethanol (80 ml) and water (80 ml). Let this The reaction mixture was gently refluxed overnight. Analysis by TLC showed that the reaction was incomplete, so an additional amount of potassium hydroxide (2.0 g, 0.035 mol) was added. After 1 hour, the solvent was evaporated to half the volume. Water (400 ml) The solution was diluted and extracted with ethyl acetate (2 × 300 ml). The aqueous solution was acidified with 3 molar HC1 and the resulting precipitate was filtered, washed with water and dried to provide 28.9 g (99%) of the product as a white solid. c. Preparation of compound 28 (c) (6-bromo-2- (4-fluorophenyl) -5-methoxybenzofuran-3-metanoic acid).

Compound 28 (b) (28.9 g, 0.101 mole) was dissolved in anhydrous, 4-dioxane (725 ml) under argon. The resulting solution was degassed in a gas dispersion tube under argon for 10 minutes. Bromine (8.8 ml, 0.170 mol) was added dropwise via a syringe over 45 minutes. After the addition was complete, the reaction was allowed to stir at room temperature for 30 minutes. An additional amount of bromine (0.5 ml, 0.01 mole) was added dropwise over 5 minutes. The mixture was diluted with ethyl acetate (1800 ml), washed with water (5 X 350 ml), and dehydrated with sodium sulfate. The solvent was evaporated and the remaining solid was dissolved in ethyl acetate (250 mL). The solvent was removed by evaporation again. The dissolution in ethyl acetate and subsequent evaporation steps were repeated until the solvent was colorless. The resulting solid was sonicated in 80/20 hexane / ethyl acetate (500 ml), and the crude product was isolated by filtration. The mash was concentrated, and the resulting solid was sonicated in an 80/20 hexane / ethyl acetate mixture (300 ml). The solid was isolated by filtration and the 88828.doc -94- crude product was combined. The solid was washed with a 95/5 hexane / ethyl acetate mixture (100 ml) and then was taken as hexane. The solid was dried under vacuum to provide 28.4 g (77%) of the desired product as a brown solid. d. 6-bromo-2- (4-fluorophenyl) -5-methoxybenzyfuran-3-carboxylic acid methyl ester).

Add ground potassium carbonate (40.6 g, 0.294 mole) and methane iodide (92.0 ml, 1.47 mole) to compound 28 (c) (53.6 g, 0.147 mole, which can be made according to the previous steps) The solution was stirred off with methyl-2-pyrrolidone (1000 ml). The reaction mixture was allowed to stir at 50 ° C for 18 hours. Upon cooling, the reaction was diluted with water (2200 ml) and extracted with ethyl acetate (5 x 600 ml combined organics, washed with water (3 x 1000 ml) and dehydrated over magnesium sulfate. The solvent was evaporated and the crude product was allowed to Purified by 90/10 hexane / ethyl acetate mixture sonic soup for 1 hour. Filtered to remove solids, washed with hexane and dried in vacuo to provide 47.4 g (125 moles, 85%) of the desired product as a white solid. El compound 28 (en6- (3.5-dimethylisoxazol-4-yl) -2- (4-aminobenzyl) -5-methoxy-benzofuran-3-carboxylic acid methyl ester) .

88828.doc &gt; 95- 200418452 Under argon, compound 28 (d) (12.0 g, 0.03 16 mole) was dissolved in toluene (900 ml), ethanol (420 ml) and water (24 ml) . The resulting solution was degassed in a gas dispersion tube with argon for 10 minutes. Add sodium carbonate (8.37 g, 79 0 mmol), 3,5-dimethylisoxazole-4-_acid (6.69 g, 47.5 mmol) and tris-triphenylphosphine-palladium (〇) ( 1.83 g, 1.58 mmol), and the reaction was allowed to reflux gently for 21 hours. The solvent was evaporated and the reaction was diluted with ethyl acetate (500 ml) and water (300 ml). The layers were separated and the organic phase was washed with water (2 X 500 ml). The washings were combined and extracted with ethyl acetate (300 ml). The organics were combined, washed with saline and dehydrated with magnesium sulfate. The solvent was evaporated and the crude product was purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 10.4 g (83%) of the desired product as an off-white solid. Compound 28 (TV6-H.5-dimethylisoxazol-4-yl) -2- (4-fluorophenyl) -5-methoxybenzofuran_3 • carboxylic acid).

Combine compound 28 (e) (10.4 g, 26.3 mmol) with potassium hydroxide (5.90 g, 105 mmol) in ethanol (500 ml) and water (500 ml), and Gently reflux for 4 hours. After cooling, 2/3 of the solvent was evaporated and diluted with water (300 mL). The solution was filtered through a piece of CeliteTM 503 to remove a small amount of 1 bar from the previous step. The solution was acidified with 6 mol HC1, and the precipitate was filtered, washed with water and hexane, and partially dried under vacuum to provide the desired product as a white solid. The unpurified product was used directly in the next step. 88828.doc -96- 200418452 One base isoxazolyl-4-one) -2-ί4-fluorobenzyl) _5 · methylazine benzoxanthine methylformamide)). Let compound 28 (f) (10.0 g, 0.0262 mole), benzotrisol-1-yloxypyrrolidinyl hexafluorophosphate (PyBOPKMj g, 0.0315 mole) and methylamine (131 ml, Molar concentration of THF solution, 0.262 Molar) was combined in DMF (16 liters). The reaction was allowed to stir at room temperature under argon for 8 hours. The solvent was evaporated and the resulting solid was dissolved in ethyl acetate (250 ml) and water (300 ml). The layers were separated and the aqueous phase was extracted with ethyl acetate (4 × 200 mL). The organics were combined, washed with water (3 × 150 ml) and saline (300 ml), and dried over magnesium sulfate. The solvent was evaporated and the crude product was mixed with a 90/10 hexane / ethyl acetate (100 mL) mixture. The mixture was filtered and the solid was washed with hexane and dried in vacuo to provide 8.16 g (79%) of the desired product as a white solid. The crude product was later purified by crystallization (hot ethanol and water) after combining several batches of other compounds to provide the title compound as a white needle. Example 29 Preparation of 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5-methoxy-benzofuran-3-carboxylic acid formamide Compound, 2.9. (A) (2- (4-fluoro-phenyl) -5-acryl-6-methanesulfonylamino-benzofuran-3-carboxylic acid formamidine).

Boron trichloride (60 ml of a 1 molar solution of dichloromethane) was added in 10 minutes 88828.doc -97- 200418452 to 2- (4-fluoro-phenyl) -5-isopropoxy-6 -Methanesulfonylamino-benzofuran-3-methanoic acid formamidine (7.10 g, 16.9 mmol, prepared by one of the methods described in Example 21) methylene chloride (200 ml) . The mixture was allowed to stir for 20 hours, then carefully stopped at 1 equivalent of HC1 (10 mL). An additional 4 equivalents of HC1 (100 ml) was added and the mixture was allowed to stir for 24 hours.漉 The precipitated solid was removed, washed with water, dried and triturated with ethyl acetate / hexane to provide 6.39 g (100%) of the desired product as a white solid. b. Preparation of 1: 14-fluoro-phenyl) -6- (a-yuan berberine-methyl-amine) -5-methylhydroxanthran-3- # acidamine. Potassium carbonate (0.30 g, 2.17 mmol) and methane iodide (0.10 ml, 161 hamol) were added to compound 29 (a) (0.11 g, 0.291 mmol). Made of) 2-butanone (20 ml) solution. The reaction mixture was refluxed for 1 to 2 hours, then cooled to room temperature and concentrated. The crude product was dissolved in ethyl acetate and washed with 1 molar hydrochloric acid. The organic layer was concentrated and the product was purified by flash chromatography (stone gum, ethyl acetate / hexane gradient) to provide 73 mg (620/0) of the desired product as a white solid. Example 30 2- (4-Fluoro-phenyl) -5-boryl- (4-methoxy-neoxy) -6-morpholin-4-yl-benzofuran-3-carboxylic acid methyl ester Preparation of amidamine a. Preparation of compound 30 (aK2- (4-fluoro-phenyl) -5-hydroxy-6-morpholinyl-benzoanan-3 -metamic acid amine).

88828.doc -98- 200418452 Boron trichloride (1 mol xylene solution, 50 ml, 50 mmol) was added to 2 彳 4-fluoro group dissolved in dichloromethane (30 ml). -Phenyl) -5-isopropoxy-6-morpholin-4-yl · benzobenzo-3-carbamate (0.71 g, 1.7 mmol) Made) solution. The reaction mixture was refluxed for 30 minutes and allowed to cool to room temperature. The reaction mixture was cooled with 1 molar hydrochloric acid (10 ml) and stirred for 1 hour. Remove organic matter from the hair and add a saturated solution of bicarbonate steel until ρΗ = 8-9. The product was extracted with ethyl acetate and purified by column chromatography (anhydrous loading on silica gel, ethyl acetate / hexane gradient) to provide 0.53 g (84%) of the desired product. b. U4-Fluoro-jamo) -544-methylamidino-pyridyl) -6-morpholine-4-even- and the preparation of sulfan-3- # acid formamidine. Potassium carbonate (0.40 g, 2.89 mmol) and 4-methoxybenzyl chloride (0.20 ml, 1.47 mmol) were added to compound 30 (a) (0311 g, 0.84 mmol) ) In acetonitrile (20 ml). The reaction mixture was refluxed for 12 hours, cooled to room temperature and concentrated. The crude product was dissolved in ethyl acetate and washed with 1 mole hydrochloric acid. The organic layer was concentrated and the product was purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 296 mg (72%) of the desired product as a white solid. Example 3 1 2- (4-Fluoro-phenyl) -6- [methanesulfonyl- (4-methoxy-benzyl) -amino] _5_ (4-methoxy-benzyloxy)- Preparation of benzofuran-3-carboxylic acid formamidine Potassium carbonate (0.040 g, 0.285 mmol) and 4-methoxyfluorenyl chloride (0.026 ml, 0.190 mmol) are added to compound 29 (a) (0.036 Grams, 0.095 millimoles' can be prepared according to the above Example 29, step a) 2-butanone (10 ml) solution. The reaction was allowed to stir at 20 ° C for 72 hours. The reaction mixture was concentrated, and the crude product 88828.doc -99- 200418452 was dissolved in ethyl acetate and washed with 1 molar hydrochloric acid. The organic layer was concentrated and the product was purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 34 mg (58%) of the desired product as a white solid. Example 32 Preparation of 5-ethoxy-6- (ethyl-methanesulfonyl-amino) -2- (4-fluoro-phenyl;) _ benzofuran-3-carboxylic acid formamidine will be completed Potassium acid (0.10 g, 0.72 mmol) and ethane iodide (0.10 ml, 125 μmol) were added to compound 29 (a) (0.036 g, 0.095 mmol). Example 29, a solution of 2-butanone (15 ml) made in step (a), and the reaction mixture was stirred at 20 ° C for 72 hours. The reaction mixture was concentrated, and the crude product was dissolved in ethyl acetate and washed with 1 mol hydrochloric acid. The organic layer was concentrated and the product was purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 25 mg (61%) of the title compound as a white solid. Example 33 Preparation of 2- (4-fluoroyl-phenylmorpholin-4-yl-5-oxethen-2-ylmethoxy) _benzofuran-3-carboxylic acid formamide 2-Chloromethyl-Violent) 〇 Add thionyl chloride (2 ml, 27.4 mmol) to 2-hydroxymethyl ritual (0.15 g, 1.30 mmol) in dichloromethane (2 Ml) solution. The reaction mixture was heated at reflux for 3 seconds, then cooled and stirred at room temperature for 20 minutes. The reaction was concentrated, dried on a high vacuum pump, and used directly in the next step. b. K4-fluorobenzyl) -6-morpholin-4_yl_5 _ (^ Xuan 嘁 -2_ some methoxy and its benzopyridine, _3. Preparation of formamidine sulfonate 〇 carbonic acid Potassium (0.10 g, 0.72 mmol) and 2-chloromethyl ^ xazole (0021 g 88828.doc -100- 200418452, 0.157 mmol) were added to compound 3 (a) ( 0,050 grams, 0135 millimoles, which can be prepared according to the above example 30, step (a)) in acetonitrile (15 ml). The reaction was refluxed for 2 hours, and then heated at 60 ° C for 16 hours. The reaction was cooled And concentrated, the crude product was dissolved in ethyl acetate and washed with hydrochloric acid. The organic layer was concentrated and the product was purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to give 37 mg (59 %) Desired product as a white solid. Example 34 2 (4-Fluoro-benzyl) -5-isopropoxy-6- [methylbenzene gf group_ (2_oxy-propyl) _amino group ] -Benzobenzo-3-carboxylic acid formamide Preparation of 2- (4-fluoro-phenyl) -5-isopropoxy-6-methanesulfonylamino_benzofuran-3 -Formamidine carboxylate) (0.093 g, 0.221 mmol, made according to one of the methods described in Example 21) dissolved in 2-butanone 20 ml). At 20 ° C, potassium mosquito acid (0.20 g, 1.45 mmol) and acetone chloride (01 ml, 125 pen moles) were added. The reaction mixture was refluxed for 2 hours, cooled to room temperature and concentrated. The crude product was dissolved in ethyl acetate, and washed with molar hydrochloric acid. The organic layer was concentrated and the product was purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 99 mg (94%) of the title compound as a white solid. Example 35 Preparation of (4-Aroyl-Dongyl) -6-Mafulin-4-yl- 5- (ρoselam-4-ylmethoxy) -benzofuran-3-carboxylic acid formamide Potassium carbonate (0.200 g, 1.45 mmol) and 4- (chloromethyl) pyrazole hydrochloride (0.100 g, 0.588 mmol) can be added to compound 30 (a) (0.100 g, 0.270 mmol). A solution of 2-butanone (15 ml) prepared in the above Example 30, Step a). The reaction was heated at reflux for 16 hours and then cooled to room temperature. The mixture was concentrated to 88828.doc -101-200418452, and the residue was dissolved in ethyl acetate and washed with water. The organic layer was concentrated and the product was purified by column chromatography (anhydrous loading on silica gel, ethyl acetate / hexane gradient followed by 1% methanol / ethyl acetate) to provide the crude product. The solid was triturated with ethyl acetate, filtered and dried under high vacuum to provide 45 mg (36%) of the title compound as a white solid. Example 3 6 2- (4-Fluoro-phenyl) -5-isopropoxy-6-methanesulfonamido_thiazolylmethyl-amino) -benzoanan-3-methanosamine Preparation: Potassium carbonate (0.050 g, 0.357 mmol) and 4- (chloromethyl) oxazole hydrochloride (0.041 ml, 0.238 mmol) were added to 2- (4-fluoro-phenyl) -5 -Isopropoxy-6-methylalaninoamino-benzoanilic acid carboxylic acid amine (0.050 g, 0.119 millimolar, which can be made according to one of the methods described in Example 21 above) 10 ml) solution. The reaction was refluxed for 1 hour. No visible product was formed by TLC, so potassium iodide (0.020 g, 0.120 mmol) was added to the reaction. The reaction was allowed to reflux for another 2 hours and then cooled to room temperature. The reaction mixture was concentrated, and the residue was dissolved in ethyl acetate and washed with water. The product was concentrated and purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 30 mg (48%) of the desired product as a white solid. Example 37 Preparation of argon) -6- (5-fluorenylmethyl di # hexyl) -5-isopropoxy-benzocopol-3-amine-carboxylic acid amine_a · ^ Compound 37U) (4-Fluoro-phenyl> 6-methylmethyl-5-isopropoxy-benzofuran-3-carboxylic acid ethyl ester) 88828.doc -102-

Dissolve hexamethylenetetramine (3.07 g, 21.9 mmol) and compound 6 (c) (50 g, 14.6¾ moles, which can be made according to step 骡 c of the above example) in trifluoro Acetic acid (10 ml). The reaction mixture was heated to 80 ° C until 80% of the reaction was found to be redundant by TLC. The reaction mixture was allowed to cool to room temperature, concentrated in vacuo, and distinguished between ethyl alcohol and water. The aqueous layer was washed with ethyl acetate, then the combined organic layers were washed with saline, dehydrated (MgS04) and concentrated in vacuo. Purification by column chromatography (silica gel, ethyl acetate / hexane gradient) provided 2.39 g (44%) of the desired product as a white solid. 200418452 b. Preparation of compound 37 (b) (2- (4-fluoro-phenylphosphoniumimino-methyl) -5-isopropoxy-benzofuran-3-carboxylic acid ethyl ester) .

Sodium acetate trihydrate (0.497 g, 3.65 mmol) dissolved in water (10 ml) was added to compound 37 (a) (1.23 g, 3.32 mmol) in ethanol (10 ml) and THF (25 ml). ) Solution, followed by the addition of hydroxylamine hydrochloride (0.254 g, 3.65 mmol). The reaction mixture was heated gently in a hot water bath and then allowed to cool slowly to room temperature. The reaction was concentrated in vacuo and partitioned between ethyl acetate and water. The aqueous phase was washed with ethyl acetate, and the combined organic layers were washed with salt solution 88828.doc -103- 200418452, dehydrated (MgS04) and concentrated in vacuo to provide 1.44 g (&gt; 100%) of product. This product was used in the next step without further purification. c. Preparation of compound 37 (cK2- (4-fluoro-benzyl) -5-isopropoxy-6- [5- (tetrahydroxan-2-yloxymethyl) -isoindazole- 3-yl] -benzocrean-3-acetic acid ethyl ester).

A solution of compound 37 (b) (0.300 g, 0.778 mmol) in chloroform (7 ml) was added dropwise to N-chlorosuccinimide (0.44 g, 0.778 mmol) and pyridine (catalytic ) Solution in chloroform (3 ml). The reaction mixture was heated to 50 ° C for 4 hours and then cooled to room temperature. Triethylamine (0.219 ml, 1.55 mmol) was added followed by tetrahydro-2- (2-propoxy) -2H-piran (0.108 ml, 0.778 mmol). The reaction was heated to 70 ° C for 16 hours, cooled to room temperature, diluted with dichloromethane, washed with 1 mol concentration 11 (: 1 and saline solution, dehydrated (MgS04) and concentrated in vacuo. Borrow Purification by column chromatography (silica gel, ethyl acetate / hexane gradient) provided 0.22 g (54%) of the desired product as a white solid. D · Preparation—Gold 37 (d) (2- (4-fluoro- Phenyl) -6- (5- via methyl-isoamycin-3-yl) -5-isopropoxy-benzoanan-3-ethyl hexanoate).

88828.doc 104 &gt; 200418452 Pyridine salt p-toluenesulfonate (7 mg, 0.028 mmol) was added to compound 27 (c) (0.15 g, 0.28 mmol) in ethanol (5 ml) and THF (5 ml) / cereal. After 4 days of incubation at room temperature, a 1/1 mixture of ethanol / thf (10 mL) and an additional amount of pyridinium p-toluenesulfonate (7 mg, 0.0028 mmol) were added. The reaction mixture was heated to 50 C for 30 minutes, then cooled to room temperature and concentrated in vacuo. The residue was taken between ethyl acetate and water. The aqueous phase was washed with ethyl acetate, and the combined organic layers were washed with brine, dried (MgS04) and concentrated in vacuo to provide 0.13 g (100%) of the desired product. eU Compound 37 (e) (2- (4-fluoro-phenyl) -6- (5-methyl-iso-4-iso-3-yl) -5-isopropoxy-benzofuran- 3-Acid Acid).

A solution of hydroxide (4 equivalents, 0.8 ml, 0.74 mmol) was added to a suspension of compound 37 (d) (0.13 g, 0.29 mmol) in ethanol (1 ml). The reaction mixture was allowed to stir at room temperature for 16 hours, heated at reflux for 1/2 hour, and then cooled to room temperature. The mixture was neutralized with 4 mol HCl (aq) (0.18 ml, 0.74 mol), filtered and washed with ethanol / water (1 / 1,2 ml). The mother liquor was extracted with ethyl acetate (2x), washed with brine, dehydrated (MgS04) and concentrated in vacuo. The two residues were combined and purified by column chromatography (silica gel, 99/1 ethyl acetate / acetic acid) to provide 0.078 g (65%) of the desired product. f.K4-fluorenyldiphenyl) _6- (5 • Ji ^ methyl-Wu ^^ Zi_3_yl) _5_Isopropylamino dibenzoxan_3 acid ammonium formate .doc -105- 200418452 Put 4 · methylmorpholine (23 µl, 0.210 mmol) followed by isobutyl chloroformate (27 µl, 2 ml of THF solution, 0.210 mmol) Ear) Add ice-cold compound 27 (e) (0.078 g, 0.190 mmol) in THF (5 ml). Let the reaction mixture smash for 5 minutes, and then add methylamine (2 Molar THF solution, 0.19 ml, 0.38 mmol). The reaction was warmed to room temperature and stirred for 16 hours. The mixture was allowed to distinguish between ethyl acetate and water. The layers were separated and the aqueous layer was washed with ethyl acetate (2x). The combined base layers were washed with saline, dehydrated (MgS04) and concentrated in vacuo. Crystallization from ethyl acetate provided 10 mg (12%) of the title compound. Example 38 Ethoxy--2- (4-fluoro-phenyl) -6- (methanesulfonium-methyl-amine-amine and benzofuran-3-carboxylic acid formamidine Noble compound 38 (a) (5- (Third-butyl-dimethyl · silyloxy) -2_ (4-fluoro-phenyl) -6-methylpyridylamino-benzoxyl喃 _3_ Methylamine succinate).

Let compound 29 (a) (6.39 grams, 16.9 millimoles, which can be prepared according to the above Example 29, step a), imidazole (5.0 grams, 73.5 millimoles), and tertiary butyl dimethyl stone A solution of a mixture of alkyl chloride (5.00 g, 33.2 mmol) in acetonitrile (70 t liter) was stirred for 20 hours. The solvent was removed in true 2 and the crude product was dissolved in 1 equivalent of HC1 and extracted with ethyl acetate. The combined organic layers were concentrated in vacuo and purified by column chromatography (stone gum, ethyl acetate) to provide 7.20 g (87%) 88828.doc -106- 200418452 of the desired product as a white solid. b. Compound ii_ (M (5- (third-butyl-dimethyl-silyloxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl- Amine) _benzofuran-3-carboxylic acid formamidine).

A solution of compound 38 (a) (5.50 g, 11.2 mmol), potassium carbonate (8.0 g, 58 μmol) and methane iodide (17 g, 0.12 mmol) in acetonitrile (120 mL) Stir at 20 ° C for 20 hours, then pour into 1 equivalent of HC1 (100 ml). The organic solvent was removed in vacuo, and the aqueous residue was extracted with ethyl acetate. The combined organic layers were concentrated in vacuo and the resulting solid was triturated with ethyl acetate / hexane to give 5.60 g (99%) of the desired product as a white solid. C.M prepared compound 3 fluoro * yl-phenyl) -5-¾yl-6- (methyl pyrone blue-methyl-amino) -benzofuran-3-carboxylic acid formamidine).

A solution of compound 38 (b) (7.80 g, 15.4 millimoles, which can be prepared according to the previous steps) in THF (100 ml) was subjected to 1 mole of tetrabutylamine fluoride, 6 ml, 16 mmol. THF solution. After 1 hour, the solvent was removed in vacuo, and the crude product was dissolved in 1 equivalent of HC1 and extracted with ethyl acetate. Concentrated in vacuum 88828.doc -107- 200418452 The organic layer was condensed, and the resulting soil m ΛζΤζ r ^, was v. Solidified. After trituration with ethyl bismuth ethyl ester / hexane, 5.61 g (99%) of white solid was produced. Desired product. Methylfuran-3jJ formamidine aranate oxidized compound 38 (C) (0.600 g, 153 mmol), carbonic acid (0.58 g, 4.2 mmol), and Qihua acetic acid (1 • The solution was stirred under reflux for 3 hours. The solvent was removed in vacuo and the crude product was dissolved in an equivalent concentration of HC1 and extracted with ethyl acetate. The combined organic layers were concentrated in vacuo and the resulting solid was recrystallized from absolute ethanol. The precipitated product was filtered off and dried to provide 0.54 g (84%) of the title compound as a white solid. fExample 3 9

MliLlzi-based diyl) -6- (A; a methyl group, a methyl group, a 3-methylamine amine methyl group and a squeaking _5_yl methyl group 1_2_an even-benzyl I. a. ^ I ^ il2X ^ _ (2,2,7_trimethyl · benzo [1,3 &gt; Nisaki Ken_4_one); κ side. 39 (a) 4- (dimethylamino) pyridine ( DMAP) (0.40 g, 3.29 mmol) and acetone (6_27 ml, 85.44 mmol) with 4-methylsalicylic acid (10.0 g, 65.72 mmol) in 1,2-monomethoxyethoxybenzene DME) (50 ml) solution. Dissolve thionyl chloride (6.7 ml, 92.01 mmol) in DME (5 ml) and slowly add the reaction mixture. Allow the reaction to stir at room temperature for 36 hours. Concentrate the mixture and dissolve the crude The product was washed with ethyl acetate and water. The organics were concentrated and the product was purified by flash chromatography (silica 88828.doc -108- 200418452 gel, ethyl acetate / hexane gradient) to provide 14 g (11%) of a yellow solid. The desired product: bromomethyl-2,2-dimethyl-benzo [up dioxen-4-one). H3CyCH3

N-Bromosuccinimide (0.74 g, 418 mmol) and gadolinium peroxide (0.068 g, 0.279 mmol) were added to compound 39 (a) (〇67 g, 3 49 mmol) , Can be made according to the previous steps) carbon tetrachloride (15 ml) solution. The reaction was returned / watt and radiated with a heat lamp for 5 hours. The reaction was then cooled and the solids were filtered off. The filtrate was concentrated, dissolved in ethyl acetate and washed with water. The organic layer was concentrated and the product was purified by flash chromatography (silica gel, ethyl acetate / hexane gradient) to provide 175 mg (19%) of the desired product as a white solid. cl 备 化 金身 J ^ £ ^ (5_ (2,2_dimethyl-4-oxy-4H-benzo [ι, 3] -dihydrazone-7-ylmethoxy) _2_ (4_ Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid formamidine).

88828.doc -109- 200418452 Potassium carbonate (0.19 g, 1.38 mmol) and compound 39⑻ (0.25 g, 0.917 mmol) were added to compound 38 (d) (〇18 g, 0.495 mmol) Moore can be prepared according to step 38d) of the above example) in acetonitrile (15 ml). Allow the reaction mixture to return to w for 4 hours, and then shrink back. The crude product was dropped in ethyl acetate and washed with water. The organic layer was concentrated to a solid and triturated with 20% ethyl acetate / hexane, filtered and dried to provide 240 mg (90%) of the desired product as an off-white solid. d.izj2- (4-Fluoro-phenylmethanesulfonyl-monomethyl-pyrene-methylhuabenzobenzofuran-5-oxylmethyl-1_2-hydroxypyrene-benzylacetate) η monohydrate UOH (0.015 g, 0.343 mmol) was added to a suspension of compound 39 (c) (0.10 g, 0.172 mmol) in water / THF (10 ml / 10 ml). The reaction was allowed to proceed in the chamber. Stir gently for 4 hours. Remove thf by rotary evaporation and add 1 mol HC1 until acidic pH is reached. The precipitate is filtered off and dried to provide 65 mg (70%) of the title compound as an off-white solid. Example 40 Methyl-phenyl 1 ^ (5-pyrene-I-zazol-3-yl VS-methoxycap-benzylpyran-3- # acid formamidine a. Preparation of Compound 40 (&gt; 丨 〇

HO

ch3 40 (a) Let 5-hydroxy-3H-benzoxan-2-one (10 · 8 g, 71.9 mmol) and 88828.doc -110- 200418452

A solution of Amberlyst®-15 (8.0 g) in anhydrous methanol (25 ml) was stirred at 22 ° C for 72 hours. Before evaporating the solvent, the reaction mixture was filtered through CeliteTM 503 pieces. The resulting solid was purified by flash column chromatography (silica gel, 2.00 · 80 ethyl acetate / hexane) to provide 12.84 g (98%) of the desired product as a white solid. b. Preparation of compound

40 (b) A solution of 4-fluoro-benzylhydrazone (4.20 ml, 35.7 mmol) in dichloromethane (10 ml) was added dropwise over 15 minutes. A solution of compound 125 (a) (3.0 g, 16-5 mmol) and triethylamine (5.00 ml, 35.9 mmol) in dichloromethane (70 ml). The reaction mixture was allowed to stir at 22 ° C for 18 hours, then concentrated ', diluted with 1 equivalent of HC1 (100¾ liters), and extracted with ethyl acetate. The organic layer was concentrated to a crude oil and purified by flash column chromatography (silica gel, ethyl acetate / hexane gradient) to provide 6.81 g (97%) of the desired compound as a white solid. The c-fluorene 4-dagger compound 40 (c) (3- (4-fluoro group · donkey group) -5-quinyl-3H-benzofuran-2-S is the same).

40 (c) Suspend hydrogenated steel (9 5% oil solution '0.123 g, 5.13 mmol) in 0. 88828.doc -111-200418452 anhydrous THF (0 ml), and compound 125 (b) (1.05 g, 2.46 mmol) was added in one portion. The reaction mixture was allowed to stir at 22 ° C for 24 hours. After carefully stopping the heat through water, the reaction mixture was diluted with ethyl acetate, extracted with 1 equivalent of HC1 and saline, and then concentrated to produce a dark oil. This crude oil was purified by flash column chromatography (silica gel, 60% ethyl acetate / hexane) to provide 0.74 g (100%) of the desired compound. d. Preparation of compound 40 (d) (2- (4-fluoro-benzene V5-hydroxy-benzylfuran-3-carboxylic acid ethyl ester).

A solution of compound 40 (c) (0.74 g, 2.46 mmol) in anhydrous methanol (50 ml) was treated with concentrated sulfuric acid (0.2 ml), and the mixture was heated at reflux for 25 hours. The reaction mixture was concentrated and the resulting solid was purified by flash column chromatography (silica gel, 10% ethyl acetate / hexane) to provide 0.580 g (78%) of the desired product as a white solid. e. Preparation of compound 40 (e).

40 (e) This intermediate compound is essentially prepared according to the general method of Example 12, step 3 above, however, compound 40 (d) is substituted for compound 12 (a) ⑴ and 12 (a) (ii) ° 88828 .doc -112- 200418452 benzofuran-3-carboxylic acid ethyl ester).

99% of titanium tetrachloride (15.4 ml, 140 mmol) was added. (: Chloromethylmethyl acid (6.45 ¾ liter, 71.0 mmol) under argon in dichloromethane (100 ml). After the addition is complete, compound 40 (e) (200) G, 63 · 6 * mol) of dichloromethane (75 ml) was added dropwise to the solution. After the addition was completed for half an hour, the reaction was cooled in an ice bath, and water (丨 ⑻ ml) was added dropwise. Monochloro The reaction was diluted with methylbenzene until it became homogeneous. The layers were separated, and the organic layer was washed with 3 mol HC1 (1 × 100 ml) and saline (1 × 100 ml), dried over MgS04 and filtered and concentrated in vacuo. Residual in ethyl acetate (1 liter) and enough chloroform to make everything into a solution. The solution was filtered through a Florisil® stopper, concentrated in vacuo, and purified by crystallization from ethyl acetate to provide 5.90 g (27%) The required compound is g. Prepare compound_4.Q (g) (2- (4-fluoro-phenyl) -6- (guidoiminomethyl) -5-methoxy-benzo Furan-3_carboxylic acid ethyl ester).

Water (20 ml) of cool acid steel trihydrate (1.44 g, 10.6 mmol) was dissolved in 88828.doc -113-200418452, and then hydroxylamine hydrochloride (0.73 g, 10.6 mmol) ) A suspension of compound 40 (f) (3.29 g, 9.61 mmol) in THF (200 ml) was added. [After an hour, the reaction was concentrated in vacuo and the residue was suspended in water. The solid was filtered over to give 3.20 g (93%) of the desired product. The product was carried on to the next step without further purification. h. Preparation of compound 40 (h) (2- (4 · Gas-D Winteryl) -5 -methoxy-6- [5- (tetrahydro-bran-2-yloxymethyl) -isoamidine Ethazol-3-yl] -benzocran-3-acrylic acid ethyl ester).

A solution of compound 40 (g) (3.20 g, 8.95 mmol); DMF (120 ml) was added dropwise to N-chlorosuccinimide (1.19 g, 8.95 mmol) and pyridine (Catalytic amount) in DMF (60 ml). The reaction mixture was heated to 60 to 20 hours' at which time an additional amount of N-chlorosuccinimide (q.238 g, 179 mmol) was added to the reaction. After the consumption of compound 40 (b) (detected by TLC), the reaction was allowed to cool to room temperature. Add triethylamine (1.26 ml, 8.95 mmol) followed by tetrahydro-2- (2-propynyloxy) -2H-piran (2.51 ml, 17.9 mmol) . The reaction was heated to 60 ° C for 2 hours, cooled to room temperature, and extracted with ethyl acetate (2 X 100 ¾ liters). The combined organic layers were washed with ice water (several times) and saline, dehydrated (MgSCU) and concentrated in vacuo. Purification by column chromatography (silica gel, ethyl acetate / hexane gradient) provided 2.05 g (46%) of the desired product as a white solid. il plate coupling plate ^ 1 (2- (4-fluoro-phenyl) _5 • methoxy_6_ [5_ (tetrahydro_ 88828.doc -114- 200418452 peak ran-2-yloxymethyl) -Isaki-3-yl] -benzofuran-3-acid).

A potassium hydroxide solution (4 equivalents, 1.34 ml, 5.35 mmol) was added to a suspension of compound 40 (h) (1.06 g, 2.14 mmol) in ethanol (10 ml). The reaction mixture was heated at reflux for 2 hours and then cooled to room temperature. The reaction mixture was passed through 4 mol HCl (aq) (1.34 ml, 5.35 mmol), filtered, air-dried and dried under vacuum to provide 0.95 g (95%) of the desired product. J ·· Preparation of compound 40 (1) (2- (4-Fluoro-phenyl) · 5-methoxy-6- [5- (tetrazol-Iran-2-yloxymethyl) -iso 4azol-3-yl] -benzocrean-3-methanoate (formamide).

Carbonyldiimidazole (0.401 g, 2.47 mmol) was added to one of the compounds 40 g (0.958 g, 2.06 ¾ ng) of rat pit suspension. The resulting solution was allowed to stir at room temperature for 1 hour. N-methylamine (2.0 moles of thf solution, 1.55 ml, 3.09 mmol) was added and the reaction was allowed to stir at room temperature for 20 hours. The mixture was then heated at reflux for 1 hour, cooled to room temperature, and distinguished between water and dichloromethane. The aqueous layer was washed with ethyl acetate, and the combined organic 88828.doc -115- 200418452 layers were washed with saline, dehydrated (MgSCU), filtered, and concentrated in vacuo. Purification by column chromatography (stone gum 'ethyl acetate / hexane gradient) provided 046 g (46%) of the desired product. k. Preparation of (U4-yl-benzyl) -6- (5-antenuolinyl-iso4-yl) -5-methylamino-phenylchafuran-3- # formamidine. -Tosylate (7 mg, 0.028 mmol) was added to a solution of compound 40 (e) (0.135 g, 0.281 mmol) in ethanol (10 ml), thf (3 ml) and water. The reaction mixture was allowed to stir at room temperature for 20 hours. The reaction mixture was then heated to 95 C for 4 hours, cooled to room temperature and concentrated in vacuo. The residue was taken between ethyl acetate and water. The organic layer was washed with saline, dehydrated (MgSCU) and concentrated in vacuo. Purified by column chromatography (Shijiao, ethyl acetate / hexane flame gradient) and crystallized from ethyl acetate to provide 50 mg (45%) of the title compound. Example 41 2- (4-Fluoro-phenyl) -6- [4- (2-Cyclo-ethyl) · iso-π-Jun_3_yl] -5 -methoxy-benzofuran-3 -Preparation of Formamidine Carboxylic Acid a · Compound 41 (a) (2- (4-Fluoro · phenyl) -5 -methoxy-6- (3a, 4,5,6a_ tetrahydro-furan [3,2-d] -isoxazol-3-ylbenzofuran-3-carboxylic acid ethyl ester).

Add N-chlorosuccinimide (0.747 g, 5.59 mmol) and pyridine (catalytic) to compound 40 (8) (2.00 g, 5.59 mmol), according to the above example 4888828.doc -116 -200418452 (made by Buzhig) in DMF (100ml) solution. The reaction mixture was heated to 60 ° C for 20 hours. Triethylamine (0.78 ml, 5.59 mmol) was added followed by 2,3-dihydrofuran (0.85 ml, 11.2 mmol). The reaction was heated to 60 ° C 'for 1 hour', cooled to room temperature, diluted with water to 500 ml, and extracted with ethyl acetate (3 x 75 ml). The combined organic layers were washed with ice water several times, 'salt solution once', then dehydrated (MgS04) and concentrated in vacuo to provide 2.27 g (95%) of the desired product. bUf chemical 41 (b) (2_ (4-fluoro-phenyl) -5-methoxy-6- (3a, 4,5,6a-tetrahydro-octane [3,2_d] _iso4 Azole_3_yl) -benzoxanthene).

A potassium hydroxide solution (4 equivalents, 0.73 ml, 2.93 mmol) was added to a suspension of compound 41 (a) (0.500 g, 1.17 mmol) in ethanol (7 ml) and water (2 ml). liquid. The reaction mixture was heated at reflux for 1.5 hours, and then cooled to room temperature. The reaction mixture was neutralized with 4 mol HC1 (aq) (〇73 ml, 2.93 mmol), filtered, air-dried and vacuum-dried to provide 0.52 g (quantitative) of the desired product. Proceed to the next step after further purification. Fluorophenyl) _5_methoxy_6_ (3a, 4,5,6a_ tetraargon-squeeze [3,2-d] -Xing 4 ° sit-3-yl) -benzocryso_3_bet Acid amines).

88828.doc -117- 200418452 Tandiimidazole (0.20 g, 1.27 mmol) was added to a dichloromethane suspension of compound 41 (b) (0.42 g, 1.05 mmol). The resulting solution was allowed to stir at room temperature for 2 hours. Add methylamine (thf solution at 2.0 mol concentration, 0.79 t liter, 1.58 mol), and heat the mixture at reflux for 3 hours, cool to room temperature and perform in water and ethyl acetate distinguish. The aqueous layer was washed with ethyl acetate, and the combined organic layers were washed with saline, dehydrated (MgSCU), filtered, and concentrated in vacuo. The product was purified by column chromatography (silica gel, ethyl acetate / hexane gradient) to provide 0.30 g (70%) of the desired product. d. Preparation of (2- (4-fluoro-benzyl-V6- "4- (2-hydroxy-ethmyl-vinyl-1-5- 1oxy-benzofuran-3-maurate). Compound 41 (c) (0.160 g, 0.38 mmol) was suspended in 0.05 ml of ethanol) and concentrated HC1 (3 drops). The reaction was heated at reflux for 50 hours, cooled to room temperature, and between ethyl acetate and water. Differentiate. Separate the layers, wash the organic layer with brine, dehydrate (MgSCU), filter, and concentrate in vacuo. Purify by column chromatography (crumb, ethyl acetate / hexane gradient), and crystallize from ethyl acetate To provide 50 mg (31%) of the title compound. Example 42 2- (4-Fluoro-phenyl) -6-[(2-Beryl-ethyl) -methylarsino-amido] amine Preparation of methoxy-benzofuran-3-carboxylic acid formamidine a-Preparation of compound -fluoro-phenyl) -5-#-nitrophenylfurfuryl-3-carboxylic acid ethyl ester).

88828.doc -118- 200418452 Boron trichloride (106 ml, 0.106 mole) is added dropwise to the compound 21⑷ ⑵) · 5g, 0.053 mole, which can be prepared according to the procedure of the above example 21) A solution of anhydrous digas methane (264 ml). The reaction mixture was allowed to stir at room temperature overnight. The reaction was quenched with ice water and extracted with chloroform (x). The organic layers were combined, dehydrated over magnesium sulfate, filtered and evaporated. The resulting solid was shaken in the first wave, filtered and dried to provide 17 82 g (99%) of the product as a yellow solid. b.l Prepare compound 42 (b) (2- (4-fluoro-phenyl) -5-methoxy-6-nitro-benzo-3-ancarboxylic acid ethyl ester).

Add cesium carbonate (33.04 g, 0.101 mole) and methyl iodide (31.6 ml, 0.507 mole) to 1-methyl-2-pyrrolidone (42 (a) (l 7.5 g, 0.053 mole)) 250 ml) solution. The reaction mixture was heated at 50 ° C overnight, quenched with water, extracted with ethyl acetate (3X), and a portion of the insoluble product was filtered off. The organic layers were combined, dehydrated (MgS04), and concentrated. The resulting solid was combined with the previously isolated solid to provide 14.91 g (82%) of the product as a yellow solid. c. Preparation of compound 42 (c) (6-amino-2- (4-fluoro-fluorenyl) -5 -methoxy-benzyl-3 -ethyl methanoate).

88828.doc 119-200418452 10% Pd / C (0.900 g) was added to a mixture of compound 42 (b) (7.0 g, 0.0195 mol) in isopropyl acetate (32.0 ml). The reaction mixture was shaken overnight in a Parr blue shaker with 50 psig of hydrogen. The reaction mixture was filtered through CeliteTM and wet with ethyl acetate and methanol. The filtrate was concentrated in vacuo. This reaction was repeated using the same amount of solvent reactant and the products of the two reactions were combined to provide the desired product in a total amount of 12.8 g (99%) solids. d. Preparation of compound 42 (dV2-r4-fluoro-phenyl) -6-methanesulfonamido-5-methoxy-benzofuran-3-carboxylic acid ethyl ester).

CH3 42 (d) Toluenesulfonyl chloride (0.64 ml, 85.6 mmol) was added to compound 42 (c) (12.8 g '12.8 mmol) in anhydrous dichloromethane (130 ml) on ice (0). 〇 ice / water bath) solution. Then, the reaction mixture was cooled in an ethanol / ice bath, and N, N-diisopropylethylamine (16.93 ml, 97.2 mmol) was added. The reaction mixture was allowed to stir at room temperature overnight. The reaction mixture was diluted with water and extracted with dichloromethane (3X). The organic layers were combined, dehydrated over magnesium sulfate, and evaporated to provide 18.7 g (99%) of the desired product as a solid. Fluoro-phenyl; methanesulfonylamino_5_methoxy • benzocrean_3_metanoic acid).

CH, 88828.doc 120-200418452 Potassium hydroxide (51.5 g, 0.918 mmol) was added to compound 42 (d) (18.7 g, 0.0459 mole) in ethanol (200 ml) under argon and A mixture of water (100 ml). The reaction mixture was heated at reflux for about 7 hours, and then stirred at room temperature overnight. The reaction mixture was concentrated and the residue was dissolved in water. The water mixture was acidified with 6 equivalents of HC1 until a solid precipitate formed. The product was filtered, washed with water and dried to provide 15.0 g (86%) of the desired product as a brown solid. f · Preparation of compound 4-21 £) (2- (4-fluoro-phenyl) -6-methylsulfonylamino-5-methoxybenzofuran-3-carboxylic acid formamidine).

Add 1,1-carbonyldiimidazole (8.66 g, 53.3 mol) followed by methylamine (a 2.0 mol THF solution, 30.0 ml, 59.3 mmol) to compound 42 (e ) (15 g, 39.5 mmol) in dichloromethane (155 ml). The reaction mixture was allowed to stir at room temperature overnight, diluted with water, extracted with dichloromethane (3x), and a portion of the insoluble product was filtered off and set aside. The combined organic layers were dehydrated over magnesium sulfate and concentrated. The resulting solids were sonicated in water, subjected to sonication, and combined with previously separated products to provide a total of 14 42 g (92%) of the desired product. g. C2z. (4-fluoro-phenyl., ethylmethane, amine-amine 1) Preparation of methylalanyl-benzene-cough amine, g. potassium iodide (80 mg, 0.48 mmol), Potassium carbonate (2.82 g, 20.4 mmol) and dibromoethanol (3.62 ml, 51 mmol) were dissolved under argon gas 88828.doc -121-200418452 in DMF (100 ^: liter) ) Solution of compound 42 (f) (4.0 g, 10.2 mmol). Heat the mixture to 50 ° C for 7 hours, then add additional amounts of potassium iodide (80 mg, 0.48 mmol) and 2- Ethanol bromide (1.81 ml, 25.5 mmol). Stir the mixture at 50 ° C overnight, then add additional amount of potassium carbonate (19.73 g). Stir the reaction mixture at 8 5 ° C for about 4 Hours, diluted with water and extracted with ethyl acetate (3X). The organic layers were combined and evaporated. The remaining solids were diluted with water, shaken and filtered. After washing several times with water, the solids were dried to provide 3.14 g of crude product. 'It was subsequently crystallized from hot ethanol. FExample 43 5-Cyclopropyl_2- (4-fluoro-phenyl) _6 _ [(2-hydroxy_ethyl) _methanesulfonyl_amino group l · benzo Methylfuran-3-carboxylic acid Preparation of a-cyclopropyl acid _ _ cyclopropyl acid-based process according to the literature:.... Wallace, D j, Chen, c,.

Tetrahedron Lett. 2002, 43, 6987-6990, made of cyclopropylmagnesium bromide on a 4 g scale. b. Preparation of 4 ... (2- (4-fluoro-phenyl) -6_nitro_5_trifluoromethane (tested with oxy-benzo-3-an-2-acetic acid)).

43 (b) Add n, n-diisopropylethylamine (8.8 ml, 56 mmol) and 4- (dimethylamino) pyridine (0.618 g, 5.06 mmol) to compound 42 under argon (a) (17.5 grams, 50.6 millimoles, which can be made according to the above Example 42, steps &amp;) Wu 88882.doc -122- 200418452 solution in methylene chloride (ml). The reaction mixture was allowed to cool to 0 ° C in an ice / water bath, and then trifluoromethanesulfonic anhydride (9.34 ml,% mmol) was added. The human reaction was stirred at A temperature for about 5 hours, and then additional amounts of ν. Diisopropylethylamine (4.4 ml, 28 mmol) and trifluoromethanesulfonic anhydride (4.67 ml, μ mmol) were added. . The reaction was allowed to stir at room temperature overnight, diluted with water, and extracted with dichloromethane (3x). The organic layer was washed with water and "equivalent concentration 1 ^ 〇οχ), combined, dehydrated with magnesium sulfate and evaporated. The residue was recrystallized from tert-butyl methyl ether to provide a total of 20.36 g (84%) of a yellow solid. Desired product: cyclopropyl-2- (4-fluoroyl-phenyl) -6-nitro-benzofuran-3-carboxylic acid ethyl ester).

Anhydrous toluene (10.0 ml) was added to cyclopropylgopenic acid (0.271 g, 314 mmol), potassium fluoride dihydrate (0.652 g, 6.92 mmol), and sodium bromide ( A mixture of 0.216 g, 2.16 mmoles, palladium (triphenylphosphine) palladium (0) (0.073 g, 0.00629 mmoles) and compound 43 (b) (1.0 g, 2.09 mmoles). The resulting solution was degassed through a gas dispersion tube with argon for 10 minutes. The reaction mixture was refluxed and heated overnight, diluted with water and extracted with ethyl acetate (3x). The organic layers were combined, dried over magnesium sulfate and evaporated. The crude product was purified by column chromatography (silica gel, anhydrous load, hexane / ethyl acetate gradient) to provide 0.670 g of the desired product as a solid. d. Preparation of phosphonium 43 (d) (6-amino-5-cyclopropyl-2- (4-fluoro-phenyl) _benzene 88828.doc -123- 200418452 ethyl benzofuran-3-carboxylic acid ).

10% Pd / C (0.150 g) and 1 equivalent of HC1 (7 drops) were added to a solution of compound 43 (c) (0.665 g, 1.8 mmol) in ethyl acetate (70.0 ml). The reaction mixture was shaken overnight on a Parr shaker with 50 psig of hydrogen. The reaction mixture was filtered through CeliteTM and wet with ethyl acetate and methanol. The filtrate was concentrated in vacuo to provide 0.540 g (88%) of the desired product as a solid. ei prepared chemical house 43 (e) (5-cyclopropyl-2- (4-fluoro-phenyl) -6-methanesulfonylamino-benzoanan-3 -acetate).

Methanesulfonyl chloride (0.270 ml, 3.48 mmol) was added to an ice solution (0 ° C, ice / water bath) of compound 43 (d) (0.535 g, 1.58 mmol) in digas methane (6 ml). The reaction mixture was further cooled in an ethanol / ice bath, and then N, N-diisopropylethylamine (0.688 ml, 3.95 mmol) was added. The reaction was allowed to stir at room temperature overnight, diluted with water and extracted with dichloromethane (3x). The combined organic layers were dehydrated over magnesium sulfate and evaporated to provide 0.653 g (86%) of the bis (sulfonated) intermediate. 88828.doc -124- 200418452 Potassium hydroxide (1.52 g, 27 mmol) was added to the bis (sulfonated) intermediate (0.670 g, 1.35 mmol) in ethanol (1 (0.0 ml) and a solution of water (5.0 ml). The reaction was heated at reflux overnight and then concentrated in vacuo. The remaining solid was dissolved in water and the solution was acidified with 1 equivalent of HC1 until a precipitate formed. The solid was filtered and dried to provide 0.532 g (99%) of the desired product. f. Preparation of compound 43 (fl (5-cyclopropyl-2- (4-fluoro-phenyl) -6-methanesulfonyldonylamino-benzoic acid-3-amine).

Benzotri-n-syl-1 -yloxyselenium hexafluorophosphonate (PyBOP) (1.02 g, 1.97 mmol) was added to methylamine (12.0 ml, 16.3 mmol) under argon Ear, 2.0 Molar THF solution), DMF (1.0 ml) and compound 43 (e) (0.530 mg, 1.36 mmol). The reaction was allowed to stir at room temperature overnight 'and then concentrated in Shinji. The residual compound was diluted with water and extracted with ethyl acetate (3X). The organic layers were combined, washed with water, dehydrated with magnesium sulfate and air-dried to provide 0.347 g (63%) of the crude product. A portion of the crude product (100 mg) was purified by reverse phase HPLC (acetonitrile / water gradient) to provide 0.050 g of the desired product. g. Preparation of Jj_Compound 43 (g) 5-cyclopropyl-2- (4-fluoro-phenyl) -6- [methanecontinyl- (2-phenoxy-ethyl) -amine] -Benzoan-3-methylmetanosylamine). 88828.doc -125-200418452

Potassium carbonate (0.125 g, 0.91 mol) and fluorenyl 2-bromoethyl ether (0.105 ml, 0.67 mol) were added to compound 43 (g) (0.120 g, 0.0003 mol) under argon. Acetonitrile (1.5 ml) solution. The reaction mixture was heated at reflux overnight, diluted with water and extracted with dichloromethane (3x). The organic layers were combined, dried over magnesium sulfate and evaporated. The crude product was purified by recrystallization from ethyl acetate / hexane, and the isolated solid was directly subjected to the next step without further purification. hG · Cyclopropyl-2 · ί4-Fluoro-Benzene) -6-ΙΎ2-Hydroxy-ethyl Vmethane acid group · • Amino group 1-Benzowan-3-carboxylic acid formamidine) preparation). 10% Pd / C (0.100 g) was added to a mixture of compound 43 (g) (0.162 g, 0.41 mmol) in ethyl acetate (20 ml). The reaction mixture was shaken overnight on a Pair shaker at 50 psig of hydrogen. The reaction mixture was filtered through CeliteTM and wet with ethyl acetate and methanol. The filtrate was concentrated in vacuo and the crude product was dissolved in ethyl acetate and precipitated with hexane. The solid was isolated by filtration to provide 0.083 g of the desired product as a brown solid. Example 44 Preparation of ethyl-2- (4-fluoro-phenyl) _6_methanesulfonamido-benzofuran_3_carboxylic acid formamidine trifluoro-methanesulfonic acid 2_ (4 _Fluoro-phenylmethyl 88828.doc -126- 200418452 (sulfofluorenylamino-3-methylaminomethylfluorenyl-benzofuran-5-yl ester).

A solution of N-phenyl triflimide (14.2 g, 3 9.68 mmol) in anhydrous dichloromethane (20 ml) followed by triethylamine (5.4 ml, 52.9 mmol) was introduced under argon. 38 (a) An anhydrous dichloromethane (10 ml) solution of (10 g, 26.45 mmol, which can be prepared according to the above-mentioned Example 38, step (a)). The reaction mixture was allowed to stir at room temperature overnight. The reaction mixture was poured into water (150 ml) and the layers were allowed to separate. The aqueous layer was extracted with dichloromethane (3 x .100 ml). The combined organic layers were dehydrated (MgSCU) and concentrated in vacuo. The crude product was purified by recrystallization (1: 1 ethyl acetate / hexane) to provide 127 g (94%) of the desired product as pale orange crystals. b. Rebecca Compound 44 (b) (2- (4-fluoro-phenyl) -6-methanesulfonylamino-5-vinyl-benzofuran-3-carboxylic acid formamidine).

Lithium chloride (498 mg, 11.75 mmol), triphenylphosphine (0) (90 grams, 0.08¾ mole), triphenylphosphine (83 mg, 0.31 mmol) and 2,6-Di-tert-butyl-4-cresol (approximately 16 mg, 0.08 mmol) was added to compound 44 (a) (2.0 g, 3.92 mmol) under argon anhydrous Dioxane (17.6 ml) 88828.doc -127- Falling liquid. Anti-Ma Yi Λτ #%, oxygen degassing of sperm lice for 15 minutes. Introduce tri-n-butyl ethylenyl tin (1 7 7 _ ± 1 \ • gross liter) through a syringe 'Then, the reaction was heated to 1000 ° C for 18 hours until the mouth was poured. A saturated aqueous solution of potassium fluoride (50 ml) was added, and the mixture was vigorously dissipated for 4 hours. Tokuhisa Hachiba The layers were cut off, and the aqueous layer was extracted with dichloromethane (3 x 50 ml). ^ The combined organic layers were washed with a 10% ammonium hydroxide (3 x 50 ml) solution. After extraction with-* m-water layer (5G ml). All organic layers were combined, dehydrated (MgS04) and concentrated. The residue was purified by flash chromatography (hard gum, hexane, and then a methyl chloride / hexane gradient) and recrystallized (ethyl acetate) to provide 1.10 g (72%) of the desired product. Benzyl X-methanefluorenylamino. Benzowalan: i_-carboxylic acid_formamidine _ t 〇 刼 10 /. Pd / C (50 * g) was added to a mixture of compound 44 (b) (500 mg, 1.29 mmol) and ethyl acetate (50 ml). The reaction mixture was shaken with Parr at 50 psig of hydrogen for 2 days. The reaction mixture was filtered through CeliteTM, wet with ethyl acetate and ethanol, and purified by HpLC (reverse phase, acetonitrile / water gradient plus 0.1% acetic acid) to provide 342 mg (74%) of the desired product. Example 45 Preparation of 5-ethyl-2- (4-fluoro-phenyl) -6- (methanesulfonyl_fluorenyl-amino) _benzofuran-3-carboxylic acid formamidine The above is made according to the general method of the above Example 3 8. Step 骡 b. However, the 5-ethyl-2- (4-fluoro-phenyl) -6-methylamine g benzoamino_benzo Formamidine furan-3-carboxylate (which can be prepared according to Example 44) replaces compound 38 (a). The crude product was purified by HPLC to provide the product in 64% yield. -Example 46 88828.doc -128- 200418452 &gt; Ethyl-2- (4-fluoro-phenyl) -6-[(2-Cyclo-ethyl) -formyl-amino-amino]- Preparation of benzofuran-3-carboxylic acid formamidine 46 (.gjL (6K2-ethoxy-ethyl) -methylbenzene g-boxyl-amino group] 2- (4-fluoro-phenyl) _5_Ethylfluorenyl_benzocrean-3-amine acid formate).

Benzyl-2-bromoethyl ether (448 µl, 2.82 mmol) was added to compound 44 (b) (500 mg, 1.28¾ mole) made according to the above Example 44, Step 骡 ab under argon pressure. With potassium carbonate (534 mg, 3.86 mmol) in anhydrous acetonitrile (6.4 ml). The mixture was heated at reflux for 12 hours, poured into water (100 ml), and extracted with chloroform (3 x 100 ml). The organic layers were combined, washed with saline (1000 liters) ', dehydrated with MgSCU and concentrated. The crude product was purified by flash chromatography (Shi Xijiao, 1 murine / methanol gradient) to provide 650 mg (97%) of the desired product. Preparation of bj-ethyl-2- (4-pentanyl-phenyl) -6-"(2_Transferred-ethylmethylcarbofluorenyl-amino 1-benzylpyran-3-carboxylic acid formamide Jing. Add 10% Pd / C (50 mg / day three times, 150 mg total) to a mixture of compound 46 (a) (650 mg, 1.28 mmol) in ethyl acetate (65 ml). Let the reaction The mixture was shaken in a parr shaker under 50 psig of hydrogen for 4 days. The reaction mixture was filtered through CeliteTM and wet with ethyl acetate. The filtrate was concentrated in vacuo and the solids were separated. The crude product was subjected to HPLC (reverse phase, acetonitrile / water gradient). Purified with addition of 0.1% acetic acid) to provide 398 mg (78%) of the title compound. Example 47 88828.doc -129- 200418452 6- (1-ethyldonyl_pyrrolidin_2_yl) 2- (4- Preparation of Fluoro_phenyl) _5_methoxy-benzofuran-3-carboxylic acid formamidine • Bromo-2- (4-fluoro · phenyl) -5-methoxy-benzofuran -3-carboxylic acid formamidine).

47 (a) The intermediate compound is substantially prepared according to the general method of Example 28, Step 骡 g described above. However, Compound 28 (c) is substituted for Compound 28 (f). b '^ i ^^ iaK2- [2- (4-fluoro group_phenylmethoxy_3-methylaminomethanyl-benzofuranyl) • pyrrole minor acid tert-butyl ester).

At room temperature, solid Na2CO3 (371 mg, 3.5 mmol) and (triphenylphosphine) palladium (0) (81 mg, 0.07 mmol) were added to compound 47 (a) (527 mg , 1.40 ¾ mole, which can be made according to the general method of the previous steps), (Third-butoxycarbonyl) -pyrrole-2-_acid (445 mg, 2.10 mmol) toluene / ethanol / water Liter / 10¾ liter / 0.5 ml) of degassed solution. At 85. After stirring for 20 hours under argon pressure, the reaction was quenched with water and extracted with ethyl acetate. The organic phase was washed with water and brine, dried over MgS04 and concentrated under reduced pressure. The crude 88828.doc -130- 200418452 product was purified by column chromatography (silica gel, 20% ethyl acetate / hexane) to give 550 mg (85%) of the desired product as a pale yellow solid. c · pan jf compound 4 ″ ×× ^ 1 (2- [2- (4-fluoroyl-phenyl) -5-methoxy-3-methylaminomethylamido-benzofuran-6-yl]- Pyrrole-1-carboxylic acid-tertiary-butyl ester).

Activated 10% Pd / C (200 mg, 10% by weight) was added to a 4: 1 ethyl acetate: ethanol solution of compound 47 (b) (500 mg, 1.08 mmol). The mixture was shaken overnight at room temperature in a parr shaker under 50 psig of hydrogen. Add another portion of activated 10% Pd / c (200 mg, 10% weight). The mixture was shaken in a Parr shaker under 50 psig of hydrogen at room temperature for 24 hours. The reaction was then allowed to pass through and wet with ethyl acetate. The filtrate was concentrated to give 480 mg (95%) of the pure expected compound as a white solid. d. Preparation of compounds "· 7 (ά) (2- (4-fluoro-phenyl) -5-methoxy-6-external 1: Luodian-2 -yl-epoxy and octane-3 -bet Acid-amine formate).

A solution of compound 47 (c) (450 mg, 0.96 mmol) in 20% (volume) trifluoromethylene chloride was expanded at room temperature: stir for 1 hour. Then, the solvent 88828.doc -131-200418452 ′ was removed under reduced pressure and dissolved; once burned in dichloromethane, and treated with triethylamine for 30 minutes. The solvent was removed in vacuo and the residue was used in the next step without further purification. e.izXlz ethynyl jb bite diyl · Benmou) _5_methanyl_t-furan-3_dicarboxylic acid formamidine H. Acetic anhydride (18 μl, 0.186 mmol) was added dropwise. Solution of compound 47 (c) (45 * g, 0.124¾ mole) in methylene chloride. The resulting solution was stirred at 0 ° C to room temperature for 24 hours. The reaction was quenched with water and extracted into ethyl acetate. The organic layer was washed with NaHC03 and a saline solution, dehydrated with Na2SO4, and reduced in number: hair. The crude material was purified by column chromatography (Shijiao, 4% 10% methanol in ethyl acetate) to provide 40 gram (80%) of the desired product as a white solid. Example 48 Preparation of 2- (4-fluoro-phenyl) -5-methoxy-6- (2-oxy ^ azolidinylbenzofuran-3-carboxylic acid formamidine Compound J? 48 (a) (2- (4-fluoro-phenyl) -6-methylfluorenyl-5-methoxy-benzofuran-3-carboxylic acid formamide).

TiCl4 (276 μl, 3.0 mmol) was slowly added to a solution of α, α-dichloromethyl methyl ether (107 μl, 1.20 mmol) in dichloromethane (1 mL). To this was added a suspension of compound 47 (a) (300 mg, 1 millimolar, which can be prepared according to the above Example 47, step a) in methylene chloride). After the addition is complete, remove the ice bath. The mixture was allowed to stir at room temperature for 15 hours, then poured into ice water and extracted 88828.doc -132- 200418452 with ethyl acetate. The organic phase was washed with water and saline, dehydrated, and concentrated under reduced pressure. The crude product was purified by column chromatography (stone gum, 30-50% ethyl acetate in hexane) to give 196 mg (60%) of a white solid. B. $ 备 m48_ {九) (6- (chloro-trimethylsilyloxy · methyl) _2- [2- (4-fluoro-phenyl)]-5-methoxy-benzene Benzofurancarboxylic acid formamidine).

48 (b) Add Znl2 (catalytic amount) to 0 ° C compound 48 (a) (80 mg, 0.25 mmol) and trimethylsilyl cyanide (40 μl, 0.3 mmol) Methyl chloride (1 mL) mixture. After stirring at 0 ° C for 30 minutes, another portion of trimethylsilane cyanide (30 µl) was added. The resulting mixture was allowed to stir at room temperature for 2 hours and at room temperature for 2 hours. The reaction was quenched with water and extracted with dichloromethane. The organic phase was washed with water and saline, dried over MgS04 and concentrated under reduced pressure. The crude product (90 mg) was taken to the next step without further purification. c · Rabbit Compound 48 (c) (6- (2-Amino-1-¾lyl-ethyl) -2- (4-Amino-phenyl) -5-methoxy-benzofuran-3 -Formamidine carboxylate).

Activated 10% Pd / C (20 mg) was added to a solution of compound 48 (c) (90 mg of 10: 1 ethanol / acetic acid). The mixture was shaken at 50 psig in Parr 88828.doc -133- 200418452 in the surplus state at room temperature for 48 hours. The reaction mixture was filtered through a CeliteTM sheet and wet with ethyl acetate. The filtrate was concentrated under reduced pressure to provide 60 mg (90% purity by lc / MS) of the product. Fluoro-phenylsulfan-6_ (2_hydrogen-sakizidine_5_some) -moth

Fill a sealed tube with a magnetic stir bar, compound 24 (b) (1.22 g, 30 millimoles, which can be prepared according to the above example 24, step b), palladium acetate (11) (34 mg, 0.015 mmol) Mol), [1, Γ-bis (diphenylphosphino) propane] (Dppp) (136 mg, 0.33 mmol), butyl ethyl ether (1.92 ml, 15 mmol) and K2C03 (622 Mg, 4.5 mmol) in DMF (5 ml). Fill the tube with -134- 88828.doc 200418452 with argon, seal and heat to 10 (rc for 24 hours, then cool to room temperature. Add 5% Ηα (20 ml) dropwise over 20 minutes and let acetic acid The mixture was extracted with acetamidine. The organic layer was washed with water and saline solution, dehydrated with MgSCu, and concentrated under reduced pressure. The crude material was purified by column chromatography (silica gel, 20% ethyl acetate in hexane) to produce 0 · 94 g (85%) of the desired product. Preparation: Compound 4_2χ ^ 6_ethylamido-2- (4-fluoro-phenyl) -5-hydroxy-benzyfuran-3-carboxylic acid formamidine ).

Slowly add boron trichloride (27.1 ml, dichloromethane solution at 1.0 mole concentration) to the compound 49 (a) (5.0 g, 13.6 mmol) at 0 ° C under argon. Dichloromethane (58 mL) solution. The mixture was allowed to stir at 0 ° C to room temperature for 1 hour. The mixture was poured into ice water (250 ml) and extracted with ethyl acetate. The organic layer was washed with saturated NaHC03 and a saline solution, dried over MgS04 and concentrated under reduced pressure. The crude material was purified by column chromatography (silica gel, 30% ethyl acetate in hexane) to yield 3.85 g (87%) of the desired product. c. Preparation of the compound fluorenyl-2- (4-fluoro-phenyl) -5-methoxy-aspartyl-3-methanomethamine.

88828.doc _ 135-200418452 Methane iodide (0.65 ml, 10.2 mmol) was added to compound 49 (bKl.35 g, 4.1¾ mole) and cesium carbonate (2.7 g, 8.3 mmol) NMP (2 ml) mixture. The resulting mixture was allowed to stir at room temperature for 24 hours. The reaction was quenched with water (50 ml), and extracted with ethyl acetate. The organic layer was washed with water and brine, dried over MgSCU and concentrated under reduced pressure. The crude product was purified by column chromatography (silica gel, 3 5% ethyl acetate in hexane) to yield 117 g (83%) of the desired product. Preparation of fluorophenyl light-l-methyl-1-methyl-ethyl-methyl benzoate. Compound 49 (c) (500 mg, 1.5 millimoles) in THF (1 ml) was added to 0 t: of / methyl magnesium odor (toluene / thF of 1.4 mole moles, 2.6 ml , 3.6 millimoles). The resulting mixture was allowed to stir at 0 ° C to room temperature for 1 hour. The reaction was quenched with ΝβΙΙ (1 mL) and extracted with ethyl acetate. The organic layer was washed with water and saline, dehydrated with MgSO and concentrated under reduced pressure. The crude material was purified by column chromatography (silica gel, 50% ethyl acetate in hexane) to provide 361 mg (70%) of the desired product. Example 50 2- (4-Gas-fungyl) _5-methoxy-6- (5 · methyl- "1,2.4] ρ-Wa-3-yl) Benzofuran-3-carboxylic acid methyl Preparation of amidoamine cyano-2- (4-fluoro-phenyl) _5-methoxy_benzoanan-3 -metanoate methyl ester).

88828.doc -136- 200418452 Anhydrous 1-methylpyrrolidone (60 ml) was added to compound 28 (d) (2.2 g, 5.80 mmol, which can be prepared according to the above example 28, step ad) and subcyanide A mixture of copper (1) (1.04 g, 11.61 mmol) and heated to 170 ° C. After stirring for 6 hours under argon, the reaction mixture was cooled to room temperature. Water (200 ml) and ethyl acetate (300 ml) were added, and the solution was filtered through CeliteTM tablets' and wet with ethyl acetate. The organic layer was separated, washed with water (3 X 100 ml) and brine, dried over MgS04, and concentrated under reduced pressure. The crude material was purified by column chromatography (stone gum, 20-40% ethyl acetate in hexane) to yield 11.5 g (79%) of the desired product. b. Compound 50 (b) (2- (4-Fluoro-phenyl) -6- (N-hydroxyiminoaminomethyl) -5-methoxy-benzocran_3_ Methyl a few acid).

Hydroxylamine hydrochloride (182 mg, 2.615 mmol) was added to compound 50 (a) (340 ¾ g, ιο46 * mol) in ethanol (50 ml) and triethylamine (393 μl, 2.842¾ mole) &lt; Stir the suspension. The mixture was allowed to stir for 12 hours, cold to warm to room temperature, diluted with water (100 mL) and filtered. The separated solid was washed with water and hexane and dried in a vacuum oven to produce 300 mg (80%) of the desired compound.

-[1,2,4] 'monofluoren-3-yl) -benzocran-3-methylacetate). 88828.doc -137- 200418452

Add 5% (65 g, 3.35 19 mol) followed by acetic anhydride (237 μl, 2.55 ¾ mol) with compound 50 (b) (300 mg, 0.838 mol) 1'2-chloroethane (10 ml) solution. After refluxing under argon pressure for 12 hours, the reaction mixture was cooled to room temperature, diluted with water and extracted with dichloromethane. The organic layer was washed with water and saline, dehydrated with MgSO and concentrated. The crude product was purified by hydration chromatography (silica gel, 10-30% ethyl acetate in hexane) to provide 3.80 * g (50%) of the desired product. Methane-6-Γ5-methan- "1 9 carboxylic acid formazaninaceae. The title compound (5.55 mg) was essentially prepared according to the general method of Example 15, step b, step ^ above. However, in step 骡 b, compound 5〇 (cU compound 15 (a) is used. Generation is proficient in selecting suitable starting materials, and can be made into other compounds of this subject according to the previous examples. Therefore, the preparation is further Representative examples of benzoxanthan derivatives and analogues are listed in Table 1 below.

88828.doc -138- 200418452 Instance number Ri R2 r3 R4 Rs r6 1. Η -〇ch3 HH ch3 2. Η -〇cf3 HH ch3 3. Η -och3 HH ch3 4. Η -OCH (CH3) 2 HH ch3 H 5. Η -〇ch (ch3) 2 HH ch3 6. Η -OCH (CH3) 2 ΟνΛ H ch3 ^ 0 ^ F 7. Η -〇chf2 HH ch3 8. Η -OCH (CH3) 2 -NH (CH2) 2OCH3 H ch3 9. Η -ch3 HH ch3 10. Η -ch3 HH ch3 11. Η -och2cf3 HH ch3 12 · Η -och3 HH ch3 heart F 13. Η -och3 Br H ch3 14. Η -och3 ch3 H ch3 15 Η -OCH (CH3) 2 ρΛ i ^ NH ch3 ^ 0 ~ F 16. Η -och (ch3) 2 nh2 H ch3 17. Η -〇ch3 nh2 H ch3 18. Η -och3 -NH (C = 0) CH3 H ch3 19. Η -OCH (CH3) 2 -nhch3 H ch3 -139- 88828.doc 200418452 Example number Ri R2 R3 R4 Rs Re 20. Η -OCH (CH3) 2 -n (ch3) 2 H ch3 21. Η -OCH (CH3) 2 -NH (S02) CH3 H ch3 22. Η -och (ch3) 2 -NHCH2CH3 H ch3 23. Η -OCH (CH3) 2 -N (CH2CH3) 2 H ch3 24. Η -och (ch3) 2 〇〇Λ H ch3 25. ch3 -och3 HH ch3 26. Η -CN HH ch3 27. Η -OCH (CH3) 2 HH ch3 28 · Η -och3 h3c ch3 H ch3 29. Η -och3 -N (CH3) S02CH3 H ch3 30. Η &gt; 〇〇Λ H ch3 31. Η &gt; H3C ^ O ^ N ^ I 1 2 ch3 H ch3 32. Η -OCH2CH3 -n (ch2ch3) so2ch3 H ch3 33. Η 〇〇Λ H ch3 34. Η -OCH (CH3) 2 ch3 H ch3 35. Η 4S1 0 N ~ 〇〇Λ H ch3 -140- 88828.doc 200418452 Example number Ri R2 R3 R4 Rs r6 36. Η -OCH (CH3) 2 H ch3 ^ 〇-F 37. Η -OCH (CH3) 2 ho'Vn H ch3 38. Η -OCH2CH3 / S〇2 π 1 ch3 H ch3 39. Η OH V / S〇2 π in3 H ch3 \ Qn 40. Η -och3 HO X〇-NH ch3 ^ 0 &quot; f 41. Η -och3 0-NH ch3 F〇 ~ f 42. Η '-OCH3 H, s \ 4, HO H ch3 43. Η / S〇2 -7 π OH H ch3 44. Η -CH2CH3 -nhso2ch3 H ch3 45. Η -CH2CH3 ^ so2, Η3〇 &quot; νΛ ch3 H ch3 ^ 0 &quot; f 46. Η -CH2CH3 OH H ch3 47. Η -0CH3 HH ch3 48. Η -OCH3 〇H ch3 -141-88828.doc 200418452 Example number Ri R2 R3 R4 Rs 49. Η -och3 -C (OH) (CH3) 2 H ch3 ^ 0 ~ F 50. Η -〇ch3 h3c H ch3 51. Η -0 (CH2) 3-〇H h3c ch3 H ch3 ^ 0 &quot; f 52. Η QV 1 ch3 H ch3 ^ 0 &quot; F 53. Η VHH ch3 54. Η -〇ch3 HH ch3 ^ O ~ 0CH3 55. Η -och3 HH ch3 .Cp3 56. Η -och3 HH ch3 K ^ CF; 57. Η -OC H2CH3 HH ch3 58. Η -OCH3 HH ch3 59. Η -OCH (CH3) 2 HH ch3 60. Η -0 (CH2) 3CH3 HH ch3 61. Η -0 (CH2) 2CH3 HH ch3 62 · Η -och3 HH ch3 63. Η -0CH3 H ch3 ch3 64. Η -OCH2CF3 HH ch3 65. Η -OCH (CH3) 2 HH ch3 -142- 88828.doc 200418452

Example number Ri r2 r3 R4 Rs R6 66. Η -och3 HH ch3 Cl 67. Η Η och3 H ch3 68. Η -〇ch3 HH ch3 69. Η -och3 HH ch3 70. Η -och3 HH ch3 K3 ^ Br 71. Η -och3 HH ch3 ch3 K ^ f 72. Η -och3 H ch3 ch3 73. Η &quot; Cl HH ch3 74. Η t-butyl HH ch3 75. Η Cl HH ch3 ^ 0-CH3 76. Η -och3 HH ch3 Cl 77 · och -och3 HH ch3 78. Η -ch2och3 HH ch3 79. Η -OCH (CH3) 2 ch3 H ch3 80. Η -OCH (CH3) 2 H ch3 ch3 81. Η -〇ch3 ch3 82. Η FHH ch3 83. Η FHH ch3 ^ Q-ch2ch3 84. Η -ch2ch3 HH ch3 \ Q

88828.doc -143- 200418452 Instance number Ri R2 R3 R4 Rs R6 85. Η -och3 HH ch3 Cl 86. Η -ch (ch3) 2 HH ch3 87. Η -och2ch3 HH ch3 Cl 88. Η -och3 HH ch3 89 Η Cl HH ch3 K) 90. Η -OCH (CH3) HH ch3 91. Η -och (ch3) 3 HH ch3 92. Η -〇ch (ch3) 2 Br H ch3 93. Η -och3 HH ch3 94. Och -och3 och3 H ch3 95. Η -OCH (CH3) 2 HH ch3 96. Η FHH ch3 97. Η -OCH (CH3) COOH ch3 H ch3 98. Η -och (ch3) 2 -NH (C = 0) CH3 H ch3 99. Η -OCH (CH3) 2 HH ch3 100. Η -OCH (CH3) 2 o, H ch3 101. Η -OCH (CH3) 2 〇Λ H ch3 102. Η -och3 -〇ch3 H ch3 -144- 88828.doc 200418452 Example number Ri R2 r3 R4 Rs 103. Η-och3 〇〇Λ ch3 104. Η -OCH (CH3) 2 H Η ch3 105. Η -och (ch3) 2 H Η ch3 OH 106 Η -och (ch3) 2 H Η ch3 ^ 〇 ~ cn 107. Η -och3 H Η ch3 108. Η -och (ch3) 2 H3C ^ S〇2 Η ch3 109. Η -OCH (CH3) 2 ΟνΛ Η ch3 110. Η -OCH (CH3) 2 ρΛ HO Η ch3 111. Η -OCH (CH3) 2 -N (CH3) S02CH3 Η ch3 ^ 0 ~ F 112. Η -OCH (CH3) 2 Η ch3 113. Η- OCH (CH3) 2 H〇v ^ HO 'Η ch3 ^ 0 &quot; F 114. Η -och (ch3) 2 -NHCH (CH3) 2 Η ch3 115. Η -och (ch3) 2 Η ch3 116. Η -och3 Η ch3 117. Η 〇〇Λ Η ch3 ^ 0 ^ F 118. Η -ch2oh Η Η ch3 119. Η -OCH (CH3) 2 η3〇- ° ^ χνΛ ch3 Η ch3 H〇 ~ f -145-88828.doc 200418452 Example 1 number, K1 R2 R3 R4 Rs iu 120. Η cr ° ^ nh2 H ch3 121. Η -OCH (CH3) 2 HH ch3 122. Η -och3 -NH (S02) CH3 H ch3 123. Η -och (ch3) 2 H ch3 124. Η -OH 〇〇Λ H ch3 125. Η 〇〇Λ H ch3 ^ 〇-F 126. Η -och3 Cl H ch3 K ^ f 127. Η -OCH (CH3) 2 ch3 h H ch3 KD ^ f 128. Η 〇〇Λ H ch3 ^ 0 ~ F 129. Η -OCH (CH3) 2 -CN H ch3 130. Η -och3 HH -ch2ch3 131. Η -OCH (CH3) 2 1 HH ch3 \ ^ \) rY 132. Η -OCH (CH3) 2 H ch3 133. Η -OCH (CH3) 2 c 丨 ^^ H H ch3 Heart F 134. O -OCH (CH3) 2. Fen H ch3 135. Η -〇ch (ch3) 2 -NHC (= 0) NH2 H ch3 136. Η -OCH (CH3) 2 -n (ch (ch3) 2so2ch3 H ch3 -146- 88828.doc 200418452 Example number Ri r2 R3 R4 Rs R6 137. Η -OCH (CH3) 2 〇 &gt; -νΛ H3C VH ch3 138. Η -OCH (CH3) 2 ch3 H ch3 139. Η -OCH (CH3) 2 ν · ν-λ V % H ch3 140. Η -OCH (CH3) 2 ννH H ch3 141. Η -OCH (CH3) 2 OH H ch3 142. Η -OCH (CH3) 2 〇0 ^ H ch3 143. Η -OCH (CH3) 2 -so2nhch3 H ch3 144. Η -OCH (CH3) 2 -S02N (CH3) 2 H ch3 145. Η -och (ch3) 2 -NH (S02) CH (CH3) 2 H ch3 146. Η -och (ch3 ) 2 -C (= 0) NH2 H ch3 147. Η -OCH (CH3) 2 H ch3 148. Η -och (ch3) 2 -NHC (CH3) 3 H ch3 149. Η -OCH (CH3) 2 -so2nh2 H ch3 ^ 〇-p 150. Η -OCH (CH3) 2 crK8 H ch3 151. Η -OCH (CH3) 2 H ch3 -147- 88828.doc 200418452 Example number Ri R2 r3 R4 R5 R6 152. Η -OCH ( CH3) 2 H ch3 153. Η -OCH (CH3) 2 H ch3 ^ 0 &quot; F 154. Η -OCH (CH3) 2 〇》 si H ch3 155. '' O -OCH (CH3) 2 4 0 H ch3 Heart F 156. * Η -OCH (CH3) 2 h3c &gt; H ch3 157. Η -OCH (CH3) 2 H ch3 158. Η -OCH (CH3) 2 -och3 H ch3 159. Η -och (ch3) 2 h3C \ ch3 H ch3 160. Η -och (ch3) 2 -C (= 0) HH ch3 161. Η -OCH (CH3) 2 FNH ch3 162. Η -OCH (CH3) 2 -CH2NHS02CH3 H ch3 163. Η -OCH (CH3) 2 CH,. 0 H ch3 ^ 0 &quot; f 164. Η -〇ch (ch3) 2 Η〇 ～ νΛ H3cA H ch3 hChF 165. Η OH -och3 H ch3 166. Η -OCH2CH3 〇〇Λ H ch3 -148- 88828.doc 200418452 Example number Ri R2 R3 R4 Rs 167. Η Fxx〇v &gt; 〇0 ^ H ch3 168. Η -OCH (CH3) 2 H ch3 169. Η -OCH (CH3) 2 H ch3 170. Η -OCH (CH3) 2 FM FH ch3 171. 'Η -och (ch3) 2 H ch3 f〇 ~ F 172. Η -ochf2 〇〇Λ H ch3 173. Η Cr ° &gt; 〇〇Λ H ch3 174. Η -OH -nhso2ch3 H ch3 175. Η -OCH (CH3) 2 H ch3 176. Η -OCH (CH3) 2 p. HO H ch3 177. Η -OCH (CH3) 2 H ch3 Heart F 178. Η -〇ch (ch3) 2 h3c, H ch3 \ Όη 179. Η -OCH (CH3) 2 -30 ^ H ch3 ^ 〇-f 180. Η 〇〇Λ H ch3 -149- 88828.doc 200418452 Example number Ri R2 r3 R4 Rs R6 181. Η -och3 (ΧοΛ Η ch3 182. Η -OH -nh2 Η ch3 183. Η 0uv &gt; Η ch3 184 … -OCH (CH3) 2 〇Γ Η ch3 185, Η -och (ch3) 2 Η2ΝγΝ ^ 〇Η ch3 186. Η -OCH (CH3) 2 3〇Λ Η ch3 187. Η -OCH (CH3) 2- COOH Η ch3 188. Η -OCH (CH3) 2 ννΛ Η ch3 189. Η -OCH (CH3) 2 Η ch3 190. Η -〇ch (ch3) 2 Η ch3 191. Η -OCH (CH3) 2 0 Η ch3 192. Η -OH -ορ Η ch3 193. Η -OCH (CH3) 2 η /. 2 Η ch3 ^ 0 &quot; f 194. Η -OCH (CH3) 2 (ΤοΛ Η ch3 -150- 88828.doc 200418452 Example Number Ri r2 Ra R4 ^ 5 R6 195. Η -OCH (CH3) 2 ^ so2, H3C, ΝΛ ch2 Η ch3 196. Η -OCH (CH3) 2 -C (= 0) CH3 Η ch3 197. Η -och ( ch3) 2 -nhso2ch3 Η -CH (CH3) 2 198 .: Η -〇ch (ch3) 2 y = ^ N h3c Η ch3 199, Η -OCH (CH3) 2 -NHS02CH3 Η fO-F 200. Η -OCH (CH3) 2 -NHSO2CH3 Η -ch2ch3 201. Η 〇〇Λ ch3 202. Η -och (ch3) 2 -C (CH3) 20H Η ch3 Heart F 203. Η ch3 CH3 ^ 〇〇λ λ ch3 204. Η ch3 H3C ^ X〇v h3c &gt; 〇〇λ ch ch3 205. Η -OCH (CH3) 2 \ ^ N Η ch3 ^ 〇-F 206. Η Cl— ^ Jf 〇〇Λ Η ch3 207. Η HC / TO N. Human V 〇〇Λ Η ch3 heart F 208. Η -och3 -OH ch3 -151-88828.doc 200418452 Example number Ri R2 r3 R4 Rs 209. Η ν ^ μ 〇〇Λ ch3 210. Η / CH3 〇〇Λ ch3 211. Η -och3 Η ch3 212. Η F ^ rv CH3 〇〇Λ Η ch3 213. Η Nlv 〇〇λ ch ch3 ^ 0 ^ F 214. Η Corpse 3 0 〇, person 〇〆〇〇λ ch3 215. Η -0CH2C (= 0) CH3 〇〇λ Η ch3 216. Η 9 〇〇λ Η ch3 217. Η n ^ ch3 h3c 〇〇λ Η ch3 ^ 0 &quot; f 218. Η 〇0Λ Η ch3 219. Η -OCH (CH3) 2 Η ch3 220. Η -OCH (CH3) 2 Η ch3 -152- 88828.doc 200418452 instance number Ri R2 R3 R4 Rs 221. Η -och3 ^ so2, H3C ΝΛ h3c human ^ ch3 H ch3 ^ 0 ^ F 222. Η -OCH (CH3) 2 -CH (OH ) CH3 H ch3 223. Η -och (ch3) 2 H ch3 Heart F 224. Η -OCH (CH3) 2 -ch2oh H ch3 225. Η 〇〇Λ H ch3 226. * Η -0 (CH2) 20CH3 〇〇Λ H ch3 227. Η -OCH (CH3) 2 H ch3 228. Η h3C \ / N, n Wv Cl 〇〇Λ H ch3 229. Η ch3 〇〇λ H ch3 ^ 0 &quot; F 230. Η -och (ch3) 2 H ch3 231. Η -och (ch3) 2 cf77-\ η3 H ch3 232. Η -OCH (CH3) 2 fY ^ NN h3c H ch3 233. Η -och (ch3) 2 h3c H ch3 234. Η -〇ch (ch3) 2, S〇2, ¥ V \ Cl H ch3 -153-88828.doc 200418452 instance number Ri R2 r3 R4 r5 Re 235. Η -och (ch3) 2 ch3 h3c H ch3 236. Η -och3 H ch3 H〇 ^ f 237. Η -OCH (CH3) 2 -CH2N (CH3) 2 H ch3 238. Η -OCH (CH3) 2 -CH (OH) CH (CH3) 2 H ch3 239. Η- OCH (CH3) 2 r H ch3 240. Η -och3 s 〇, ch3 H ch3 241. Η -OCH (CH3) 2 r H ch3 242. Η -OCH (CH3) 2 H3C-〇H ch3 243. Η H- nhso2ch3 H ch3 244. Η -och (ch3) 2 H ch3 H〇 ^ f 245. Η -OCH (CH3) 2 ch3 H ch3 ❹F 246. Η -OCH (CH3) 2 ch3 it ch3 H ch3 H〇 ^ f 247 Η -OCH (CH3) 2 H ch3 Η〇 ^ ρ -154- 88828.doc 200418452 Example number Ri R2 R3 R4 Rs R6 248. Η -och (ch3) 2 rN ch3 Η ch3 249. Η -och (ch3) 2 -CH2N (CH3) S〇2CH3 Η ch3 ^ 0 ^ F 250. Η ΗΟν ch3 〇〇Λ Η ch3 251. Η Xv h3c r 〇〇Λ Η ch3 252. Η OH H3C ^^ 〇yi 〇〇Λ ch ch3 ^ 0 ~ F 253. Η -OCH (CH3) 2 ho, ^ ch3 &gt; ο2 h3c Η ch3 254 Η CH3 〇〇Λ Η ch3 255. Η -OCH (CH3) 2 s〇2 h3c Η ch3 ^ 0 &quot; f 256. Η -och3 ch3 H CH3 Η ch3 257. Η -OCH (CH3) 2 〇 &quot; 7 H CH3 Η ch3 258. Η V〇'ch3 Η Η ch3 ^ 0 &quot; f 259. Η H〇 &gt; XX〇y Η ch ch3 ^ 0 ~ F 260. Η ° γ-0Η Η ch ch3 -155-88828.doc 200418452 Example number Ri r2 r3 R4 Rs 261. Η -och3 -C (= 0) CH3 H ch3 262. Η 〇〇Λ H ch3 ^ 0'F 263. Η V0kch3 〇〇Λ H ch3 264. Η -OCH (CH3 ) 2 ch3 H3C CH3 H ch3 265. Η -OCH (CH3) 2 cr ^ H ch3 266. Η -och3 -CN H ch3 267. Η η〇ΛΧΧ〇 ^ 〇〇Λ H ch3 \ Qn 268. Η ° γ- ΟΗ 〇〇Λ H ch3 269. Η -OCH (CH3) 2 h3c-so2 ch3 H ch3 270. Η -OCH (CH3) 2 h3C 10, ch3 H ch3 271. Η -OCH (CH3) 2 S-3 N Gas ch3 H ch3 V \ jTy 156- 88828.doc 200418452 Example number Ri R2 r3 R | Rs R6 272. Η -OCH (CH3) 2 h3c-OH H ch3 ^ 〇-f 273. Η -OCH (CH3) 2 H ch3 heart F 274. Η -OCH (CH3) 2 〇-NH ch3 heart F 275. Η -OCH (CH3) 2 ct7 S〇2 CH3 H ch3 276. Η -OH -C (= 0) CH3 H ch3 277. Η -och3 Η3〇 ^ 〇2-νΛ h3c &gt; H ch3 278. Η -och3 Η n H ch3 279. Η -OCH (CH3) 2 H ch3 280. Η -〇ch3 ch3 〇, ch3 H ch3 ^ 0 &quot; f 281. Η -OCH (CH3) 2 η ”〇 2. Λ H ch3 282. Η -OCH (CH3) 2 ^ .so2, H3C, νΛ ch3 H ch3 Heart F 283. Η -OCH (CH3) 2 ON H ch3 -157- 88828.doc 200418452 instance number Ri r2 r3 R4 Rs R6 284. Η -och (ch3) 2 ^ so2 ¥ H3C ^ H ch3 285. Η -OCH (CH3) 2 cv H ch3 ^ 0F 286. Η -OCH (CH3) 2 〇H ch3 287. Η -OH / s〇2, ch3 H ch3 ^ 〇-F 288. Η H2c ^^ ° y ^ so2 ^ ch2 H ch3 289. Η -och3 / S〇2, H3C H3cA〇H ch3 290. Η -och3 η "\ λ NC ^ 〇h3 H ch3 291. Η -och3 Η / \ Λ ct1 H ch3 ^ 〇-ρ 292. Η -OCH (CH3) 2 / SO, ¥ 〇H ch3 293. Η h3c ch3 0 乂 0 V 〇〇Λ H ch3 -158- 88828.doc 200418452 Examples 5 Tiger Ri r2 r3 R4 Rs Re 294. Η h3c ch3 0 乂 0 ό ^ ° V / S02 -T ¥ 'Λ h3c 」H ch3 295. Η -och3 H ch3 296 ., Η -och3 H ch3 ^ 0F 297. Η -OH / S〇2 Μ H3c '' H ch3 298. Η -ochf2 / S〇2 -T H3C ch3 H ch3 ^ 0 ~ F 299. Η -och3 h 广 302, Λ (y H ch3 300. Η -ch3 -C (CH3) 2〇HH ch3 301. Η -ch3 -C (= 0) CH3 H ch3 H〇 ^ f 302. Η h3c ch3 〇X〇V / S〇2 -r H3C &quot; νΛ ch3 H ch3 303. Η -〇ch3哕 丫 \ h3〆, H ch3 304. Η -och3 H3C ^ yZZ7 HN ch3 H ch3 305. Η 〇-ch3 ° &quot; χλ V / S〇2 -r ΊΛ ch3 H ch3 ^ 0 &quot; f 159- 88828.doc 200418452 Example series 5 Tiger Ri R2 R3 «4 Rs R6 306. Η Y〇-CH3 δ, V ^ so2 ^ CH3 H ch3 307. Η -och3 FH ch3 308. Η -och3 c— H ch3 ^ 0 ^ F 309. 4 Η -och3 Ct7 f〇2 ch3 H ch3 310. Η -och3 V 0, ch3 H ch3 311. Η OH V ch3 H ch3 312. Η ° Y〇HV / S02 1 CH3 H ch3 313. Η -och3 Vn H ch3 314. Η -OH h3c ch3 H ch3 315. Η -och3 〇H ch3 -160- 88828.doc 200418452 instance number Ri r2 R3 R4 Rs 316. Η -och3 〇'cf3 H ch3 317. Η -och3 H ch3 318. Η -och3 h3c ch3 H ch3 〇h3c &gt; 319. Η / ^ N s person V ^ so2, H ^ c ch3 H ch3 320. Η HC-s person 〇yJ ^ S〇2 1 H3C ch3 H ch3 321. Η / S〇2 ^ ¥ ch3 H ch3 322. Η -OCH (CH3) 2 / S〇2 -7 \-^ OH Φ FH ch3 ^ 0 &quot; f 323. Η -〇ch3 CC ch3 H ch3 324. Η n ^ ch3 ch3 / S〇2 -T h3c νΛ ch3 H ch3 ^ 〇-F 325. Η 〇XH3 V / S〇2 -7 ¥ ch3 H ch3 326. Η -OH / S02 ^ π H3C y1 ch3 H ch3 -161-88828.doc 200418452

Example number Ri R2 R3 R4 Rs 327. Η ° Α V / S02 -r ch3 H ch3 328. Η 〇, V / S02 1 ch3 H ch3 329. Η h3c η3〇 ^ ° Τ ° V / S〇2 1 H3C ch3 H ch3 330. Η -och3 / S〇2-, ¥ H ch3 ^ 0 &quot; F 331 · Η -och3 η / \ Λ VN h3c H ch3 ^ 0 &quot; f 332. Η -F / S02 1 HH ch3 ^ 0 ~ F 333. Η -F / S〇2 -r h3c ^ H ch3 ^ 0 ~ F 334. Η -och3 h3c, so2 H ch3 ^ OκF 335. Η -CH2CH3??. H ch3 ^ 0 * ~ f 336. Η -OCH3 H3C \, ch3 H ch3 ^ 0F -162- 88828.doc 200418452

Instance number Ri r2 R3 R4 Rs R6 337. Η -CH2CH3 Άλ FH ch3 338. Η -o (ch2) 2ch3 ch3 H ch3 339. Η -CH2CH3 -c (ch3) 2oh H ch3 ^ 0 ^ F 340. Η -ch2ch3 -C (= 0) CH3 H ch3 hcyp 341… Η -OH ηνΛ h3c ^ H ch3 hcyp 342. C1 -h3c ^ h3c ^ H ch3 F〇 ~ f 343. Η -CH2CH3 ¥ cf .H ch3 \ Qn 344. Η -OCH3 h3C \ H ch3 345. Η -OCH3 〇H ch3 \ Qr ^ 346. Η; AV / S02 ^ H3C, νΛ 1 ch3 H ch3 ^ 0 ~ F 347. ΗCHV / S02 1 H3 ° ννΛ ch3 H ch3 348. Η -0 (CH2) 2CH3 / S〇2 -T CH3 H ch3 ❹F -163- 88828.doc 200418452 instance number Ri r2 R3 «4 Rs Re 349. Η H2C'v / S02 -r H3C &quot; Λ CH3 H ch3 350. Η • och3 h3c ^ ° 〇-n H ch3 351. ^ ^ SOz 1 h3 ° ch3 H ch3 352. Η 〇 / CH3 / 〇h3c ° y / S02 ¥ ch3 H ch3 353. Η so. HsC Χχ V / S〇2 -TH ^ c ch3 H ch3 ^ o ~ p 354. Η -OH HV 〇H ch3 355. Η 0, ch3 ^ so2 ^ 1 ch3 H ch3 \ Qn 356. Η NV / S02 ¥ ch3 H ch3 \ QtY 357. Η V / S〇2 -T ¥ CH3 H ch3 358. Η -och3 H ch3 -164- 88828.doc 200418452 Example number Ri R2 R3 R4 Rs R6 359. Η Ιν Ν r 〇-Λ ch3 ^ S02 1 π 1 ch3 H ch3 ^ 0 ^ F 360 ... Η F ^ so2 ^ ¥ CH3 H ch3 ^ 0 &quot; f 361. * Η -OCH (CH3) 2 ^ so2, ¥ cy H ch3 362. Cl -och3 N 7 h3c ^ H ch3 ^ 0F 363. Cl -och3 h3c ^ H ch3 364. Η -OH h3c ^ H ch3 365. Η Br h3c '' H ch3 366. Η h3c ^ H ch3 367. Η HC HN ^ h3c ^ H ch3 hG ^ f 368. Η -och3 rr ^ VN ΓΝΗ2 H ch3 \ Qn 369. Η h3c r / S02 1 ¥ CH3 H ch3 -165- 88828.doc 200418452 instance number Ri R2 R3 R4 Rs R6 370. Η ΟΗ Human V h3c ^ / S〇2 -T H3C CH3 H ch3 371. Η Ν ^ κ, V V CH3 ^ so2 H3 ° ννΛ ch3 H ch3 372. Η • och3 h3c 0 〇-NH ch3 373. Η / S, N h3c 〆H3C ^ ^ S〇2 1 H3C, ΝΛ 1 CH3 H ch3 374. Η / S02 1 HaC ννΛ 〇h3 H ch3 Heart F 375. Η -OCH (CH3) 2 HzN ^ HO \ ch3 H ch3 376. Η -och (ch3) 2 h3c ^ η3〇Λ ^ H ch3 ^ 0 ~ F 377. Η -och3 〇H ch3 378. Η -och3 ch3 it ch3 H -ch2ch3 ^ 0 ^ F 379. Η -och3 ch3 jealous ch3 H -CH (CH3) 2 F〇 ~ f 380. Η -och3 ch3 ch3 H ^ 0F 381. Η -OCH (CH3) 2 〇H ch3 -166- 88828.doc 200418452 Example number Ri R2 r3 R4 Rs R6 382 . Η h3c ^ so2 i h3c νΛ έπ3 H ch3 ^ 0 ^ F 383. Η -〇ch3 H3CV ^^-nh H ch3 384. Η -och3 H, C H3C NH2 H ch3 \ Qn 385. Η -och3 h3c H H3U NH &gt; hCH3 〇H ch3 386. Η j_〇h〇 ^^ / S〇2 -T HaC ch3 H ch3 387. Η -och3 ch3 H ch3 \ J \ JTY 388. Η ^ so2 ^ H3 ° χνΛ ch3 H ch3 ^ 〇-f 389. Η -och3 0 H ch3 390. Η -och3 HX NH h3c'S〇2 H ch3 391. Η V ς Br ^ H ch3 392. Η r ° y ch3 / so: i ch3 H ch3 393 Η ho y / S〇2 -7 ¥ ch3 H ch3 -167- 88828.doc 200418452 instance number Ri r2 r3 R4 Rs R6 394. Η -och3 'Λ ch3 H ch3 ^ 0 ^ F 395. Η Νν ν ^ so2 , H3C ch3 H ch3 396. Η ^ so2 H ^ c CH3 H ch3 397. &quot; Η, ^ Ν / S02, ch3 H ch3 398. Η CCv / S〇2 1 H3C &quot; νΛ I ch3 H ch3 ^ 0F 399 Η 0.0, / S〇2 ^ H3C ch3 H ch3 400. Η -och3 h3c ch3 H ch3 F 401. Η &lt; χν H, C ch3 H ch3 H〇 ~ f 402. Η Η? Ν Ίν ^ so2 H3C έπ3 H ch3 heart F 403. Η h3c, ν ^ μ ν ^ ν CI / S02-, H3C ch3 H ch3 404. Η ϋ ~ ν / S〇2-, H3C 'ch3 H ch3 f〇 ~ F 405. Η / S 〇2 -7 H ^ c CH3 H ch3 ❹F 406. Η -〇ch3 H -7 ηΛ H ch3 -168- 88828.doc 200418452 instance number Ri R2 r3 R4 Rs 407. Η OWCH3 ch3 ^ S02 1 ¥ H Η ch3 408. Η 〇γν ch3 ^ so2, CH3 Η ch3 409. Η y〇, N h3cAA ^ o ^ h3c ch3 Η ch3 \ Qn 410. Η HaC ch3 Η ch3 411. Η H -C (= 0) CH3 Η ch3 K ^ f 412. Η -H ^ ch3 h3c Oy ^ so2 1 CH3 Η ch3 ^ 0F 413. Η H, producing V h3c / S02 -7 ΊΛ ch3 Η ch3 414. Η -OCH2CH3 h3c ch3 Η ch3 415. Η / S〇2 ”H3C ch3 Η ch3 416. Η / S02 ^ H ^ c ch3 Η ch3 F〇 ~ f 417. Η h3c h3c ^ X 1 3 NN 1 HV \, s〇2-, HaC ννΛ ch3 Η ch3 \ Qn 418. Η / S02 1 π Η ch ch3 Ky-- 169- 88828.doc 200418452 Example number Ri r2 R3 R4 Rs R6 419. Η V h3c it ch3 H ch3 420. Η ^ so2, H3C 'νΛ HH ch3 421. Η Ίν Η / S02 -T ¥ Ά 1 ch3 H ch3 422 〇 户 〇2 H3C H ch3 ^ 0F 423. Η -OCH2CH3 叩 一 &quot; νΛ η3〇 ^ H ch3 424. Η 0 ^ so2 π in3 H ch3 ^ 0F 425. Η ch3 / S〇2 -Γ H3C ch3 H ch3 426. Η H rS〇2 H3C, νΛ Η H ch3 ^ 0 &quot; f 427. Η V ^ v ch3 h3c ch3 H ch3 ^ 〇-F 428. Η h3c ch3 H ch3 429. Η 〇YCH3 ch3 HC 'tt ch3 H ch3 V \ JTY 430. Η -och3 h3c H ch3 -170- 88828.doc 200418452 Example number Ri R2 r3 R4 Rs 431. Och -och3 N Η0 &lt; Λλ H ch3 432. Cl -och3 H3C ^ N ^ Λ / h3c H ch3 heart F 433. Η QV h3c ch3 H ch3 434. Η .0 ~ V h3c CH3 H ch3 435. Η-/ = =: NS 丄 HH ch3 436. Η -och3 -C (= 0) CH20H H ch3 Heart F 437. Η / s〇2 ch3 H ch3 438. Η -OH ， S〇2 -7 π <νΛ * Y ^ h3 OH H ch3 439. Η -och3 ^ so2 ik ^ 〇H3 OH H ch3 440. Η -ch2ch3 Y0 h3c H ch3 ^ 0 &quot; f 441. Η a ^ so2 ^ ¥, νΛ HH ch3 442. Η -och3 a &quot; H ch3 -171-88828.doc 200418452

Example number Ri R2 R3 R4 Rs 443. Η -0 (CH2) 2CH3 / S〇2, π l H ch3 444. Η -OH in3 H ch3 ^ 0F 445. Η -0 (CH2) 2CH3 ^ so2, H ch3 ^ 0 ~ F 446. * Η Vv / S〇2 -T l H ch3 447. Η N / S〇2 -7 π l H ch3 448. Η -OCH (CH3) 2 H ch3 heart F 449. Η -och3 H ch3 ^ 〇-F 450. Η a ch3 H ch3 \ Qn 451. Η -OH / S02 1 1 FH ch3 ^ 0 &quot; F 452. Η -och3 HH ch3 453. Η -OH HH ch3 \ Q 172- 88828.doc 200418452 Table 2. Additional experimental data for the examples listed in Table 1. Table 2 Examples No.Name-NMR data Mass Spec HCV pol -BB7 IC5〇 (μΜ) A = 彡 0 · 5 / iM B = 03 to &lt;: 5.0 C = 5.0 to ^ 30 D = &gt; 30 μΜ replicon (liM) 1. _ 2. Fulfanyl-5-methoxy-phenylsulfan-3-carboxylic acid formamidine 醯 (M + H) ^ 272 B &lt; 30 2. 2-Benzyl-5-trifluoromethoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in Dimethyl- ^ Sulfoxide (DMSO): 8.47-8.49 (d, J = 4.69 Hz, H); 7.88-7.91 (dd, J = 1.76Hz, 8.21Hz, 2H); 7.80-7.83 (d, J = 9.38Hz, 1H); 7.50-7.57 (m, 3H); 7.38-7.41 (d , J = 8.79Hz, 1H); 2.83-2.84 (d, J = 4.69Hz, 3H) (M + H) + = 336 B 氺 氺 氺 3. 2- (3,4-difluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.44 (s, 1H); 7.98 (m, 1H); 7.74 (m, 1H); 7.60 (m, 2H) ; 7.12 (m, 1H); 7.03 (m, 1H); 3.82 (s, 3H); 2.85 (d, J = 4.2Hz, 3H) (M + H) + = 318 A &lt; 10 4. 2- [4- (Ethylamidoamino-methyl) -xyloyl] -5-isopropoxy-benzofuran-3-chimonoformamidine * H NMR in DMSO: 835 (bm, 2H); 7.78 (d, 2H, J = 8.21); 7.52 (d, 1H, J = 8.79); 7.36 (d, 2H, J = 7.03); 7.04 (d, 1H, J = 2.34); 6.93 (dd, 1H, J = 8.79, 2.34); 4.59 (m, 1H); 4.28 (d, 2H, J = 5.86); 2.80 (d, 3H, J = 4.69); 1.87 (s, 3H); 1.26 (d, 6H, J = 5.86) (M + H) + = 381 B &lt; 30 5. 2- (4-Hydroxy-phenyl) -5-isopropoxy-benzoporan-3-carboxylic acid formamidine'H NMR in DMSO: 9.91 (s, 1H); 8.20 (d, 1H, J = 4.69); 7.70 (d, 2H, J = 8.79); 7.47 (d, 1H, J = 8.79); 7.02 (d, 1H, J = 2.34); 6.86 (m, 3H); 4.57 (m, 1H); 2.79 (d, 3H, J = 4.69); 1.26 (d, 6H, J = 5.86) (MH) · = 324 B &lt; 10 6. 2- (4-Fluoro-phenyl) -5-isopropoxy-6 · ^ than Gyodo-1-Li-private 17-furan-3-carboxylic acid formamidine 1H NMR in DMSO: 8.26 (d, J = 4.84, 1H); 7.89-7.84 (m, 2H); 7.31 (t, J = 8.79, 2H); 6.98 (s, 1H); 6.90 (s, 1H); 4.56 ( septet, J = 6.15, 1H); 3.33-3.29 (m, 4H); 2.81 (d, 1 = 4.40, 3H); 1.90-1.86 (m, 4H); 1.29 (d, J = 6.15, 6H) (M + H) + = 397 A &lt; 1 7. 5-Difluoromethoxy-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid formamidine 1HNMR in dichloromethane 4 (0) 03): 7.92 ( m, 2H); 7.61 (d, 1H, J = 2.93); 7.48 (d, 1H, 1 = 8.79); 7.22-7.13 (m, 3H); 6.54 (t, 1H, J = 74); 5.80 (brs , 1H); 3.00 (d, 3H, J = 5.27) (M + H) + = 336 B &lt; 10 8. 2- (4-Fluorophenyl) -5-isopropoxy each (2-methoxy-ethylamino) -benzofuran-3-carboxylic acid amidine 1H NMR in DMSO: 8.25 (d, J = 4.69, 1H); 7.88-7.83 (m, 2H); 7.31 (t, J = 8.79, 2H); 6.97 (s, 1H); 6.83 (s, 1H); 5.04 ( t, J = 5.27, 1H); 4.62-4.50 (septet, J = 5.27, 1H); 3.56 (t, J = 5.27, 2H); 3.33-3.30 (m, 5H); 2.82 (d7 J = 4.69, 3H ); 1.31 (d, J = 5.86, 6H) (M + H) + = 401 A &lt; 1 9. 5-methyl-2-phenyl-benzofuran-3-carboxylic acid formamidine * H NMR in CDCI3: 7.91-7.86 (m, 2H); 7.66 (s, 1H); 7.52- 7.37 (m, 4H); 7.14 (d, J = 8.8Hz, lH); 5.8t (brs, 1H); 2.97 (d, J = 4.7Hz, 3H); 2.46 (s, 3H) (M ten H) + = 266 B &lt; 10 173- 88828.doc 200418452 Example, No. Name NMR data Mass Spec HCV pol -BB7 IC50 (/ iM) A = ^ 0.5 μΜ B = 0.5 to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μM replicon_) 10 · 5-methyl-2- (4-imidyl-phenyl) -benzofuran-3-carboxylic acid formamide kH NMR in CDCb: 7.97-7.93 (rn, 2H); 7.59 (s, 1H); 7.39 (d, J = 8.2Hz, 1H); 7.19-7.14 (m, 3H); 5.81 (brs, 1H); 3.02 (d, J = 5.3Hz, 3H); 2.47 (s, 3H) (M + H) + = 284 B &lt; 10 11. 2-phenyl-5- (2,2,2-trifluoro-ethoxy) -benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.87 (dd, 2H) ; 7.65 (dd, 1H); 7.47-7.54 (m, 4H); 7.08 (dd, 1H); 5.8 (s, br, 1H); 3.93 (s, 2H); 2.97 (d, 3H) ppm (M + H) + = 350 D &lt; 30 12. 2- (Fluoro-fluorenyl) di 5: methoxy-benzofuran-3-carboxylic acid amidine 1H NMR in DMSO: 8.37 (br.s, iH); 7.91- 7.96 (ra, 2H); 7.56-7.58 (d, J = 8.79Hz 1H); 7.34-7.40 (t, J = 8.79Hz, 2H); 7.09-7.10 (d, J = 2.35Hz, 1H); 6.97- 7.00 (dd, J = 2.35Hz, 8.79Hz, 1H); 3.82 (sr 3H); 2.83-2.8 (d, J = 4.69Hz, 3H) (M + H) + = 299.9 A &lt; 10 13. 6-bromo-2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.42 (d, J = 4.69Hz, 1H); 8.01 (s, 1H); 7.90-7.94 (m, 2H); 7.35-7.41 (t, J = 8.79Hz, 2H); 7.23 (s, 1H); 3.91 (s, 3H); 2.83-2.85 (d, J = 4.69Hz, 3H) Tochigi A &lt; 1 14. 5-Methoxy-6-methyl-2-phenyl-benzofuran-3-quinic acid formamidine 1H NMR in DMSO: 8.34-8.36 (d, J = 4.69Hz, IH) ; 7.83-7.86 (dd, J = 1.76Hz, 8.79Hz, 2H); 7.43-7.53 (m, 4H); 7.04 (s, 1H); 3.85 (s, 3H); 2.83-2.84 (d, J = 4.69 Hz, 3H); 2.28 (s, 3H) (M + H) + = 296 A &lt; 1 15. 6_ (3-Aminopyridine-1 -yl) -2- (4-fluoro-phenyl) -5-isopropoxy-2,3-dihydro-benzofuran -3- Methofenamine * 氺 氺 (M + H) + = 412 C &lt; 30 16. 6-amino-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.82 (dd, 2H , J = 5.5 and 8.7Hz); 7.22 (s, 1H); 7.18 (t, 2H, J = 8.7Hz); 6.84 (s, 1H); 5.76 (bs, 1H); 4.61 (heptuplet, J = 6. iHz); 2.96 (d, J = 4.9Hz, 3H); 1.92 (bs, 2H); 1.40 (d, J = 6.1Hz, 6H) (M + H) + = 343 A &lt; 10 17. 6-Amino-2- (4-Hexyl-phenyl) -5-methoxy-benzofuran-3-quinoline formamidine 1H NMR in methanol-Mountain (CD3〇D) : 7.81 (m, 2H); 7.20 (m, 2H); 7.02 (s, 1H); 6.91 (s, 1H); 4.72 (s, 1H); 3.91 (s, 3H); 2.93 (s, 3H) ( M + H) + = 315 B &lt; 10 18. 6-acetamido-2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.95 (bs, 1H); 7.83 (ra, 2H); 7.46 (m, 1H); 738 (s, IH); 7.28 (m, 2H); 5.76 (bs, 1H); 3.96 (s, 3H); 2.98 (s, 3H ); 2.21 (s, 3H) (Μ + ΗΓ = 357 A &lt; 1 19. 2- (4-Fluoro-phenyl) -5-isopropoxy-6-methylamino-benzofuran-3-¾carboxylic acid formamidine NMR in CDC13: '7.81 (dd, J = 8.7 Sc 5.iHz, 2H); 7.25 (s, 1H); 7.14 (t, J = 9.3Hz, 2H); 6.66 (s, 1H); 5.78 (bs, IH); 4.63 (septupled J = 6.3 Hz, 1H); 4.55 (bs, 1H); 2.97 (d, J = 4.8Hz, 3H); 2.91 (s, 3H); 1.37 (d, J = 6.3Hz, 6H) (M + H) + = 357 A &lt; 1 -174- 88828.doc 200418452 Example number name, NMR data Mass Spec HCY pol -BB7 IC50 (/ tM) A = μ, Μ B = (K5 to i 5.0 / iM C = 5.0 to ^: 30 μΜ D = &gt; 30 μM replicon (μM) 20. 6 dimethylamino-2- (4-fluoro-phenyl) -5-isopropoxy-benzoanan-3-¾ acid Diamine NMR in CDCh: 7.51 (dd, J = 8.7 &amp; 5.1Hz, 2H); 7.28 (s, 1H); 7.26 (m, 3H); 5.80 (bs, 1H); 4.70 (septupled J = 6.3Hzt 1H); 2.98 (d, J = 4.9Hz, 3H); 2.91 (s, 6H); 1.42 (d, J = 6.3Hz, 6H) (M + H) + = 371 A &lt; 1 21. 2- (4-Fluoro-phenyl) -5-isopropoxy-6-methanesulfonylamino-benzyl-4-3-carboxylic acid formamidine 1H NMR in CDC13 : 7.81 (dd, J = 8.7 &amp; 4.1Hz, 2H); 7.73 (s, 1H); 7.42 (s, 1H); 7.19 (U = 8.7Hz, 2H); 6.90 (s, 1H); 5.81 (bs , 1H); 4.75 (septuple ^ J = 6.3Hz, 1H); 2.98 (s, 3H); 2.95 (d, J = 2.6Hzt 3H); 1.40 (d, J = 6.3Hz, 6H) (M + H) + = 421 A &lt; 1 22. 6-Ethylamino-2- (4-amino-phenyl) -5-isopropoxy-wood and sulfan-3--3-carboxylic acid formamidine 1H NMR in CDCh: 7.81 ( ddt J = 8.8, 5.3Hz, 2H); 7.18 (s, 1H); 7.16 (t, J = 8.8Hz, 2H); 6.67 (s, 1H); 5.76 (bs, 1H); 4.61 (heptuplet, J = 6.2HzT 1H,); 3.20 (quaduplet, J = 7.0Hz, 2H); 2.97 (d, J = 4.8Hz, 3H); 1.38 (d, J = 6.2Hz, 6H); 1.32 (t, J = 7.0Hz , 3H) (M + H) + = 371 A &lt; 1 23. 6 Ditriethylamino-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran · 3-acid formamidine'HNMRinCDCb: 7.83 (dd, J = 8.8,5.3Hzt 2H); 7.26 (s, 1H); 7.15 (d, J = 8.8Hz, 2H); 7.05 (s, 1H); 5.78 (bs, 1H ,; 4.17 (heptuplet, J = 6.1Hz , 1H); 3.18 (m, 4H); 2.95 (d, 5.0Hz, 3H); 1.38 (d, J = 6.1HzT 6H); 1.32 (tt J = 7.0Hz, 6H) (Μ + ΗΓ = 399 A &lt; 1 24 .: 2- (4-Fluoro-phenyl) -5-, isopropoxy-6-morpholin-4-yl-benzoanan-3-carboxylic acid formamidine 1HNMRin DMSO : 8.30-8.3 l (d, J = 4.69Hz, 1H); 7.88-7.93 (m, 2H); 7.31-7.37 (t, J = 8.79Hz, 2H); 7.19 (s, 1H); 7.07 (s, 1H); 4.58-4.66 (septet, J = 6.45Hz, 1H); 3.75-3.77 (m, 4H); 3.02-3.05 (m, 4H); 2.82-2.83 (dt J = 4.69Hz, 3H); 1.29- 1.31 (d, J = 6.45Hz? 6H) (M + H) + = 413 A &lt; 1 25. 5-Methoxy-4-methyl-2-benzene: benzobenzo-3-methylimineamine 1H NMR in CDC13: 7.84-7.81 (m, 2H); 7.48-7.40 ( m, 3H); 7.30-7.26 (m, 1H); 6.93 (d, J = 8.7Hz, 1H); 3.86 (s, 3H); 3.01 (d, J = 4.8Hz, 3H); 2.40 (sy 3H) (M + H) + = 296 D &gt; 30 26. 5-cyano-2-phenyl-benzofuran-3-carboxylic acid amidine 1H NMR in CDCl3: 8.32 (s, 1H); 7.89-7.85 (m, 2H); 1.62-1 ΛΊ (ra, 5H); 5.80 (s, 1H); 2.98 (d, J = 5.1Hz, 3H); (M-Η) '= 275 C &lt; 30 27. 5-isopropoxy-2-pyridin-4-yl-pyrano-p-furan-3-methylamine succinate NMR in CDCl3: 8.70 (d, J = 5.4Hz, 2H); 7.84 (dd, J = 1.2Hz, 4.2HZ, 2H); 7.43 (d, J = 8.7Hz, 1H); 7.21 (d, J = 2.7Hz, 1H); 7.00 (dd, J = 2.1Hz, 8.7Hz , 1H); 5.91 (bs, 1H); 4.54 (m, 1H); 3.07 (d, J = 5.1Hz, 3H); 1.36 (d, J = 5.7Hz, 3H) (M + H) '= 311 C &gt; 30 28. 6- (3,5-dimethyl-isopurazol-4-yl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxyl Formamidine acid 1H NMR in CDCl3: 7.85-7.89 (m, 2H); 7.43 (s, 1H); 7.25 (s, 1H); 7.18-7.23 (t, J = 8.79 Hz, 2H); 5.79 (brs, 1H); 3.86 (s, 3H); 3.00-3.02 (d, J = 5.2 ^ Hz, 3H); 2.32 (s, 3H); 2.18 (s, 3H) (M + H) + = 395 A &lt; 1 175-88828.doc 200418452 Example No. Name NMR data Mass Spec HCV pol -BB7 IC5〇 〇iM) A = μΜ B = 0 * 5 to &lt; 5.0 μΜ C = 5.0 to ^ 30 fiM D = &gt; 30 μΜ replicon_) 29. 2- (4-fluoro-phenyl) -6 · (methanesulfonyl-methyl-amino)- 5-methoxy-benzofuran-3-carboxylic acid methochloramine * H NMR in CDC13: 7.86 (m, 2H); 7.56 (s, 1H); 7.45 (s, IH); 7.28 (U 8.3Hz, 2H); 5.77 (brs, 1H); 3.98 (s, 3H); 3.33 (s, 3H); 2.98 (d, J = 5.2Hz, 3H); 2.96 (s, 3H) (M + H) + = 407 A &lt; 1 30. 2- (4-Fluoro-phenyl;)-5- (4-methoxy-benzyloxy) -morpholin-4-yl-benzofuran-3-carboxylic acid formamidine Amine 1H NMR in CDCi3: 7.84 (dd, J = 8.4, 5.2Hz, 2H); 7.40 (d, J = 8.3Hz, 2H); 7.37 (s, 1H); 7.15 (t, J = B.4Hz, 2H ); 7.06 (s, 1H); 6.93 (dt J = 8.8Hz, 2H); 5.82 (d, J = 3.9Hz, 1H); 5.09 (s, 2H); 3.85 (t, J = 4.4Hz, 4H) ; 3.82 (s, 3H); 3.11 (t, J = 4.4Hz, 4H); 2.97 (d, J = 4.8Hz, 3H) (M + H) + = 491 A &lt; 1 31. 2- (4-Fluoro-phenyl) -6- [methyl clay acid- (4-methoxy · fluoren 10-amino) -5- (4-methoxy- Benzyloxy) _benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.38 (d, J = 4.1Hz, 1H); 7.88 (dd, J = 8.4, 5.2Hz, 2H); 7.48 (d , J = 8.8Hz, 2H); 7.34 (t, J = 8.8Hz, 2H); 7.29 (s, 1H); 7.28 (s, 1H); 7.12 (d, J = 8.8Hz, 2H); 7.00 (d , J = 8.2Hz, 2H); 6.79 (d, J = 8.8Hz, 2H); 5.13 (s, 2H); 4.60 (br rn, 2H); 3.77 (s, 3H); 3.66 (s, 3H); 2.94 (s, 3H); 2.80 (d, J = 4.7Hz, 3H) (M + H) + = 619 A &lt; 1 32, 5-ethoxy-6- (ethyl-methanesulfonyl-amino) -2- (4-fluoro-phenyl) -benzofuran-3-¾formamidine 1H NMR in DMSO: 8.41 (d, J = 4.1Hz, IH); 7.94 (dd, J = 8.2, 5.3Hz, 2H); 7.55 (s, 1H); 7.36 (t, J = 8.2Hz, 2H); 7.16 (s, 1H); 4.14 (q, J = 7.0Hz, 2H); 3.62 (q, J = 7.0Hz, 2H); 3.01 (s, 3H); 2.82 (d, J = 4.7Hz, 3H); 1.38 (t, J = 7.0Hz, 3H); 1.05 (t, J = 7.0Hz, 3H) (M + H) + = 435 A &lt; 1 33. 2 · (4 · -amino-phenyl) -6_morpholin-4-yl-5-0 sezol-2-ylmethoxy) -benzopyran-3-carboxylic acid Formamidine 1H NMR in DMSO: 8.35 (d, J = 4.4Hz, 1H); 7.95-7.80 (m, 4H); Ί35-125 (m, 4H); 5.49 (s, 2H); 3.78 (m, 4H ); 3.06 (in, 4H); 2.83 (d, J = 4.4Hz, 3H) (M + H) + = 468 A &lt; 1 34. 2- (4-Amino-phenyl) -5_ isopropoxy-6- [methanesulfonyl- (2-oxy-propyl) -amino] -benzyl- Formamidine 3-carboxylic acid [H NMR in DMSO: 8.38 (d, J = 4.8Hz, 1H); 7.94 (dd, J = 8.4, 5.3Hz, 2H); 7.71 (s, 1H); 7.36 (t, J = 8.8Hz, 2H); 7.15 (s, lH); 4.77 (septet, J = 6.1Hz, 1H); 4.04 (s, 2H); 3.04 (s, 3H); 2.81 (d, i = 4.4Hz, 3H); 2.11 (s, 3H); 1.36 (d, J = 6.1Hz, 6H) (M + H) + = 477 A &lt; 1 35. 2- (4-Fluoro-phenyl) -6-morpholin ^-^-5-(oroxazol-4-ylmethoxy) -benzofuran; formamidine carboxylic acid Amine 1H NMR in CDCl3: 8.84 (d, 1H, J = 1.76); 7.88 (m, 2H); 7.44 (s, 2H); 7.17 (t, 2H, J = 8.79); 7.10 (s, 1H); 5.77 (brs, 1H); 5.37 (s, 2H); 3.89 (m, 4H); 3.16 (m, 4H); 3.00 (d, 3H, J = 4.69) (M + H) + = 468 A &lt; 1 176- 88828.doc 200418452 Example No. Name NMR data Mass Spec HCV pol -BB7 IC50 (μΜ) A = fiM B = 03 to ^ 5.0 / iM C = 5.0 to &lt; 30 pM D = &gt; 30 μM replicon_) 36. 2_ (4-amino-phenyl) -5_ isopropoxy-6- (methanesulfonyl-pyrimazol-4-ylmethyl- Amine) -Benzanan-3-formamide Methylamine 1H NMR in CDC13: 8.69 (d, 1H, J = 2.20 Hz); 7.77 (m, 2H); 7.40 (s, 1H); 7.37 (s , lH); 7.30 (d, 1H, J = 2.20 Hz); 7.18 (t, 2H, J = 8.79 Hz); 5.67 (brs, 1H); 5.03 (brs, 2H); 4.79 (m, lH); 3.07 (s, 3H); 2.95 (d, 3H, J = 4.84 Hz); 1.44 (d, 6H, J = 5.72 Hz) (M + H) + = 518 A &lt; 1 37. 2- (4-amino-phenyl) -6- (5-hydroxymethyl-isoazazol-3-yl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine Amine 1H NMR in CD3OD: 7.94 (s, 1H); 7.92 (dd, J = 9.2, 5.3 Hz, 2H); 7.32 (s, 1H); 7.25 (apparent triplet, J = 8.8 Hz, 2H); 6.87 (s , lH); 4.75 (m, 1H); 4.72 (s, 2H); 2.95 (s, 3H); 1.39 (d, J = 5.7 Hz, 6H) (M + H) + = 425 A &lt; 1 38. 5-ethoxy-2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino): benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.39 (d, J = 4.0Hz, 1H); 7.92 (dd, J = 8.8t 5.3Hz, 2H); 7.59 (s, 1H); 7.36 (t, J = 8.8Hz, 2H); 7.17 (s, 1H); 4.16 (q, J = 7.0Hz, 2H); 3.19 (s, 3H); 3.01 (s, 3H); 2.81 (d, J = 4.4Hz, 3H); 1.40 (t, J = 7.0Hz, 3H) (M + H) + = 421 A &lt; 1 39. 4- [2- (4-Fluoro-phenyl) -6- (formamidine, fluorenyl-methyl: amino) -3-methylaminomethyl-benzoyl- 5-Methoxymethyl] -2-Hexyl-arsanoic acid 1H NMR in DMSO: 8.39 (brd, 1H, J = 4.69Hz); 7.93 (m, 2H); 7.84 (d, 1H, J = 8.21Hz); 7.72 (s, 1H); 7.39 (t, 2H, J = 8.79Hz); 7.30 (s, 1H); 7.12 (m, 2H); 5.27 (s, 2H); 3.24 (s, 3H); 3.00 (s , 3H); 2.83 (d, 3H, J = 4.69Hz) (MH) · 541 A &lt; 10 40.2 (4-Fluoro-phenyl) -6- (5-hydroxymethyl-isohumazol-3-yl) -5-methoxy-benzofuran-3-m acid Amidine NMR in DMSO: 8.44 (bq, J = 4.83Hz, 1H); 7.97 (m, 3H); 7.39 (t, J = 8.79Hz, 2H); 7.29 (s, 1H); 6.80 (d, J = 0.879Hz, 1H); 5.66 (t, J = 6.15 &amp; 5.71 Hz, 1H); 4.63 (d, J = 6.15Hz, 2H); 3.93 (s, 3H); 2.86 (d, J = 4.39Hz, 3H ) (M + H) + = 397.0 A &lt; 1 41. 2- (4-Fluoro-phenyl) -6- [4- (2-acyl-ethyl) -isopurin-3-yl] -5-methyllactyl-epoxy Benzene-3-¾methamidine 1H NMR in CDC13: 8.40 (s, 1H); 7.86 (dd, J = 5.27, 8.79 Hz, 2H); 7.52 (s, 1H); 7.45 (s, 1H); 7.20 (t, J = 8.35, 8.79 Hz, 2H); 5.81 (bs, 1H); 3.87 (s, 3H); 3.69 (q, J = 6.15 Hz, 2H); 3.00 (d, J = 4.83 Hz, 3H) ; 2.64 (t, J = 6.15 HzT 2H); 1.45 (t, J = 5.27,5.71 Hz, 1H). (M + H) + = 411 A &lt; 1 42. 2- (4-Fluoro-phenyl) -6-[(2-hydroxy-ethyl) -methanesulfonyl-amino] -5-methoxy-benzofuran-3- Carboxamide carboxylate NMR in DMSO: 8.49 (d, J = 4.84 Hz, 1H); 7.96-7.90 (m, 2H); 7.66 (s, 1H); 7.41 (t, J = 7.03 Hz, 2H); 7.2 (s, 1H); 4.75 (t, J = 5.71 Hz, 2H); 3.9 ((s, 3H); 3.44 (bs, 1H); 3.41 (d, J = 5.27 Hz, 2H); 3.05 (s, 3H ); 2.84 (d, J = 4.39 Hz, 3H) (M + H) + = 437 A &lt; i 43. 5- ^ propyl-2- (4-fluoro-phenyl) -6-[(2-methyl-ethylmethanesulfonyl-amino) -benzofuran each carboxylic acid Lamine 1H NMR in CDC13: 7.90-7.85 (m, 2H); 7.55 (s, 1H); 7.35 (s, 1H); 7.22-7.16 (m, 2H); 5.74 (bs, 1H); 4.09-4.03 ( m, 1H); 3.75 (s, 3H); 3.14 (s, 3H); 2.99 (d, J = 4.40Hz, 3H); 2.40-2.30 (m, 1H); 1.95 (m, 1H); i.10 -0.98 (m, 2H); 0.88 (m, 1H); 0.68 (m, IH) (M + H) + = 447 A &lt; 1 177- 88828.doc 200418452 Example No. Name NMRdata Mass Spec HCV pol -BB7 IC5〇 (μΜ) A = / iM B = 03 to &lt;: 5.0 μΜ C = 5.0 to ^: 30 μΜ D = &gt; 30 μΜ replicon (μΜ) 44. 5-ethyl-2- (4-fluoro-phenyl) -6-methanesulfonylamine Benzene-benzobenzamidine'3-chiamate formamidine'H NMR in DMSO: 9.20 (bs, 1H); 8.61 (m, 1H); 7.93 (dd, J = 5.3 & 8.8 Hz, 2H); 7.60 ( s, 1H); 7.48 (s, 1H); 7.37 (t, J = 8.8 Hz, 2H); 3.05 (s, 3H); 2.83 (d, J = 4.7 Hz, 3H); 2.81 (q, J = 7.7 Hz, 2H); 1.21 (ζ J = 7.7 Hz, 3H) (M + H) + = 391 A &lt; 10 45. 5-ethyl-2- (4-fluoro-phenyl) -6- (methanesulfonyl-fluorenyl-amino) -benzofuran-3-carboxylic acid formamidine 1H NMRinDMSO : 8.50 (m, 1H); 7.94 (dd, J = 5.3 & 8.8Hz, 2H); 7.89 (s, 1H); 7.54 (s, 1H); 7.60 (t, J = 8.8Hz, 2H); 3.29 (q, 1 = 7 ^ 2H); 3.21 (s, 3H); 3.13 (s, 3H); 2.83 (d, J = 4.7Hz, 3H); 1.21 (t, J = 7.0Hz, 3H) (M + H) + = 405 A &lt; 1 46. 5-Ethyl-2- (4-amino-methyl) -6-[(2-hydroxy-ethyl) -methyl pentoxide S &amp; yl-amino] -benzofuran-3 -Formamidine carboxylic acid 1H NMR in DMSO: 8.45 (m, 1H); 7.94 (dd, J = 5.3 & 9.4Hz, 2H); 7.81 (s, 1H); 7.55 (s, 1H); 7.39 (t , J = 8.8Hz, 2H); 3.72 (m, 1H); 3.58 (m, 1H); 3.4 (m, 3H); 3.15 (s, 3H); 2.84 (d, J = 4.7Hz, 3H); 2.82 (q, J = 7.0Hz, 2H); 1.25 (t, J = 7.0Hz, 3H) (M + H) + = 435 A &lt; 1 47. ό- (1-Ethyl-p-p-p-Yodo-2-yl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxy Formamidine acid 1H NMR in CDC13: 7.85 (m, 2H); 7.36 (s, 1H); 7.20 (m, 3H); 5.78 (brs, 1H); 5.40 (in, 1H); 3.92 (s, 3H) ; 3.40-3.91 (m, 2H); 2.99 (d, J = 4.8Hz, 3H); 1.51-2.0 (m, 4H); 1.85 (s, 3H) (MH) · 411.1 A &lt; 1 48. 2- (4-Amino-phenyl) -5_methoxy-6- (2-oxy-oxazolyt-5-yl) -benzobenzoan-3-carboxylic acid formamidine Amine * H NMR in (CD3) 2CO: 8.03 (m, 2H); 7.68 (s, 1H); 7.40 (brs, 1H); 7.20-7.31 (4H); 5.14 (ra, 1H); 3.90 (s, 3H ); 3.60 (m, 1H); 3.38 (m, 1H); 2.94 (d, J = 4.8 Hz, 3H) (M + H) + = 385.0 A &lt; 10 49. Fluoro-phenyl) yl-1-methyl-ethyl) -5-methoxy-benzofuran-3-methanoic acid formamidine 1H NMR in CDC13: 7.85 (m, 2H) ; 7.50 (s, 1H); 7.39 (s, 1H); 7.20 (m, 2H); 5.75 (brs, 1H); 4.17 (s, 1H); 3.99 (s, 3H); 2.98 (d, J = 4.8 Hz, 3H); 1.66 (s, 6H) (M + H) + = 358.1 A &lt; 1 50. 2- (4-Fluoro-phenyl) -5 · -methoxy-6- (5-methyl_ [1,2,4] pyridazol-3-yl) -benzo Tetramethyl-3 -¾formamidine 1H NMR in CDC13: 8.12 (s, 1H); 7.90-7.86 (m, 2H); 7.48 (s, 1H); 7.24-7.18 (m, 2H); 5.78 (s , 1H); 4.03 (s, 3H); 3.0 (d, J = 4.8 Hz, 3H); 2.67 (s, 3H) (M + H) + = 382 A &lt; 1 51. 6- (3,5-dimethyl-isoxazol-4-yl) -2- (4-fluoro-phenyl) -5- (3-hydroxy-propoxy) -benzene Benzene-3-carboxylic acid formamidine 1H NMR in DMSO: 8.41-8.43 (d, J = 4.69 Hz, 1H); 7.92-7.97 (m, 2H); 151 (sT 1H); 7.35-7.41 (t , J = 8.79 Hz, 2H); 7.23 (s, 1H); 4.49-4.52 (t, J = 5.28 Hz, 1H); 4.06-4.11 (t, J = 6.45 Hz, 2H); 3.43-3.49 (q, J = 5.86 Hz, 2H); 2.84-2.86 (d, J = 4.69 Hz, 3H); 2.29 (s, 3H) (M + H) + = 439.0 A &lt; 1 178- 88828.doc 200418452 Example number name NMRdata Mass Spec HCV po! -BB7 IC50〇QiM) A = 彡 0 · 5 μΜ B = 0.5 to ^ 5.0 μΜ C = 5.0 to ^ 30 / iM D = &gt; 30 replicon trans) 52. Gas-phenyl) (Methanesulfonyl-methyl-amino) -5- (2-morpholin-4-yl-ethoxy) -benzofuran-3 -Formamidine carboxylic acid 1H NMR in DMSO: 8.40 (brd, J = 4.40 Hz, 1H); 7.94 (m, 2H); 7.60 (s, 1H); 7.38 (t, J = 8.79 Hz, 2H); 7.24 (s, 1H); 4.21 (t, J = 5.28 Hz, 2H); 3.57 (1¾ 4H); 3.23 (s, 3H); 3.10 (s, 3H); 2.84 (d, J = 4.84 Hz, 3H); 2.76 (t, J = 5.28 Hz, 2H); 2.48 (m, 4H). (M + H) + = 506 A &lt; 1 53. 5-(. monobenzyl-2-plug-methoxy) -2-phenyl-benzofuran-3-carboxylic acid formamidine * H NMR in DMSO: 2.82 (d, 3H) ; 5.0 (s, 2H) 6.96 (m, 1H); 7.32-7.96 (m, 16H); 8.34 (d, 1H) ppm (M + H) + = 434 C &lt; 30 54. 5-methoxy-2- (4-methoxy-phenyl) -benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.31 (br s, 1H); 7.82- 7.84 (d, J = 7.03Hz, 2H); 7.52-7 ^ 5 (d, J = 8.79Hz, 1H); 7.06-7.10 (m, 3H); 6.93-6.96 (dd, J = 2.35Hz, 8.79Hz , 1H); 3.83 (s, 3H); 3.81 (s, 3H); 2.81-2.83 (d, J = 4.69Hz, 3H) 氺 氺 * B &lt; 10 55. 5-methoxy-2- (3-trifluoromethyl-phenyl) -benzofuran formamidine carboxylic acid 1H NMR in DMSO: 8.47-8.49 (d, J = 4.69Hzt 1H ); 8.19 (s, 1H); 8.15-8.18 (d, J = 7.62Hz, 1H); 7.74-7.84 (m, 2H); 7.61-7.64 (d, J = 9.38Hz, 1H); 7.13 (d, J = 2.34Hz, 1H); 7.01-7.05 (dd, J = 2.34Hz, 7.62Hz, 1H); 2.83-2.85 (d, J = 4.69Hz, 3H) 氺 氺 氺 B &lt; 30 56. 5-methoxy-2- (4-trifluoromethyl-phenyl) -benzofuran-3-carboxylic acid formamidine JH NMR in DMSO: 8.48-8.49 (d, Ι = 4.69 Ηζ, 1H); 8.06-8.09 (d, J = 8.21Hz, 2H); 7.88-7.90 (d, J = 8.21Hz, 2H); 7.61-7.64 (d, J = 8.79Hz, 1H); 7.12-7.13 (d, J = 2.93Hz, 1H); 7.02-7.06 (dd, J = 2.93, 8.79Hz, 1H); 3.83 (s, 3H); 2.85-2.86 (d, J = 4.69Hz, 3H) 氺 氺 氺B &lt; 10 57. 5-ethoxy-2-phenyl-benzofuran-3-carboxylic acid formamidine'H NMR in CDCb: 7.85 (dd, 2H); 735-7.52 (m, 5H); 6.95 (d, 1H); 5.8 (s, br, 1H); 4.14 (q, 2H); 2.97 (d, 3H) 1.41 (t, 3H) ppm (M + H) + = 296 B &gt; 30 58.2 -(2-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.05-8.07 (d, J = 4.69Hz, 1H); 7.72-7.77 (t of d, J = 1.76Hz, 7.62Hz, 1H); 7.52-7.63 (in, 2H); 7.37-7.39 (d, J = 7.62Hz lH); 7.33-7.38 (m, 1H); 7.18-7.19 (d, J = 2.35Hz, 1H); 6.99-7.03 (m, 2H); 3.83 (s, 3H); 2.75-2.76 (d, J = 4.69Hz, 3H) (M + H) + = 300 B &lt; 10 59. 5-isopropoxy-2-phenyl-benzofuran-3-carboxylic acid formamidine'H NMR in CDCb: 7.87 (d, 2H); 7.52-7.37 (m, 5H); 6.94 (d, 1H); 5.78 (s, br, 1H); 4.6 (m, 1H); 2.98 (d, 3H); 1.38 (d, 6H) ppm (M + H) + = 310 B &lt; 30 60. 5-Yoxy-2-phenyl-benzofuran-3-carboxylic acid formamidine * H NMR in CDCb: 7.87 (m, 2H), 7.51-7.3 (m, 5H); 6.97 (d, 1H); 5.78 (s, br, 1H); 4.06 (m, 2H); 2.98 (d, 3H); 1.83-1.54 (m, 4H); 1.02 (m, 3H) ppm (M + H) + = 324 B &lt; 30 61. 2-phenyl-5-propoxy-benzofuran-3-methanoic acid formamide (H NMR in CDCb: 7.86 (ra, 2H); 7.5-7.27 (m, 5H); 6.96 (dd, 1H); 5.76 (s, br, 1H); 3.99 (t, 2H); 2.98 (d, 3H); 1.84 (m, 2H); (t, 3H) ppm (M + H) + = 310 B &lt; 30 62. 5-methoxy-2- (2,4,5-trifluoro-phenyl) -benzofuran-3-carboxylic acid methylamine 1H NMR in DMSO: 8.08-8.09 (d, J = 4.69Hz, 1H); 7.86-7.95 (m, 1H); 7.71-7.80 (m, 1H); 7.58-7.61 (d, J = 9.38Hz, 1H); 7.22-7.23 (d, J = 2.35Hz , 1H); 7.02-7.06 (dd, J = 2.93Hz, 9.38Hz, 1H); 3.83 (s, 3H); 2.76-2.77 (d, J = 4.69Hz, 3H) 氺 氺 氺 C &lt; 30 179- 88828.doc 200418452 Example No. Name NMRdata Mass Spec HCV pol -BB7 IC50〇iM) A = &lt; 0 * 5 / iM B = 05 to ^ 5.0 fiM C = 5.0 to ^: 30 μΜ D => 30 / iM replicon (μΜ) 63. 5-methoxy-7-methyl-2-benzene Benzene-benzoic acid-3-ammonium acetamide 1H NMR in DMSO: 8.33-8.34 (d, J = 4.69Hz, 1H); 7.87-7.89 (d, J = 7.62Hz, 2H); 7.45-7.55 (m, 3H); 6.89-6.90 (d, J = 2.34HzT 1H); 6.83-6.84 (d, J = 2.34Hz, 1H); 3.80 (s, 3H); 2.82-2.84 (d, J = 4.69Hz , 3H); 2.50 (s, 3H) (M + H) + = 296 B &lt; 10 64. 2- (4-Fluoro-phenyl)-: 5- (of 2,2-trifluoro-ethyllactyl) -benzyl-3-carboxylic acid formamidine 1HNMR in CDC13 : 8.06 (dd, 1H); 7.41 (dd, 2H); 7.17 (m, 2H); 7.02 (dd, 1H); 5.76 (m, br, 1H); 4.42 (q, 2H); 2.99 (d, 3H) ) ppm (M + H) + = 368 B 氺 氺 氺 65. 2_ (4-Gas-phenyl) -5_ isopropoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.90 (dd, 2H); 7.29 (dd, 2H); 7.16 (dd, 1H); 6.92 (dd, 1H); 5.82 (s, br, 1H); 4.58 (m, 1H); 2.99 (d, 3H); 1.34 (s, 3H) (M + H) + = 328 B &lt; 30 66. 2_ (2-Chloro-phenyl) -5-methylpyrene-wood-p-furan-3-carboxylic acid formamidine 1H NMR in DMSO: 7.85-7.86 (d, J = 4.69Hz , 1H); 7.47-7.69 (m, 5H); 7.27-7.28 (d, J = 2.34HzT 1H); 7.00-7.04 (dd, J = 2.93Hz, 9.38Hz, 1H); 3.84 (s, 3H); 2.72-2.73 (d, J = 4.69Hz, 3H) (M + ΗΓ = 315.9 C &gt; 30 67. 6-methoxy-2-phenyl-benzofuran formamidine carboxylic acid * H NMR in CDC13 : 7.86 (m, 2H); 7.73 (d, J = 8.87Hz, 1H); 7.51-7.42 (m, 3H); 7.04 (d, J = 2.4Hz, 1H); 6.94 (d of d, J = 8.8 Hz, 1H); 5.81 (brs, 1H); 3.87 (s, 3H); 2.98 (d, J = 4.7Hzt 3H) (M + H) + = 282 B &lt; 10 68. 2-Furan-2-yl-5-methoxy-benzofuran-3-quinoformamidine 1HNMR in DMSO: 8.28-8.29 (d, i = H.10Hz 1H); 7.92 ( s, 3H); 7.54-7.57 (d, J = 8.79Hz, 1H); 7.18-7.19 (d, J = 3.52Hz, 1H); 7.15-7.16 (d, J = 2.35Hz, 1H); 6.96-7.00 (dd, J = 2.35, 8.79Hz, 1H); 6.71-6.72 (m, 1H); 3.82 (s, 3H); 2.84-2.86 (d, J = 4.10Hz, 3H) M = 271 B &lt; 30 69. 2- (3-1ylmethylmethyl-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.42 (s, 1H); 7.63 (in, 3H); 7.43 (m, 1H); 7.09 (m, 1H); 7.00 (m, 1H); 3.82 (s, 3H); 2.84 (d, J = 4.8Hz, 3H); 2.30 (s, 3H) (M + H) + = 314 A &lt; 10 70. _2- (4-Bromo-phenyl) -5-methoxy-benzofuran formamidine carboxylic acid 1H NMR in DMSO: 8.41 (m, 1H); 7.81 (d, J = 7.5Hz, 2H); 7.72 (d, J = 8.4Hz, 2H); 7.58 (d, J = 9.3Hz, 1H); 7.09 (s, 1H); 7.01 (d, J = 8.7Hz, 1H); 3.82 (s, 3H); 2.83 (d, J = 4.2Hz, 3H) (Μ + ΗΓ = 361 A &lt; 10 71. 2- (4-Fluoro-3-methyl-phenyl) -5-methoxy-benzofuran-3-carboxylic acid methylamine 1H NMR in DMSO: 8.33 (ra, 1H) ; 7.80 (dd, J = 8.1, 1.8Hz, 1H); 7.75 (m, 1H); 7.56 (d, J = 9.0Hz, 1H); 7.29 (m, 1H); 7.09 (d, J = 2.4Hz, 1H); 6.97 (dd, J = 8.1, 2.1Hz, 1H); 3.81 (s, 3H); 2.84 (d, i = 4.2Hz, 3H); 2.35 (s, 3H) (M + H) + = 314 A &lt; 30 72. 2- (4-Gas-Phenyl) -5_methoxy-7-methyl-benzoanan-3-acid methylamine 1H NMR in DMSO: 8.3 (d, br, 1H); 7.94 (dd, 2H); 7.35 (dd, 2H); 6.89 (d, 1H), 6.81 (d, 1H); 3.83 (s, 3H); 2.80 (d, 3H); 2.47 (s, 3H ) ppm (M + H) + = 314 A &lt; 10 73. 5-Gas-2- (4-fluoro-phenyl) -benzoanan-3H-methylamine 1H NMR in CDCl3: 7.96-7.91 (ra, 2H); 7.81 (d , J = 2.4Hz, 1H); 7.42 (d, J = 8.7Hz, 1H); 7.30 (d, d, J = 2.4, 8.7Hz, 1H); 7.21-7.16 (m, 2H); 5.789 (s, IH); 3.01 (d, J = 4.8Hz, 3H) (M + H) + = 304.27, 306.13 B &lt; 10 180- 88828.doc 200418452 Example No. Name NMRdata Mass Spec HCV pol -BB7 ic50 〇iM) A = &lt; 0 * 5 / iM B = 03 to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &30; 30 nM replicon (μΜ) 74. 5-tertiary-butyl-2-phenyl-benzofuran Formamidine-3-chitoate * Η NMR in CDC13: 7.87-7.84 (m, 3H); 7.52-7.39 (m, 5H); 5.79 (br s, 1H); 2.99 (d, J = 4.7Hz, 3H ); 139 (s, 9H) (M + H) + = 308 A &lt; 10 75. 5 Dichloro-2-p-methyl-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.90 (d, J = 1.8Hz, 1H); 7.75 (d, J = 7.8Hz, 2H); 7.43-7.40 (m, 1H); 7.32-7.27 (in, 3H); 2.97 (d, J = 4.8Hz, 3H); 2.43 (s, 3H) (M + H) + = 300 A &lt; 10 76. 2- (3-chloro4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine * H NMR in CDC13: 8.62 (s, 1H) ; 8.08 (dd, J = 7.2,1.8Hz, 1H); 7.88 (m, 1H); 7.58 (m, 2H); 7.10 (d, J = 2.4Hz, 1H); 6.98 (dd, J = 8: l , 2.4Hz, 1H); 3.82 (s, 3H); 2.84 ((t J = 4.8Hz, 3H) (M + H) + = 334 B &lt; 10 77. 2- (4-Chloro-3-fluoro-phenyl) &gt; 5-methoxy 4-methyl-3-carboxylic acid methylamine * Η NMR in CDC13: 8.48 (s, IH ); 7.93 (d, J = 1.2Hz, 1H); 7.90 (m, 2H); 159 (d, J = 9.0HzT 1H); 7.12 (d, J = 2.4Hz, 1H); 7.04 (dd, J = 9.0, 2.4Hz, 1H); 3.82 (s, 3H); 2.85 (d, J = 4.5Hz, 3H) (M + H) + = 334 A &lt; 10 78. 5-methoxymethyl-2-phenyl-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.90 (d of d, J = 8.2Hz, 2H); 7.83 (sT 1H); 7.51-7.42 (m, 4H); 7.34 (d, J = 8.8Hz, 1H); 5.83 (brs, 1H); 4.56 (s, 2H); 3.41 (s, 3H); 3.00 (d, J = 4.7Hz, 3H) (M + H) + = 296 B &lt; 30 79. 2_ (4-amino-phenyl) -5_ isopropoxy-6-methyl-benzofuran-3-carboxylic acid formamidine 1H NMR in CD30D: 7.85 (dd, 2H); 7.31 (s, 1H); 7.20 (dd, 2H); 7.10 (s, 1H); 4.61 (ra, 1H); 2.92 (s, 3H); 2.29 (s, 3H); 1.37 (d, 6H) ppm ( M + H) + = 342 A &lt; 10 80. _2- (4-Gas-phenyl) -5-isopropoxy-7-methyl-benzofuran-3-methanoformamidine 1H NMR in CD30D: 7.85 (dd, 2H ); 7.25 (d, 1H); 7.20 (dd, 2H); 6.80 (d, 1H); 4.61 (m, 1H); 2.92 (s, 3H); 2.38 (s, 3H); 1.37 (d, 6H) ppm (M + H) + = 342 B &lt; 30 81. 2- (4-Gasyl-benzyl) -5-methoxy-6-methyl-benzofuran-3-carboxylic acid formamidine 1H NMR in CDCI3: 7.9 (dd, 2H) ; 7.26 (st 1H); 7.22 (s, 1H); 7.16 (dd, 2H); 5.78 (s, 1H, br); 3.89 (s, 3H); 2.98 (d, 3H); 2.33 (s, 3H) ppm (M + H) + = 314 A &lt; 10 82. 5-Fluoro-2- (4-fluoro-epoxy) -benzofuran-3-carboxylic acid formamide 1H NMR in CDCi3: 7.93-7.88 (in, 2H); 7.48 (dd , J = 2.7HzT 8.4Hz, 1H); 7.41 (dd, J = 3.9Hz, 8.7Hz, 1H); 7.21-7.14 (m, 2H); 7.06 (td, J = 2.7Hz, 8.7Hz, 1H); 5.86 (s, 1H); 2.98 (d, J = 4.8Hz, 3H) (M + H) + = 288 B &lt; 30 83. 2- (4-ethyl-phenyl) -5-fluoro-benzofuran-3-carboxamide 1H NMR in CDC13: 7.77 (d, J = 7.8Hz, 2H); 7.59 (dd, J = 2.7Hz, 8.4Hz, 1H); 7.41 (dd, J = 4.5Hz, 8.7Hz, 1H); 7.33 (d, J = 8.4Hz, 2H); 7.03 (td, J = 2.4Hz, 8.7Hz, 1H); 5.79 (s, 1H); 2.96 (d, J = 5.1Hz, 3H); 2.72 (q, J = 7.8Hz, 15.3Hz, 2H); 1-29 (t, J = 7.5Hz , 3H) (M + H) + = 298 A &lt; 10 84. 5-ethyl-2-phenyl-benzofuran-3-carboxylic acid methylamine 1H NMR in CDCb: 7.89 (m, 3H); 7.70 (s, 1H); 7.5-7.37 (m , 3H); 7.15 (m, 1H); 5.81 (br s, 1H); 3.0 (d, 3H); 2.76 (q, 2H); 1.25 (t, 3H) (Μ + ΗΓ = 280 B &lt; 30 85. 2- (5-chlorosethen-2-yl) -5-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.32 (s, 1H); 7.67 (d, J = 4.2Hz, 1H); 7.54 (d, J = 9.0Hz, 1H); 7.22 (d, J = 4.2Hz, 1H); 7.15 (s, 1H); 6.98 (d, J = 6.9Hz , 1H); 3.81 (s, 3H); 2.84 (d, J = 4.5Hz, 3H) (Μ + ΗΓ = 322 A &lt; 10 181-88828.doc 200418452 Example number name NMR data Mass Spec HCV pol -BB7 IC50 (μΜ) A = μΜ. B = 03 to ^ 5.0 μΜ C = 5.0 to ^ 30 D = &gt; 30 μΜ replicon (μΜ) 86.5 5-isopropoxy-2-phenyl-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.87 (m, 2H); 7.74 (s, 1H); 7.54-7.43 (m, 4H); Ί21-123 (m, 1H); 5.82 (br s, 1H); 3.10-3.00 (m + d, 4H); 1.33 (d, 6H) (2M + Na) + = 609.2 A &lt; 10 87. 2- (5-Gas-p-phenen-2-yl) -5-ethoxy-benzofuran-3-carboxylic acid formamide 1HNMRinCDCl3: 7.72 (d, J = 3.6Hz, 1H); 738 (d, J = 8.1HzT 1H); 7.14 (d, J = 2.4Hz, 1H); 6.95 (d, J = 3.9Hz, 1H); 6.92 (d, J = 2.4HzT 1H); 5.98 (s, 1H) 4.10 (q, 2H); 3.07 (d, J = 4.5Hz, 3H); 1.45 (t, 3H) (M + H) + = 336 A &lt; 10 88. 5-Methoxy-2-pyrimin-2-yl-benzofuran-3-quinoformamidine 1H NMR in DMSO: 8.38 (s, 1H); 7.83 (d, J = 3.3 Hz, 1H); 7.76 (d, J = 5.4Hzt 1H); 7.55 (d, J = 9.0Hz, 1H); 7.21 (m, 1H); 7.11 (cU = 2.1Hz, 1H); 6.97 (dd, J = 9.0, 2.4Hz, 1H); 3.82 (s, 3H); 2.86 (dT J = 4.5HzT 3H) (M + H) + = 288 B &lt; 30 89. 5-Chloro-2-pyridin-3-yl-benzofuran-3-chitoic acid formamidine. Ή NMR in CDC13: 9.15-9.14 (m, 1H); 8.68-8.66 (m, 1H); 8.33-8.29 (m, 1H); 7.77 (d, J = 2.1Hz, 1H); 7.49-7.39 (m, 2H); 7.34 (dd, J = 2.1Hz, 8.7Hz, 1H); 6.0 ( s, 1H); 3.04 (cU = 4.8Hz, 3H) (M + H) + = 286.9 B &gt; 30 90. 2- (4-bromo-3-fluorophenyl) -5 · isopropoxy -Benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.45 (d, J = 3.9Hz, 1H); 7.88 (dd, J = 8.4, 2.4Hz, 1H); 7.85 (d, J = 3.0 Hz, 1H); 7.67 (dd, J = 9.0, 1.8Hz, 1H); 7.57 (d, J = 8.1Hz, IH); 7.10 (d, J = 2.4Hz, 1H); 7.02 (dd, J = 9.3 , 2.7Hz, 1H); 4.64 (m, 1H); 2.84 (d, J = 4.8Hz, 3H); 1.29 (d, J = 6.0Hz, 6H) (M + H) + = 406 A &lt; 10 91. 2- (2,4-difluoro-phenyl) -5-isopropoxy-benzofuran-3-methanoic acid formamide NMR in DMSO: 8.04 (d, J = 7.2Hz , 1H); 7.82 (d, J = 6.3Hz, 1H); 7.56 (d, J = 9.3Hz, 1H); 7.46 (d, J = 9.3Hz, 1H); 7.30 (d, J = 2.4Hz, 1H ); 7.20 (d, J = 2.1Hz, 1H); 6.99 (dd, J = 8.1T 2.4Hz, 1H); 4.61 (m, 1H); 2.75 (d, J = 4.8Hz, 3H); 1.30 (d , J = 6.0Hz, 6H) (Μ + ΗΓ = 345 A &lt; 30 92. 6-bromo-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine * 氺 氺 (M + H) + = 406 A &lt; 1 93. 5-methoxy-2- (4-morpholin-4-yl-benzene grave) -benzofuran-3-carboxylic acid amidine 'H NMR in CDC13: 7.76 (dd, J = 4.8, 3.0Hz, 2H); 7.37 (m, 2H); 6.97 (dd, J = 9.0, 1.8Hz, 2H); 6.89 (dd, J = 8.1, 2.1Hz, 1H); 5.84 (m, 1H) ; 3.87 (s, 3H); 3.88 (t, 4H); 3.27 (t, 4H); 2.96 (d, J = 5.4Hz, 3H) (M + H) + = 367 B &gt; 30 94. 5,6 -Dimethoxytolyl-benzobenzamidine-3-Heptachlor methionamine 1H NMR in CDC13: 7.79 (d, 6.4Hz, 2H); 7.52-7.40 (m, 3H); 7.38 (s, 1H ); 7.06 (s, 1H); 5.78 (brs, 1H); 3.96 (s, 3H); 3.94 (s, 3H); 2.96 (d, J = 4.7Hz, 3H) (M + H) + = 312 A &lt; 1 95. 5-Isopropoxylyl-2- (4-1 ^ pyridin-1-yl-phenyl) -benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO:. 8.16 ( s, iH); 7.71 (d, J = 8.1Hz, 2H); 7.45 (d, J = 8.1Hz, 1H); 7.01 (d, J = 1.8Hz, 1H); 6.85 (dd, J = 8.1, 2.1 Hz, 1H); 6.62 (d, J = 8.1Hz, 2H); 4.58 (m, 1H); 2.81 (d, J = 3.9Hz, 3H); 2.00 (m, 4H); 1.38 (d, J = 6.0 Hz, 6H) (M + H) + = 379 C &lt; 30 96. 5-amino-2-17-pyridin-4-yl-benzofuran carboxylic acid formamidine 1H NMR in CDCb: 8.75-8.73 (m, 2H); 7.87-7.84 (m, 2H ); 7.53-7.43 (m, 2H); 7.18-7.10 (m, 1H); 5.92 (bs, 1H); 3.09 (d, J = 4.8Hz, 3H) (M + H) + = 271 B &gt; 30 182- 88828.doc 200418452 Instance data name NMR data Mass Spec HCV pol -BB7 ICs〇 (/ iM) A = 彡 0 * 5 / iM B = 03 to ^ 5.0 C = 5.0 to ^ 30 μM D = &gt; 30 fiM Replicon (μM) 97.… 2- [2-0-Fluoro-phenyl> 6-methyl-3-methylamine Shen-benzo-benzo-5-yloxy] -propionic acid lH NMR in acetic-rfj acid-rf (CD3C02D): 8.75-8.73 (m, 2H); 7.87-7.84 (m, 2H); 7.53-7.43 (mT 2H); 7.18-7.10 (m, 1H); 5.92 ( bs, 1H); 3.09 (d, J = 4.8Hz, 3H) (M + H) + = 371 c &gt; 30 98. 6-Ethylamido-2- (4-fluoro-phenyl)- 5-isopropoxy-benzofuran-3- # methaneformamide 1H NMR in CDC13: 8.66 (s, 1H); 7.99 (s, 1H); 7.82 (dd, 2H, J = 5.2 & 8.7 Hz); 7.37 (s, 1H); 7.18 (t, 2H, J = 8.7Hz); 5.78 (bs, 1H); 4.70 (heptuplet, J = 6.1Hz); 2.96 (df 3H, J = 4.9Hz); 2.24 (s, 3H); 1.41 (d, 6H, J = 6.1Hz) (M + H) + = 85 A &lt; 10 99. 2- (4-Amino-phenyl) -5_ isopropoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.64-7.67 (d, J = 8.79Hz, 2H); 7.41-7.42 (d, J = 2.93Hz, 1H); 7.32-7.35 (d, J = 8.79Hz, 1H); 6.86-6.90 (dofd, J = 2.33Hz, 8.79Hz, 1H); 6.74- 6.77 (d, J = 7.03Hz? 2H); 5.84 (br.s, 1H); 4.56-4.64 (septet, J = 6.45Hz, 1H); 2.96-2.97 (d, J = 4.69Hz, 3H); 1.35 -1.37 (d, J = 6.45Hz, 6H) (M + H) + = 325 B &lt; 30 100. 2- (4-Dentyl-epiyl) -5_ isopropoxy-6- (2-morpho-pson 4-yl-ethylamine plug) -benzofuran-3-fatanoate Lamine 1H NMR in DMSO: 8.22-8.24 (d, J = 4.69Hz, 1H); 7.82-7.87 (m, 2H); 7.28-7.34 (t, i = 8.79Hz, 2H); 6.98 (s, 1H) ; 6.79 (s, 1H); 5.28 (brs, 1H); 4.56 (brs, 1H); 3.60 (brs, 3H); 3.23 (brs, 3H); 2.81-2.82 (d, J = 4.69Hz, 3H); 2.61 (brs, 1H); 2.43 (brs, 3H); 1.31-1.33 (d, J = 5.86Hz, 6H) (M + H) + = 456 B &lt; 30 101. 2- (4-Fluoro-phenyl) -5-isopropoxy-6-hexahydroethan-1-yl-benzoanan-3-carboxylic acid amidine 1H NMR in CDCI3: 7.89-7.84 (m, 2H); 7.23 (s, 1H); 7.14 (t, J = 8.79, 2H); 7.04 (s, 1H); 5.78 (bs, 1H); 4.69-4.29 (septet, J = 6.15, 1H); 3.05-3.01 (ra, 4H); 2.98 (d, J = 5.27, 3H); 1.77-1.72 (m, 4H); 1.60-1.59 (rn, 2H); 1.36 (d, J = 6.15, 6H) (M + H) + = 411 A &lt; 1 102. 2_ (4-fluoro-phenyl) -5,6-dimethoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.85-7.81 (m, 2H); 7.32 (s, 1H); 7.25-7.20 (m, 2H); 7.05 (s, 1H); 5.75 (brs, 1H); 3.96 (s, 3H); 3.947 (s, 3H); 2.98 (d, J = 4.2Hz, 3H) (M + H) + = 330 A &lt; 1 103. 2- (4-Gasyl-epoxy) -5-methoxyi-6-morpho ^ 7 Lin-4-i-dong and bitanan-3-carboxamide TH NMR in CDCl3 : 7.85-7.81 (m, 2H); 7.30 (s, IH); 7.17 (t, J = 8.8Hz, 2H); 7.08 (s, 1H); 3.94 (s, 3H); 3.94-3.91 (m, 4H ); 3.11-3.09 (m, 4H); 2.98 (d, J = 4.7Hz, 3H) (M + H) + = 385 A &lt; 1 104. 2- (4- &gt; Stylo-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDCI3: 7.80 (d, 2H, J = 8.79); 7.61 (d, 2H, J = 8.79); 7.39 (d, 1H, J = 8.79); 7.28 (d, 1H, J = 2.34); 6.94 (dd, 1H, J = 8.79, 2.34); 5.80 (brs, 1H); 4.58 (m, 1H); 3.01 (d, 3H, J = 4.69); 1.36 (d, 6H, J = 6.45), (M + H) + = 288 A &lt; 10 105. 2- (4-Fluoro-3-hydroxy-phenyl) -5-isopropoxy-benzofuran-3-methanoic acid formamidine 1H NMR in DMSO: 10.18 (brs, 1H) ; 8.32 (d, 1H, J = 4.69); 7.50 (rn, 2H); 7.26 (in, 2H); 7.03 (d, 1H, J = 2.34); 6.93 (dd, 1H, J = 8.79, 2.34); 4.58 (m, 1H); 2.81 (d, 3H, J = 4.69); 1.26 (d, 6H, J = 5.86) (M + H) + = 344 C &lt; 30 106. 2_ (4-Gasyl-benzyl) -5-isopropoxy-benzocarboxamidine carboxylic acid formamide NMR in CDCI3: 8.11 (d, 2H, J = 8.21); 7.74 (d, 2H, J = 8.79); 7.43 (d, 1H, J = 9.38); 7.20 (d, 1H, J = 2.34); 7.00 (dd, IH, J = 8.79, 2.34); 5.88 (brs, 1H ); 4.58 (m, IH); 3.06 (d, 3H, J = 4.69); 1.36 (d, 6H, J = 6.45) (M + H) + = 335 B &lt; 30 183-88828.doc 200418452 Example No. Name NMRdata Mass Spec HCV pol -BB7 IC5〇 QiM) A = &lt; 0 * 5 / «MB = 0 * 5 to s5.0 / tM C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ replicon (μΜ) 107.5 5-methoxy-2-pyridylbenzyl- 1H NMR in CDC13: 8.72 (d, J = 5.4H3, 2H); 7.83 (dd, J-1.8H3, 4.5H3, 2H); 7.45 (d, J = 9.0H3, 1H); 7.20 (d, J = 2.2H3, 1H); 7.01 (dd, J = 2.7H3, 8.7H3, 1H); 5.90 (bs, 1H); 3.88 (s, 3H); 3.08 (d , J = 4.8H3, 3H) (M + H) + = 283 B &lt; 100 108. 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (3-methylsulfonyl-St-yl-E4Yodo small group) -benzoxan-3-a Formamidine acid 1U NMR in DMSO: 7.90 (dd, J = 1.8,5.3Hz, 2H); 7.33 (t, J = 8.8Hz, 2H); 7.07 (s, 1H); 7.05 (s, 1H); 4.63 (p, J = 6.4Hz, 1H); 3.96-3.86 (m, 2H); 3.49-3.32 (m, 2H); 3.03 (s, 3H); 2.82 (s, 3H); 231 (m, 2H); 1.33 (d, J = 1.2Hzt 6H) (M + H) + = 475 A &lt; 1 109. 6-trimethylenepentamin-1-yl_2_ (4-amino-phenyl) -5-iso-methyl-benzyl-3-carboxylic acid formamidine 1H NMR in CDC13: 7.82 (dd, J = 5.3, 8.8Hz, 2H); 7.13 (s, 1H); 7.13 (t, J = 8.2Hz, 2H); 6.54 (s, 1H); 4.60 (p, J = 5.9Hz (1H); 3.96 (t, J = 7.6Hz, 4H); 2.97 (d, J = 5.3Hz, 3H); 2.29 (p, J = 7.0Hz, 2H); 1.36 (d, J = 6.4Hz, 6H ) (M + H) + = 383 A &lt; 1 110. hydrazone (4-fluoroi-phenyl) -6- (3-meryl-p-pyrolodin-1-yl) -5-isopropoxy-benzofuran-3-chinoic acid Amine (M + H) + = 413 A &lt; 1 111. 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (methanesulfonyl-methyl-amino) -benzofuran-3-fatty acid formamidine Amine * H NMR in CDC13: 7.81 (2H, dd, J = 5.3, 8.8Hz); 7.56 (1H, s) 7.42 (1H, s); 7.20 (2H, r, J = 8.8Hz); 5.70 (1H, bs); 4.80 (1H, heptuplet, J = 6.2Hz); 3.32 (3H, s); 2.98 (3H, s); 2.96 (3H, s); 1.42 (3H, d, J = 6.2Hz) (M + H) + = 435 A &lt; 1 112. 2_ (4-Aminophenyl) -6 _ [(crean-3_ylmethyl) -amino] -5-isopropoxy-benzocran-3-chinoic acid Lamine 1H NMR in CDC13: 7.76-7.81 (m, 2H); 7.37 (d, J = U7, 1H); 7.17 (s, 1H); 7.086-7.145 (t, J = 8.79, 2H); 6.746 (s , 1H); 6.319-6.328 (m, 1H); 6.242-6.252 (d, J = 2.93, 1H); 5.86 (bs, 1H); 4.565-4.645 (septet, J = 6.45, 1H); 4.365 (s, 2H); 2.940 -2.955 (d, J = 4.69, 3H); 1.375-1.254 (d, J = 6.45,6H) (M + H) + = 423 A &lt; 1 113. 6- (2,3-Dimethynylpropylamine grave) -2- (4-Gasyl-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid methyl ester Amidine (Η NMR in CDCl3: 7.78 (bs, 2H); 7.12 (rn, 4H); 6.72 (bs, 1H); 5.84 (d, J = 4.7 Hz, 1H); 4.60 (p, J = 5.9 Hz, 1H); 4.01 (m, 1H); 3.80 (dd, J = 3.52, 11.1 HZ, IH); 3.66 (dd, J = 5.9, 11.1 Hz, 1H); 2.96 (d, 1 = 4.1 Hz, 3H); 1.37 (dd, J = 1.8, 5.9 Hz, 6H) (M + H) + = 417 B &lt; 10 114. 2_ (4-Fluoro-phenyl) -5-isopropoxy-6-isopropylamino-benzofuran-3-methanoate * H NMR in CDCI3: 7.805 -7.834 (m, 2H); 7.151 (s, 1H); 7.100-7.127 (m, 2H); 6.680 (s, lH); 5.900 (bs, 1H); 4.580-4.600 (septet, J = 5.861, 1H ); 3.662-3.686 (septet, J = 7.033, 1H); 2.955 -2.971 (d, J = 4.688, 3H); 2.057 (s, 1H); 1.361 -1.381 (d, J = 5.861, 6H); 1.258- 1.277 (d, J = 5.861,6H) (M + H) + = 385 A &lt; 1 184- 88828.doc 200418452 Instance number name NMRdata Mass Spec HCV pol -BB7 IC50 (μΜ) A = μΜ B = 03 to ^ 5.0 / iM C = 5.0 to ^ 30 μΜ D = &gt; 30 / iM Copy (ΜΜ) 115. 6- (Cyclopropylmethyl-amino) -2- (4-amino-winteryl) -5-isopropoxy-benzofuran-3-carboxylic acid methylamine 1H NMR in CDC13: 7.780-7.866 (m, 2H); 7.176 (s, IH); 7.104 -7.160 (m, 2H); 6.664 (s, 1H); 5.781 (bs, 1H); 4.567-4.647 (septet, J = 5.86l, 1H); 3.000 -3.024 (d, J = 7.033,2H); 2.965-2.981 (d, J = 4.689, 3H); 1.502-1.676 (m, 1H); 1.383 -1.402 (m, 1H) ; 1.211-1.172 (m, 1H); 0.557 -0.619 (m, 1H); 0.262-.0311 (m, 1H) (M + H) + = 397 A &lt; 1 116. 2- (4-Fluoro-phenyl) -5 ^ methoxy-6-pyrrolidin-1-yl-benzofuran-3-methaneformate 1H NMR in CDC13: 8.28 (d, 1 = 4.40, 1H); 7.89-7.84 (m, 2H); 7.31 (t, J = 8.79, 2H); 7.00 (s, 1H); 6.91 (s, 1H); 3.81 (s, 3H) ; 3.29 (m, 4H); 2.82 (d, J = 4.40, 3H); i.88 (m, 4H) (M + HT = 369 A &lt; 1 117.5 5'-Methoxy-2- (4-fluoro-phenyl) -6-morpholine &gt; --- NMR in CDCb: 7.788-7.83 (m, 2H); 7.60-7.09 (m, 9H); 5.71 (bs, 1H); 5.19 (s, 2H); 3.90-3.87 (m, 4H); 3.17- 3.15 (m, 4H); 2.98 (d, J = 51.Hz, 3H) (M + H) + = 461 A &lt; 1 118. 5-Hydroxymethyl-2-phenyl, benzofuran-3-methanoate, 1H NMR in CDC13: 7.98-7.87 (m, 3H); 7.53-7.43 (mT 4H); 7.38 (d, J = 7.0Hz, 1H); 5.84 (br s, 1H); 4.83 (d, J = 6.0Hz, 2H); 2.99 (d, J = 5.3Hz, 3H) (M + H) + = 282 C &gt; 100 119. 2- (4-Amino-phenyl) -5-isopropoxy-6-K2-methoxy-ethyl) -methyl-amino] -benzofuran Amidine * H NMR in CDCI3: 7.86-7.82 (m, 2H); 7.26-7.24 (m, 1H); 7.15 (t, J = 8.35Hz, 2H); 7.08 (s, 1H); 5.76 (s, 1H ); 4.70-4.62 (septet, J = 6.15Hz, 1H); 3.59 (tt J = 6.15Hz, 2H); 3.37-3.35 (m, 2H); 3.33 (s, IH); 2.98 (d, J = 4.83 Hz, 3H); 2.92 (s, 3H); 1.39 (d, J = 6.15Hz, 6H) (M + H) + = 415 A &lt; 1 120. 6-Amino-5-benzyloxy-2- (4-fluoro-phenyl) -benzofuran-3-guidate formamidine 1H NMR in CDC13: 7.86-7.80 (m, 2H); 7.45-7.33 (m, 5H); 7.287 (s, 1H); 7.17-7.12 (m, 2H); 6.85 (s, 1H); 5.71 (brs, 1H); 5.15 (s, 2H); 2.97 (d, J = 5.3Hz, 3H) (M + H) + = 391 A &lt; 10 121. 5-Isopropyloxy-succin-2-yl) -benzofuran-3-carboxylic acid formamidine 1H NMR in CDCI3: 7.664-7.674 (d, J = 2.931, 1H); 7.512-7.518 (d, J = L.759, 1H); 7.319-7.348 (d, J = 8.792, 1H); 6.893-6.932 (d of d, J = 2.931, 5.861, 1H); 6.721 (bs, 1H ); 6.448-6.453 (d, J = 1.759, IH); 4.584-4.664 (septet, J = 5.861, 1H); 3.006-3.024 (d, J = 5.275, 3H); 2.322 (s, 3H); 1.344- 1.363 (d, J = 5.861, 6H) 氺 氺 氺 B &lt; 30 122. 2_ (4-fluorophenyl) -6_methanesulfonylamino-5-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.37 (m, 1H) ; 7.93 (dd, J = 5.1 & 9.1 Hz, 2H); 7.56 (s, 1H); 7.36 (t, J = 8.8Hz, 2H); 7.17 (s, iH); 3.90 (s, 3H); 2.98 (s, 3H); 2.83 (d, J = 4.9 Hz, 3H) (M + H) + = 393 A &lt; 1 185-88828.doc 200418452 Example number name NMR data Mass Spec HCV pol -BB7 IC50 (μΜ) A = μΜ B = 0 J to ^ 5.0 μ, Μ C = 5.0 to ^ 30 fiM D = &gt; 30 μM replicon &lt; JiM) 123. 2- (4-Fluoro-phenyl) -5-isopropoxy-6-[(tetramus-4an-2-ylmethyl grave) -amino] -benzofuran- 3-carboxylic acid formamidine 1H NMR in DMSO: 8.27 (d, br, 1H); 7.88 (dd, 2H); 7.31 (dd, 2H); 6.92 (s, 1H); 6.84 (s, 1H); 4.98 (m, 1H); 4.57 (m, 1H); 4.11 (m, 1H); 3.8-3.64 (mt 2H); 3.16 (m, 1H); 2.82 (d, 3H); 1.84-1.42 (m, 4H) ; 1.35 (d, 6H) (M + H) + = 427 A &lt; 10 124. .5 (4-fluoro-phenyl) -5-year-old f-yl-6-morphoρ · fluoren-4-yl-benzofuran-3-quinoline formamidine 1H NMR in CDC13 : 8.00-7.95 (m, 2H); 7.36-7.26 (m, 2H); 7.21 -7.18 (m, 2H); 6.98 (bs, 1H); 5.83 (bs, 1H); 3.95-3.92 (m, 4H) ; 3.04 (d, J = 5.1Hz, 3H); 2.97-2.96 (m, 4H) (M + H) + = 370 B &lt; 10 125. 5-Cyclopropylmethoxy-2- (4-fluoro-phenyl) -6-morphol 4-4-yl-benzofuran-3-carboxylic acid formamidine 1H NMR in CDCb: 7.89-7.84 (m, 2H); 7.30 (s, 1H); 7.22-7.16 (m, 2H); 7.08 (s, 1H); 5.76 (bs, 1H); 3.94 -3.97 (m, 6H); 3.20-3.17 (m, 2H); 3.01 (d, J = 4.8, 2H); 0.71-0.64 (m, 2H); 0.42-0.38 (m, 2H) (M + H) + = 425 A &lt; 1 126. 6-Ethyl-2- (4-amino-winteryl) -5-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.86-7.81 (m, 2H); 7.54 (s, 1H); 7.42 (s, 1H); 7.23-716 (m, 2H); 5.77 (brs, 1H); 3.96 (S, 3H); 2.98 (d,) = 4.1 Hz, 3H ) (M + H) + = 334.0 A &lt; 1 127.6- (2,5-dimethyl-2H-pyrazol-3-ylamino) -2- (4-fluoro-phenyl) · 5-isopropoxy-benzo4 Methane-3-carboxylic acid formamidine * H NMR in CDC13: 7.782-7.826 (m, 2H); 7.352 (s, 1H); 7.137-7.194 (m, 2H); 6.840 (s, 1H); 6.069 (s , 1H); 5.930 (s, iH); 5.795 (bs, 1H); 4.686-4.746 (septet, J = 6.447, 1H); 3.695 (s, 3H); 2.986-3.004 (d, J = 5.275, 3H) ; 2.287 (s, 1H); 1.645 (bs, 2H); i.436-1.457 (d, J = 6.447, 3H) (M + H) + = 437.0 C 氺 氺 氺 128. 2_ (4_fluoro group- Phenyl) -6-morpholin plin-4-methyl-5-(^ 7bipyridin-4-ylmethoxy) -benzofuran-3-chimonate formamidine'H NMR in CDC13: 8.68-8.65 (m, 2H); 7.87-7.82 (m, 2H); 7.40-7.43 (m, 3H); 7.25-7.15 (ra, 3H); 5.70 (bs, 1H); 5.23 (3, 2H): 3.98-3.92 (m, 4H); 3.15-3.21 (m, 4H): 2.99 (d, J = 48 Hz, 3H) (M + H) + = 462 A 氺 氺 氺 129. 6-yl-2- (4-gas Methyl-phenyl) -5-isoamyloxy-benzofuran-3-quinoline formamidine * H NMR in CDC13: 7.87-7.82 (m, 2H): 7.67 (s, iH); 7.45 (s, 1H); 7.26-7.19 (m, 2H); 5.73 (bs, 1H); 4.75-4.67 (m, iH); 2.98 (d, J = 4.8 Hz, 3H); 1.43 (d, J = 6.3 Hz, 6H ) (M + H) + = 353 A 氺 氺 氺 130. 5-methoxy-2-phenyl-benzoxan-3-acetamidine 1H NMR in CDC13: 7.86 (dd, J = 2.1, 7.4 Hz, 2H); 7.47 (m, 3H); 7.39 (ra, 2H); 5.78 (brs, 1H); 3.88 (s, 3H); 6.94 (dd, J = 2.6, 9.0 Hz, 1H); 3.48 (dq, J = 1.3, 7.2 Hz, 2H); 1.17 (t, 7.2 Hz, 3H) (M + H) + = 295 C &lt; 10 131. 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (4-amidoamino) -benzofuran-3-carboxylic acid formamidine 1H NMR in CDCi3 : 8.29-8.31 (d, 2H, J = 5.86Hz); 7.80-7.84 (m, 2H); 7.51 (s, iH); 7.36 (s, 1H); 7.13-7.19 (t, 2H, J = 8.21Hz ); 6.95-6.98 (m, 2H); 6.62 (s, 1H); 6.13-6.15 (d, 1H, J = 4.69Hz); 4.60-4.68 (septet, lH, J = 5.86Hz); 2.97-2.99 ( d, 3H, J = 5.28Hz); 1.37-1.39 (d, 6H, J = 5.86Hz) (M + H) + = 420 B &lt; 30 186- 88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 IC50 (μΜ) A = ί0.5 · / ιΜ B = (K5 to 彡 5.0 / iM C = 5.0 to ^ 30 / iM D = &gt; 30 μM replicon_ 132. 2- (4-fluoro-phenyl) -5-isopropoxy-6- (4-methyl-hexahydropyrine-1-yl) -benzofuran complex Methylamine 1H NMR in DMSO: 7.80-7.86 (m, 2H); 7.21 (s, 1H); 7.09-7.15 (t, 2H, J = 8.79Hz); 6.99 (s, 1H); 6.12-6.14 ( d, 1H, J = 4.69Hz); 4.58-4.66 (septet, 9H, J = 6.45 Hz); 3.10 (brs, 4H); 2.95-2.96 (dT 3H, J = 4.69Hz); 2.58 (brs, 4H) ; 2.34 (s, 3H); 134-1.36 (d, 6H, J = 6.45 Hz) (M + H) + = 426 C &gt; 30 133. Gas-propyl: fe-1-phenylamino -2- (4-Fluoro-phenyl) -5-isopropoxy-benzo-p-furan-3-methanamine'H NMR in DMSO: 9.1 i (s, lH); 8.37 (m , 1H); 7.92 (dd, J = 8.8 & 5.7 Ha 2H); 7.56 (s, 1H); 7.36 仏 J = 8.8 Hz, 2H); 7.16 (s7 IH); 4.74 (heptuplet, J = 5.7 Hz, IH); 3.74 (t, J = 6.6Hz, 2H); 3.21 (m, 2H); 2.82 (d, J = 4.8Hz, 3H); 2.21 (m, 2H); 135 (d, J = 5.7 Hz, 6H) (MH) = 481; 483 B &lt; 1 134. 6- (1,1-Dioxy-1λ6-isopyrimidin-2-yl) -2- (4-amino-phenyl) -5-isonanoxy! yl-benzyl Wean · 3_carboxylic acid formamidine 1H NMR in DMSO: 8.40 (ra, 1H); 7.92 (dd, J = 5.5 d 9.2 Hz, 2H); 7.60 (s, 1H); 7.37 (t, J = 9.2 Hz, 2H); 7.19 (s, 1H); 4.69 (heptuplet, J = 5.9 Hz, 1H); 3.75 (t, J = 7.0 Hz, 2H); 3.37 (m, 2H); 2.82 (d, J = 4.9 Hz, 3H); 2.43 (p, J = 7.0 Hz, 2H); 1.34 (d, J = 5.9 Hz, 6H) (M + HT = 447 B &lt; 10 135.2 2- (4-fluoro-phenyl)- &lt; Isopropoxy-6-adenosyl-benzofuran-3-metanoformamide'H NMR in DMSO: 8.38 (s, 1H); 8.28 (m, 1H); 7.87 (dd, J = 5.3 & 9.2 Hz, 2H); 7.30 (t, J = 8.8 Hz, 2 H); 7.09 (s, 1H); 6.39 (bs, 2H); 4.62 (heptuplet, J = 6.1 Hz, 1H); 2.80 (d , J = 4.8 Hz, 3H); 1.88 (s, 1H); 1.32 (d, J = 5.7 Hz, 6H) (M + H) + = 486 A &lt; 10 136. 2- (4-Amino-phenyl) -5_ isopropoxy-6- (isopropyl-methanesulfonyl-amino) -benzofuran stomach 3-metamethamine lH NMR in DMSO: 8.40 (m, 1H); 7.90 (dd, J = 5.3 & 8.84 Hz, 2H); 7.69 (s, 1H); 7.36 (t, J = 8.8 Hz, 2H); 7.11 (s, 1H); 4.75 (heptuplet, J = 6.6 Hz, 2H); 4.22 (heptuplet, J = 7.1 Hz, 1H); 3.06 (s, 3H); 2.80 (d, J = 7.1 Hz, 3H); 1.32 (t, J = 6.6 Hz, 6H); 1.20 (d, J = 7.1 Hz, 3H); 1.05 (d, J = 7.1 Hz, 3H) (M + H) + = 463 A &lt; 1 137.6- (Cyclopropylmethyl-methylsulfonyl-amino) &gt; 2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid Formamidine 1H NMR iQ DMSO: 8.44 (m, 1H); 7.94 (dd, J = 5.1 & 9.1 Hz, 2H); 7.57 (s, 1H); 7.38 (t, J = 8.8 Hz, 2H); 7.16 (s, 1H); 6.78 (heptuplet, J = 5.7Hz, 1H); 3.01 (s, 3H); 2.83 (d, J = 4.4 Hz, 3H); 1.33 (d, J = 5.7 Hz, 6H); 0.85 (m, 1H); 0.37 (m, 2H) (M ten H) + = 475 A &lt; 1 138.6 6- (2,6-dimethyl-morpho 14-yl) -2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-metanoic acid Formamidine 1H NMR in CDC13: 7.89-7.84 (m, 2H); 7.28 (d, J = 8.79 Hz, 1H); 7.17 (T, J = 8.79 Hz, 2H); 7.04 (s, 1H); 5.77 ( s, 1H); 4.69-4.61 (septet, J = 6.15 Hz, IH); 3.95-3.89 (m, 2H); 3.46 (d, J = 11.43 Hz, 2H); 2.98 (d, J = 4.84 Hz, 3H ); 2.37 (T, J = l0 '. 55 Hz, 2H); 1.37 (d, J = 6.15 Hz, 6H); 1.25 (d, J = 6.15 Hz, 6H) (M + H) + = 441 B &lt; 10 139. 2- (4 ** Fluoro-phenyl) -5_ isopropoxy-6- (1Η-tetra-5-yl) -phenylbenzofuran-3-carboxylic acid formamide 1H NMR ia CDCi3: 8.547 (s, 1H); 7.89-7.84 (m, 2H); 7.61 (s, 1H); 7.60-7.20 (m, 2H); 5.8 (bs, 1H); 5.0-4.92 (m, 1H) ; 3.26 (bs, 1H); 2.99 (d, J = 5.iHz, 3H); 1.52 (d, J = 6.0Hz, 6H) (M + H) + = 3% B &gt; 30 187- 88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 IC50 〇iM) A = μΜ B = 03 to ^ 5.0 / iM C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ replicon (μΜ) 140. 2- (4 -Fluoro-phenyl) -6- (4-hydroxy-hexahydropyridine-1-yl) &gt; 5-isopropoxy-benzofuran-3-chinoic acid methylamine 1H NMR in DMSO: 8.28 ( d, J = 4.84Hz, 1H); 7.92-7.86 (m, 2H); 7.33 (t, J = 8.79Hz, 2H); 7.16 (s, 1H); 7.03 (s, 1H); 4.64-4.56 (m , 2H); 3.61 (m, 1H); 3.35 (m, 2H); 2.82 (d, J = 4.40Hz, 3H); 2.74-2.67 (m, 2H); 1.88-1.85 (m, 2H); 1.62- 1.52 (m, 2H); 1.29 (d, J = 5.72Hz, 6H) (M + H) + = 427 B &lt; 10 141. 2- (4-Fluoro-phenyl) -6- (3-hydroxy-hexahydroxyl) &gt;1-yl;)-5-isopropoxy-benzofuran-3- Formamidine m acid 1H NMR in DMSO: 8.29 (d, J = 4.84Hz, 1H); 7.92-7.87 (m, 2H); 7.33 (t, J = 8.79HzT 2H); 7.14 (s, 1H); 7.03 (s, 1H); 4.73 (ci J = 4.84Hz, 1H); 4.63-4.55 (septet, J = 6.15Hz, 1H); 3.67 · 3 · 65 (m, 1H); 3.49 (d, J = 8.79Hz, 2H); 2.82 (d, J = 4.40Hz, 3H); 2.5 (m, 1H); 2.33 (t, J = 9.67Hz, 1H); 1.95-1.91 (m, 1H); 1.74 (m, 1H); 1.62-1.58 (m, 2H); 1.29 (d, J = 6.15Hz, 3H); 1.28 (d, J = 5.71, 3H) (M + H) + = 427 B &lt; 10 142.2 2- (4-fluoro-phenyl): 5-isopropyllactyl ^ -6- (morpholin ^ sulfonyl) -benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.48-8.47 (d, J = 4.69Hz, 1H); 8.01 (s, 1H); 8.00-7.95 (m, 2H); 7.44-7.38 (t, J = 8.79Hz, 2H); 734 ( s, iH); 4.91-4.83 (septet, J = 5.86Hz, 1H); 3.62-3.59 (m, 4H); 3.16-3.13 (m, 4H); 2.85-2.84 (d, J = 4.69Hz, 3H) ; 1.37-1.35 (d, J = 5.86Hz, 6H) (M + H, = 477 A &lt; 10 143. 2- (4-Fluoro-phenyl) -5-isopropoxy-6-methyl monthanite s & i-benzoanan-3-carboxylic acid formamidine 1H NMR in DMSO: 8.46-8.45 (d, J = 4.10Hz, 1H); 7.99-7.95 (m, 2H); 7.95 (s, 1H); 7.43-7.37 (t, J = 8.79Hz, 2H); 7.32 (s , 1H); 6.64 (d, J = 4.69Hz, 1H); 4.90-4.82 (septet, J = 5.86Hz, 1H); 2.85-2.83 (d, J = 4.69Hz, 3H); 2.48-2.46 (d, J = 4.69Hz, 3H); 1.38-1.36 (d, J = 5.86Hz, 6H) (M + ΗΓ = 421 A &gt; 30 144. 6-dimethylaminesulfonyl- -2- (4-gas (Phenyl-phenyl) -5-isopropoxy-benzo-4anthidine carboxylic acid formamide 1H NMR in DMSO: 8.461 = 8.451 (d, J = 4.689Hz, 1H); 8.016-7.949 (m, 3H) ; 7.436-7.377 (t, J = 8.791Hz, 2H); 7.323 (s, 1H); 4.904-4.823 (septet, J = 5.861Hz, 1H); 2.848-2.832 (dT J = 4.689Hz, 3H); 2.775 (s, 6H); 1.365-1.344 (d, J = 6.447Hz, 6H) (M + H) + = 435 A &lt; 30 145. 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (propanesulfonylamino) -benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO : 8.85 (s, 1H); 8.36 (m, 1H); 7.91 (dd, J = 9.2, 5.3Hz, 2H); 7.59 (s, 1H); 736 (t, J = 8.8HzT 2H); 7.13 (s , 1H); 4.75 (heptuplet, J = 5.6Hz, 1H); 3.21 (heptuplet, J = 5.5Hz, 1H); 2.82 (d, J = 4.9Hz, 3H); 1.36 (d, J = 5.5Hz, 6H ); 1.28 (d, J = 5.6Hz, 6H) (M + H) + = 449 B &lt; 10 146. 2- (4-Syridyl-phenyl) -5_ isopropoxy-benzofuran-3,6-dicarboxylic acid 6-amidamine-3-carboxamide 1U NMR in CDC13: 8.33 (s, 1H); 8.10 (bs, 1H); 7.88-7.84 (m, 2H); 7.48 (s, 1H); 7.25-7.18 (m, 2H); 5.88 (bs, 1H); 5.75 (bs, 1H) ); 4.88-4.80 (in, 1H); '2.99 (d, J = 5.4Hz, 3H); 1.46 (d, J = 6.3Hz, 6H) (M + H) + = 371 B &gt; 30 147.2 -(4-Gasyl-wood-based) -5-isopropoxymethyl-benzoylpyranoate, 1H NMR in DMSO: 9.13 (s, 1H); 8.99 (s, 2H); 8.41 ( q, br, 1H); 7.92 (m, 2H); 7.82 (s, 1H); 7.36 (m, 2H); 7.27 (s, 1H); 4.64 (m, 1H); 2.83 (d, 3H); 1.23 (d, 6H) (M + H) + = 406 A &lt; 10 188- 88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 IC50 (μΜ) A = B = 0 »5 to 彡 5.0 / iM C = 5.0 to ^ 30 μΜ D = &gt; 30 / iM Replicon (μM) 148. 6-Third-butylamino-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine NMR in CDC13: 7.85-7.80 (m, 2H); 7.18 (s, 1H); 7.14 (t, J = 8.79Hz, 2H); 6.98 (s, 1H); 5.74 (bs, 1H); 4.60-4.52 (septet, J = 6.15Hz, 1H); 4.57 (s, 1H); 2.97 (d, J = 4.84Hz, 3H); 1.41 (s, 9H); 1.37 (d, J = 6.15Hz, 6H) (M + H) + = 399 A &lt; 10 149. 2- (4-Gas-wood-based) -5_ isopropoxy-6-aminosulfonyl-benzene + furan-3-methanamine jH NMR in DMSO: 8.39-8.37 (d, J = 4.69Hz, 1H); 7.97-7.93 (m, 2H); 7.91 (s, 1H); 7.39-7.33 (t, J = 8.79Hz, 2H); 7.07 (s, 1H); 4.66 ( septet, J = 6.45Hz, 1H); 2.84-2.82 (d, J = 4.69Hz, 3H); 1.30-1.28 (d, J = 6.45Hz, 6H) (MH) = 406.0 C &gt; 30 150. 6 -Cyclobutylamine-2-methyl-4- (4-amino-phenyl) -5-isopyroxy-benzo-4an-3-carboxylic acid formamidine 1H NMR in CDC13: 8.057 (st 1H) ; 7.869-7.823 (m, 2H); 7.522 (s, 1H); 7.248-7.205 (rat 2H); 5.766 (bs, 1H); 5.156-5.125 (d, J = 9.377Hz, 1H); 4.895-4.813 ( septet, J = 5.862Hz, 1H); 3J87-3.707 (sextet, J = 8.206Hz, 1H); 2.984-2.969 (d, J = 4.689Hz, 3H); 2.063-1.967 (m, 2H); 1.828-1.734 (m, 2H); 1.580-1.512 (m, 2H); 1.494-1.475 (d, J = 5.862Hz, 6H) (M + H) + = 461.0 B &lt; 30 151. 2- (4-Fluoro-phenyl) -6_ sulfan-2-yl-5-iso and oxy-benzoxan-3-chimonic acid formamidine 1H NMR in CDCl3: 7.96 (s, iH); 7.88 (m, 2H); 7.48 (d, 1H); 7.37 (s, 1H); 7.17 (m, 2H); 7.08 (d, IH); 6.51 (d, 1H); 5.75 ( s, br, 1H); 4.79 (m, IH); 2.99 (d, 3H); 1.45 (d, 6H) (M + H) + = 394 A &lt; 30 152. 2- (4-Gas-phenyl) -6-furan-3-yl-5-isopropoxy-benzofuran-3-carboxylic acid formamidine * H NMR in CDCb: 8.12 (s , 1H); 7.90 (m, 2H); 7.61 (s, 1H); 7.48 (d, 1H); 7.38 (s, 1H); 7.18 (m, 2H); 6.83 (d, 1H); 5.75 (s, br, 1H); 4.79 (mT 1H); 2.99 (d, 3H); 1.45 (d, 6H) (M + H) + = 394 A &lt; 10 153. 2- (4-Fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine NMR in CDC13: 8.80 (d, 1H); 8.57 (dd, 2H); 7.92 (m, 3H); 7.45 (s, 2H); 7.33 (dd, 1H); 7.20 (m, 2H); 5.80 (s, br, 1H); 4.56 (m, 1H); 2.99 (d , 3H); 1.28 (d, 6H) (M + H) + = 405 A &lt; 10 154. 2- (4-Fluoro-phenyl) &gt; 5: isoamyloxy-6-debiloline-1-phenylfluorenyl-benzobenzo-3-carboxylic acid formamidine 1H NMR in DMSO: 8.455-8.471 (m, 1H); 8.028 (s, 1H); 7.996-7.949 (m, 2H); 7.436-7.375 (m, 2H); 7.321 (s, 1H); 4.918-4.838 (septet , J = 5.861Hz, 1H); 2.846-2.832 (d, J = 4.103, 3H); 2.512-2.486 (peatet, J = 1.758Hz, 4H); 1.779-1.736 (t, J = 6.447Hz, 4H); 1.371-1.350 (d, J = 6.447Hzt 6H) (M + H) + = 461.0 A &lt; 10 155. 6-Phosylpropylamine, 2- (4-muryl-phenyl) -5-isopropoxy-benzo-4an-3-carboxylic acid formamidine 1H NMR in DMSO : 8.47-8.46 (d, J = 41.0Hz, 1H); 8.03 (s, 1H); 8.00-7.94 (m, 2H); 7.44-7.38 (t, J = 8.79Hz, 2H); 7.32 (s, 1H ); 7.21 (s, 1H); 4.B9-4.85 (septet, J = 5.86Hz, 1H); 2.85-2.83 (d, J = 4.69Hz, 3H); 2.17 (m, 1H); 1.38-136 ( cl, J = 5.86Hz, 6H); 0.44 (m, 4H) (M + H) + = 447.0 A &lt; 10 156. Ethylaminesulfonyl-2- (4-ranyl-private) -5-isopropoxy · benzobenzo-3-carboxylic acid formamidine 1H NMR in DMSO: 8.87 (s, 1H); 8.36 (m, 1H); 7.91 (dd, J = 9.0, 5.3Hz, 2H); 7.56 (s, 1H); 7.36 (t, J = 8.8Hz, 2H); 7.14 (s , 1H); 4.75 (heptuplet, J = 6.1Hz, 1H); 3.05 (quadruplet, J = 7.5Hz, 2H); 2.82 (cl, J = 4.8Hz, 3H); 1.33 (d, J = 6.1Hz, 6H ); 1.26 (t, J = 7.5Hz, 3H) (M + H) + = 435 A &lt; 10 189- 88828.doc 200418452 Example No. Name NMRdata Mass Spec HCV pol -BB7 IC50 (μΜ) A = μΜ B = 03 to ^ 5.0 μΜ C = 5.0 to &lt; 30 μΜ D = &gt; 30 μΜ replicon (μΜ) 157.2 2- (4-isopropoxy-6-vinyl-benzofuran-3-quinoline formamidine 1H NMR in DMSO: .8.39 (q, br, 1H); 7.91 (dd, 2H); 7.82 (s, 1H); 7.35 (dd, 2H); 7.12 (s, 1H); 7.05 (dd, 1H); 6.89 (d, 1H); 5.27 (d, 1H); 4.60 (m, 1H); 2.81 (d, 3H); 1.31 (d, 6H) (M + H) + = 354 A &lt; 10 158.2. 2- (4-Fluoro-phenyl) -5-isopropoxy-6-methoxy-benzofuran-3-methaneformamide 1HNMRinCDCl3: 7.86 (m, 2H); 7.34 (s, 1H); 7.16 (t, J = 8.79Hz, 2H); 7.05 (s, 1H); 5.75 (brs, 1H); 4.55 (m, 1H); 3.91 (s, 3H); 2.99 (d , J = 4.69Hz, 3H); 1.39 (d, J = 5.86Hz, 6H) (M + H) + = 358 A &lt; 10 159. 6- (3,5-dimethyl-isoxazolone: 10-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-gui Formamidine acid 1HNMRinCDCl3: 7.90-7.85 (m, 2H); 7.63 (s7 2H); 7.23-7.17 (m, 3H); 5.78 (brst 1H); 4.52-4.48 (m, 1H); 3.0 (d, J = 4.8Hz, 3H); 2.32 (s, 3H); 2.20 (s, 3H); 1.24 (d, J = 6.3Hz, 6H) (M + H) + = 423 A &lt; 1 160. 2- (4-methylfluorenyl-5-isopropoxy-benzofuran-3-quinic acid formamidine 1H NMR in CDC13: 10.524 (s, 1H); 7.93 (s, 1H) ; 7.90-7.85 (m, 2H); 7.44 (s, 1H); 7.25-7.19 (m, 2H); 5.78 (br, 1H); 4.76 (pent, 1H); 2.98 (d, 3H); 1.43 (d , 6H) (M + H) + = 355.9 A &lt; 30 161. 2- (4-Fluoro-phenyl) amino group-3-yl) -5-isopropoxy-benzofuran-3-quinoline formamidine * H NMR in CDCb: 8.52 (s, 1H); 8.45 (d, 1H); 7.88 (dd, 2H); 7.45 (s, 1H); 7.38 (m, 1H); 7.26 (s, 1H); 7.20 (dd, 2H); 5.77 (s, br, 1H); 4.55 (m, 1H); 2.99 (d, 3H); 1.24 (d, 6H) (M + H) + = 423 A &lt; 10 162. 2- (4-Fluoro-phenyl) -5-isopropoxy6-6- (methylaminoamino-methyl) -benzofuran-3-carboxylic acid formamidine lH NMR in CDC13: 7.85-7.81 (m, 2H); 7.44 (s, 1H); 7.41 (s, 1H); 7.23-7.17 (m, 2H); 5.73 (s, 1H); 4.98 (t, J = 5.4Hz, 1H); 4.78-4.71 (m, 1H); 4.39 (d, J = 6.6Hz, 3H); 2.97 (d, J = 4.8Hz, 3H); 2.74 (s, 3H); 1.40 (d, J = 5.7Hz, 6H) (M + H) + = 435 B &lt; 10 163. 6- (Cyclopentyl-methanesulfonyl-amino) -2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine Amine 1H NMR in DMSO: 8.42 (m, 1H); 7.94 (dd, J = 6.2 & 8.8Hz, 2H); 7.53 (s, 1H); 7.38 (t, J = 8.8Hz, 2H); 7.13 (s , 1H); 4.76 (heptupiet, J = 5.7Hz, 1H); 4.28 (quintuplet, J = 8.8Hzt 1H); 3.11 (s, 3H); 2.83 (m, 3H); 1.93 (m, 2H); 1.45 ( m, 2H); 1.34 (m, 4H) (M + H) + = 489 A &lt; 1 164.2 2- (4-Fluoro-phenyl) _6-[(2-hydroxy-ethyl) _methanesulfonyl-amino] -5-isopropoxy-benzofuran-3- Carboxamide 1H NMR in DMSO:, 8.41 (m, 1H); 7.93 (dd, J = 5.2Hz, 2H); 7.60 (s, 1H); 7.38 (t, J = 8.8Hz, 2H); 7.16 (s, 1H); 4.78 (heptupiet, J = 5.8Hz, 1H); 4.67 (t, J = 5.7Hz, 1H); 3.60 (bs, 1H); 3.04 (s, 3H); 2.83 (d, J = 4.8Hz, 3H); 1.34 (d, J = 5.7Hz, 6H) (M + H) + = 465 A &lt; 10 190- 88828.doc 200418452 Instance data name NMRdata Mass Spec HCV pol -BB7 IC50 (μΜ) A = / tM B = 0 * 5 to ii.O / iM C = 5.0 to ^ 30 μΜ D = &gt; 30 μ, M replicon 0M) 165.2 2- (4-Gas-phenyl) -5-lightyl-6-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.94 (m, 2H); 7.28 (s, 1H); 7.15 (t, 2H, J = 8.79 Hz); 7.04 (s, 1H); 5.82 (brs, 1H); 5.59 (s, 1H); 3.97 (s, 3H); 3.01 (d, 3H, J = 5.28 Hz) (M + H) &quot; = 316 C &gt; 30 166. 5-Ethoxy-2- (4-amino-phenyl) -6-? Fluoroline-4-yl-benzoanan-3-methanoate * H NMR in DMSO: 8.30 (m, 1H); 7.88 (m, 2H); 7.32 (t, 2H, J = 8.79 Hz) ; 7.16 (s, 1H); 7.04 (s, 1H); 4.06 (q, 2H, J = 7.03 Hz); 3.74 (bm »4H); 3.02 (bm, 4H); 2.80 (d, 3H, J = 4.69 Hz); 1.36 (t, 3H, J = 7.03 Hz) (M + H) + = 399 B &lt; 10 167. 5- (4-Fluoro- ¥ oxy) -2- (4-denyl-phenyl) -6-morpholin-4-yl-phenylbenzfuran-3-carboxylic acid Lamine 1H NMR in DMSO: 8.30 (m, 1H); 7.88 (m, 2H); 7.55 (m, 2H); 7.33 (t, 2H, J = 8.79 Hz); 7.27-7.20 (m, 4H); 5.14 (s, 2H); 3.72 (bm, 4H); 3.03 (bm, 4H); 2.82 (d, 3H, J = 4.69) (M + H) + = 479 B &lt; 1 168. 2_ (4-Gasyl-phenyl) -5_ isopropoxy-6-azet-5-yl-benzofuran-3-methanoic acid formamidine 1H NMR in CDC13: 7.91- 7.83 (m, 4H); 7.69 (s, 1H); 7.41 (s, 1H); 7.22- 7.14 (m, 2H); 5.79 (bs, 1H); 4.86-4.78 (m, 1H); 2.99 (d, J = 4.8Hz, 2H); 1.46 (d, J = 6.3Hz, 6H) (M + H) + = 395 A &lt; 10 169. 2- (4-Fluoro-phenyl) -6- (4-Cyclo-hexaarginyl-1-continyl) -5-isopropoxy-benzofuran-3 -Formamidine carboxylate 1H NMR in DMSO: 8.47-8.49 (d, 1H, J = 4.69Hz); 8.01 (s, 1H); 7.95-8.00 (m, 2H); 738-7.44 (t, 2H, J = 8.79Hz); 7.32 (s, 1H); 4.82-4.90 (septet, 1H, J = 5.86Hz); 4.67-4.69 (d, 1H, J = 4.10Hz); 3.58-3.59 (in, 1H); 3.35 -3.45 (m, 2H); 3.24-3.30 (m, IH); 2.92-3.00 (m, 2H); 2.84-2.85 (d, 3H, J = 4.69Hz); 1.69-1.73 (in, 2H); 1.36 -1.41 (m, 1H); 1.34-1.36 (d, 6HT J = 5.86Hz) (M + H) + = 491 A &lt; 1 170. 6- (4,4-difluoroyl-hexahydropyridine-1 -yl) -2- (4-pyridylfluoro-phenyl) -5-isopropoxy-benzofuran- 3-Hydroxymethoxamine 1H NMR in CDC13: 7.87 (m, 2H); 7.31 (s7 1H); 7.17 (UJ = 8.35 Hz, 2H); 7.07 (s, 1H); 5.74 (s, 1H); 4.69 -4.61 (septet, J = 6.16 Hz, 1H); 3.23-3.19 (m, 4H); 2.98 (d, J = 5.27 Hz, 3H); 2.24-2.11 (m, 4H); 1.39 (d, J = 6.16 Hz, 6H) (M + H) + = 447 C &lt; 1 171.2 2- (4-Fluoro-phenyl) -6- (4-fluoro-hexahydropyridine-1-yl) -5-isopropoxy-benzofuran-3-¾ Formamidine acid 1H NMR in CDC13: 7.89-7.83 (m, 2H); 7.28 (s, 1H); 7.16 (t, J = B.79 Hz, 2H); 7.07 (s, IH); 5.76 (s, 1H); 4.92-4.72 (m, 1H); 4.69-4.61 (septet, J = 6.16 Hz, 1H); 3.24-3.22 (m, 2H); 3.08-3.01 (m, 2H); 2.98 (d, J = 4.84 Hz, 3H); 2.18-2.02 (m, 4H); 1.38 (d, J = 5.71 Hz, 6H) (M + H) + = 429 B &lt; i 172. 5-Difluoromethoxy-2- (4-fluoro-phenyl) &gt; 6-morpholin plin-4-ser-benzocaran-3-carboxylic acid formamidine 1H NMR in CDCI3: \ 7.87 (dd, J = 8.8,5.7Hz, 2H); 7.54 (s, 1H); 7.16 (t, J = 8.8Hz, 2H); 7.11 (s, 1H); 6.57 (t, J = 75.6Hz, 1H); 5.92 (d, J = 4.7Hz, 1H); 3.87 (t, J = 4.0Hz, 4H); 3.08 (t, J = 4.0Hz, 4H); 2.98 (d, J = 4.9Hz , 3H) (M + H) f = 421 A &lt; 1 191-88828.doc 200418452 Instance number name NMRdata Mass Spec HCVpol -BB7 ic50 0iM) A = μ, Μ B = 05 to ^ 5.0 μΜ C = 5.0 to ^ 30 D = &gt; 30 μΜ replicon (μΜ) 173. 5-Cyclopentyloxy-2- (4-fluoro-benzyl) -6-morpholin-4 tomb-Dongfanganan-3 -carboxamidine carboxylic acid * H NMR in CDC13: 7.86 (dd, J = 9.4, 5.3Hz, 2H); 7.28 (s, 1H); 7.16 (t, J = 9.4Hz, 2H); 7.04 (s, 1H); 5.74 (brs, 1H); 4.90 (in, 1H); 3.90 (t, J = 4.7Hzt 4H); 3.11 (t, J = 4.7Hz, 1H); 2.98 (d, J = 4.7Hz, 3H); 1.95 (m, 4H); 1.80 (m, 2H ); 1.70 (m, 2H) (MH) = 437 A &lt; 1 174. 2- (4 • Fluoro-phenyl) -5- mesyl-6-methanesulfonylamino-benzofuran-3-methanoformamide 1H NMR in DMSO: 8.36 (dt J = 4.7Hzt 1H); 7.91 (dd, J = 8.8, 3.0Hz, 2H); 7.48 (s, 1H); 7.36 (ζ J = 8.8Hz, 2H); 7.08 (s, 1H); 2.98 (st 1H ); 2.82 (d, J = 4.7Hz, 3H) (M + H) + = 379 B &lt; 30 175. 2- (4-Gasyl-phenyl) -5_isopropoxy-6- (thiomorpholine »Lin_4- &gt; 5 buy brewer group) -Priprofuran-3-carboxy Formamidine acid 1H NMR in DMSO: 8.47-8.48 (d, 1H J + 4.10Hz); 8.03 (s 1H); 7.95-8.00 (m, 2H); 7.38-7.44 (t, 2H, J = 8.79Hz) ; 7.33 (s, 1H); 4.84-4.92 (septet, 1H, J = 6.45Hz); 3.42-3.46 (m, 4H); 2.83-2.85 (d, 3H, J = 4.69Hz); 2.62-2.65 (in , 4H); 1.35-1.37 (d, 6H, J = 5.86Hz) (M + H) + = 493 A &lt; 1 176. 2- (4-Fluoro-phenyl) -6- (3-hydroxy-pyrrolidin-1 -continyl) -5-isopropoxy-benzocran-3 -renic acid Formamidine 1H NMR in DMSO: 8.46-8.48 (d, 1H, J = 4.69Hz); 8.03 (s, 1H); 7.95-7.99 (m, 2H); 7.38-7.43 (t, 2H, J = 8.79Hz ); 7.31 (s, 1H); 4.99 (br.s, 1H); 4.82-4.80 (septet, 1H, J = 5.86Hz); 4.24 (br.s, 1H); 3.38-3.46 (m, 4H); 3.07-3.11 (dd, 1H, J = 2.35Hz, 9.96Hz); 2.83-2.84 (d, 3H, J = 4.69Hz); 1.79-1.86 (m, 1H); 1.68-1.77 (m, 1H); 1.35 -1.37 (d, 6H, J = 5.86Hz) (M + H) + = 477 A &lt; 1 177. 2- (4-Fluoro-phenyl) -5-oxopropoxy-6-0 to 1 ^ -4-yl-benzofuran each #methanoformamine NMR in DMSO: 8.6 i (m, 2H); 8.42 (s, 1H); 7.94 (dd, 2H); 7.72 (s, 1H); 7.60 (d, 2H); 7.36 (dd, 2H); 7.25 (s, 1H); 4.6 (m, 1H); 2.84 (d, 3H); 1.22 (d, 6H) (M + H) + = 405 A &lt; 10 178. * 2- (4; fluoro-benzene: &)-5_ isopropoxy-6- (3-methanesulfonyl-phenyl) &gt; benzofuran-3-carboxylic acid formamidine Amine NMR in DMSO: 8.42 (m, 1H); 8.16 (m, 1H); 7.98-7.88 (m, 4H); 7.72 (s, 1H); 7.69 (t, 1H); 7.39 (dd, 2H); 7.27 (s, 1H); 4.60 (m, 1H); 3.26 (s, 3H); 2.86 (d, 3H); 1.29 (d, 6H) (M + H) + = 482 A &lt; 10 179. 2- (4-Gasyl-phenyl) -5-isopropoxy-6- (4-methanesulfonyl-epoxy) -primofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.43 (m, 1H); 7.99-7.94 (m, 4H); 7.84 (d, 2H); 7.70 (s, 1H); 7.41 (dd, 2H); 7.27 (s, IH); 4.62 ( m, 1H); 3.28 (s, 3H); 2.85 (d, 3H); 1.24 (d, 6H) \ (M + H) + = 482 A &lt; 10 180. 5 &lt; 2-Chloro-ethoxy) -2- (4-fluoro-phenyl) -6-morpholin plin-4-yl-benzene odorless 3-carboxylic acid quiltamine 1H NMR in CDCb: 7.85-7.80 (m, 2H); 7.32 (s, 1H); 7.20-7.15 (m, 2H); 7.08 (s, 2H); 5.75 (bs, 2H); 4.37-4.33 (m, 2H); 4.94-4.89 (m, 6H); 3.17-3.14 (m, 4H); 2.97 (d, J = 5.4Hz, 3H) (M + H) + = 433 A &gt; 30 192- 88828.doc 200418452 instance number name NMR data Mass Spec HCV pol -BB7 ICs〇〇iM) A = μΜ B = 03 to i5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ replicon (μΜ) 181.6 -(4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine [H NMR in DMSO: 7.80 (dd, J = 8.8, 5.3Hz, 2H); 7.50 ( m, 2H); 7.40 (m, 3H); 7.34 (s, 1H); 7.16 (t, J = 8.8Hz, 2H); 7.05 (s, 1H); 5.75 (br d, J = 4.7Hz, 1H) ; 5.22 (s, 1H); 3.96 (s, 3H); 2.99 (d, J = 4.7Hz, 3H) (M + H) + = 406 A &lt; 10 182.6 6-Amino-2- (4-fluoro-phenyl) -5-acyl-benzo &lt; Amino-3-carboxylic acid amine NMRinDMSO: 10.55 (br s, 1H); 8.40 (d, J = 4.7Hz, 1H); 7.90 (dd, J = 8.8, 5.3Hz, 2H); 7.61 (sT 1H ); 7.34 (t, J = 8.8Hz, 2H); 7.16 (s, 1H); 2.79 (dt J = 4.7Hz, 3H) (M + H) + = 301 B &lt; 30 183. 5,6-bis-benzyloxy-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid formamidine'H NMR in DMSO: 8.29 (m, lH) ; 7.86 (m ^ H); 7.49-7.30 (m, 13H); 7.23 (s, 1H); 5.22 (s, 2H); 5.14 (s, 2H); 2.80 (d, 3H, J = 4.10) (M + H) + = 482 D &lt; 10 184.2 Pefoxy county) -5-isopropoxy-6- (5-trifluoromethyl- [1,2,4] pyridazol-3-yl) -benzofuran-3 -Formamidine carboxylate 1H NMR in CDCi3: 8.17 (s, 1H); 7.91-7.86 (mT 2H); 7.54 (s, 1H); 7.25-7.19 (mT 2H); 5.77 (bs, 1H); 4.81- 4.73 (m, 1H); 3.0 (d, J = 4.8Hz, 3H); 1.44 (d, J = 6.3Hz, 6H) (M + H) + = 464 B &lt; 30 V 185. [2- (4-Gasyl-phenyl) -5_ isopropoxy-3-methylmonthlyl methylbenzo-6-yl] -Hexane 17- 1-carboxylic acid amidine 1H NMR in CDC13: 7.87-7.81 (m, 2H); 7.31 (s, 1H); 7.16 (t, J = 8.35 Hz, 2H); 7.03 (s, 1H); 5.80 (s, 1H); 4.69-4.61 (septet, J = 6.15 Hz, 1H); 4.53 (s, 2H); 3.60-3.57 (m, 4H); 3.12-3.09 (m, 4H); 2.98 (d, J = 5.27 Hz , 3H); 1.38 (d, J = 6.15 Hz, 6H) (M + H) + = 455 C &lt; 10 186. 2- (4-Aminophenyl) -5_ isopropoxy-6-thiomorpholin_4_yl-donganan-2-methylcarboxamidine 3-carboxylic acid * H NMR in CDCl3 : 7.87-7.83 (m, 2H); 7.29 (s, 1H); 7.16 (t, J = 8.35 Hz, 2H); 7.05 (s, 1H); 5.73 (s, 1H); 4.65-4.62 (septet, J = 5.71 Hz, 1H); 3.34 (m, 4H); 2.98 (d, J = 4.84 Hz, 3H); 2.84 (m, 4H); 1.37 (d, J = 6.15Hz, 6H) (M + H) + = 429 A &lt; 1 187. 2- (4-Amino-winteryl) -5_ isopropoxy-3-methylmonthlylmethyl-benzoan-6-carboxylic acid lH NMR in CDC13: 8.41-8.42 (d, 1H, J = 4.69Hz); 7.93-7.97 (m, 2H); 7.80 (s, 1H); 7.35-7.41 (t, 2H, J = 8.79Hz); 7.20 (s, 1H); 4.58- 4.66 (septet, 1H, J = 5.86Hz); 2.83-2.84 (d, 3H, J = 4.69Hz); 1.28-1.30 (d, 6H, J = 5.86Hz) (M-Η) '= 370 C &lt; 10 188. 2- (4-Amino-phenyl) -5_ isopropyllactyl-6- (1-lactyl-thiomorpholine lin- ^ · -yl-)-melfuran carboxylic acids Formamidine 1H NMR in CDC13: 7.84-7.82 (m, 2H); 7.34 (s, 1H); 7,18 (t, J = 8.35, 2H); 7.13 (s, 1H); 5.76 (s, 11H) ; 4.69-4.65 (septet, J = 5.71 Hz, 1H); 3.75-3.68 (m, 2H); 3.39-3.35 (m, 2H); 3.10 (s, 4H); 2.99 (d, J = 4.40 Hzt 3H) ; 1.41 (d, J = 6.15 Hz, 6H) (M + H) + = 445 C &lt; 10 193 88828.doc 200418452: Instance number name NMRdata Mass Spec HCV po! -BB7 IC50O1M) A = B = 03 to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ replicon (μΜ) 189 . {P- (4-Fluoro-phenyl) -5-isopropoxy-3-methylaminomethyl-benzoyl-benzo-6-yl] -methanesulfonyl-aminoacetic acid lH NMR in DMSO: 10.9 (s, iH); 8.43 (m, IH); 7.96 (m, 2H); 7.66 (s, 1H); 7.38 (m, 2H); 7.17 (s, 1H); 4.79 (heptuplet , J = 6.1Hz, 1H); 4.28 (s, 2H); 3.08 (s, 3H); 2.83 (d, J = 4.8 Hz, 3H); 1.35 (d, J = 6.1Hz, 6H) (M + H ) + = 479 B &lt; 1 190. 6- (Cyclobutylmethanesulfonyl-amino) -2- (4-amino-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine Amine 1H NMRinDMSO: 8.43 (in, 1H); 7.93 (dd, J = 3.1 & 6.6Hz, 2H); 7J7 (s, 1H); 7.39 (t, J = 8.8Hz, 2H); 7.15 (s, 1H ); 4.78 (heptuplet, J = 6.1Hz, 1H); 3.2 (m, 1H); 3.02 (s, 3H); 2.83 (d, J = 5.8Hz, 3H); 2.46 (m, 6H); 2.38 (d , 6.1Hz, 6H) (M + H) + = 475 A &lt; 1 191.2. 2- (4-Fluoroyl) -5-isopropoxy-6-j: alkanesulfonyl- (2-morpholin-4-yl-ethyl) -amino group] -Benzofuran-3-carboxylic acid formamidine * H NMR in DMSO: 8.42 (d, J = 4.7Hz, 1H); 7.93 (dd, J = 7.0 & 9.4 Hzt 2H); 7 ^ 8 (s, 1H); 7.38 (t, J = 8.8 Hz, 2H); 7.16 (s, 1H); 4.79 (heptuplet, J = 5.8Hz, 1H); 3.50 (t, J = 4.6Hz, 4H); 3.16 (m, 2H); 3.06 (s, 3H); 2.83 (d, J = 4.6Hz, 3H) (M + H) + = 534 A &lt; 1 192. 2- (4-Gas-private) -5,6-diaxyl-benzofuran carboxylic acid methylamine 1H NMR in DMSO: 8.25 (brs, 1H); 7.83 (m, 2H); 7.28 (m, 2H); 6.96 (d, 1H, J = 2.34 Hz); 6.90 (d, 1H, J = 2.34 Hz); 2.77 (brd, 3H, J = 6.45 Hz) (M + H) + = 302 C &gt; 30 193. 2- (4-Fluoro-phenyl) -5_ isoamyloxy-6- [methyl fluorenyl- (2-fluorenyl-ethyl) -amino &gt; Benzofuran-3-carboxylic acid formamidine NMR in DMSO: 8.48 (m, 1H); 7.95 (dd, J = 5.2 & 8.7 Hz, 2H); 7.53 (s, 1H); 7.39 (t, J = 8.8Hz, 2H); 7.17 (s, 1H); 4.79 (heptuplet, J = 5.9 Hz, 1H); 3.34 (m, 6H); 3.18 (s 3H); 3.05 (s, 3H); 2.83 (d , J = 4.7Hz, 3H); 1.34 (d, J = 5.8Hz, 6H) (M + H) + = 479 A &lt; 1 194. 6-Ethoxy-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.85 (m, 2H); 7.47 (m, 2H); 7.41-7.31 (m, 4H); 7.15 (t, 2H, J = 8.79 Hz); 7.08 (s, 1H); 5.75 (brs, 1H); 5.17 (s, 2H ); 4.55 (m, 1H); 2.99 (d, 3H, J = 5.28 Hz); 1.38 (d, 6H, J = 6.45 Hz) (M + H) + = 434 B wood chip 195.6- (ene Propyl-methanesulfonyl-amino) -2- (4-fluorotai-phenyl) -5-isopropoxy-benzofuran-3-¾formamidine'H NMR in DMSO: 8.41 ( ra, 1H); 7.93 (dd, J = 5.3 &amp; 8.8Hz, 2H); 7.38 (s, 1H); 7.34 (t, J = 8.8Hz, 2H); 5.81 (m, 1H); 5.10 (dd, J = 1.8 &amp; 17 Hz, 1H); 5.02 (dd, J = ll & 10 Hz, 1H); 4.79 (heptuplet, J = 6.4 Hz, 1H); 4.22 (m, 2H); 3.06 (s, 3H ); 2.82 (d, J = 4.7 Hz, 3H) (M + H) + = 461 A &lt; 1 196. 6-Ethyl-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-methanoformamidine 1H NMR in CDC13: 7.88 (s, 1H); 7.86 (m, 2H); 7.41 (s, 1H); 7.18 (m, 2H); 5.77 (brs, 1H); 4.79 (m, 1H); 3.00 (d, J = 4.8Hz, 3H); 2.69 (s, 3H); 1.44 (d, J = 6.0 Hz, 6H) (M + H) + = 370.0 A &lt; 1 194- 88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 IC50 (μΜ) A = s (K5 μΜ B = to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ Copy (ΜΜ) 197.2 2- (4-Gasyl-benzyl) -5-isopropoxy-6-methanesulfonylamino, benzobenzo-3-carboxylic acid isopropylamine * H NMR in CDC13: 7.85-7.80 (m, 2H); 7.74 (s, 1H); 7.43 (s, 1H); 7.19 a J = 8.79 Hz, 2H); 6.95 (s, 1H); 5.53-5.50 (m, IH) ; 4.78-4.70 (septet, J = 6.15 Hz, 1H); 4.38-4.26 (septet, J = 7.03 Hz, 1H); 2.95 (s, 3H); 1.40 (d, J = 5.44 Hz, 6H); 1.18 ( d, J = 6.49 Hz, 6H) (M + H) + = 449 C &lt; 10 198.2. 2- (4-Gasyl-phenyl) -5_isopropoxy-6- (5-methyl_ [1,2,4bamboobiphenyl-3-yl) -benzo Furan-3-carboxylic acid formamidine * HNMR inCDCl3: 8.07 (s, 1H); 7.92-7.87 (m, 1H); 7.49 (s, 1H); 7.23-7.17 (m, 2H); 5.80 (bs, 1H ); 4.70-4.64 (s, 1H); 3.00 (d, J = 4.8Hz, 3H); 2.65 (s, 3H); 1.41 (d, J = 6.3Hz, 6H) (M + H) + = 410 A &lt; 1 199. 2- (4-Fluoro-phenyl) &gt; 5-isopropoxy-6-methanesulfonylamino-benzopyran-3-carboxylic acid cyclopropylamidine 1H NMR in CDC13 : 7.79-7.74 (m, 2H); 7.73 (s, 1H); 7.47 (s, 1H); 7.20 (T, J = 8.79Hz, 2H); 6.95 (s, 1H); 5.8 (s, 1H); 4.78-4.70 (septet, J ^ .lSHz, 1H); 2.95 (s, 3H); 2.90-2.86 (m, 1H); 1.40 (d, J = 6.15Hz, 6H); 0.89-0.82 (m, 2H) ; 0.53-0.48 (m, 2H) (M + H) + = 447 A &lt; 1 200. 2- (4-Fluoro-phenyl) -5-isopropoxy-6-methanesulfonylamino-benzofuran-3-carboxylic acid acetamidine 1H NMR in CDCI3: 7.85-7.79 (m, 2H); 7.74 (s, 1H); 7.44 (s, 1H); 7.19 (t, J = 8.35Hz, 2H); 6.95 (s, 1H); 5.7 (s, 1H); 4.80 -4.68 (septet, J = 6.15Hz, 1H); 3.52-3.43 (m; 2H); 2.95 (s, 3H); 1.39 (d, J = 5.71, 6H); 1.17 (T, J = 7.47, 3H) (M + H) + = 435 A &lt; 1 201. 2- (4-Dentyl-phenyl) -5- (2-methyl-pyrazol-4-ylmethoxy) -6-morpholine-4-yl-benzop-furan -3-Formamidine carboxylate 1H NMR in CDCi3: 7.89 (m, 2H); 7.41 (s, 1H); 7.16 (m, 3H); 7.10 (s? 1H); 5.78 (brs, 1H); 5.25 ( s, 2H); 3.90 (m, 4H); 3.16 (m, 4H); 3.00 (d, 3H, J = 4.69 Hz); 2.74 (s, 3H) (M + H) + = 482 A &lt; 1 202. 2_ (4-Gasyl-phenyl) _6- (1- # stemyl-1-methyl-ethyl) -5-isopropoxy-benzofuran-3-quinic acid formamidine Amine 1H NMR in CDCI3: 7.84 (m, 2H); 7.49 (s, 1H); 7.39 (s, 1H); 7.19 (m, 2H); 5.73 (brs, 1H); 3.56 (m, 1H); 2.99 ( d, J = 4.8 Hz, 3H); 1.38 (d, J = 6.1Hz, 6H) (M + H) + = 386.1 A &lt; 1 203. 5- [5- (3,5-Difluorenyl-isopurazol-4-yl)-[1,2,4] fluorenediazole-3-ylmethoxy)]-2- (4-Fluoro-phenyl) -6-morphol # -4-yl-phenylsulfan-3-carboxylic acid formamidine NMR in CDCI3: 7.86 (m, 2H); 7.52 (s, 1H) ; 7.18 (t, 2H, J = 8.79 Hz); 7.12 (s, 1H); 5.75 (brs, 1H); 5.36 (s, 2H); 3.92 (m, 4H); 3.19 (in, 4H); 2.98 ( d, 3H, J = 4.69 Hz); 2.81 (s, 3H); 2.59 (s, 3H) (M + Hwide = 548 B &lt; 10 195-88828.doc 200418452 Example No. Name NMR data Mass Spec HCV pol -BB7 ic50 〇iM) A = μΜ B = 03 to ^ 5.0 μΜ C = 5.0 to &lt; 30 D = &gt; 30 μΜ replicon (μΜ) 204. 5- (5-Third-butyl- [1,2,4] humidin-3-ylmethoxy) -2- (4 -Fluoro-phenyl-> 6-morpholin · 4-yl-benzoanan-3-methylacetamidine * H NMR in DMSO: 8.28 (br 叽 1H); 7.90 (m, 2H); 7.33 (t, 2H, J = 8.79 Hz); 7.24 (s, 1H); 7.22 (s, 1H); 5.28 (s, 2H); 3.74 (m, 4H); 3.06 (m, 4H); 2.81 (d , 3H, J = 4.69); 1.40 (s, 9H) (M + H) + = 509 A &lt; 1 205.2 2- (4-fluoro-phenyl) -5-isopropoxy each [1,2,4] indoxazol-3-yl-benzene # furan-3-carboxylic acid formamide 1HNMRinCDCl3 : 8.75 (s, 1H); 8.14 (s, 1H); 7.93-7.88 (m, 2H); 7.53 (s, 1H); 7.24-7.17 (m, 2H); 5.78 (bs, 1H); 4.70 ^. 68 (m, 1H); 3.0 (d, J = 4.8Hz, 3H); 1.42 (d, J = 5.7Hz, 6H) (M + H) + = 396 A &lt; 1 206. 5- (5-Chloro- [1,2, examidine; methoxy) -2- (4-fluoro-phenyl) -6-morpholine-4-yl -Benzofuran-3-carboxylic acid methylamine 1H NMR in DMSO: 8.38 (brdr 1H, J = 4.69 Hz); 7.95 (m, 2H); 7.76 (s, 1H); 7.58 (s, 1H); 7.38 (t, 2H, J = 8.79 Hz); 4.75 (s, 2H); 3.52 (m, 4H); 2.98 (in, 4H); 2.80 (d, 3H, J = 4.69 Hz) (M + H) + = 504 B &lt; 1 207.2 2- (4-Amino-phenyl) -6-? Bead-4-yl ^ -5-(5 -p-tolyl- [1,3,4] fluorenediazole-2ylmethoxy) -benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO : 8.31 (brd, 1H, J = 4.69 Hz); 7.90 (m, 4H); 7.43 (d, 2H, J = 7.62 Hz); 7.34 (m, 3H); 7.25 (s, 1H); 5.48 (s, 2H); 3.69 (m, 4H); 3.02 (m, 4H); 2.81 (d, 3H, J = 4.69 Hz); 2.40 (s, 3H) (M + H) + = 543 C &lt; 10 208. 2- (4-Gasyl-phenyl) -6- # yl-5-methoxy-benzofuran-3-carboxylic acid formamidine'H NMR in DMSO: 9.33 (s, 1H) ; 8.28 (d, J = 4.4HzT 1H); 7.85 (dd, J = 8.8, 5.3Hz, 2H); 7.30 (t, J = 8.8Hz, 2H); 7.06 (s, 1H); 7.02 (s, 1H ); 3.81 (s, 3H); 2.80 (d, J = 4.4Hzt 3H) (M + H) + = 316 B &lt; 30 209.2 2- (4-Amino-phenyl) -5- (1-methyl-1H-tetrazol-5-ylmethoxy) glypholine-4-yl-benzoxan -3-carboxylic acid formamidine 1H NMR in DMSO: 8.31 (d, J = 4.4Hz, 1H); 7.88 (dd, J = 8.8, 5.3Hz, 2H); 7.36 (t, J = 8.8Hz, 2H) ; 7.33 (s, lH); 7.25 (s, lH); 5.54 (s, 2H); 4.14 (s, 3H); 3.68 (t, J = 4.4Hz, 4H); 2.98 (t, J = 4.4Hz, 4H); 2.81 (d, J = 4.4Hz, 3H)) (M + H) + = 467 B &lt; 10 210. 2- (4-Fluoro-phenyl) -5- (3-methoxy-benzyloxy) -6-morpholin-4-yl-benzofuran-3-carboxylic acid Lamine 1H NMR in DMSO: 8.30 (d, J = 4.4Hz, 1H); 7.88 (dd, J = 8.8, 5.3Hz, 2H); 7.32 (ra, 3H); 7.22 (s, 1H); 7.19 (s , 1H); 7.07 (m, 2H); 6.87 (m, 1H); 5.13 (s, 2H); 3.76 (s, 3H); 3.73 (brs, 4H); 3.05 (brs, 4H); 2.81 (d, J = 4.4Hz, 3H) (M + H) * = 491 A &lt; 1 196- 88828.doc 200418452 Example 5 Tiger name NMRdata Mass Spec HCY pol -BB7 IC50〇tM) A = μ, Μ B = 03 to ^ 5.0 C = 5.0 to ^ 30 μΜ. D = &gt; 30 / iM replicon (μM) 211.2 2- (4-fluoro-phenyl) -5methoxy-6- (1-methyl-1H-tetramethyl-5-ylmethoxy) -benzo Furan-3-carboxylic acid formamidine 1H NMR in DMSO: 8.32 (d, J = 4.4Hz, 1H); 7.87 (dd, J = 8.3, 5.7Hz, 2H); 7.55 (s, 1H); 7.33 (t , J = 8.8Hz, 2H); 7.11 (s, 1H); 5.56 (s, 2H); 4.15 (s, 3H); 3.81 (s, 3H); 2.80 (d, J = 4.4Hz, 3Η »(M + H) + = 412 A &lt; 1 212.2 2- (4-Gasylphenyl) -5- [l- (4-fluoro-phenyl) -ethoxy] -6-morpho 4 Tomb of winter wood-benzopyran- 3-carboxamidine 1H NMR in CDC13: 7.86 (dd, J = 8.8, 5.3Hz, 2H); 7.38 (dd, J = 8.8, 5.3Hz, 2H); 7.12 (t, J = 8.8Hz, 2H ); 7.03 (t, J = 8.8Hz, 2H); 5.62 (d, J = 4.9Hz, 1H); 5.37 (q, J = 6.1Hz, 1H); 3.88 (m, 4H); 3.14 (m, 4H ); 2.92 (d, J = 4.9 Hz, 3H); 1.65 (d, J = 6.1Hz, 3H) (M + H) + = 493 A &lt; 1 213. (4-cyano-fluorenylmethoxy) -2- (decafluoro ^ &gt; phenyl) -6-morpholin-4-yl-benzofuran-3-carboxylic acid formamidine Amine'H NMR in DMSO: 8.28 (dr J = 4.4Hz, 1H); 7.88 (m, 4H); 7.70 (d, J = 8.0Hz, 2H); 7.33 (t, J = 8.8Hz, 2H); 7.24 (s, 1H); 7.20 (s, lH); 5.27 (s, lH); 3.74 (m, 4H); 3.04 (m, 4H); 2.81 (d, J = 4.4Hz, 3H) (M + H) + = 486 B &lt; 10 214.1 1- (4-fluoro-phenyl) -5- [5- (4-methoxy-phenyl)-[1,2,4] pyridine-3-ylmethoxy] -6-morpholine-4-yl-benzoanan-3 -carboxylic acid formamidine 1H NMR in DMSO: 8.35 (d, J = 4.4Hz, 1H); 7.92 (m, 4H); 7.37 (m , 3H); 7.25 (s, 1H); 7.17 (d, J = 8.8Hz, 2H); 5.47 (s, 2H); 3.84 (s, 3H); 3.69 (s, 4H); 3.02 (s, 4H) ; 2.80 (d, J = 4.4Hz, 3H) (M + H) + = 559 B &lt; 1 215.2 2- (4-Amino-phenyl) -6-morpholin-4-yl-5- (2-oxy-propoxy) -benzofuran-3-carboxylic acid sulfonamide lH NMR in DMSO: 8.26 (d, J = 4.4Hz, 1H); 7.87 (dd, J = 8.3, 5.7 HzT 2H); 7.32 (t, J = 8.8Hz, 2H); 7.20 (s, lH); 7.00 (s, lH); 4.80 (s, 2H); 3.76 (t, J = 4.7Hz, 4H); 3.06 (t, J = 4.7Hz, 4H); 2.80 (d, J = 4.8Hz, 3H); 2.21 (s, 3H) (M + H) + = 427 B &lt; 10 216. 5- (1-fluorenyl-1H-taste group oligomethoxy) -2- (4-fluoro-phenyl) -fluorene_morpholin p-4 Methyl-3-carboxamidine * H NMR in DMSO: 8.26 (brd, 1H, J = 4.69 Hz); 7.90 (m, 2H); 7.35-7.16 (m, 10H); 6.94 (m, 1H) ; 5.37 (s, 2H); 5.17 (s, 2H); 3.66 (m, 4H); 2.95 (m, 4H); 2.82 (d, 3H, J = 4.69 Hz) (M + H) + = 541 A &lt; 1 217. 5- (3,5-Dimethyl-isoinzolylmethoxy) _2- (4-Gasyl-tolyl) -6-morpholine 1H NMR of sulfan-3-carboxylic acid formamidine in DMSO: 8.30 (d, 1H, J = 4.39); 7.82 (m, 2H); 7.33 (t, 2H, J = 8.79); 7.20 (m, 2H) ; 5.00 (s, 2M); 3.69 (m, 4H); 2.98 (m, 4H); 2.82 (d, 3H, J = 4.39 Hz); 2.39 (s, 3H); 2.26 (s, 3H) (M + H) + = 480 B &lt; 10 197- 88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 IC50 (μΜ) A = μΜ B = 0 * 5 to s5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ Copy 〇iM) 218. 2- (4-Fluoro-phenyl) -5- (5-methyl-isoxazol-3-ylmethoxyfurin-4-yl-benzofuran-3- Formamidine carboxylate'H NMR in DMSO: 8.28 (brd, 1H, J = 4? 39 Hz); 7.90 (m, 2H); 7.33 (t, 2HT J = 8.79); 7.22 (m, 2H); 6.34 (s, 1H); 5.18 (s, 2H); 3.73 (m, 4H); 3.03 (m, 4H); 2.82 (d, 3H, J = 4.39 Hz); 2.42 (s, 3H) (M + H) + = 466 A &lt; 1 219. 2- (4-Gasyl-phenyl) -5-isopropoxy-6-0 sulfan-2-yl-benzene # crean-3-chitoic acid formamidine 1H NMR in DMSO : 8.50 (s, lH); 8.46-8.47 (d, J = 4.69Hz, 1H); 7.97- 8.02 (m, 3H); 7.80-7.81 (d, J = 3.5Hz, 1H); 7.38-7.44 (ζ J = 8.79Hz, 2H); 7.36 (s, 1H); 4.97- 5.06 (septet, J = 6,45Hz, 1H); 2.84-2.86 (d, J = 5.27Hz, 3H); 1.47-1.49 (d, J = 5.86Hz, 6H) (M + H) + = 410.9 A &lt; 10 220. 2- (4-Amino-phenyl) -5_isopropoxy-6- (1fluorene-pyrrole · 2-yl) -benzofuran-3-carboxylic acid methyl S & biNMRNMRCDCla: 7.90-7.86 (m, 2H); 7.77 (s, 1H); 7.43 (s, lH); 7.26-7.17 (m, 3H); 6.90 (s, 1H); 6.67 (s, 1H); 631 (s, 1H); 5.8 (s, 1H, br); 4.78 (m, 1H); 3.0 (d, 3H); 1.46 (d, 6H) (M + H) + = 393 A &lt; 10 221. fluorene- (4-fluoro-phenyl) -6- (isopropyl-methanesulfonyl-amino) -5-methoxy-benzofuran-3-carboxylic acid formamidine lH NMR in DMSO: 8.44 (ιη, ΙΗ); 7.94 (dd, 2H, J = 5.28, 8.8Hz); 7.556 (s, 1H); 7.39 (t, J = 8.8Hz, 2H); 7.20 (s, lH ); 4.27 (heptuplet, J = 6.4Hz, lH); 3.86 (s, 3H); 3.09 (s, 3H); 2.84 (d, J = 4.7Hz, 3H); 1.21 (d, J = 7.lHzf 3H ); 1.01 (d, J = 6.5Hz, 3H) (M + H) + = 435 A &lt; 1 222.2 2- (4-fluoro-phenyl) -6- (1 -¾-yl-ethyl) -5_ isopropoxy-benzo-4-an-3-carboxylic acid formamidine 1H NMR in CDCb : 7.87-7.83 (m, 2H); 7.50 (s, 1H); 734 (s, 1H); 7.21-7.16 (m, 2H); 5.72 (bs, lH); 5.19-5.13 (m, 1H); 4.78 -4.69 (m, 1H); 2.98 (d, J = 5.1Hz, 3H); 2.78 (d, J = 5.1Hz, 1H); 1.55 (d, J = 6.6Hz, 3H); 1.41 (dd, J = 3.6Hz, 6,0Hz, 6H) (M + H) + = 372 A &lt; 1 223. 2- (4-Gasyl-phenyl) -5_ isopropoxy-6-morpho-4 wood-4 · -yl-yl-phenyl nonanhydro-3-carboxylic acid formamidine 1H NMR in CDC13: 7.89-7.84 (m, 2H); 7.57 (s, 1H); 7.31 (s, 1H); 7.20-7.16 (m, 2H); 5.74 (bs, 1H); 4.64-4.60 (m, 1H ); 3.75-3.72 (m, 4H); 3.64 (s, 2H); 2.98 (d, J = 5.1Hz, 3H); 2.55-2.52 (m, 4H); 1.36 (d, J = 6.3Hz, 3H) (M + H) + = 427 C &lt; 10 224. 2- (4-Gas-phenyl) -6- via i-5-isopropoxy-benzofuran-3-¾formamidine IHNMRCDCI3: 7.87-7.83 (in, 2H ); 7.43 (s, 1H); 7.35 (s, 1H); 7.21-7.15 (m, 2H); 5.73 (bs, 1H „4.76-4.68 (m, 3H); 2.98 (d, J = 5.1Hz, 3H ); 2.52-2.50 (m, 1H); 1.40 (d, J = 6.0Hz, 6H) (M + H) + = 358 A &lt; 10 225. _ 2- (4-Fluoro-phenyl) -5-C3H-imidazol-4-ylmethoxy) -6-morpholin-4-yl-benzofuran-3carboxylic acid Lamine 1H NMR in DMSO: '8.27 (brd, 1H, J = 4.39 Hz); 7.89 (m, 2H); 7.33 (t, 2H, J = 8.79 Hz); 7.28 (s, IH); 7.19 (s, 1H); 7.15 (brs, 1H); 6.90 (brs, 1H); 5.10 (s, 2H); 3.69 (ra, 4H); 3.02 (m, 4H); 2.83 (d, 3H, J = 4.39 Hz) ( M + H) + = 451 A &lt; 10 198- 88828.doc 200418452 Example number name NMR data Mass Spec HCV pol -BB7 IC5〇 (/ iM) A = ^: 0.5 B = 03 to ^ 5.0 μΜ C = 5.0 to ^ 30 D = &gt; 30 μΜ Replicon (μM) 226. 2- (4-Fluoro-phenyl) -5- (2-methyl | yl-ethoxy) -6-morpholin-4-yl-benzofuran; carboxylic acid methyl Amidine 1H NMR in DMSO: 8.28 (d, 1H, J = 4.69 Hz); 7.89 (m, 2H); 7.32 (t, 2H, J = 8.79 Hz); 7.16 (s, 1H); 7.06 (s, 1H ); 4.13 (in, 2H); 3.72 (ra, 6H); 3.33 (s, 3H); 3.04 (m, 4H); 2.81 (d, 3H, J = 4.69 Hz) (M + H) + = 429 A &lt; 1 227. 2- (4-Gas-Dongyl) -5_-Isopropoxy-6-thiazol-5-yl-benzoic acid 3 -Metylamine metabolite * H NMR in DMSO: 9.07 (s, 1H); 8.53 (s, 1H); 8.41-8.42 (d, J = 4.69 Hzt 1H); 8.19 (s, 1H); 7.93-7.98 (m, 2H); 7.36-7.42 (t, J = 8.79 Hz, 2H); 7.28 (s, 1H); 4.82-4.90 (septet, J = 5.86Hz, 1H); 2.84-2.86 (d, J = 4.69Hz, 3H); 1.38-1.40 (d, J = 5.86Hz, 6H) (M + H) + = 411 A &lt; 1 228. 5- (4-chloro-1-methyl-1H-pyridin-3-ylmethoxy) -2- (4-airyl-benzene; -6-morpho 57 lin-4 -Methyl-benzofuran-3-carboxylic acid formamidine * Η NMR in COCh: 7.93 (mt 2H); 7.47 (s, 1H); 7.39 (s, 1H); 7.17 (t, 2H, J = 8.79 Hz ); 7.08 (s, 1H); 5.86 (brs, 1H); 5.17 (s, 2H); 3.89 (m, 7H); 3.16 (m, 4H); 3.04 (d, 3H, J = 4.84 Hz) (M + H) + = 499 A &lt; 1 229. 5-fluorenyl-methyl-methoxy) te (terfluorofluoro-phenyl) -6-morpholin-4-yl-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.90 (m, 2H); 7.52 (s, 1H); 7.17 (m, 3H); 5.84 (brs.lH); 5.17 (q, 1H, J = 7.03 Hz); 3.89 (t, 4H, J = 4.69 Hz); 3.20 (ra, 2H); 3.00 (m, 5H); 1.80 (d, 3H, J = 6.45 Hz) (M + H) + = 424 A &lt; 10 230. 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (2H-pyridin-3-yl) -phenylphosphofuran-3-carboxylic acid formamide 1H NMR in CDC13: 7.87 (m, 2H); 7.80 (s, 1H); 7.62 (d, J = 2.4Hz, 1H); 7.49 (s, 1H); 7.24 (m, 2H); 6.69 (d, J = 2.4 Hz, 1H); 5.77 (brs, 1H); 4.83 (mt 1H); 2.99 (d, J = 5.4Hz, 3H); 1.48 (d, J = 5.7Hz, 6H) (M + H) + = 394.1 A &lt; 10 231. 2- (4-Amino-epoxy) -5_isopropoxy-6- (2-methyl-2H-pyrazol-3-yl) -benzofuran lH NMR in CDC13: 7.88 (m, 2H); 7.52 (d, J = 1.8 Hz, 1H); 7.45 (s, 1H); 7.39 (s, 1H); 7.22 (m, 2H); 6.26 (d, J = 1.8Hz, 1H); 5.87 (brs, 1H); 4.48 (m, 1H); 3.76 (s, 3H); 3.00 (d, J = 4.8Hz, 3H); 1.23 (d, J = 5.7Hz, 6H ) (M + H) + = 408.1 A &lt; 1 232. 2- (4-Gasyl-benzyl) -5-isopropoxy-6- (1-methyl-1H-pyrazolyl) -benzofuran-3-metanoic acid formamidine Amine 1H NMR in CDC13: 8.10 (s, 1H); 7.87 (m, 2H); 7.37 (d, J = 2.1 Hz, 1H); 7.36 (s, 1H); 7.18 (m, 2H); 6.91 (d, J = 2.1Hz, 1H); 5.82 (brs, 1H); 4.67 (m, 1H); 3.96 (s, 3H); 2.99 (d, J = 4.8Hz, 3H); 1.39 (d, J = 6.0Hz, 6H) 4 (M + H) + = 408.1 B &lt; 10 233. 2- (4-Gasyl-benzyl) -5-isopropoxy-6- (3-methyl-isohumant-5-yl) -benzoconan-3-¾ acid Selenium 1H NMR in DMSO: 8.42 (dt J = 4.8Hz, 1H); 8.03 (s, 1H); 7.95 (dd, J = 5.7, 5.2, 8.8Hz, 2H); 7.37 (apparent triplet, J = 8.8 Hz, 2H); 7.28 (s, 1H); 6.79 (s, 1H); 4.84 (m, 1H); 2.83 (d, J = 4.4Hz, 3H); 2.30 (s, 3H); 1.38 (d, J = 5.7Hz, 6H) (M + H) + = 409.21 B &lt; 30 199- 88828.doc 200418452 Instance data name NMR data Mass Spec HCV pol -BB7 ICse (/ iM) A = μΜ B = to ^ 5.0 μΜ C = 5.0 to i30 / iM D = &gt; 30 aM replicon_ ) 234. 6-[(5-Mutyl- [1,2,4] acetodiazol-3-ylmethyl) -methanesulfonyl-amino group> 2- (4-fluoro-phenyl group ) -5-Isoyloxy-5-yl-benzofran-3-carboxylic acid methylamine'H NMR in CDC13: 7.81 (m, 2H); 7.69 (s, 1H); 7.40 (s, 1H); 7.19 (t, 2H, J = 8.79 Hz); 5.69 (brs, 1H); 5.09 (brs, 2H); 4.78 (m, 1H); 3.09 (s, 3H); 2.95 (d, 3H, J = 4.84 Hz); 1.42 (d, 6H, J = 6.15 Hz) (M + H) + = 553 A &lt; 10 235. 6- (3,5-dimethyl-isodiamidinoamino) -2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-gui Formamidine acid 1H NMR in CDC13: 7.79-7.74 (m, 2H); 7.32 (s, 1H); 7.14 (t, J = 8.79 Hz, 2H); 6.43 (s, 1H); 5.73 (s, 1H) ; 5.50 (s, 1H); 4.73-4.67 (septet, J = 6.15 Hz, 1H); 2.97 (d, J = 5.27, 3H); 2.32 (s, 3H); 2.13 (s, 3H); 1.43 (d , J = 6.15 Hz, 6H) (M + H) + = 438 C &gt; 30 236. 2- (4-fluoro-phenyl) -5-methoxy-6-t7 Benzofuran-3-carboxylic acid formamidine * H NMR in DMSO: 8.75 (s, 1H); 8.55 (s, 1H, br); 8.43 (d, 1H); 7.98-7.93 (m, 2H); 7.68 (s, IH); 7.49-7.35 (ra, 3H); 7.26 (s, 1H); 3.84 (s, 3H); 2.84 (dT 3H) (M + H) + = 377 A &lt; 1 237.6 6-Dimethylaminomethyl-2- (4-fluoro-phenyl) -5-isopropoxy-5-yl-benzofuran-3-¾formamidine lH NMR in CDC13: 7.89-7.84 (m, 2H); 7.54 (s, iH); 7.31 (s, 1H); 7.21-7.15 (m, 2H); 5.55 (bs, 1H); 4.66-4.60 (m, 1H); 3.64 (S &gt;2H); 2.99 (d, J = 5.1Hz, 3H); 2.34 (s, 6H); 1.37 (d, J = 5.7Hz, 6H) (M + H) + = 385 C &lt; 30 238. 2- (4-Fluoro-phenyl) -6- (1-hydroxy-2-methyl-propyl) -5-isopropoxy-benzofuran-3-carbamate Amine 1H NMR ia CDC13: 7.89-7.84 (m, 2H); 7.43 (s, 1H); 7.32 (s, 1H); 7.22-7.16 (m, 2H); 5.76 (bs; 1H); 4.74-4.60 (m , 2H); 2.99 (d, J = 4.8Hz, 3H); 2.61 (d, J = 6.5Hz, 1H); 2.14-2.09 (m, 1H); 1.40 (dd, J = 11.7, 6.0Hz, 6H) ; 1.04 (d, J = 6.6Hz, 3H); 0.85 (d, J = 6.9Hz, 3H) (M + H) &quot; = 400 A &lt; 1 239. 2- (4-Fluoro-phenyl) -5_ isopropoxy-6- (1βpyrazolidyl) -benzofuran-3-carboxylic acid formamidine 1H NMR in CDCb: 8.10 (s, 2H); 7.87 (m, 2H); 7.65 (s, 1H); 7.39 (s, 2H); 7.18 (m, 2H); 5.79 (brs, 1H); 4.72 (m, 1H); 3.00 ( d, J = 5.1Hz, 3H); 1.41 (d, J = 6.0 Hz, 6H) (M + H) + = 394.1 C &lt; 10 240. 2- (4-Gas-Winter) -6- [methanesulfonyl- (2-methoxy-ethyl) -amino] -5-methoxy-benzoanan Formamidine-3-chitoate 1H NMR ia DMSO: 8.49 (m, IH); 8.00 (dd, J = 5.1 & 8.8 Hz, 2H); 7.63 (s, 1H); 7.42 (t, J = 8.8 Hz , 2H); 7.26 (s, 1H); 3.97 (s, 3H); 3.78 (m, 1H); 3.35 (m, 6H); 3.25 (s, 3H); 3.11 (s, 3H); 2.90 (d, J = 3.3 Hz, 3H) (Μ + ΗΓ = 451.1 A &lt; 1 241.6 6- (3-Cyclopropyl-isohumazol-5-yl) -2- (4-fluorophenyl) -5-isopropoxy-benzofuran formamide lH NMR ia DMSO: 8.44 (broad quartet, J = 4.4Hz, 1H); 8.02 (s, 1H); 7.96 (dd, J = 5.7, 5.3, 9.2 Hz, 2H); 7.39 (apparent triplet; J = 8.8, 9.2 Hz, 2H); 7.29 (s, 1H); 6.64 (s, lH); 4.84 (m, IH); 2.85 (d, J = 4.8Hz, 3H); 2.08 (m, 1H); 1.39 (d, J = 5.7Hz, 6H); 1.05 (m, 2H); 0.84 (m, 2H) (M + H) if = 435 B &lt; 10 -200- 88828.doc 200418452 Example number name NMR data Mass Spec HCV po! -BB7 IC50 〇iM) A = / iM B = to ^ 5.0 / iM C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ Replicon (μΜ) 242.2 2- (4-Amino-phenyl) -5_-isopropoxy-6- (3-methoxymethyl-isofluorene-5-yl) -benzofuran-3-le Formamidine acid 1H NMR in DMSO: 8.45 (broad quartet, J = 4.8Hz, 1H); 8.10 (s, 1H); 7.97 (dd, J = 5.7, 8.8Hz, 2H); 7.40 (t, J = 8.8 Hz7 2H); 7.32 (s, 1H); 6.92 (s, 1H); 4.88 (quintet, 1H); 4.55 (sT 2H); 3.29 (s, 3H); 2.85 (d, J = 4.4Hz, 3H); 1.40 (d, J = 6.1Hz, 6H) (M + H) + = 439 B 30 243. 2- (4-fluoro-phenyl) -6-methanesulfonylamino-benzofuran-3- Formamidine mesitamine 1H NMR m DMSO: 8.37 (m, 1H); 7.93 (ddt J = 5.7 &amp; 8.8Hz, 2H); 7.53 (d, J = 8.8Hz, 1H); 7.45 (d, J = 1.7 Hz, 1H); 736 a J = 8.8Hz, 2H); 7.14 (dd, J = 1.7 & 8.8Hz, 1H); 4.17 (bst 1H); 2.96 (s, 3H); 2.82 (d, Ι = 4.8 Ηζ, 3H) (M + H) + = 363 B &lt; 10 244.4 2- (4-Amino-phenyl) -6- (lH-imidazol-2-yl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 10.70 (s, 1H); 8.43 (s, 1H); 7.86-7.81 (m, 2H); 7.48 (s, 1H); 7.21-7.15 (m, 3H); 7.12 (s, 1H); 5.96 ( s, 1H); 4.91-4.83 (m, 1H); 2.99 (d, J = 4.8Hz, 3H); 1.49 (d, J = 6.0Hz, 6H) (M + H) + = 394 A &lt; 1 245.6- (2,5-dimethyl-2H-pyrazol-3-yl) 2- (4-fluoroyl-phenyl) -5-isopropoxy-benzopyran- 3-Hydroxyformamidine 1H NMR in CDC13: 8.08 (s, 1H); 7.88 (m, 2H); 7.35 (s, 1H); 7.19 (m, 2H); 6.67 (s, 1H); 5.78 (brs , 1H); 4.67 (m, 1H); 3.84 (s, 3H); 3.00 (d, J = 4.8Hz, 3H); 2.33 (s, 3H); 1.39 (d, J = 6.0Hz, 6H) (M + H) + = 422.1 B &lt; 10 246. 6- (3,5-Dimethyl-1H-P than Jun-4-yl) -2- (4-fluoroyl-dongyl) -5-hexylpropoxy-benzofuran- 3-Hydroxymethamamine 1H NMR ia CDC13: 7.91 (ra, 2H); 7.40 (s, 1H); 7.28 (s, lH); 7.18 (ra, 2H); 5.80 (brs, 1H); 4.36 (m , iH); 3.00 (d, J = 5.4Hz, 3H); 2.21 (s, 6H); 1.20 (d, J = 5.7 Hz, 6H) (M + H) + = 422.1 A &lt; 1 247.4 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (5-methyl-2H-pyrazol-3-yl) -benzofuran-3- double acid Formamidine 1H NMR in CDCl3: 7.87 (in, 2H); 7.75 (s, 1H); 7.47 (s, 1H); 7.20 (m, 2H); 6.47 (s, 1H); 5.75 (brs, 1H); 4.82 (m, 1H); 2.99 (d, J = 5.1Hz, 3H); 2.36 (s, 3H); 1.46 (d, J = 6.0Hz, 6H) (M + H) + = 408.1 B &lt; 10 248. 6- (1,5-Dimethyl-1H-pyrazol-3-yl) -2- (4-fluoroyl-phenyl) -5-isopropoxy-benzofuran Formamidine acid 1H NMR in CDC13: 7.88 (m, 2H); 7.44 (s, 1H); 7.38 (s, 1H); 7.20 (m, 2H); 6.04 (s, 1H); 5.68 (brs, 1H) ; 4.44 (m, 1H); 3.68 (s, 3H); 3.00 (dt J = 4.8Hz, 3H); 2.32 (s, 3H); 1.25 (d, J = 6.3Hz, 6H) (M + H) + = 422.1 B &lt; 10 249.2 2- (4-Fluoro-phenyl) -5-isopropoxy-6-[(methanesulfonyl-methyl-amino) -methyl] -benzofuran-3- Formamidine carboxylate 1HNMR ia CDC13: 1 7.86-7.83 (m, 2H); 7.58 (s, 1H); 7.37 (s, IH); 7.22-7.17 (m, 2H); 5.75 (s, 1H); 4.74 -4.66 (m, 1H); 4.47 (s, 2H); 2.99 (d, J = 5.lHz, 3H); 2.87 (d, J = 5.7Hz, 6H); 1.39 (d, J = 6.3Hz, 6H ) (M + H) + = 449 A &lt; 10 201-88828.doc 200418452 Example No. NMR data Mass Spec HCV pol -BB7 IC5〇 (μΜ) A = / iM B = 03 to 5: 5.0 / iM C = 5.0 to &lt; 30 / iM D = &gt; 30 / iM replicon (μM) 250. 2- (4-amino-phenyl) -5- (2-quinyl-2-methyl-propoxy) -6 -Morphine-4-Tomb-Benzofuran-3-carboxylic acid formamide. LHNMRinCDCl3: 7.87 (dd, J = 8.8 & 5.3 Hz, 2H); 7.40 (s, 1H); 7.20 (U = 8.8 Hz, 2H); 7.12 (s, 1H); 5.80 (brs, 1H); 3.98 (s, 2H); 3.92 (t, J = 4.4 Hz, 4H); 3.10 (t, J = 4.4 Hz, 4H ); 2.96 (d, J = 4.4 Hz, 3H); 1.35 (s, 6H) (M + H) + = 443 B &lt; 10 251. -5- (2-Ethyl-2-methyl-butoxy) -6-morphol 51 Lin-4-yl-benzofuran carboxylic acid formamide 1HNMRinCDCi3: 7.86 (dd, J = 8.8, 53 Hz, 2H); 7.40 (s, 2H); 7.22 (t, J = 8.8 Hz, 2H); 7.12 (s, 1H); 5.90 (brs, 1H); 4.00 (m, 2H); 3.95 (t, J = 4.4 Hz, 4H); 3.10 (t, J = 4.4 Hz, 4H); 2.95 (dt J = 4.4 Hz, 3H); 2.30 (brs, 1H); 1.70 (in, 2H); 1.24 (s, 3H); 0.95 (t, J = 7.0Hz, 3H) (M + H) + = 457 B &lt; 10 252. _ 2- (4-Fluoro-phenyl) -5- (2-hydroxy-propoxy) -6-morpholine? 4-L-yl-rate-pyranfuran-3- Formamidine carboxylate 1H NMR in DMSO: 8.28 (d, J = 4.4 Hz, 1H); 7.88 (dd, J-5.3 & 8.8 Hz, 2H); 7.32 (t, J = 8.8 Hz, 2H); 7.16 (s, 1H); 7.06 (s, 1H); 4.82 (d, J = 4.7 Hz, 1H); 4.00-3.90 (m, 3H); 3.74 (brs, 4H); 3.04 (brs, 4H); 2.81 ( d, J = 4.0 Hz, 3H); 1.19 (d, J = 4.7 Hz, 3H) (M + H) + = 429 B &lt; 10 253. 2- (4-Fluoro-phenyl) _6-[(2_year-old to propyl) -methanesulfonyl-amino] -5-isopropoxy-benzofuran- 3-carboxylic acid methylamine 1H NMR ia DMSO: 8.40 (dt J = 4.4 Hz, 1H); 7.94 (dd, J = 8.8 & 5.3 Hz, 2H); 7.63 (brs, 1H); 7.36 (t, J = 8.8 Hz, 2H); 7.14 (s, 1H); 4.77 (septet, J = 6.1 Hz, 1H); 4.62 (brs, 1H); 3.60-3.40 (m, 3H); 3.00 (s, 3H); 2.81 (d, J = 4.4 Hz, 3H); 1.33 (d, J = 6.1 Hz (M + H) + = 479 A &lt; 1 254.2 2- (4-Gasyl-phenyl) -6_ morpholine benzyl-5- (1-¾ thio-2-yl-ethoxy) -benzofuran-3-carboxylic acid methyl Amidine 1H NMR in CDC13: 7.88 (dd, J = 8.8,5.3Hz, 2H); 7.76 (d, J = 3.1Hz, 1H); 7.33 (brs, 2H); 7.14 (t, J = 8.8Hz, 2H ); 7.08 (s, 1H); 5.82 (q, J = 6.6Hz, 1H); 5.79 (brs, 1H); 3.83 (m, 4H); 3.15 (ra, 4H); 2.97 (d, J = 4.9Hz , 3H); 1.78 (d, J = 6.1Hz, 3H) (M + H) + = 482 A &lt; 1 255.6 6- (ethyl-methanesulfonyl-amino) -2- (4-gas-phenyl) 5-isopropoxy-benzofuran-3-m formamidine 1H NMR ia CDCi3: 7.83 (dd, J = 8.3, 3.1Hz, 2H); 7.51 (s, 1H); 7.40 (s, 1H); 7.20 (t, J = 8.3Hz, 2H); 5.72 (brs, 1H) ; 4.78 (septet, J = 6.1Hz, 1H); 3.72 (brs, 2H); 2.97 (d, J = 4.4Hz, 3H); 2.96 (s, 3H); 1.40 (d, J = 6.1Hz, 6H) ; 1.13 (t, J = 7.0Hz, 3H) (M + H) + = 449 A &lt; 1 256.6- (3,5-dimethyl-1H-pyrazol-4-yl) -2- (4-fluoroyl-phenyl) -5-methoxy-benzofuran-3- Formamidine carboxylate * H NMR ia CDC13: 7.88 (m, 2H); 7.39 (s, 1H); 7.26 (s, 1H); 7.19 (m, 2H); 5.78 (brd, 1H); 3.86 (s, 3H); 3.01 (d, J = 4.8Hz, 3H); 2.25 (s, 6H) '(M + H, = 394.1 A &lt; 1 257. 2- (4-Fluoro-phenyl) &gt; 5-isopropoxy-6- (5-methyl-1H-pyrazol-4-yl) -benzofuran-3-carboxylic acid Formamidine NMR in CDC13: 7.87 (m, 2H); 7.74 (s, 1H); 7.38 (s, 2H); 7.18 (m, 2H); 5.81 (brs, 1H); 4.52 (m, 1H); 3.00 (d, J = 5.4Hz, 3H); 2.38 (s, 3H); 1.28 (d, J = 6.0Hz, 6H) (Μ + ΗΓ = 408.1 A &lt; 1 202-88828.doc 200418452 Instance number name NMRdata Mass Spec HCV pol -BB7 IC50 (μΜ) A = μΜ B = 03 to ^ 5.0 / iM C = 5.0 to ^ 30 μΜ D = &gt; 30 nM replicon ( μM) 258.3 3- [2- (4-Fluoro-phenyl) -3-methylaminomethylmethyl-benzofuran-5-yloxymethyl] methyl gallate 1H NMR in DMSO: 8.34 ( brd, 1H, J = 4.10Hz); 8.07 (s, 1H); 7.92 (m, 3H); 7.76 (d, 1H, J = 7.62Hz); 7.56 (m, 2H); 735 (t, 2H, J = 7.03Hz); 7.21 (dt 1H, J = 2.34Hz); 7.07 (ddt 1H, J = 8.79, 2.34Hz); 5.24 (s, 2H); 3.86 (s, 3H); 2.81 (d, 3H, J = 4.69Hz) (M + H) + = 434 A &gt; 30 259. 4- [2 · (4-Gas-phenyl) -3-methylaminomethylmethyl-benzofuran 5-yloxy Methyl) benzyl acid 1H NMR in DMSO: 8.38 (brd, 1H, J = 4.10Hz); 7.90 (m, 4H); 7.56 (d, 1H, J = 8.79Hz); 7.35 (m, 4H); 7.20 ( s, 1H); 7.05 (d, 1H, J = 9.38Hz); 5.13 (s, 2H); 2.82 (d, 3H, J = 4.69Hz) (MH) '= 418 B &lt; 30 260. 3- [2- (ί-fluoro-phenyl) · -3-methylaminomethylmethyl-benzofuran-5-yloxymethyl] gallic acid JH NMR in DMSO: 12.98 ( brs, 1H); 834 (br m, 1H); 8.05 (s, 1H); 7.91 (m, 3H); 7.72 (d, 1H, J = 6.45Hz); 7.56 (m, 2H); 7.35 (t, 2H, J = 8.79Hz); 7.21 (s, 1H); 7.08 (d, 1H, J = 8.79Hz); 5.23 (s, 2H); 2.81 (d, 3H, J = 6.71Hz) (MH) '= 418 A &gt; 30 261. 6-Ethyl-2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-quinoformamidine'H NMR in CDC13: 7.84 ( m, 2H); 7.83 (s, 1H); 7.37 (s, 1H); 7.19 (m, 2H); 5.95 (brs, 1H); 3.97 (s, 3H); 3.00 (d, J = 4.8Hz, 3H ); 2.64 (s, 3H) (M + H) + = 342.1 A &lt; 1 262. 4- [2- (4-Fluoro-phenyl)-3-methylaminomethylcarbamoyl fulin-4-yl-benzopyran-5-yloxymethyl] LH NMR in CDCl3: 8.09 (d, 2H, J = 8.21Hz); 7.85 (m, 2H); 7.57 (d, 2H, J = 8.21Hz); 7.42 (s, 1H); 7.18 (t, 2H, J = 8.21); 7.12 (s, 1H); 5.72 (brs, 1H); 5.24 (s, 2H); 3.94 (s, 3H); 3.89 (m, 4H); 3.16 (m, 4H); 2.98 (d, 3H, J = 4.69Hz) (M + H) + = 519 A &lt; 10 263. 3- [2- (4-Fluoro-phenyl) -3-methylamine formamyl-6-morpho 57 lin-4-yl-benzoan-5-yloxymethyl Table] 1H NMR of Methyl Esterate in CDC13: 8.25 (s, 1H); 8.05 (d, 1H, J = 8.21Hz); 7.87 (m, 2H); 7.67 (d, 1H, J = 7.62Hz); 7.51 (t, 1H, J = 7.62Hz); 7.45 (s, 1H); 7.20 (t, 2H, J = 8.79Hz); 7.13 (s, 1H); 5.75 (brs, 1H); 5.24 (s, 2H ); 3.97 (s, 3H); 3.93 (m, 4H); 3.18 (m, 4H); 3.00 (d, 3H, J = 5.28) (M + H) &quot; = 519 A &lt; 10 264.2 2 (4-Mono-phenyl-isopropyloxy-6- (l, 3,5-trimethyl-1H-pyridine-4-yl) -benzofuran-3- Formamidine carboxylate 1H NMR in CDC13: 7.90 (m, 2H); 7.38 (s, 1H); 7.25 (s, 1H); 7.18 (m, 2H); 5.78 (brs, 1H); 4.36 (in, 1H) ); 3.79 (s, 3H); 3.01 (d, J = 4.8 Hz, 3H); 2.17 (s, 3H); 2.14 (s7 3H); 1.20 (d, J = 6.0 Hz, 6H) (M + HV = 436.1 B &lt; 10 265. 2_ (4_Gas-Dongyl) -5_isopropoxy-6 · Epgoline-2-yl-benzoanan-3 -carboxylic acid formamidine 1H NMR in CDC13: 7.82 (m, 2H); 7.52 (s, 1H); 7.32 (s, 1H); 7.18 (m, 2H); 6.76 (brs, 2H); 5.80 (brs, 1H); 4.75 (m, 1H); 4.72 (m, IH); 3.28 (m, 2H); 2.97 (d, J = 5.4 Hz, 3H); 2.28 (m, 1H); 2.03 (m, 3H); 1.41 (d, J = 6.0 Hz, 6H) (M + H) + = 397.1 C &gt; 30 266.6 6-Gas-2- (4-Gas-Mulyl) -5-methoxy-benzoanan-3-methanoic acid NMR in CDC13: 7.89 -7.83 (m, 2H); 7.83 (s, 1H); 7.45 (s, 1H); 7.25-7.20 (m, 2H); 5.74 (s, 1H); 3.99 (s, 3H); 2.99 (d, J = 5.6 Hz, 3H) (M + H) + = 325 A &lt; 1 203 &gt; 88828.doc 200418452 Example number name NMR data Mass Spec HCV pol -BB7 IC50〇tM) A = μΜ B = 03 to ^ 5.0 / iM C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ Copy (ΜΜ) 267. 4- [2- (4-Gasyl-phenyl) -3-methylaminomethylmethyl-6-morpholin-4-yl-mycyl-5-yloxy Methyl] -benzoic acid 1H NMR in DMSO: 8.32 (brdT 1H, J = 4.69Hz); 7.90 (m, 4H); 7.41 -7.31 (rn, 4H); 7.23 (s, 2H); 5.16 (s, 2H ); 3.75 (m, 4H); 3.07 (m, 4H); 2.84 (d, 3H, J = 4.10) (Μ + ΗΓ = 505 A &lt; 10 268. 3- [2- (4-Fluorobenzyl-3-methylamine T-methyl morpholine_4-yl-benzofuran-5-yloxymethyl j-gallate 1H NMR in DMSO: 8.33 (brd, 1H, J = 4.69Hz); 8.02 (s, 1H); 7.92 (m, 2H); 7.80 (d, 1H, J = 7.03Hz); 7.41-7.26 (in, 4H) ; 7.23 (d, 2Ht J = 4.10Hz); 5.16 (s, 2H); 3.76 (m, 4H); 3.07 (m, 4H); 2.84 (d, 3H, J = 4.10Hz) (M + H) + = 505 A &lt; 10 269. 2- (4-Fluorophenyl) -5-isopropoxy each [methanesulfonyl- (1-methyl-1H-tetrazolylmethyl) -amino] -benzo 1H NMR in DMSO: 8.43 (brd, 1H, J = 4.69); 7.92 (m, 2H); 7.60 (s, 1H); 737 (t, 2H, J = 8.79Hz) ; 7.14 (s, 1H); 5.19 (s, 2H); 4.78 (m, 1H); 4.10 (s, 3H); 3.20 (s, 3H); 2.82 (d, 3H, J = 4.69Hz); 1.35 ( d, 6H, J = 6.45Hz) (M + H, = 517 A &lt; 1 270. 4-({[2- (4-Fluoro-phenyl) -5-isopropoxy-3-methylamine methylamidino-benzofuran-6-yl] -formaldehyde Ethyl-amino group} -methyl) -coate methyl ester'H NMR in CDCi3: 7.91 (d, 2H, J = 8.21Hz); 7.75 (m, 2H); 7.41 (s, 1H); 7.34 (d , 2H, J = 8.21Hz); 7.20-7.14 (m, 3H); 5.66 (brs, 1H); 4.84 (br m, 3H); 3.87 (s, 3H); 3.04 (s, 3H); 2.94 (d , 3Hf J = 5.27Hz); 1.48 (d, 6H, J = 5.86Hz) (M + H) + = 569 A &lt; 1 271. 2- (4-Fluoro-phenyl) -5 ^ isopropoxy-6- [methanesulfonyl- (2-methyl-thiazolylmethyl) -amino] -benzene 1H NMR in CDCl3: 7.80 (m, 2H); 7.43 (s, 1H); 7.39 (s, 1H); 7.18 (t, 2H, J = 8.79Hz); 7.07 ( s, 1H); 5.68 (brs, 1H); 4.93 (brs, 2H); 4.78 (m, 1H); 3.06 (s, 3H); 2.95 (d, 3H, J = 4.69Hz); 2.63 (s, 3H ); 1.43 (d, 6H, J = 6.45Hz) (M + H) + = 532 A &lt; 10 272. 4-({[2- (4-Fluoro-phenyl) 5-isopropoxy-3-methylaminemethylamido-benzofuranyl] -methanesulfonyl-amine 1H NMR in DMSO: 8.36 (brd, 1H, J = 4.69 Hz); 7.89-7.82 (m, 4H); 7.40 (m, 3H); 7.32 (t, 2H, J = 8.79 Hz); 7.10 (s, 1H); 4.80 (br m, 3H); 3.13 (s, 3H); 2.79 (d, 3H, J = 4.10 Hz); 1.38 (d, 6H, J = 5.86 Hz) \ (M + H) + = 555 A &lt; 1.0 273. 2- (4-Gasyl-phenyl) -5-isopropoxy-6- (5-methoxymethyl-iso-azine-3-yl) -benzofuran-3-benzyl Formamidine acid 1H NMR in DMSO: 8.43 (q, J = 4.4 Hz, 1H); 7.98 (s, 1H); 7.97 (dd, J = 5.3, 8.8 Hz, 2H); 7.39 (apparent triplet, J = 8.8 Hz, 2H); 7.29 (s, 1H); 6.93 (s, 1H); 4.76 (m, J = 6.1, 5.7 Hz, 1H); 4.62 (s, 2H); 3.36 (s, 3H); 2.85 (d , J = 4.4 Hz, 3H); 1.34 (d, J = 6.1 Hz, 6H) (M + H) + = 439.05 A &lt; 1 204- 88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 IC50 〇iM) A = iO-5 μΜ B = 0.5 to ^ 5.0 μΜ C = 5.0 to ^ 30 / iM D = &gt; 30 μΜ Replicon (μM) 274.6- (5-cyclopropyl-isoxazol-3-yl) -2- (4-amino-phenyl) -5-isopropoxy-benzofuran-3- Formamidine carboxylate * H NMR in DMSO: 8.42 (q, J = 4.4 Hz, 1H); 7.96 (dd, J = 5.3, 8.8 Hz, 2H); 7.92 (s, 1H); 7.38 (apparent triplet, J = 8.8 Hz, 2H); 7.26 (s, 1H); 6.61 (s, 1H); 4.72 (m, J = 6.15Hz, iH); 2.84 (d, J = 4.4 Hz, 3H); 2.22 (m, 1H ); 1.33 (d, J = 6.15 Hz, 6H); 1.10 (m, 2H); 0.94 (m, 2H) (M + H) + = 435.12 A &lt; 1 275. Fluoro-phenyl) -5-isopropoxy-6- (1-methane transverse acid-p-pyridine-2-yl) -benzofuran-3-chitoic acid formamidine lH NMR in CD € 13: 7.84 (m, 2H); 7.56 (s, 1H); 7.30 (s, 1H); 7.21 (mt 2H); 5.73 (brs, 1H); 5.21 (dd, J = 8.4 Hz, 2.4 Hz, IH); 4.69 (m, 1H); 3.70 (m, 1H); 3.55 (m, 1H); 2.97 (d, J = 3.9 Hz, 3H); 2.84 (s, 3H); 2.35 (m, 1H); 1.95 (m, 3H); 1.39 (d, J = 6.3 Hz) (M + H) + = 475.1 A &lt; 1 276. 6-Ethylfluorenyl-2- (4-fluoro-winteryl) -5-: ¾-yl-benzofuran-3-carboxylic acid mepanimine 1H NMR in CDC13: 12.16 (s, 1H ); 8.03 (m, 2H); 7.87 (s, 1H); 7.19 (ra, 2H); 5.86 (br, 1H); 3.02 (d, J = 4.8Hz, 3H); 2.71 (s, 3H) (M + H) + = 328.0 B &lt; 10 277.6 6- (Ethyl-methanesulfonyl-amino) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine ' H NMR ia DMSO: 8.43 (d, J = 4.69Hz, 1H); 7.96-7.91 (ra, 2H); 7.6 (s, 1H); 7.38 (t, J = 8.79Hz, 2H); 7.21 (s, 1H ); 3.9 (s, 3H); 3.62 (q, J = 7.03, 2H); 3.02 (s, 3H); 2.84 (d, J = 4.69HzT 3H); 1.02 (t, J = 7.03Hz, 3H) ( M + H) + = 421.1 A &lt; 1 278. 4- [2- (4-Fluoro-phenyl) -5-methoxy-3-methylamine formamido-benzocran-6-yl] -2-oxy- Pyrrolidine-3-carboxylic acid formamidine'H NMR ia DMSO: 8.36 (q, 1H, br); 8.00 (q, 1H, br); 7.97-7.68 (ra, 3H); 7.53 (s, 1H); 7.77 (m, 2H); 7.U (s, 1H); 4.20 (q, 1H); 3.84 (s, 3H); 3.57 (m, 2H); 3.16 (t, 1H); 2.82 (d, 3H) ; 2.57 (d, 3H) (M + H) + = 440 A &lt; 10 279. 2- (4 · Fluoro-phenyl) _5_ isopropoxy-6- · (4Η · [1,2,4] triazol-3-yl) -benzo4an-3- Formamidine carboxylate 1H NMR in CDC13: 8.47 (s, 1H); 8.03 (s, 1H); 7.84-7.89 (m, 2H); 7.57 (s, 1H); 7.19-7.25 (t, 2H, J = 8.79 Hz); 5.80 (br.s, 1H); 4.90-4.98 (septet, 1H, J = 5.86 Hz); 2.98-3.00 (d, 3H, J = 4.69 Hz); 1.52 -1.54 (d, 6H, J = 6.45 Hz) (M + H) + = 395.0 A &lt; 30 280. 2- (4-Fluoro-phenyl) -5-methoxy-6- (5-methoxymethyl-3-methyl-isoxan-4-yl) -benzofuran Formamidine-3-carboxylic acid * H NMR in CDCi3: 7.86 (dd, J = 8.8 and 5.1 Hz, 2H); 7.43 (s, 1H); 7.35 (s, 1H); 7.21 (apparent t, J = 8.8 and 8.4 Hz, 2H); 5.78 (brs 1H); 4.42 (s, 2H); 3.86 (s, 3H); 3.36 (s, 3H); 3.01 (d, J = 5.1 Hz, 3H); 2.21 (s, 3H) (M + H) + = 425 A &lt; 1 205-88828.doc 200418452 Example No. Name NMR data Mass Spec HCV pol -BB7 IC5〇 (μΜ) A = / iM B = to ^: 5.0 μΜ C = 5.0 to &lt;: 30 / iM D = &gt; 30 / iM replicon (μM) 281.2 2- (4-fluoro-phenyl) -5_ isopropoxy-6- [methanesulfonyl- (4-methyl Oxy-fluorenyl) -amino] -benzoanan-3-carbamidine 1H NMR in CDC13: 7.76 (m, 2H); 7.38 (s, 1H); 7.20-7.12 (m, 5H) ; 6.75 (d, 2H, J = 8.79 Hz); 5.86 (brs, 1H); 4.90-4.70 (br m, 3H); 3.74 (s, 3H); 3.03 (s, 3H); 2.95 (d, 3H, J = 4.69 Hz); 1.47 (d, 6Hy J = 6.45 Hz) (MH) = 539 A &lt; 1 282.2 2- (4-Fluoro-phenyl) -5-isopropoxy-6- [methylsulfonyl- (5-methyl-isoammonium 3-ylmethyl) -amine Benzyl] -benzofuran-3-methanomethamine 1H NMR in CDCi3: 7.79 (m, 2H); 7.42 (s, 1H); 7.34 (s, 1H); 7.19 (t, 2H, J = 8.79 Hz ); 6.21 (s, 1H); 5.86 (brs, 1H); 4.83 (br m, 3H); 3.04 (s, 3H); 2.96 (d, 3H, J = 4.69 Hz); 2.38 (s, 3H); 1.45 (d, 6H, J = 5.86 Hz) (MH) * = 514 A &lt; 1 283. 2- (4-Gasyl-benzene grave) -5_ isopropoxy-6- (5-methyl-iso-17ajun-3 -yl) -benzofuran-3-carboxylic acid form Lamine 1H NMR in CDCb: 8.015 (s, 1H); 7.87 (dd, J = 5.3, 8.3 Hz, 2H); 7.43 (s, 1H); 7.19 (apparent triplet, d, J = 8.3 Hz, 2H); 6.58 (s, 1H); 5.79 (bs, 1H); 4.68 (m, 1H); 2.99 (d, J = 4.8 Hz, 3H); 2.48 (s, 3H); 1.38 (d, J = 5.7 Hz, 6H ) 氺 氺 氺 A &lt; 1 284 .; 6-[(3,5-dimethyl-isoindazol-4-ylmethyl) -methanesulfonyl-amino] -2- (4-fluoro-phenyl)- 5-isopropoxy-benzofuran-3-menfate methamidamine 1H NMR in DMSO: 8.41 (brd, 1H, J = 4.69 Hz); 7.91 (m, 2H); 7.36 (m, 3H); 7.12 (s, 1H); 4.79 (m, 1H); 4.64 (br m, 2H); 3.13 (s, 3H); 2.82 (d, 3H, J = 4.69 Hz); 2.08 (s, 3H); 2.05 ( s, 3H); 1.37 (d, 6H, J = 5.86 Hz) (M + H) + = 530 A &lt; 10 285. 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (formamidine-pyrimidinyl-pyrazol-2-ylmethyl-amino) -benzofuran -3- Formamidine Carboxylate NMR in DMSO: 8.42 (brd, 1H, J = 4.69 Hz); 7.92 (ra, 2H); 7.67 (d, 1H, J = 3.52 Hz); 7.65 (d, 1H, J = 3.52 Hz); 7.45 (s, 1H); 7.36 (t, 2H, J = 8.79 Hz); 7.18 (s, 1H); 5.12 (brs, 2H); 4.83 (m, 1H); 3.16 (s, 3H ); 2.82 (d, 3H, J = 4.69 Hz); 1.39 (d, 6H, J = 6.45 Hz) (M + H) + = 518 A &lt; 1 286. 2-([[2: όίϋ phenyl) -5-isopropoxy-3-methylaminofluorenyl-benzofuran-6-yl] -methyloxofluorenyl-amino ) -Ethyl acetoethyl carboxylate'H NMR in DMSO: 8.49 (s, 1H); 8.42 (brd, 1H, J = 4.10 Hz); 7.93 (m7 2H); 7.54 (s, 1H); 7.37 (t, 2H, J = 8.79 Hz); 7.20 (s, 1H); 5.13 (brs, 2H); 4.84 (m, 1H); 4.25 (q, 2H, J = 7.03 Hz); 3.18 (s, 3H) ; 2.82 (d, 3H, i = 4.69 Hz); 1.39 (d, 6H, J = 6.45 Hz); 1.26 (t, 3H, J = 7.03 Hz) '(M + H) + = 590 A &lt; 10 206- 88828.doc 200418452 .Instance number name NMRdata Mass Spec HCV pol -BB7 IC50 〇iM) A = μΜ B = 03 to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 / iM replicon OiM) 287.2 2- (4-Fluoro-phenyl) -5-hydroxy-6- (methanesulfonyl-methyl-amino) -benzocaran-3-carboxylic acid formamidine 1H NMR in DMSO: 9.98 (s, 1H); 8.39 (d, J = 4.4 Hz, 1H); 7.91 (mT 2H); 7.51 (s, 1H); 7.35 (UJ = 8.8 Hz, 2H); 7.09 (s, 1H ); 3.20 (s, 3H); 3.08 (s, 3H); 2.80 (d, J = 4.4Hz, 3H) (M + H) + = 393 A &lt; 10 288.6 6- (fluorenyl-methanesulfonyl-amino) -5-fluorenylpropoxy-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid formamidine Amine 1H NMR in DMSO: 8.40 (dt J = 4.7 Hz, 1H); 7.93 (dd, J = 9.0, 5.3 Hz, 2H); 7.57 (s, 1H); 7.35 (t, J = 9.0 Hz, 2H); 7.33 (s, 1H); 6.10 (mT 1H); 5.80 (m, 1H); 5.50 (m, 1H); 5.30 (m, 1H); 5.10 (m, 1H); 5.00 (ra, 1H); 4.70 ( d, J = 3.5 Hz, 2H); 4.20 (brs, 2H); 3.05 (s, 3H); 2.81 (d, J = 4.7 Hz, 3H) (M + H) + = 459 A &lt; 1 289. 6- (Ethylfluorenyl-methanesulfonyl-amino) -2- (4-_fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine Amine 1H NMR in DMSO: 8.48 (d, J = 4.39 HzT 1H); 7.96-7.91 (m, 2H); 7.86 (s, IH); 7.39 (t, J = 8.79 Hz, 2H); 7.27 (s, 1H ); 3.93 (s, 3H); 3.49 (s, 3H); 2.84 (d, J = 4.39, 3H); 1.89 (s, 3H) (M + H) + = 435.0 A &lt; 1 29. 6-[(3,5-Difluorenyl-isopurazol-4-ylmethylmethanesulfonyl-amino group) &gt; Oxy-benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.44 (m, 1H); 7.94-7.90 (m, 2H); 7.43-7.33 (m, 3H); 7.16 (s, 1H) ; 4.67 (bs, 2H); 3.9 (s, 3H); 3.13 (ra, 3H); 2.84-2.82 (m, 3H); 2.11 (ct J = 3.52 Hz, 3H); 2.06 (d, J = 3.52, 3H) (M + H) + = 502.1 A &lt; 10 291. 2- (4-Fluoro-phenyl) -6-((A: K-Cyridin-4-ylmethyl-amino) -5-methoxy-benzoanan- 3-Methylmetamidine 1H NMR in DMSO: 9.01 (s, 1H); 8.41 (d, J = 4.84 Hz, 1H); 7.93-7.88 (m, 2H); 7.55 (m, 1H); 7.48 (s , 1H); 7.36 (t, J = 8.35 Hz, 2H); 7.17 (s, 1H); 4.93 (bs, 2H); 3.90 (s, 3H); 3.15 (st 3H); 2.83 (d, J = 4.84 hz, 3H) (M + H) + 490.0 A &lt; 1 292. 2-({[2- (4-Fluoro-phenyl) -5-isopropoxy-3-methylaminomethylmethyl-benzofuran-6-yl] -pyranesulfonate Fluorenyl-aminomethyl) -thiazole-4-carboxylic acid * H NMR in DMSO: 8.42 (brm, 2H); 7.93 (m, 2H); 7.53 (d, 1H, J = 1.17 Hz); 7.36 (t, 2H, J = 8.79 Hz); 7.19 (s, 1H); 5.12 (brs, 2H); 4.84 (m, 1H); 3.19 (s, 3H); 2.82 (d, 3H, 1 = 3.52 Hz); 1.39 ( d, 6H, J = 5.28 Hz) (M + H) + = 562 A &gt; 100 293. 5- (2,2-dimethyl-4-oxy-4H-benzo [1,3] -di Ringen-5-ylmethoxy) -2- (4-amino-phenyl) -6-morpholin-4-yl-benzofuran-3-carboxylic acid amidine 1H NMR in DMSO: 8.32 (brd, 1H, J = 4.40 Hz); 8.08 (s, 1H); 7.90 (m, 2H); 7.80 (d, 1H, J = 8.79 Hz); 7.35 (t, 2H, J = 8.79 Hz); 7.26 -7.19 (m, 3H); 5.20 (s, 2H); 3.77 (m, 4H); 3.06 (m, 4H); 2.83 (d, 3H, J = 4.00 Hz); 1.72 (s, 6H) (M + H) + = 561 B &lt; 10 207- 88828.doc 200418452 example editor &quot; 5 Tiger name NMRdata Mass Spec HCV pol -BB7 IC50〇iM) A = MB only = 03 to ^ 5.0 C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ Replicon (μΜ) 294. 5- (2,2-Dimethyl-4-oxy-4H-benzo [1,3] -diginyl · 5-ylmethoxy) -6- (ethyl -Methanesulfonyl-amino) -2- (4-fluoro-phenyl) -benzobenzamine-3-carboxylic acid formamidine * H NMR in DMSO: 8.42 (brd, 1H, J = 4.40 Hz ); 8.05 (d, 1H, J = 1.76 Hz); 7.93 (m, 2H); 7.85 (d, 1H, J = 8.35 Hz); 7.65 (s, 1H); 7.39 (ζ 2H, J = 8.79 Hz) ; 7.34 (s, 1H); 7.19 (d, 1H, J = 8.35 Hz); 5.26 (s, 2H); 3.63 (m, 2H); 2.93 (s, 3H); 2.84 (d, 3H, J = 4.40 Hz); 1.71 (s, 6H); 1.03 (t, 3H, J = 7.03 Hz) (M + H) + = 597 A &lt; 1 295. 2- (4-Fluoro-phenyl) -6- (1fluoren-imidazol-4-yl;)-5-methoxy-benzofuran-3-carboxylic acid formamidine 1H NMR ia CDC13: 7.96-7.85 (m, 3H); 7.74 (s, 1H); 7.61 (s, 1H); 7.45 (s, 1H); 7.24-7.18 (m, 2H); 5.82 (s, 1H); 4.04 ( s, 3H); 3.0 (d, J = 4.8Hz, 3H) (M + H) + = 466 A &lt; 10 296. 2_ (4-Gas-wood-based) -6- (1fluoren-imidazol-2-yl) -5-methoxy-benzofuran-3-carboxylic acid formamidine'H NMR in CDC13 : 10.6 (s, 1H); 8.48 (s, 1H); 7.88-7.84 (m, 2H); 7.50 (s, 1H); 7.26-7.20 (m, 3H); 7.18 (s, 1H); 7.13 (s , 1H); 5.84 (s, 1H); 4.14 (s, 3H); 3.0 (d, J = 6.8Hz, 3H) (M + H) + = 466 A &lt; 1 297.6 6- (Ethyl-methanesulfonyl-amino) -2- (4-fluorophenyl) -5- # yl-benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 9.96 (s, 1H); 8.40 (d, J = 4.4Hz, 1H); 7.92 (dd, J = 8.8, 5.3Hz, 2H); 7.46 (s, 1H); 7.37 (t, J = 8.8 Hz, 2H); 7.09 (s, 1H); 3.60 (q, J = 7.0Hz, 2H); 3.01 (s, 3H); 2.80 (d, J = 4.4Hz, 3H); 1.00 (t, J = 7.0 Hz, 3H) (MH) * = 405 A &lt; 10 298. 5-Difluoromethoxy-2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzofuran formamidine carboxylic acid 1H NMR in CDCb: 7.86 (dd, J = 8.8, 5.3Hz, 2H); 7.70 (s, 1H); 7.62 (s, 1H); 7.24 (t, J = 8.8Hz, 2H); 6.69 (t, J = 73.4Hz, 1H); 5.74 (brs, 1H); 3.33 (s, 3H); 3.03 (s, 3H); 2.98 (d, J = 4.8Hz, 3H) (M + H) + = 443 A &lt; 1 299.2 2- (4-Fluoro-phenyl) -6_ (methanesulfonyl-eridin-4-ylmethyl-amino) -5-methoxy-benzo 4-4- Formamidine carboxylate * (M + H) + = 484 A &lt; 1 300. 2- (4-Fluoro-phenyl) -6- (1-meryl small methyl_ethyl) _5_methyl-benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.95 (m, 2H); 7.69 (s, 1H); 7.56 (s, 1H); 7.16 (mt 2H); 5.83 (brs, 1H); 3.02 (d, J = 4.6 Hz, 3H); 2.69 ( s, 1H); 2.64 (d, J = 3.9 Hz, 3H); 1.72 (s, 6H) (M + H) &quot; = 342.1 A &lt; 10 301. 6-Ethyl-2- (4-fluoro-phenyl) -5-methyl-benzofuran medonylamine of each carboxylic acid 'H NMR in CDC13: 7.94 (m, 2H); 7.79 (s, 1H); 7.69 (s, 1H); 7.20 (m, 2H); 5.83 (brs, 1H); 3.02 (d, J = 4.8 Hz, 3H); 2.64 (s, 3H); 2.96 (s , 3H) (M + H) + = 326.1 A &lt; 10 208-88828.doc 200418452: Instance data name NMR data Mass Spec HCV pol -BB7 IC50 (μΜ) A = μΜ B = 0.5 to 2: 5.0 fiM C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ Copy 〇iM) 302. 5- (2,2-Difluorenyl-4 · oxy-4H-benzo [1,3] -difluorene 4-7-ylmethoxy) -2- (4-denyl -Phenyl) -6- (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid formamidine NMR in DMSO: 8.39 (brd, 1H, J = 4.69 Hz); 7.92 (m , 3H); 7.74 (s, 1H); 7.37 (m, 3H); 7.29 (d, 2H, J = 1.76 Hz); 5.32 (brs, 2H); 3.23 (s, 3H); 3.01 (s, 3H) ; 2.82 (d, 3H, J = 4.10 Hz); 1.71 (s, 6H) (M + H) + = 583 A &lt; 1 303. 2- (4-Fluoro-phenyl) methanesulfonyl-methylpyridyl-amino) -ethyl] -5-methoxy-epimethyl-3-carboxylic acid formamidine lH NMR in CDC13: 7.89-7.84 (m, 2H); 7.50 (s, 1H); 7.39 (s, 1H); 7.27-7.19 (m, 2H); 5.76 (s, 1H); 5.63-5.56 (m, 1H); 3.95 (s, 3H); 3.00 (d, J = 4.8Hz, 3H); 2.82 (s, 3H); 2.69 (s, 3H); i.65 (d, J = 6.9Hz, 3H) ( M + H) + = 435 A &lt; 1 304. --2- (fluorenyl-fluoro-benzyl) -5-methoxy-6- (1-methylamino-ethyl) -benzofuran-3-carboxylic acid formamidine 1H NMR in CDC13: 7.88-7.83 (m, 3H); 7.47 (s, 1H); 7.33 (s, 1H); 7.21-7.16 (m, 6H); 5.75 (s, 1H); 4.20-4.16 (m, 1H) ); 3.92 (s, 3H); 3.47 (s, 1H); 2.99 (d, J = 4.5Hz, 3H); 2.34 (s, 3H); 1.44 (d, J = 6.3Hz, 3H) (M + H ) + = 357 B &gt; 30 305. 4- [2- (4-Fluoro-phenyl) -6- (methylpyridyl-fluorenyl-amino) -3-methylaminomethyl- Benzofuran-5-yloxymethyl] -benzoic acid methyl esterΉ NMR in DMSO: 8.40 (brd, 1H, J = 4.69); 8.02 (d, 2H, J = 8.21); 7.93 (m, 2H) ; 7.70 (111, 3H); 7.39 (t, 2H, J = 8.79 Hz); 7.34 (s, 1H); 5.34 (s, 2H); 3.87 (s, 3H); 3.22 (s, 3H); 2.97 ( s, 3H); 2.84 (d, 3H, J = 4.10Hz) (M + H) + = 541 A &lt; 1 306. 2- [2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino group; H3-methylaminomethylmethyl-benzo-benzoan-5- Methyloxyformate 1H NMR in DMSO: 8.39 (brd, 1H, J = 5.28 Hz); 8.15 (s, 1H); 7.93 (ra, 3H); 7.82 (d, 1H, J = 7.62 Hz); 7.68 ( s, 1H); 7.58 (ζ 1H, J = 7.62 Hz); 7.37 (m, 3H); 5.32 (s, 2H); 3.86 (s, 3H); 3.20 (s, 3H); 2.94 (s, 3H) ; 2.82 (d, 3H, J = 4.10 Hz) (M + H) + = 541 A &lt; 1 307.6 6-((2-Fluoro-ethyl) -methyl ^ complete guaranyl-amine plug] -2- (4-fluoro-phenyl) -5-methoxy-benzofuran Formamidine-3-carboxylic acid * H NMR in DMSO: 8.43 (m, 1H); 7.93 (dd, J = 5.3 &amp; 8.8Hz, 2H); 7.62 (s, 1H); 7.39 (t, J = 8.8 Hz, 2H); 7.22 (s, 1H); 4.54 (t, J = 5.3Hz, 1H); 4.39 (t, J = 4.7Hz, 1H); 3.92 (m, 4H); 3.84 (m, 1H); 3.06 (s, 3H); 2.83 (d, J = 4.7Hz, 3H) (M + H) + = 439 A &lt; 1 308. _2- (4-Fluoro-phenyl) -6- [methanesulfonyl- (2,2,2-trifluoroethyl) -amino] -5-methoxy-benzo 1H NMR of stilbene 3-carboxylate in DMSO: 8.45 (m7 1H); 7.93 (dd, J = 5.3 &amp; 8.8Hz, 2H); 7.65 (s, 1H); 7.39 (t, J = 8.8Hz , 2H); 7.25 (s, IH); 4.40 (m, 2H); 3.94 (s, 3H); 3.10 (s, 3H); 2.83 (d, J = 4.7Hz, 3H) (M + H) + = 475 A &lt; i 209- 88828.doc 200418452 Instance data name NMR data Mass Spec HCV pol -BB7 ICs〇〇iM) A = / iM B = 0 0 J to ^ 5.0 / iM C = 5.0 to ^ 30 / iM D = &gt; 30 μΜ replicon (μΜ) 309.2- (4-fluoro-phenyl) -6- (1-methanesulfonyl-pyrrolidin-2-yl) -5-methoxy-xylo-amino-3 -Formamidine chitomate NMR in CDC13: 7.84 (m, 2H); 7.58 (s, 1H); 7.26 (s, 1H); 7.18 (m, 2H); 5.76 (brs, 1H); 5.22 (m, 1H) ); 3.91 (s, 3H); 3.75 (m, 1H); 3.55 (m, 1H); 3.18 (m, 1H); 3.00 (d, J = 4.6 Hzt 3H); 2.84 (s, 3H); 1.92 ( m, 2H); 1.84 (m, 2H) M + = 446 (GCVMS) A &lt; 1 310. 6- (3-Cyclopropyl-5-methoxymethyl-isoindan-4-yl) -2- (4-amino-phenyl) -5-methoxy-benzo Furfuryl 4-3-carboxylic acid formamidine 1H NMR in CDCl3: 7.87 (dd, J = 8.8 and J = 5.1Hzt 2H); 7.44 (s, 1H); 7.42 (s, 1H); 7.20 (apparent t, J = 8.8 and 8.4 Hz, 2H); 5.81 (brs, 1H); 4.40 (s, 2H); 3.87 (s, 3H); 3.34 (s, 3H); 3.01 (d, J = 4.8Hz, 3H); 1.65 (m, 1H); 1.02 (m, 2H); 0.88 (m, 2H) (M-Η) '= 449 A &lt; 1 311. 4- [2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -3-methylaminomethylmethyl-benzofuran-5- 1H NMR in DMSO: 8.41 (brd, 1H, J = 4.10Hz); 7.95 (mt 4H); 7.69 (s, 1H); 7.58 (d, 2H, J = 8.21Hz); 7.37 (mt 3H); 5.29 (s, 2H); 3.21 (s, 3H); 2.94 (s, 3H); 2.84 (d, 3H, J = 4.69Hz) (M + H) + = 527 A &lt; 10 312. 3- [2_ (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -3-methylaminomethyl-benzoxan-5- 1H NMR in DMSO: 8.41 (brd, 1H, J = 4.10Hz); 8.14 (s, 1H); 7.94 (m, 3H); 7.80 (d, 1H, J = 7.62Hz) ; 7.69 (s, 1H); 7.57 (t, 1H, J = 8.21Hz); 7.38 (m, 3H); 5.33 (s, 2H); 3.22 (s, 3H); 2.95 (s, 3H); 2.84 ( d, 3H, J = 4.10Hz) (M + H) + = 527 A &lt; 1 313. 2- (4-Fluoro-phenyl) -5-methoxy-6- (5-methoxymethyl-isohumic acid lH NMR in CDCl3: 8.03 (s, 1H); 7.87 (ddt J = 5.27 &amp; 8.8Hz, 2H); 7.45 (s, 1H); 7.20 (apparent triplet, J = 8.8 &amp; 8.3Hz, 2H); 6.83 (s, 1H); 5.80 (bs, 1H); 4.61 (s, 2H); 3.96 (s, 3H); 3.48 (s, 3H); 3.00 (d, J = 4.8Hz, 3H) (M + H) + = 411 A &lt; 1 314.6. 6- (3,5-dimethyl-isohumazol-4-yl) -2_ (4-fluoro-phenyl) &gt; 5-hydroxy-benzofuran-3-carboxylic acid methyl alcohol Amine 1H NMR in CDC13: 7.90 (m, 2H); 7.56 (s, 1H); 7.22 (mT 3H); 6.04 (brs, 1H); 5.83 (brs, 1H); 3.00 (d, 3H, J = 4.69Hz ); 2.36 (s, 3H); 2.22 (s, 3H) (M + H) + = 381 A &lt; 1 315. 2- (4-Fluoro-phenyl) -5_methoxy-6- (5-oxy-pyrrolidin-3-yl) benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.36 (m, 1H, br); 7.92 (dd, 2H); 7.64 (s, 1H, br); 7.54 (s, 1H); 7.34 (dd, 2H); 7.11 (s, 1H); 3.89 (m, 1H); 3.86 (s, 3H); 3.6 (m, 1H); 3.21 (m, 2H); 2.81 (d, 3H); 2.48-2.37 (m, 2H) (M + H) + = 383 A &lt; 10 316. 2- (4-Gasyl-wood-based) -6_ [methanesulfonyl- (2-tris-methoxy-ethyl-tomb) -moonyl] -5-methoxy-benzo Furan-3-carboxylic acid formamidine * H NMR in DMSO: 8.42 (m, 1H); 7.94 (dd, J = 5.9 & 8.8Hz, 2H); 7.57 (s, 1H); 7.38 (t, J = 8.8Hz, 2H); 7.23 (s, 1H); 4.11 (m, 2H); 3.92 (m, 5H); 3.06 (s, 3H); 2.84 (d, J = 4.7Hz, 3H) (M + H) + = 505 B &lt; 1 210- 88828.doc 200418452 Example No. Name NMRdata Mass Spec HCV po BB7 ICs〇 (μΜ) A = J / iM B = 0 * 5 to s5.0 μΜ C = 5.0 to &lt;: 30 D = &gt; 30 m replicon_ 317.2 2- (4-fluoro-phenyl) -5-methoxy-6- (1Η-pyrrole θ-yl) -benzene 弁 pfran- Formamidine 3-carboxylic acid {H NMR in CDC13: 832 (m, 1H); 7.89 (m, 2H); 7.66 (s, 1H); 7.42 (m, 1H); 7.33 (s, 1H); 7.25 ( m, 2H); 6.86 (m, 1H); 6.67 (in, 1H); 5.81 (q, 1H); 3.96 (s, 3H); 3.01 (d, 3H) (M + H) + = 365 C &lt; 1 318. 6- (3,5-dimethyl-isoazazolyl) -2- (2-ethoxy-4-fluoro-phenyl) -5-methoxy-benzofuran 1H NMR of 3-carboxylic acid formamidine in CDC13: 7.63 (s, 1H); 7.54-7.60 (m, 1H); 7.24-7.26 (m, 1H); 7.227 (s, 1H); 6.80-6.86 (t of d, 1H, J = 2.34Hz &8.21Hz); 6.75-6.79 (d of d, 1H,); J = 2.34 &amp;11.14Hz); 5.80 (brs 1H); 4.05-4.12 (q, 2H, J = 7.03Hz); 3.87 (s, 3H); 2.32 (s, 3H); 2.18 (s, 3H); 1.37-1.42 (t, 3H, J = 7.03Hz) (M + H) + = 439.1 A &gt; 30 319. 2- (4- (methanesulfonyl-methyl-amino) -5- (thiazol-4-ylmethoxy) -benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO : 9.17 (d, 1H, J = 1.76Hz); 8.40 (brd, 1H, J = 4.69Hz); 7.95 (m, 2H); 7.86 (d, 1H, J = 2.34Hz); 7.65 (s, 1H) ; 7.39 (m, 3H); 5.39 (s, 2H); 3.20 (s, 3H); 2.97 (s, 3H); 2.85 (d, 3H, J = 4.69Hz) (M + H) + = 490 B &lt; 1 320. 2- (4-Gasyl-benzyl) -6- (methanesulfonyl-methyl-amino) -5- (2-methyl-oxan-4-ylmethoxy ) -Benzofuran carboxylic acid amidine 1H NMR in DMSO: 8.41 (brd, 1H, J = 4.10Hz); 7.95 (m, 2H); 7.64 (s, 1H); 7.60 (s, 1H); 7.38 (m, 3H); 5.28 (s, 2H); 3.20 (s, 3H); 3.00 (s? 3H); 2.85 (d, 3H, J = 4.69Hz); 2.68 (s, 3H) (M + H) + = 504 A &lt; 1 321. 5- (3-Chlorofluorenyl- [1,2,4] ¥ 2. Sit-5-yloxy tomb) -2- (4-lactyl-phenyl) -6- (methanesulfonate Fluorenyl-methyl-amino) -benzofuran-3-carboxylic acid formamidine 1H NMR in DMSO: 8.49 (brd, 1H, J = 4.69Hz); 8.19 (s, 1H); 7.99 (m, 2H ); 7.90 (s, 1H); 7.43 (t, 2H, J = 8.79Hz); 4.74 (s, 2H); 3.16 (s, 3H); 3.10 (s, 3H); 2.82 (d, 3H, J = 4.10Hz) (M + H) + = 524.9 A &lt; 1 322.2 2- (4-Fluoro-phenyl) -6-{[2- (4-fluoro-phenyl) _2 side-group-ethyl] -formyl-amino group- 5-isopropoxy-benzoxan-3-carboxylic acid formamidine 1H NMR in DMSO: 8.40 (d, J = 4.4Hz, 1H); 7.90 (m, 2H); 7.37 (t, J = 8.8 Hz, 2H); 7.30-7.10 (m, 6H); 5.50 (m, 1H); 4.78 (septet, J = 6.lHz, IH); 4.50 (m, 1H); 3.90 (m, 1H); 3.42 ( m, 1H); 3.00 (s, 3H); 2.82 (d, J = 4.2Hz, 3H); 1.31 (d, J = 6.1Hz, 6H) (M + H) + = 559 A &lt; 1 323. 2- (4-Fluoro-phenyl) -5-methoxy-6- (2-methyl-2fluorene- [1,2,4] -trimethyl-3-yl) -benzene 1H NMR in DMSO: 8.46-8.48 (d, 1H, J = 4.69Hz); 8.01 (s, 1H); 7.94-7.99 (ra, 2H); 7.71 (s, IH); 7-36-7.43 (t, 2H, J = 8.79Hz); 7.31 (s, 1H); 3.89 (s, 3H); 3.69 (s, 3H); 2.86-2.87 (d, 3H, J = 4.69Hz) (M + H) + = 381 A &lt; 1 211-88828.doc 200418452 Instance data name NMR data Mass Spec HCV pol -BB7 IC50 (fiM) A = μ, M. B = to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ Replicon (_ 324.5 bis (3,5-dimethyl-isopurazolidinylmethoxy) -2- (4-amino-phenyl) -6- (formamidinesulfonyl-methyl -Amine) -benzofuran-3-carboxylic acid formamide 1H NMR in DMSO: 8.45 (brd, 1H, J = 4.69Hz); 7.94 (m, 2H); 7.70 (s, 1H); 7.39 (m, 3H); 5.05 (s, 2H); 3.14 (s, 3H); 2.94 (s, 3H); 2.85 (d, 3Hf J = 4.i0Hz); 2.44 (s, 3H); 2.27 (s, 3H) ( M + H) + = 502 A &lt; 1 325. 2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5- (3-fluorenyl-benzyloxy) -benzofuran each Carboxylic acid-formamide 1H NMR in DMSO: 8.40 (brdT 1H, J = 4.10Hz); 7.93 (m, 2H); 7.70 (s, 1H); 7.42-7.31 (iru 4H); 7.12 (m, 2H) ; 6.92 (d, 1H, J = 8.21Hz); 5.21 (s, 2H); 3.77 (s, 3H); 3.21 (s, 3H); 2.97 (s, 3H); 2.84 (d, 3H, J = 4.10 Hz) (M + H) + = 513 A &lt; 1 326. hydrazone (4-fluoro-phenyl) -5-hydroxy-6- (isobutyl-methanepic acid-amine) -benzofuran-3-carboxylic acid-methaneamine NMRinDMSO : 10.05 (s, 1H); 8.40 (d, J = 4.4HzT 1H); 7.93 (dd, J = 5.3 & 8.8Hz, 2H); 7.48 (s, 1H); 7.35 (t, J = 8.8Hz, 2H); 7.10 (s, iH); 3.40 (d, J = 7.5Hz, 2H); 2.98 (s, 3H); 2.80 (d, J = 4.4Hz, 3H); 1.50 (m, 1H); 0.88 ( d, J = 6.6Hz, 6H) (M + H) + = 435 B &lt; 30 327. 2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5- (4-methoxy- + oxy) -benzoyl- 3-carboxylic acid-formamidine 1H NMR in DMSO: 8.40 (brd, 1H, J = 4.69Hz); 7.94 (m, 2H); 7.66 (s, 1H); 7.47 (d, 2H, J = 8.79Hz) ; 7.39 (m, 3H); 6.98 (d, 2H, J = 8.79Hz); 5.15 (s, 2H); 3.78 (s, 3H); 3.17 (s, 3H); 2.90 (S, 3H); 2.85 ( d, 3H, J = 4.69Hz) '(M + H) &quot; = 513 A &lt; 1 328.2 2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5- (pyridin-4-ylmethoxy) -benzofuran-3 -Carboxylic acid-formamide NMR in DMSO: 8.62 (d, 2H, J = 5.86Hz); 8.40 (brd, 1H, J = 4.69Hz); 7.93 (m, 2H); 7.74 (s, 1H); 7.55 (d, 2H, J = 5.28Hz); 7.39 (t, 2H, J = 8.79Hz); 7.31 (s, 1H); 5.32 (s, 2H); 3.26 (s, 3H); 3.02 (s, 3H ); 2.83 (d, 3H, J = 4.69Hz) (M + H) + = 484 A &lt; 1 329. 5- (2,2-Difluorenyloxy-4H-benzo [1,3] -diginyl-6-ylmethoxy) -2- (4-fluoro-benzene ; &)-6- (methanesulfonyl-fluorenyl-amino) -benzofuran-3-carboxylic acid sulfonamide * H NMR in DMSO: 8.41 (brd, 1H, J = 4.69 Hz); 8.06 (s, 1H); 7.94 (m, 2H); 7.87 (dd, 1H, J = 8.21 &amp;2.34Hz); 7.69 (s, 1H); 7.37 (ra, 3H); 7.19 (d, 1H, J = 8.79Hz); 5.27 (s, 2H); 3.20 (s, 3H); 2.95 (s, 3H); 2.84 (d, 3H, J = 4.69Hz); 1.72 (s, 6H) (M + H) + = 583 A &lt; 1 330. 6- (Cyclopropylmethyl-methanesulfonyl-amino) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-methyl Amidine NMR in DMSO: 8.44 (m, 1H); 7.94 (dd, J = 5.9 & 9.4Hz, 2H); 7.62 (s, 1H); 7.38 (ζ J = 8.8Hz, 2H); 7.20 (s , 1H); 3.90 (s, 3H); 3.44 (m, 2H);? .92 (s, 3H); 2.84 (d, J = 4.7Hz, 3H); 0.87 (m, 1H); 0.35 (d, J = 1.7Hz, 2H); 0.05 (m, 2H) (M + H) + = 447 A &lt; 1 331.2 2- (4-Fluoro-phenyl) -6 '' (methanesulfonyl-methylaminomethylmethylmethyl-amino) -5-methoxy-benzocran-3 -Folic acid-formamidine 4 醯 NMR in DMSO: 8.42 (m, 1H); 7.94 (dd, J = 5.9 & 9.4 Hz, 2H); 7.90 (s, 1H); 7.83 (m, 1H); 7.38 ( t, J = 8.8 Hz, 2H); 7.20 (s, 1H); 4.17 (s, 2H); 3.92 (s, 3H); 3.12 (s, 3H); 2.84 (d, J = 4.7Hz, 3H); 2.58 (dT J = 4.7Hz, 3H) (M + H) + = 464 A &lt; 1 212- 88828.doc 200418452 Example number name NMR data Mass Spec HCV pol -BB7 IC50 (μΜ) A = μΜ B = to ^ 5.0 / iM C = 5.0 to ^ 30 / iM D = &gt; 30 μΜ Copy (ΜΜ) 332.5 5-formyl-2- (4-amino-phenyl) -6-methanesulfonylamino-benzo-p-furan-3 -formylmethanamine 1H NMR in CDC13: 7.89-7.85 (m, 2H); 7.87 (d, J = 6.3 Hz, 1H); 7.70 (d, J = 9.9 Hz, 1H); 7.24-7.19 (m, 2H); 656 (s, 1H); 5.74 (s, 1H); 3.04 (s, 1H); 2.99 (d, J = 4.8Hz, 3H) (M + H) + = 381 B &lt; 10 333. 6- (ethyl-methanesulfonyl-amino) -5-fluoro Dong (4-fluoro-phenyl) -benzofuran-3-carboxylic acid-formic acid amine 1H NMR in CDC13 : 7.90-7.86 (m, 2H); 7.66 (d, J = 10.5 Hz, 1H); 7.57 (d, J = 6.0 Hz, 1H); 7.24-7.18 (m, 2H); 5.74 (s, 1H); 3.77 (q, J = 2.4 & 14.4 Hz, 2H); 2.99-2.98 (m, 6H); U7 (t, J = 7.5 Hz, 3H) (M + H) + = 409 A &lt; 10 334. 2- (4-Gasyl-benzyl) -6- (1-methanesulfonyl-pyrrolidin-3-yl) -5-methoxy-benzoanan-3-¾ acid -Formamidine * H NMR in CDCb: 7.85 (m, 2H); 7.36 (s, 1H); 7.32 (s, 1H); 7.20 (m, 2H); 5.78 (brs, 1H); 3.91 (s, 3H ); 3.83 (m, 2H); 3.60 (m, iH); 3.47 (m, 1H); 3.00 (d, J = 4.8Hz, 3H); 2.87 (s, 3H); 2.34 (m, 1H); 2.16 (m, 1H) (M + H) + = 447 A &lt; 1 335.5: ethyl-2: (4: formyl-phenyl) -6- [methanesulfonyl- (2-methoxy-ethyl) &gt; amino] benzofuran-3 -Chloric acid_formamidine j ---- * H NMR in DMSO: 8.45 (ra, 1H); 7.94 (dd, J = 5.3 & 9.4 Hz, 2H); 7.78 (s, 1H); 7.56 (s , 1H); 7.39 (t, J = 8.8Hz, 2H); 3.32 (in, 2H); 3.30 (s, 3H); 3.13 (s, 3H); 2.84 (d, J = 4.7 Hz, 3H); 2.82 (q, J = 7.1Hz, 2H); 1.24 (t, J = 7.1 Hz, 3H) (M + H) + = 449 A &lt; 1 336.2 2- (4-fluoro-phenyl) -5-methoxy-6- (3-methoxymethyl-5-methyl-isoxazol-4-yl &gt; Pyran-3-carboxylic acid-formamidine * H NMR in CDC13: 7.87 (dd, J = 7.0 and 5.1Hz, 2H); 7.41 (s, 1H); 7.40 (s, 1H); 7.20 (t, J = 8.8Hz, 2H); 5.81 (brs, 1H); 4.45 (s, 2H); 3.86 (s, 3H); 3.30 (s, 3H); 3.00 (d, J = 4.8Hz, 3H); 2.35 (s, 3H) (M + H) + = 425 A &lt; 1 337. 5-Ethyl-6-[(2-fluoro-ethyl) -fluorene-continuous-amino-amino] -2- (4-fluoro-phenyl) benzofuran-3- Carboxylic acid-formamide * H NMR in DMSO: 8.47 (m, 1H); 7.94 (dd, J = 5.3 & 8.8Hz, 2H); 7.84 (s, 1H); 7.57 (s, 1H); 7.39 ( t, J = 8.8Hz, 2H); 4.65-4.25 (m, 2H, F-coupling); 3.98 (t, J = 4.1Hz, 1H); 3.89 (t, J = 4.1Hz, 1H); 3.14 (s , 3H); 2.84 (d, J = 4.7Hz, 3H); 2.82 (q, J = 7.6Hz, 2H) 1.24 (t, J = 7.6Hz, 3H) (M + H) + = 437 A &lt; 1 38. 2- (4-Fluoro-phenyl) -6- (methylfetrapyridyl-propyl-amino) -5-propoxy-benzofuran-3carboxylic acid-pyridamine lH NMR in DMSO: 8.40 (d, J = 4.7Hz, iH); 7.90 (m, 2H); 7.56 (s, 1H); 7.36 (t, J = 8.2Hz, 2H); 7.17 (s, 1H); 4.04 (t, J = 6.5Hz, 2H); 3.53 (s, 2H); 2.99 (s, 3H); 2.82 (d, J = 4.7Hz, 3H); i.80 (m, 2H); 1.39 (m , 2H); 1.02 (t, J = 7.6Hz, 3H); 0.85 (t, J = 4.1Hz, 3H) (M + H) + = 463.1 A &lt; 1 339.3 5-ethyl-2- (4-fluoro-phenyl) -6- (1- # presenting group-1-methyl-ethyl) -benzofuran-3-carboxylic acid-formyl Amidine NMR in CDCl3:, 7.90 (m, 2H); 7.66 (s, IH); 7.65 (s, IH); 7.17 (m, 2H); 5.80 (brs, 1H); 3.08 (q, J = 7.5Hz , 2H); 3.02 (d, J = 4.8Hz, 3H); 1.73 (s, 6H); 1.33 (t, J = 7.5Hz, 3H) (M + H) f = 356.1 A &lt; 1 34.6. 6-Ethyl-5-ethyl-2_ (4-fluoro-phenyl) -phenylsulfan-3-carboxylic acid-formamide NMR in CDCb: 7.95 (m, 2H ); 7.80 (s, iH); 7.69 (s, IH); 7.19 (m, 2H); 5.82 (brs, 1H); 3.01 (d, J = 4.8Hz, 3H); 2.62 (s, 3H); 2.97 (q, J = 7.5Hz, 2H); 1.22 (U = 7.5Hz, 3H) (M + H) + = 340.1 A &lt; 1 213- 88828.doc 200418452 Example No. Name NMR data Mass Spec HCV pol -BB7 ICso (mM) A = / iM B = 0.5 · 5 to 彡 5.0 μΜ C = 5.0 to &lt; 30 μM D = &gt; 30 replicon (iM) 341.4 4-ranyl-6-ethylamino-2- (4-fluorophenyl) -5-hydroxybenzofuran-3-gui Acid-formamide NMR in DMSO: 9.82 (s, 1H); 8.38 (d, J = 4.4 Hz, 1H); 7.88 (dd, J = 8.8, 5.3 Hz, 2H); 7.35 (tT J = 8.8 Hz, 2H); 6.89 (s, 1H); 4.48 (t, J = 7.0 Hz, 1H); 3.37 (q, J = 7.0 Hz, 2H); 2.80 (d, J = 4.4 Hz, 3H); 1.07 (t, J = 7.0 Hz, 3H) (M + H) + = 363 B &gt; 100 342. Methanesulfonyl 4-chloro-6-ethylamino-2- (4-amino-phenyl) methyl Aminopyrene-benzo-2-an-5-yl radical NMR in DMSO: 8.42 (dT J = 3.7 Hz, 1H); 7.90 (dd, J = 8.8,5.3 Hz, 2H); 7.46 (s, 1H) ; 7.37 (t, J = 8.8 HzT 2H); 4.96 (t, J = 6.8 Hz, 1H); 3.48 (s, 3H); 3.39 (pent, J = 7.0 Hz, 2H); 2.80 (d, J = 3.7 Hz, 3H); 1.10 (U = 7-0 Hz, 2H) (M + H) + = 441 A &lt; 10 343. Methyl-2- (4-fluoro-phenyl) -6- (methanesulfonyl-pyrimazol-4-ylmethyl-amine) Amidine 1H NMR in DMSO: 9.06 (d, J = 1.8Hz, 1H); 8.43 (m, 1H); 7.91 (dd, J = 5.3 & 8.8 Hz, 2H); 7.59 (s, 1H); 7.45 ( m, 2H); 7.38 (t, J = 8.8Hz, 2H); 5.01 (d, J = 4.9Hz, 1H); 4.83 (d, J = 4.9Hz, 1H); 3.14 (s, 3H); 2.81 ( d, J = 4.7Hz, 3H); 2.65 (q, J = 7.6Hz, 2H); 1.24 (t, J = 7.6Hz, 3H) (M + H) + = 488 A &lt; 1 344. 6- (5-Cyclopropyl-3-methoxymethyl · iso-p-wow ice sheet) (4-fluoro-phenyl) -5-methoxybenzo 4-ran-3-carboxy Acid-formamidine 1H NMR in CDCb: 7.87 (dd, J = 8.8 and 5.4Hz, 2H); 7.46 (s, 1H); 7.41 (s, 1H); 7.20 (apparent t, J = 8.8 and 8.4Hz, 2H); 5.80 (brs, 1H); 4.44 (s, 2H); 3.87 (s, 3H); 3.28 (s, 3H); 3.00 (d, J = 5.1Hz, 3H); 1.92 (m, 1H); 1.13 (m, 2H); 0.97 (m, 2H) (M + H) + = 451 A &lt; 1 345. 6- (1-Ethyl-p-pylonol-3-yl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid -Formamidine 1H NMR in CDC13: 7.85 (m, 2H); 7.32 (m, lH); 7.25 (m, 3H); 5.77 (brs.lH); 3.92 (s, 3H); 3.71-4.12 (m, 2H); 3.32-3.70 (m, 3H); 2.99 (d, J = 4.8Hz, 3H); 2.18-2.39 (m, 2H); 2.10 (s, 3H) (M + H) + = 411 A &lt; 10 346. 5- (3,4-difluoro-benzyloxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzo Furan-3-carboxylic acid-formamidine * Η NMR in DMSO: 8.39 (d, J = 4.4Hz, 1H); 7.91 (m, 2H); 7.70 (s, IH); 7.55-7.30 (m, 6H) ; 5.21 (s, 2H); 3.18 (s, 3H); 2.96 (s, 3H); 2.82 (mT 3H) (M + H) + = 519.0 A &lt; 1 347. 5- (2-Difluorofluorenyl-benzyloxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzo Furan carboxylic acid-formamide 1H NMR in CDCb: 7.86 (m, 2H); 7.57-7.42 (m, 3H); 7.31-7.20 (m, 5H); 6.63 (t, 1H, J = 73.4Hz); 5.74 (brs, 1H); 5.24 (s, 2H); 3.28 (s, 3H); 2.99 (d, 3H, J = 4.84Hz); 2.81 (s, 3H) (M + H) + = 549 A &lt; 1 348. 2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-yl) -5-propoxy-benzofuran each carboxylic acid-fluorenamine'H NMR in DMSO: 8.39 (brd, 1H, J = 5.86); 7.92 (m, 2H); 7.60 (s, 1H); 7.36 (t, 2H, J = 8.79Hz); 7.18 (s, 1H); 4.04 (t , 2H, J = 7.03); 3.20 (s, 3H); 3.02 (s, 3H); 2.82 (d, 3H, J = 4.10Hz); 1.82 (m, 2H): 1.03 (t, 3H, J = 7.03 Hz) (M + H) + = 435 A &lt; 1 214- 88828.doc 200418452 Example No. Name NMRdata Mass Spec HCV pol -BB7 ICsoOiM) A = μΜ B = to ^ 5.0 μΜ C = 5.0 to &lt; 30 μΜ D = &gt; 30 μΜ name (μΜ) 349.5 5-methylpropoxy-2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino)- Benzofuran-3-carboxylic acid-formamidine 1U NMR in DMSO: 8.37 (brm, 1H); 7.92 (m, 2H); 7.63 (s, 1H); 7.36 (t, 2H, J = 8.79Hz); 7.21 (s, 1H); 6.18-6.06 (m, 1H); 5.47 (m, 1H); 5.30 (m, 1H); 4.70 (d, 2H, J = 4.69Hz); 3.20 (s, 3H); 3.02 (s, 3H); 2.82 (d, 3H, J = 4.10Hz) (M + H) + = 433 A &lt; ι 350. 6- (5-ethoxymethyl-isoamyl-3-yl) -2- (4-amino-phenyl) -5-methoxy-benzofuran-3- # complex Acid-formamide 1H NMR in CDC13: 8.03 (s, 1H); 7.87 (dd, J = 5.28 & 8.79Hz, 2H); 7.45 (s; IH); 7.20 (ζ J = 8.79Hz, 2H); 6.82 (s, 1H); 5.79 (bs, 1H); 4.64 (s, 2H); 3.96 (s, 3H); 3.65 (q, J = 7.03Hz, 2H); 3.00 (d, J = 4.84Hz, 3H ); 1.276 (t, J = 7.03, 6.59Hz, 3H) (Μ + ΗΓ = 425.21 A &lt; 1 351. 5-Cyclopropylmethoxy-2- (4-fluoro-phenyl) -6- (methane continuous-methyl-amino-)-benzofuran-3-carboxylic acid-methyl Lamine 1H NMR in DMSO: 8.38 (d, J = 4.4Hz, 1H); 7.92 (m, 2H); 7.60 (s, 1H); 7.38 (tt J = 9.2Hz, 2H); 7.16 (s, 1H) ; 3.95 (d, l = 7.0Hz, 2H); 3.25 (s, 3H); 3.08 (s, 3H); 2.83 (d, J = 4.4Hz, 3H); 1.20 (m, 1H); 0.62 (d, J = 7.0Hz, 2H); 0.39 (d, J = 5.3Hzi 2H) (M + H) + = 447 A &lt; 1 352.5 5- (3,5-Dimethoxy-benzyloxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzene Benzofuran-3-¾ acid-formamidine'H NMR in DMSO: 8.39 (brd, 1H, J = 4.69); 7.93 (ra, 2H); 7.71 (s, 1H); 7.38 (t, 2H, J = 8.79); 7.31 (s, 1H); 6.72 (d, 2H, J = 2.34); 6.46 (m, 1H); 5.17 (s, 2H); 3.75 (s, 6H); 3.22 (s, 3H); 3.00 (s, 3H); 2.83 (d, 3H, J = 4.69Hz) · (M + H) + = 543 A &lt; i 353. 2- (4-Fluoro-phenyl) -5- (4-methanesulfonyl-benzyloxy) -6- (methylsulfanyl-methyl-amino) -benzo Furan-3-metanoic acid-amidamine * H NMR in DMSO: 8.39 (brd, 1H, J = 4.40Hz); 7.98-7.89 (m, 4H); 7.80 (dt 2H, J = 8.4Hz); 7.7 i (s, 1H); 7.37 (m, 3H); 5.36 (s, 2H); 3.28 (s, 3H); 3.22 (s, 3H); 2.98 (s, 3H); 2.8 l (d, 3H, J = 4.40Hz) (MH) '= 559 A &lt; 1 354.2 2- (4-Amino-winteryl) -5_hydroxy-6- [methanesulfonyl- (2-oxy · propyl) -amino] -benzofuran-3-chinic acid · Formamidine 1H NMR in CDCb: 8.15 (s, 1H); 7.93 (in, 2H); 7.39 (s, 1H); 7.15 (t, J = 2.5Hz, 2H); 5.79 (s, 1H); 4.54 (s, IH); 4.49 (s, 1H); 334 (s, 3H); 3.24 (s, 1H); 3.19 (s, 1H); 1.79 (s, 2H) (Μ + ΗΓ = 437.22 B &lt; 10 355.2 2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5- [2- (4-methoxy-phenyl) _2_oxy -Ethoxy] -benzofuran-3-carboxylic acid-formamidine 1H NMR in DMSO: 8.36 (d, J = 4.8Hz, lH); 8.04 (d, J = 8.79Hz, 2H); 7.90 ( m, 2H); 7.60 (s, 1H); 7.36 (t, J = 8.79Hz, 2H); 7.28 (s, 1H); 7.08 (dt J = 9.35Hz, 2H); 5.67 (s, 2H); 3.86 (s, 3H); 3.29 (s, 3H); 3.07 (s, 3H); 2.77 (d, J = 4.41Hz, 3H) (Μ + ΗΓ = 541 A &lt; 1 215- 88828.doc 200418452 Example number name NMR data Mass Spec HCV pol -BB7 IC50〇tM) A = / iM B = 0〇to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ Replicon (μΜ) 356.5 5- (3 · Cyano-Ethyloxy) -2- (4-amino-phenyl) -6-(methanesulfonyl-methyl-amino) · benzofuran -3-carboxylic acid-formamidine 1H NMR in DMSO: 8.39 (brd, 1H, J = 4.69Hz); 8.00 (s, 1H); 7-94- 7.81 (m, 3H); 7.72 (s, 1H) ; 7.64 (t, 2H, J = 7.62Hz); 7.37 (t, 2H, J = 8.79Hz); 7.30 (s, 1H); 5.29 (s, 2H); 3.19 (st 3H); 2.97 (s, 3H ); 2.82 (d, 3H, J = 4.69Hz) (M-Η). = 506 A &lt; 1 357. Methyl-fluorenyl) -2- (4-fluoro-winteryl) -6- (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine Amine'H NMR in DMSO: 8.37 (brd, 1H, J = 4.84Hz); 7.90 (m, 4H); 7.72 (m, 3H); 7.37 (t, 2H, J = 8.79Hz); 730 (s, 1H ); 5.33 (s, 2H); 3.21 (s, 3H); 2.97 (s, 3H); 2.81 (d, 3H, J = 4.0Hz) (M + H) + = 508 A &lt; 1 358.2. 2- (4-Amino-phenyl) -5-methoxy-6- (2H- [1,2,4] triazol-3-yl) -benzofuran-3-dec 1HNMR in CDCl3: 8.49 (s, 1H); 8.05 (s, 1H); 7.86-7.91 (m, 2H); 7.58 (s, 1H); 7.20-7.26 (m, 2H); 5.82 (brs , 1H); 4.15 (s, 3H); 3.00-3.02 (d, 3H, J = 5.28Hz) (M + H) + = 366 GCMS A &lt; 1 35. 4- {2- [2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -3-methylaminomethyl-benzo-benzo Furan-5-yloxy] -ethylammonium aminopeptanoic acid ethyl ester'H NMR in DMSO: 10.37 (s, 1H); 8.39 (brd, 1H, J = 4.84Hz); 7.91 (m, 4H) ; 7.75 (d, 2H, J = 8.35Hz); 7.70 (s, 1H); 7.37 (t, 2H, J = 8.79Hz); 7.20 (s, 1H); 4.93 (s, 2H); 4.28 (q, 2H, J = 7.03Hz); 3.28 (s, 3H); 3.14 (s, 3H); 2.78 (d, 3H, J = 4.40Hz); 1.30 (t, 3H, J = 7.03Hz) (M-Η) '= 596 A &lt; 10 360. 2- (4-Gas-phenyl) -5- [2- (4-fluoro-phenyl) -2-oxy-ethoxy] -6- (methanesulfonyl- Methyl-amino) -benzofuran-3-carboxylic acid-methaneamine 1H NMR in DMSO: 8.38 (brd, 1H, J = 5.28Hz); 8.17 (m, 2H); 7.90 (m, 2H); 7.62 (s, 1H); 7.45-7.31 (m, 5H); 5.73 (s, 2H); 3.29 (s, 3H); 3.06 (s, 3H); 2.78 (d, 3H, J = 4.69Hz) (MH ) · = 527 A &lt; 1 36. 6- (fluorenyl-methanesulfonyl-amino) -2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-chi SH-formamidine Amine * H NMR in DMSO: 8.38 (brd, 1H, J = 4.69Hz); 7.86 (m, 2H); 7.33 (t, 2Ht J = 8.79Hz); 7.28-7.16 (m, 6H); 7.10 (s, 1H); 4.80 (brm, 3H); 3.11 (s, 3H); 2.79 (d, 3H, J = 4.69Hz); 1.38 (d, 6H, J = 5.86Hz) (M + H) + = 511 A &lt; 1 362.6 4-Chloro-6- (ethyl-methyl-amino) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid- Formamidine 1H NMR in DMSO: 8.38 (d, J = 4.4HzT 1H); 7.90 (m, 2H); 7.36 (t, J = 8.4Hz, 2H); 7.05 (s, 1H); 3.86 (s, 3H ); 3.09 (q, J = 7.03Hz, 2H); 2.81 (d, J = 4.4Hz, 3H); 2.75 (s, 3H); 0.93 (t, J = 7.1Hz, 3¾ (Μ + ΗΓ = 391.0 A &lt; 10 363. 4-Chloro-6-ethylamine ^ yl-2- (4-fluoroyl-benzene: ^)-5-methoxy-toluene-benzofuran-3.-carboxylic acid-formyl Lamine 1H NMR in DMSO: 8.34 (d, J = 4.8Hz &gt;1H); 7.86 (m, 2H); 7.33 (t, J = 9.2Hz, 2H); 6.99 (s, 1H); 4.67 (t, J = 6.6Hz, 1H); 3.89 (s, 3H); 3.38 (q, J = 7.04Hz, 2H); 2.80 (d, J = 4.4Hz, 3H); 1.07 (t, J = 7.0Hz, 3H) ( M + H) + = 377.0 A &lt; 1 216- 88828.doc 200418452 Example number name NMR data Mass Spec HCV pol -BB7 ICse 〇iM) A = μΜ B = 0.5 to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 / iM replicon (μΜ) 364.6 6-Ethylamino-2- (4-amino-phenyl) -5-hydroxy-benzofuran-3-carboxylic acid-formamidine * H NMR in DMSO: 8.20 (d, J = 4.7Hz, iH); 7.88 (dd, J = 8.8, 5.3Hz, 2H); 7.29 (t, J = 8.8Hz, 2H); 6.83 (s, 1H); 6.66 (s, 1H); 4.83 ( t, J = 5.0Hz, 1H); 3.11 (ra, 2H); 2.79 (d, J = 4.7Hz, 3H); 1.19 (t, J = 7.0Hz, 3H) * (M + H) + = 329 B &gt; 30 36. 5_ (3-bromo-propoxy) -6- 6-aminoamino-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid-methaneamine 1H NMR in DMSO: 8.30 (d, J = 4.7Hz, 1H); 7.86 (dd, J = 8.8, 5.3Hz, 2H); 7.30 (t, J = 8.8Hz, 2H); 6.93 (s, 1H); 6.75 ( s, 1H); 5.20 (t, J = 5.0Hz, IH); 4.14 (t, J = 4.8Hz, 2H); 3.78 (t, J = 6.7Hz, 2H); 3.20 (m, 2H); 2.81 ( d, J = 4.7HzT 3H); 2.36 (m, 2H); 1.23 (t, J = 7.0Hz, 3H) (M + H) + = 499,451 A &lt; 1 366. 5-Hydroxypropoxy-6-ethylamino-2- (4-fluoro-phenyl) -benzoanan-3 -chitoic acid · methanamine'HNMR in DMSO: 8.20 (d, J = 4.7Hz, 1H); 7.80 (dd, J = 8.8, 5.3Hz, 2H); 7.31 (t, J = 8.8Hz, 2H); 6.93 (s, 1H); 6.74 (s, 1H) ; 6.10 (m, 1H); 5.50 (m, 1H); 5.30 (m, 1H); 5.00 (t, J = 5.0Hz, 1H); 4.60 (m, 2H); 3.18 (m, 2H); 2.80 ( d, J = 4.7Hz, 2H); 1.20 (t, J = 7.0Hz, 3H) (M + H) + = 369 A &lt; 1 367. 5- (3-ethoxy-propoxy tomb) -6-ethylamino-2- (4-fluoroxylbenzoanan-3-metanoic acid-formamidine 1H NMR in DMSO: 8.20 (d, J = 4.4Hz, 1H); 7.80 (dd, J = 8.8, 5.3Hz, 2H); 7.31 (t, J = 8.8Hz, 2H); 6.90 (s7 1H); 6.72 (s, 1H); 5.01 (U = 5.7Hz, 1H); 4.07 (ζ J = 6.5Hz, 2H); 3.56 (UJ = 6.4Hz, 2H); 3.42 (q, J = 7.0Hz, 2H); 3.20 (m, 2H); 2.80 (d, J = 4.4Hz, 3H); 2.00 (t, J = 6.5Hz, 2H); 1.20 (t, J = 7.0Hz, 3H); 1.10 (t, J = 7.0Hz, 3H) (M + H) + = 415 A &lt; 1 368. 2- [2- (4-Ranyl-phenyl) -5-methoxy-3-methylamine formamidine-benzofuran-6-yl] -pyrrole sulfonate Amine * H NMR in CDC13: 7.83 (m, 2H); 7.15 (s, 1H); 7.14 (s, 1H); 7.10 (m, 2H); 5.76 (brs, 1H); 5.18 (d, J = 8.353Hz , 1H); 4.25 (s, 2H); 3.93 (s, 3H); 3.72 (m, 2H); 2.99 (d, J = 4.836Hz? 3H); 1.89 (m, 2H); 1.25 (s, 2H) (M + H) + = 412 A &lt; 1 369. 2- (4-Gas-phenyl) -6_ (methanesulfonyl-methyl-amino) -5- (2-oxy-propoxy) -benzonan-3 -Carboxylic acid-formamide NMR in DMSO: 8.38 (brd, 1H, J = 4.69Hz); 7.90 (m, 2H); 7.62 (s, 1H); 7.36 a 2H, J = 8.79Hz); 7.12 (s , iH); 4.97 (s, 2H); 3:24 (s, 3H); 3.04 (s, 3H); 2.81 (d, 3H, J = 4.10Hz); 2.20 (s, 3H) (MH) * = 447 A &lt; 1 37. 2- (4-Fluoro-phenyl) -5- (2-hydroxy-propoxy) -6- (methanesulfonyl-methyl-amino) -benzofuran-3- Carboxylic acid-amine NMR ia DMSO: 8.41 (brd, 1H, J = 4.69Hz); 7.94 (m, 2H); 7.60 (s, 1H); 7.38 (t, 2H, J = 8.79Hz); 7.20 ( s, 1H); 4.87 (d, 1H, J = 4.69Hz); 4.06 (m, iH); 3.96 (m, 2H); 3.24 (s, 3H); 3.06 (s, 3H); 2.84 (d, 3H , J = 4.69Hz); 1.22 (d, 3H, J = 5.86) (MH) '= 449 A &lt; 1 371. _2- (4--Fluoro-phenyl) each (methanesulfonyl-methyl-amino) -5- (1-methyl-1H-tetramethyl-5-ylmethoxy ) -Benzofuran-3-carboxylic acid-formamidine 1H NMR ia DMSO: 8.44 (brd, iHt J = 4.10Hz); 7.94 (in, 2H); 7.76 (s, 1H); 7.48 (s, 1H) ; 7.40 (t, 2H, J = 8.79); 5.65 (s, 2H); 4.18 (s, 3H); 3.18 (s, 3H); 3.02 (s, 3H); 2.86 (d, 3H, J = 4.10Hz ) (Μ + ΗΓ = 489 A &lt; 1 217- 88828.doc 200418452 Example number name NMR data Mass Spec HCV pol -BB7 IC50 〇iM) A = μΜ 0 * 5 to 彡 5.0 fiM C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ replicon ( μM) 372.2 2- (4-Fluoro-phenyl) -6- (5-isopropoxymethyl-isopentetyl) -5-methoxy-benzofuran-3-carboxylic acid-methyl Lamine 1HNMR in CDC13: 7.96 (s, 1H); 7.85 (dd, J = 5.28 &amp; 8.79Hz, 2H); 7.40 (s, 1H); 7.18 (t, J = B.35 & 8.79Hz, 2H) ; 6.78 (s, 1H); 5.98 (bs, 1H); 4.64 (s, 2H); 3.94 (s, 3H); 3.78 (septet, J = 6.15Hz, 1H); 3.01 (d, J = 4.83Hzt 3H ); 1.25 (d, J = 6.15Hz, 6H) (M + H) + = 439 A &lt; 1 373. 5- (5-Diethylamino- [1,2,4] pyridine 3-ylmethoxy) -2- (4-fluoroyl-phenyl) 6- (methane Sulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-methaneamine 1H NMR in DMSO: 838 (brd, 1H, J = 4.40Hz); 7.94 (m, 2H); 7.61 (s , 1H); 7.37 (m, 3H); 5.22 (s, 2H); 3.47 (brm, 4H); 3.28 (s, 3H); 3.08 (s, 3H); 2.84 (d, 3H, J = 4.84Hz) ; 1.18 (t, 6H, J = 7.03Hz) (M + H) + = 562 A &lt; 1 374. 5- [5- (Cyclopropylmethyl-amine tomb)-[1,2, exobijun-3-ylmethoxy] -2 &lt; 4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino-benzofuran-3-guinic acid-formamidine 1H NMR in DMSO: 8.60 (bnn, 1H); 838 ( brd, 1H, J = 4.10Hz); 7.94 (m, 2H); 7.61 (s, 1H); 7.38 (m, 3H); 5.19 (brs, 2H); 3.26 (s, 3H); 3.18 (ζ 2H7 J = 5.86Hz); 3.07 (s, 3H); 2.84 (d, 3H, J = 4.69Hz); 1.10 (m, 1H); 0.48 (m, 2H); 0.24 (m, 2H) (M + H) + = 560 A &lt; 1 375.6 6- (2-Amino small hydroxy-1-methyl-ethyl) -2- (4-fluoro-phenyl) -5-isopropoxy-benzoanan-3- Formamidine chitoate'H NMR in CDCl3: 7.85 (m, 2H); 7.71 (s, 1H); 7.19 (s, 1H); 7.16 (m, 2H); 6.35 (brs, 1H); 4.76 (in, 1H); 4.60 (brs, 2H); 3.48 (m, 2H); 2.99 (d, J = 4.69 Hz, 3H); 1.47 (s, 3H); 1.40 (d, J = 5.86 Hz, 3H); 1.37 ( d, J = 5.86 Hz, 3H) (M + H) &quot; = 401.1 B &lt; 30 376. 6- (1-Amine-i-methyl-ethyl) -2- (4-fluoro-phenyl) -5-isopropoxy-benzoanan lH NMR in CDC13: 7.84 (ra, 2H); 7.49 (s, 1H); 7.37 (s, 1H); 7.26 (m, 2H); 5.74 (brs, 1H); 4.84 (septet, J = 6.15 Hz, 1H ); dd 4.53 (brs, 2H); 2.99 (d, J = 2.64 Hz, 3H); 1.67 (s, 6H); 1.47 (d, J = 6.16 Hzt 6H) (M + H) + = 386 A &lt; 1 377. 2- [2- (4-Fluoro-phenyl) -5-methoxymethylmethylformamidine-benzofuran-6-yl] -ρ-bilodine-1-read _ fee-formamidineΉ NMR in CDCI3: 7.85 (m, 2H); 734 (s, 1H); 7.30 (s, 1H); 7.18 (ra, 2H); 5.77 (s, 1H); 4.03 (d, J = 4.39 Hz, 1H); 3.94 (s, 3H); 3.71 (m, 2H); 2.99 (d, J = 1.32 Hz, 3H); 2.71 (d, J = 1.32 Hz, 3H); 2.38 (ra, 1H); 1.86 (m, 3H) (M + H) + = 426 A &lt; 10 378. 6- (3,5-Dimethyl-isophosphinobenzyl) _2_ (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-acetamidine Amine 1H NMR in DMSO: 8.53 (s, 1H); 7.94-7.99 (m, 2H); 7-61 (s, 1H); 7.37-7.43 (t, 2H, J = 9.38Hz); 7.22 (s, 1H ); 3.85 (s, 3H); 3.36-3.40 (t, 2H, J = 5.86Hz); 2.31 (s, 3H); 2.12 (s, 3H); 1.16-1.20 (t, 3H, J = 5.28Hz) (M + H) + = 409 A &lt; 1 • 218 · 88828.doc 200418452 1 Instance number name NMR data Mass Spec HCV pol -BB7 IC50 〇iM) A = μΜ B = 0 * 5 to 彡 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μM replicon (μM) 379.6- (3,5-dimethyl-isoxazolone) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3- Carboxylic acid-isopropylamidine 1HNMR inDMSO: 8.42-8.45 (dT 1H, J = 8.21Hz); 7.93-7.98 (m, 2H); 7.59 (s, 1H); 7.37-7.42 (U 2H, J = 8.79Hz ); 7.18 (s, 1H); 4.18-4.24 (septet, 1H, J = 7.03Hz); 3.83 (s, 3H); 2.30 (s, 3H); 2.11 (s, 3H); 1.19-1.21 (d, 6H, J = 7.03Hz) (M + H) + = 423 B &gt; 30 380. Di: methyl-isoxazole_4-yl) -2- (4-fluoro-phenyl) -5-form Oxy-benzofuran-3-metanoic acid-cyclopropylamidine 1H NMR in DMSO: 8.59-8.61 (d, 1H, J = 4.10Hz); 7.90-7.94 (m, 2H); 7.95 (s, 1H) ; 7.36-7.42 (t, 2H, J = 8.79Hz); 7.16 (s, 1H); 3.83 (s, 3H); 2.93-2.99 (m, 1H); 2.29 (s, 3H); 2.10 (s, 3H ); 0.71-0.77 (m, 2H); 0.54-0.60 (m, 2H) (M + H) + = 421 A &lt; 1 381.2 2- (4-Azo-phenyl) -5-isopropoxy-6- (5- ^ yl-2-oxy ^ oxazolyt-5-yl) -benzocran-3 -Chinoic acid-formamidine * H NMR in CDC13: 7.85 (m, 2H); 7.77 (s, 1H); 7.35 (s, 1H); 7.19 (m, 2H); 5.74 (brs, 1H); 5.03 ( brs, 1H); 4.76 (m, 1H); 3.78 (dd, J = 2.2 &amp; 8.4 Hz, 2H); 2.97 (d, J = 5.2 Hz, 3H); 1.82 (s, 3H); 1.40 (d, J = 5.2 Hz, 3H); 1.37 (d, J = 5.2 Hz, 3H) (M + H) + = 427.1 A &lt; 1 382. [2- (4-Fluoro-phenyl) -6- (methylsulfanyl-methyl-amino) -3-methylaminomethylmethyl-benzofuran-5-yl Oxy] -acetic acid tert-butyl ester 1H NMR in DMSO: 8.38 (brd, 1H, J = 4.69Hz); 7.93 (m, 2H); 7.63 (s, 1H); 738 (t, 2H, J = 8.79 Hz); 7.10 (s, 1H); 4.82 (s, 2H); 3.26 (s, 3H); 3.07 (s, 3H); 2.82 (d, 3H, J = 4.69Hz); 1.46 (s, 9H) ( M + h2〇) + = 524 A &lt; 1 383. 2- (4-Amino-phenyl) -5-methoxy-6- (5-methyl-2H- [1,2,4] triazol-3-yl) -benzo 17 Melan-3-quinic acid-formamidine * Η NMR in DMSO: 13.42 (s, 1H); 8.44-8.46 (d, 1H, J = 4.69 Hz); 8.25 (s, 1H); 7.94-7.99 (m , 2H); 7.36-7.42 (t, 2H, J = 8.79 Hz); 7.27 (s, 1H); 4.02 (s, 3H); 2.85-2.86 (d, 3H, J = 4.69 Hz); 2.34 (s, 3H) (M + H) + = 381 B &lt; 10 384. 6- (1-amino-1-methyl-ethyl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-methyl Lamine 1H NMR in CDCl3: 7.84 (m, 2H); 7.51 (s, 1H); 7.32 (s, 1H); 7.17 (1¾ 2H); 5.84 (brs, 1H); 3.95 (s, 3H); 2.97 ( d, J = 4.84Hz, 3H); 2.19 (brs, 2H); 1.59 (s, 6H) (M + H-NH2) + = 340 B &lt; 30 385. 6- (1-Ethylaminoaminomethyl-ethyl) dong (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-formamidine Amine ^ NMR in CDCI3: 7.84 (m, 2H); 7.52 (s, 1H); 7.31 (s, 1H); 7.15 (m, 2H); 6.03 (brs, 1H); 5.76 (brs, 1H); 3.92 ( s, 3H); 2.96 (d, J = 4.84Hz, 3H); 1.92 (s, 3H); 1.80 (s, 6H) (M + H-NHAc) + = 340 A &lt; 1 386. [2- (4-fluoroi-phenyl) each (methanesulfonyl-methyl-amino) each methylamine methylamidino-benzofuran-5-yloxy &gt; acetic acid lH NMR in DMSO: 8.39 (brd, 1HT J = 4.69Hz); 7.93 (m, 2H); 7.62 (s, 1H); 7.38 (t, 2H, J = 8.79Hz); 7.17 (s, iH); 4.86 (s, 2H); 3.26 (s, 3H); 3.06 (s, 3H); 2.83 (d, 3H, J = 4.69Hz) (MH) * = 449 A &lt; 30 219- 88828.doc 200418452 Example No. Name NMRdata Mass Spec HCV pol -BB7 IC5〇 (μΜ) A = &lt; 0 * 5 / iM B = 0.5 to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μ, M. Replicon (μΜ) 387.6- (2,5-dimethyl_2H- [1,2,4] triazol-3-yl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-formamidine'H NMR in DMSO : 8.45-8.47 (d, 1H, J = 4.69Hz); 7.93-7.98 (m, 2H); 7.69 (s, 1H); 7.36-7.42 α 2H, J = 8.79Hz); 7.29 (st 1H); 3.88 (s, 3H); 3.60 (s, 3H); 2.85-2.86 (d, 3H, J = 4.10Hz); 2.28 (s, 3H) (M + H) + = 395 B &lt; 10 388. _2- (4-fluoro-based box) -6: (pyridinium-methyl-amino) -5 hexetantylmethoxy) -benzofuran-3-carboxylic acid- Formamidine 1H NMR in DMSO: 8.40 (brrn, 1H); 7.95 (m, 2H); 7.89 (d, 1H, J = 2.93Hz); 7.82 (d, 1H, J = 2.93); 7.70 (s, 1H ); 7.40 (m, 3H); 5.60 (s, 2H); 3.25 (s, 3H); 3.02 (s, 3H); 2.85 (d, 3H, J = 4.69Hz) (M + H) + = 490 A &lt; 1 389. 2- (4-Fluoro-phenyl) -5 · methoxy-6- (4-methyl-2,5-dioxy-imidazol-4-yl) -benzobite 1H NMR in DMSO: 10.59 (brs, 1H); 8.37 (m, 1H); 7.96 (s, 1H); 7.94 (m, 2H); 7.71 (s, lH); 7.39 (m, 2H); 7.15 (s, lH); 3.77 (s, 3H); 2.82 (d, J = 4.8Hz, 3H); 1.71 (s, 3H) (M + H) + = 412 A &lt; 10 390. 2- (4-Fluoro-phenyl) -6- (1-methanesulfonylamino-1 -methyl-ethyl) -5-methoxy-benzofuran-3 -Carboxylic acid-formamide 1H NMR in CDC13: 7.84 (m, 2H); 7.51 (s, 1H); 7.44 (s, 1H); 7.19 (m, 2H); 5.88 (s, 1H); 5.79 (brs , 1H); 4.00 (s, 3H); 2.98 (d, J = 4.84 Hz, 3H); 2.52 (s, 3H); i.82 (s, 6H) (M + H- NH- S02Me) + = 340 A &lt; 10 391. 5- (6-Bromomethyl-pyridin-2-ylmethoxy) -6-[(6-bromofluorenyl-pyridin-2-ylmethyl) -methanesulfonyl-amino ] -2- (4-fluoro-phenyl) -benzofuran-3- # polyacid-amidamine 1H NMR in DMSO: 8.38 (d, J = 4.8 Hz, 1H); 7.90 (rat 3H); 7.73 (t, J = 7.1 Hz, 1H); 7.64 (s, 1H); 7.60 (d, J = 7.5 Hz, 1H); 7.53 (d, J = 7.5 Hz, 1H); 7.48 (d, J = 7.5 Hz, 1H); 7.37 (m, 3H); 731 (s, 1H); 5.33 (s, 2H); 4.98 (s, 2H); 4.72 (s, 2H); 4.61 (s, 2H); 3.18 (s , 3H); 2.81 (d, J = 4.8 Hz, 3H) (M + H) + = 746 A &lt; 10 392. 2- [2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) each methylamine methylamido-benzofuran-5-yloxy Methylmethyl] -thiazole-4-acid ethyl ester 1H NMR in DMSO: 8.60 (s, 1H); 8.40 (brd, 1H, J = 4.69Hz); 7.95 (m, 2H); 7.73 (s, 1H) ; 7.40 (m, 3H); 5.63 (s, 2H); 4.32 (q, 2H, J = 7.03Hz); 3.27 (s, 3H); 3.06 (s, 3H); 2.84 (d, 3H, J = 4.69 Hz); 1.32 (t, 3H, J = 7.03) (M + H) + = 562 A &lt; i 393. -2- [2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -3-methylaminofluorenyl-benzofuran-5 -Alkyloxy-B-carboxylic acid lH NMR in DMSO: t 8.52 (s, 1H); 8.41 (brd, 1H, J = 4.69Hz); 7.95 (m, 2H); 7.73 (s, 1H); 7.40 (ra , 3H); 5.61 (s, 2H); 3.26 (s, 3H); 3.06 (s, 3H); 2.85 (d, 3H, J = 4.69Hz) (M-Η) '= 532 A &gt; 30 220- 88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 ICso 〇iM) A = ^ 0.5 μΜ B = 03 to ^ 5.0 / iM C = 5.0 to ^ 30 D = &gt; 30 μΜ replicon (μΜ) 394. 6-Dimethylamino-2- (4-fluoro-phenyl) -5-methoxypyridine-benzo-p-furan-3-metanoic acid-formamidine * H NMR in CDC13: 7.85 (dd, J = 8.8 &amp; 5.3Hz, 2H); 7.26 (s, 1H); 7.17 (t, J = 8.8Hz, 2H); 7.14 (s, 1H); 5.80 (brs, 1H); 3.96 (s, 3H) ; 2.98 (d, J = 4.8Hz, 3H); 2.84 (s, 6H) (Μ + ΗΓ = 343 A &lt; 1 395.5. 5-Cyanomethoxy-2- (4-fluoro-phenyl) &gt; 6- (methanesulfonyl-methyl-amino) -benzfuran-3- leptate-formamidine Amine 1H NMR in DMSO: 8.44 (brd, 1H, J = 4.10Hz); 7.93 (m, 2H); 7.77 (s, 1H); 7.41 (m, 3H); 5.32 (s, 2H); 3.22 (s, 3H); 3.08 (s, 3H); 2.84 (d, 3H, J = 4.69Hz) (M + H) + = 432; A &lt; 1 396. 2- (4-Amino-winteryl) -6- (methanesulfonyl-methyl-amino) -5- (5-methyl-isopurazol-3-ylmethoxy) ) -Benzofuran-3: carboxylic acid-methylamine 1H NMR in DMSO: 8.40 (brd, lHt J = 4.69Hz); 7.95 (m, 2H); 7.68 (s, 1H); 7.38 (m, 3H) ; 6.40 (s, 1H); 5.30 (s, 2H); 3.21 (s, 3H); 3.00 (s, 3H); 2.84 (d, 3H, J = 4.10Hz); 2.44 (s, 3H) (M + H) + = 488 A &lt; 1 397. 5- (5-Chloro- [1,2,3] pyrimidazol-4-ylmethoxy) -12- (4-amino-benzene grave) each (methanesulfonyl- Methyl-amino) -benzofuran-3-carboxylic acid-methaneamine 1H NMR in DMSO: 8.46 (brd, 1H, J = 4.10Hz); 7.98 (m, 2H); 7.69 (s, 1H); 7.51 (s, 1H); 7.40 (t, 2H, J = 8.79Hz); 5.66 (s, 2H); 3.17 (s, 3H); 2.95 (s, 3H); 2.87 (d, 3H, J = 4.69Hz ) (M + H) + = 525 A &lt; 1 39. 2- (4-Fluoro-phenyl) -6- (methanesulfonyl-fluorenyl-amino group) &gt; 5- (1-methyl-1H-imid-2-ylmethoxy Phenyl) -benzoanan-3-guinic acid-formamidine 1H NMR in DMSO: 8.42 (brd, 1H, J = 4.69); 7.98 (m, 2H); 7.70 (s, 1H); 7.52 (s, 1H); 7.39 (t, 2H, J = 8.79); 7.21 (s, 1H); 6.91 (s, 1H); 5.27 (s, 2H); 3.74 (s, 3H); 3.15 (s, 3H); 2.94 (s, 3H); 2.87 (d, 3H, J = 4.69Hz) (M + H) + = 487 A &lt; 1 399.9 5- (1-fluorenyl-1H-imidazol-2-ylmethoxy) -2- (4-fluoro-phenyl) -6 · (methanesulfonyl-methyl-amine ) -Benzofuran-3-carboxylic acid-formamidine * Η NMR in DMSO: 8.42 (brm, 1H); 7.95 (m »2H); 7.68 (s, 1H); 7.51 (s, 1H); 7.42- 7.20 (m, 8H); 7.00 (s, 1H); 5.38 (s, 2H); 5.25 (s, 2H); 3.04 (s, 3H); 2.91 (s, 3H); 2.86 (d, 3H, J = 4.10Hz) (M + H) + = 563 A 氺 氺 氺 400. "-(2,4-difluoroyl-phenyl) -6- (3,5-dimethyl-isopyridin-4-yl ) -5-methoxy-benzofuran carboxylic acid-formamide 1H NMR in DMSO: 8.10-8.12, (d, 1H, J = 4.69Hz); 7.78-7.86 (q, 1H, J = 6.45Hz ); 7.61 (s, 1H); 7.4 ^ -7.49 (ra, 1H); 7.33 (s, 1H); 7.27-7.32 (m, 1H); 3.85 (s, 3H); 2.77-2.78 (d, 3H, J = 4.69Hz); 2.29 (s, 3H); 2.10 (s, 3H) (M + H) + = 413 A 氺 氺 氺 221-88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 ICs «( / iM) A = μΜ B = 05 to &lt;: 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ replicon (μΜ) 401.6- (3,5-dimethyl-isoimonyl f-group) _2_ (4-fluoro-fluoro Yl) -5 dexazol-4-yl methoxy axe) -benzofuran-3-rebellion-methylamine 1HNMR in DMSO: 9.13 (d, 1H, J = 1.17 Hz); 8.41-8.43 (d, 1H, J = 4.69 Hz); 7.94-7.99 (m, 2H); 7.64-7.65 (d, 1H, J = U7 Hz); 7.61 (s, 1H); 7.45 (s, 1H); 7.36-7.42 (t , 2H, J = 8.79 Hz); 5.28 (s, 2H); 2.86-2.88 (d, 3H, J = 4.69 Hz); 2.29 (s, 3H); 2.1 l (s, 3H) (M + H) + = 478 A &lt; 1 402. 5- (fluorenyl-4H- [1,2,4] three ton-3-ylfluorenyloxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl -Methyl-amino) -benzo-p-furan-3-carboxylic acid-formamidine 1H NMR in DMSO: 11.94 (brs, 1H); 8.36 (brd, 1H, J = 4.69Hz); 7.93 (m, 2H); 7.57 (s, 1H); 7.36 (m, 3H); 5.96 (brs, 2H); 5.01 (s, 2H); 3.19 (s, 3H); 2.99 (s, 3H); 2.83 (d, 3H , J = 4.10Hz) (M + H) + = 489 A &lt; 1 403. 5- (4-chloromethyl-1H-pyridin-3-ylmethoxy) -2- (4-fluoro: phenyl) -6- (methanesulfonyl-methyl -Amine) -benzopyran-3-carboxylic acid-formamidine ^ NMRinDMSO: 8.44 (brd, 1H, J = 4.69Hz); 7.96 (m, 3H); 7.62 (s, 1H); 7.47 (s , 1H); 7.38 (t, 2H, J = 8.79Hz); 5.16 (s, 2H); 3.84 (s, 3H); 3.16 (s, 3H); 2.93 (s, 3H); 2.86 (d, 3H, J = 4.69Hz) (M + H) + = 521 A &lt; 1 404.2. 2- (4-Gasyl-phenyl) -6- (methanesulfonyl-methyl-unradical) -5- (2-pbicyclo-1-ylethoxy) -benzene 1H NMR in DMSO: 8.42 (brm, 1H); 7.97-7.90 (m, 3H); 7.56 (s, 1H); 7.47 (s, 1H); 7.38 (t, 2H, J = 8.79); 7.23 (s, 1H); 6.27 (m, 1H); 4.60 (brm, 2H); 4.54 (brm, 2H); 2.99 (s, 3H); 2.84 (m, 6H) (M + H) + = 487 A &lt; 1 405. _ 2- (4-Fluoro-phenyl) -5- (1Η-imid-2-ylmethoxy) -6- (methylamino-methyl-amino)- Benzofuran-3-carboxylic acid-formamidine 1H NMR in DMSO: 12.24 (brs, 1H); 8.41 (brd, 1H, J = 4.10Hz); 7.95 (m, 2H); 7.63 (s, IH); 7.47 (s, 1H); 7.39 (t, 2H, J = 8.79Hz); 7.19 (s, 1H); 6.95 (s, 1H); 5.20 (s, 2H); 3:16 (s, 3H); 2.91 (s, 3H); 2.86 (d? 3H, J = 4.69Hz) (M + H) + = 473 A &lt; 1 40. 6- (2,5-dioxy-imidazine-4-yl) -2- (4-amino-phenyl) -5-methoxy-benzofuran-3- Carboxylic acid-formamide 1H NMR in DMSO: 8.38 (m, 1H); 8.08 (s, 1H); 7.93 (m, 2H); 7.56 (s, lH); 7.34 (m, 2H); 7.15 (s, lH); 5.29 (s, lH); 3.90 (s, lH); 3.80 (s? 3H); 2.82 (d, J = 3.6Hz, 3H) (M + H) + = 398 B &lt; 10 407. 5-ά5-Dimethyl-isoxanthenyl) -2- (4-fluoro-phenyl) -6-methanesulfonamido -Formamidine ... ——j-—— * Η NMR in DMSO:, 9.18 (bs, 1H); 8.37 (d, J = 2.20Hz, 1H); 7.98-7.93 (m, 2H); 7.72 (s, 1H); 7.41-7.34 (m, 3H); 3.01 (s, 3H); 2.79 (dt J = 4.84Hz, 3H); 2.22 (s, 3H); 2.04 (s, 3H) (MH) · 456.0 &lt; 10 222-88828.doc 200418452 Example No. Name NMR data Mass Spec HCV pol -BB7 ICs〇 〇iM) A = μΜ B = 0 0 J to ^ 5.0 tM C = 5.0 to &lt; 30 / iM D = &gt; 30 μM replicon_) 408.2 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5- (1-pyrimidine Azole-2-yl-ethoxy) -benzofuran-3-carboxylic acid-amidamine 1H NMR in DMSO: 8.33 (brd, IH, J = 4.10); 7.92 (m, 2H); 7.84 (d, 1H, J = 2.93Hz); 7.75 (d, 1H, J = 2.93); 7.66 (s, 1H); 7.38 (t, 2H, J = 8.79Hz); 7.30 (s, 1H); 6.03 (q, 1H , J = 6.45Hz); 3.26 (s, 3H); 3.09 (s, 3H); 2.82 (d, 3H, J = 4.69Hz); 1.76 (d, 3H, J = 6.45) (M + H) + = 504 氺 氺 氺 &lt; 1 409.6 6- (3,5-dimethyl-isohumidazole_4-yl) -2- (4-fluoro-phenyl) -5- (5-methyl-isoxanthine-3 -Ylmethoxy) -benzofuran-3-carboxylic acid-amidamine 1H NMR ia DMSO: 8.41 (brd, iHt J = 4.69); 7.95 (m, 2H); 7.62 (s, 1H); 7.40 ( m, 3H); 6.16 (s, 1H); 5.20 (s, 2H); 2.86 (d, 3H, J = 4.69Hz); 2.41 (s, 3H); 2.28 (s, 3H); 2.i0 (s , 3H) (M + H) + = 476 A &lt; 1 41. 6- (3,5-dimethyl-iso-indolizyl-4-yl) -2- (4-lactyl-phenyl) &gt; 5- (pyrimidin-2-ylmethoxy) ) -Benzofuran-3-carboxylic acid-methylamine 1H NMR ia DMSO: 8.41 (brd, 1H, J = 4.10Hz); 7.95 (m, 2H); 7.83 (d, 1H, J = 2.34Hz); 7.75 (d, 1H, J = 2.93Hz); 7.64 (s, 1H); 7.46 (s, IH); 7.38 (t, 2H, J = 8.79Hz); 5.49 (s, 2H); 2.86 (d, 3H , J = 4.10Hz); 2.30 (s, 3H); 2.12 (s, 3H) (M + H) + = 478 A &lt; 1 41. 6-Ethylfluorenyl-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid-methaneamine 1H NMR in CD3D: 8.22 (in, 1H); 7.98 (m, 3H); 7.76 (m, 1H); 7.27 (m, 2H); 2.96 (s, 3H); 2.67 (s, 3H) (M + H) + = 312 B Copy 412.2 2- ( 4-Fluoro-phenyl) -5- (2-hydroxy-2-methyl-propoxy) -6- (formamyl-methyl-unsubstituted) -benzocran-3-chi Acid-formamide 1H NMR in DMSO: 8.41 (brra, 1H); 7.94 (m, 2H); 7.64 (s, 1H); 7.38 (t, 2H, J = 8.79Hz); 7.20 (s, 1H); 4.61 (s, IH); 3.86 (s, 2H); 3.24 (s, 3H); 3.08 (s, 3H); 2.83 (d, 3H, J = 4.69Hz); 1.28 (s, 6H) (M-Η ) '= 463 A * 氺 氺 413. 5-Diethylmethylamidomethoxy-2- (4-fluoro-phenylbenzene grave) -6- (_ burning continyl-methyl-amine)- Benzalan-3-acid-methylamine 1H NMR in DMSO: 8.42 (brd, 1H, J = 4.69Hz); 7.93 (m, 2H); 7.60 (s, iH); 7.38 (t, 2H, J = 8.79Hz); 7.10 (s, 1H); 4.98 (s, 2H); 3.36 (m, 4H); 3.27 (s, 3H); 3.09 (s, 3H); 2.81 (d, 3H, J = 4.69 Hz); 1.21 (t, 3H, J = 7.03Hz); 1.06 (t, 3H, J = 7.03) (M + H) + = 506 A 氺 氺 氺 414. 6 bis (3,5-dimethyl- Iso-slogazolyl) _5-ethoxy_2- (4-fluoro -Hydroxy] -Ferrofuran-3- # polyacid-formamidine 1H NMR in DMSO: 8.41-8.42 (d, 1H, J = 4.69 Hz); 7.92-7.97 (m, 2H); 7.58 ( s, 1H); 7.35-7.41 (t, 2H, J = 8.79 Hz); 7.21 (s, 1H); 4.05-4.12 (q, 2H, J = 7.03 Hz); 2.84-2.85 (d, 3H, J = 4.69 Hz); 2.30 (s, 3H); 2.12 (s, 3H); 1.27-1.32 (t, 3H, J = 7.03 Hz) '(M + H) + = 409.0 A 氺 氺 氺 415. 2- (4 -Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) &gt; 5- (pyrimazol-2-ylaminomethylmethylmethoxy) -benzofuran-3-carboxylic acid- Formamidine 1H NMR in DMSO: 12.30 (brs, 1H); 8.41 (brd, 1H, J = 4.69Hz); 7.92 (m, 2H); 7.67 (s, 1H); 7.51 (d, 1H, J = 3.52 Hz); 7.38 (t, 2H, J = 8.79Hz); 7.27 (d, 1H, J = 3.52Hz); 7.18 (s, 1H); 5.06 (s, 2H); 3.12 (m, 6H); 2.79 ( d, 3H, J = 4.69Hz) (MH) '= 531 A &lt; 1 223-88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 IC50 (μM) A = ^ 〇J5 μΜ B = to ^ 5.0 μΜ C = 5.0 to ^ 30 μΜ D = &gt; 30 μΜ Copy (ΜΜ) 416. Gaso-phenyl) -6_ (methanesulfonyl-methyl-amino) -5-([1,3, exedadiazol-2-ylaminemethylmethylmethoxy ) -Benzofuran-3-carboxylic acid-formamidine 1H NMR in DMSO: 12.81 (brs, 1H); 9.22 (s, 1H); 8.42 (brm, 1H); 7.92 (m, 2H); 7.67 (s , 1H); 7.39 (t, 2H, J = 8.79Hz); 7.18 (s, 1H); 5.12 (s, 2H); 3.17 (s, 3H); 3.10 (s, 3H); 2.79 (d, 3H, J = 4.10Hz) (MH) * = 532 A &lt; 1 417. 5-[(4,5-Dimethyl-thiazol-2-ylaminemethylamidino) -methoxy] -2- (4-fluoro-phenyl) each (methanesulfonyl -Methyl-amino) -benzofuran-3-valerate-formamidine * H NMR ifl DMSO: 12.05 (brs, 1H); 8.41 (brd, 1H, J = 4.10Hz); 7.92 (m, 2H ); 7.66 (s, 1H); 7.39 (t, 2H, J = 8.79Hz); 7.16 (s, 1H); 5.00 (s, 2H); 3.28 (s, 3H); 3.10 (s, 3H); 2.80 (d, 3H, J = 4.10Hz); 2.24 (s, 3H); 2.17 (s, 3H) (M + H) + = 561 A &lt; 1 418. 5-¾propyl-2- (4-Gas_phenyl) _6_methanesulfonamido-benzoanan-3-valerate-formamidine-lH NMR in DMSO: 9.32 (bs, 1H); 8.36 (m, 1H); 7.94 (dd, J = 5.3 & 8.8Hz, 2H); 7.58 (s, 1H); 7.36 (t, J = 8.8Hz, 2H); 7.14 ( s, 1H); 3.03 (s, 3H); 2.83 (d, J = 4.6Hz, 3H); 2.31 (m, 1H); 1.00 (m, 2H); 0.68 (m, 2H) (M + H) + = 403 A &lt; 1 419. 5- [2- (4-Cyano-hexahydropyridine-i-yl) -ethoxy] -6- (3,5-dimethyl-iso-pyridyl-4 -Yl) -2- (4-airyl-dongyl) -Hydroxybenzo-3-carboxylic acid-formamidine 1H NMR in DMSO: 8.41-8.43 (d, 1H, J = 4.69 Hz); 7.93- 7.97 (m, 2H); 7.58 (sT 1H); 7.35-7.41 (t, 2H, J = 8.79Hz); 7.26 (s, 1H); 4.084.12 (t, 2H, J = 5.86Hz); 2.85- 2.86 (d, 3H, J = 4.69Hz); 2.82-2.86 (m, 1H); 2.63-2.66 (ζ 2H, J = 5.86Hz); 2.50-2.55 (m, 3H); 2.31 (s, 3H); 2.26-2.31 (m, 1H); 2.14 (s, 3H); 1.77-1.84 (m, 2H); 1.63-1.70 (m, 2H) (M + H) + = 517.1 A &lt; 1 420.2 2- (4-Methanesulfonyl-amino-5-thiophen-2-yl-benzofuran-3-carboxylic acid-methaneamine 1H NMR in DMSO: 9.29 (sf 1H); 8.48 (d, J = 4.84Hz, 1H); 8.02-7.97 (m, 2H); 7.75 (s, 1H); 7.97 (s, 1H); 7.64 (d, J = 5.27Hz, 1H); 7.45-7.37 ( m, 3H); 7.19-7.16 (m, 1H); 2.94 (s, 3H); 2.84 (d, J = 4.40Hz, 3H) (MH) '= 443 A &lt; 1 421.2 2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5-methylaminomethylmethylmethoxy-benzofuran-3- Carboxylic acid-formamide'H NMR in DMSO: 8.40 (brd, 1H, J = 4.69Hz); 7.93 (m, 3H); 7.70 (s, 1H); 7.39 (t, 2H, J = 8.79Hz); 7.16 (s, 1H); 4.66 (s, 2H); 3.25 (s, 3H); 3.13 (s, 3H); 2.83 (d, 3H, J = 4.69Hz); 2.68 (d, 3H, J = 4.69Hz ) (M + H) + = 464 A &lt; 1 422.2 2- (4-fluoro-phenyl) -5- (1-hydroxymethyl-cyclopropylmethoxy) -6-[(1-methyl-¾ • propylmethyl) -Methanesulfonyl-amino group] -benzofuran-3-¾ acid-methylamine 1H NMR in DMSO: 8.53 (d, J = 4.8H2, iH); 8.07 (dd, J = 8.8, 5.3Hz, 2H); 7.72 (s, 2H); 7.52 (t, J = 8.8Hz, 2H); 4.50 (brd, 1H); 4.15 (t, J = 9.3Hz, 1H); 14.07 (d, J = 9.9Hz, 1H); 3.60 (m, 2H); 3.50 (m, 1H); 3.30 (d, J = 11.0Hz, 1H); 3.17 (s, 3H); 2.94 (d, J = 4.8Hz, 3H); 0.75 ( s, 4H) (MH) '= 545 B &lt; 10 224- 88828.doc 200418452 Instance number name NMRdata Mass Spec HCV pol -BB7 ICse 〇iM) A = / iM B = 03 to ^ 5.0 / iM C = 5.0 to ^ 30 μΜ D = &gt; 30 / iM Copy L) 423. 6-Diethylamino-5-ethoxy-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid-formamidine 1HNMRinCIX: 13: 7.85 (dd, J = 8.8T 5.3Hz, 2H); 7.30 (s, 1H); 7.77 (t, J = 8.8Hz, 2H); 6.67 (st 1H); 5.75 (brs, 1H); 4.10 (q, J = 7.0Hz, 2H); 3.20 (q, J = 7.0Hz, 4H); 1.40 (t, J = 7.0Hzt 6H); 1.30 (t, J = 7.0Hz, 3H) (M + H) + = 385 A &lt; 1 424. 5-Aminomethylamidomethoxy-2- (4-railyl-phenyl) -6- (methanesulfonyl-methyl-amino) -benzofuran each carboxylic acid-formaldehyde Amidine 'HNMR in DMSO: 8.41 (brd, 1H, J = 4.69Hz); 7.93 (m, 2H); 7.72 (s, 1H); 7.40 (m, 4H); 7.15 (s, 1H); 4.64 (s , 2H); 3.26 (s, 3H); 3.13 (s, 3H); 2.84 (d, 3H, J = 4.69Hz) (MH)-= 448 A &lt; 1 425. 5- [2- (3,5-Dimethyl-4-dazol-1-yl) -ethoxy] -2- (4-air grave-dongyl) -6- (methanesulfonium -Methyl-amino) -benzofuran-3-carboxylic acid-formamidine 1H NMR in DMSO: 8.41 (brd, 1H, J = 4.69Hz); 7.94 (m, 2H); 7.60 (sy 1H) ; 7.38 (ζ 2H, J = 8.79Hz); 7.22 (st 1H); 5.81 (s, 1H); 4.44 (brd, 2H, J = 4.69Hz); 4.40 (brd, 2H, J = 4.69Hz); 3.06 (s, 3H); 2.89 (s, 3H); 2.84 (d, 3H, J = 4.69Hz); 2.28 (s, 3H); 2.08 (s, 3H) (M + H) + = 515 A &lt; 1 426. 2- (4-Fluoro-phenyl) -5-crean-2-yl-6-methylpyridinylamino-benzofuran each carboxylic acid-formamide 1H NMR in DMSO : 9.34 (s, 1H); 8.50 (d, J = 4.40Hz, 2H); 7.99-7.96 (m, 2H); 7.91 (st 1H); 7.82 (s, 1H); 7.74 (s, 1H); 7.40 (t, J = 8.79Hz &gt;2H); 7.09 (d, J = 3.52Hz, 1H); 6.65 (s, 1H); 3.04 (s, 3H); 2.85 (d, J = 4.40Hz, 3H) (MH ) * = 427.0 A &lt; 1 427. 6- (3,5-Dimethyl-isoxazole-4.-2- (4-fluoro-phenyl) -5- (1-methyl-1H-tetramethyl-5- Methylmethoxy) -benzoanan-3 -metanoic acid-formamidine * H NMR in DMSO: 8.44-8.45 (d, 1H, J = 4.69Hz); 7.93-7.97 (m, 2H); 7.63 ( s, 1H); 7.53 (s, 1H); 7.36-7.42 (t, 2Ht J = 8.79Hz); 5.56 (s, 2H); 3.93 (s, 3H); 2.86-2.88 (dt 3H, J = 4.69Hz ); 2.24 (s, 3H); 2.07 (s, 3H) (M + H) + = 477 A &lt; 1 428. ^ 5-Cyclopropylmethoxy-6- (3,5-difluorenyl-isoazazol-4-yl) -2- (4-fluoro-phenyl) -benzofuran -3-carboxylic acid-formamidine 1H NMRinDMSO: 8.39-8.41 (d, 1H, J = 4.69Hz); 7.91-7.96 (m, 2H); 7.58 (st 1H); 7.35-7.41 (ζ 2H, J = 8.79Hz); 7.18 (s, 1H); 3.86-3.88 (d, 2H, J = 7.03Hz); 2.83-2.85 (d, 3H, J = 4.69Hz); 2.32 (s, 3H); 2.15 (s, 3H); 1.12-1.20 (ra, 1H); 0.51-0.57 (m, 2H); 0.26-0.3 l (m, 2H) (M + H) + = 435 A &lt; 1 429. 6- (3; dimethyl-isoazazolyl) -5- (3,5-dimethyl-isopurin-4-ylmethoxy) -2- (4-gas Phenyl-fungyl) -benzyl-3-acid-formamidine'H NMRinDMSO: 8.43-8.45 (d, 1H, J = 4.69Hz); 7.92-7.96 (m, 2H); 7.59 (s, 1H); 7.44 (s, 1H); 7.36-7.41 (t, 2H, J = 8.79Hz); 4.97 (s, 2H); 2.86-2.87 (d, 3H, J = 4.69Hz); 2.28 (s, 3H ); 2.2i (s, 3H); 2.03 (s, 3H); 1.97 (s, 3H) X (M + H) + = 490 A &lt; 1 430.3 2- (4-Fluoro-phenyl) -5_methoxy-6- (5-methyl_3,4? fluorenediazol-2-yl) -benzofuran-3- Carboxylic acid-formamide 1HNMRinCDCl3: 8.05 (s, 1H); 7.92-7.87 (m, 2H); 7.52 (s, 1H); 7.27-7.23 (mt 2H); 5.80 (s, 1H); 4.03 (s, 3H); 3.02 (d, J = 4.5 Hz, 3H); 2.65 (s, 3H) (M + H) + = 381 A &lt; 10 225-88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 ICsoOtM) A = μΜ 03 to ^ 5.0 μΜ. C = 5.0 to ^ 30 D = &gt; 30 μΜ replicon (μΜ) 431.6 -(3-cyano-4-hydroxy-2-oxy-2,5-dihydro-pyrrole small methyl) -2- (4-fluoro-phenyl) -5-methoxy-benzo Pyran-3-guinic acid-formamidine 1HNMRinDMSO: 8.36-8.34 (m, 1H); 7.94-7.89 (m, 2H); 7.36-7.28 (ra, 3H); 7.10 (s, 1H); 4.47 (sr .2H); 3.85 (s, 2H); 2.81 (d, J = 4.2 Hz, 3H) (M + H) + = 436 A * 氺 氺 432.4 4-amino-6- [ethyl- (2_ Oxy-ethyl group) -amino group] -2- (4-fluoro group-benzene to) -5-methoxy-benzocran-3-guinic acid-methyl group 1HNMRinCDCl3: 7.90 (ddt J = 8.3,5.3Hz, 2H); 7.40 (s, 1H); 7.20 (t, J = 8.3Hz, 2H); 5.90 (brs, 1H); 3.91 (s, 3H); 3.80-3.70 (m, 2H); 3.62 (s, 2H); 3.30 (s, 3H); 2.98 (TJ = 4.4Hz, 3H); 1.10 (t, J = 7.0Hz, 3H) (M + H) + = 343 B &lt; 10 433. 6- (3 &gt; Di-methyl-isopurine α-s_4_yl) -2- (4-amino-phenyl) -5- (2-morpholinolinylethoxy ) -Benzofuran-3-carboxylic acid-formamidine 1H NMR in DMSO: 8.41-8.42 (d, 1H, J = 4.69Hz); 7.93-7.97 (m, 2H); 7 ^ 8 (s, 1H) ; 7.35-7.41 (t, 2H, J = 8.79Hz); 7.26 (s, 1H); 4.11-4.14 (t, 2H, J = 5.28Hz); 3.52-3.55 (t, 4H, J = 4.10Hz); 2.84-2.86 (d, 3H, J-4.69HZ); 2.61-2.65 (t, 2H, J = 5.86Hz); 2.36-2.40 (t, 4H, J = 4.10Hz); 2.31 (s, 3H); 2.15 (s, 3H) (M + H) + = 494 A 氺 氺 氺 434. 6- (3,5-dimethyl-isopyridin-4-yl) -2- (4-amino-phenyl) -5- (3-Hexahydropyridine-1 -yl-is oxy) -benzofuran-3-guinic acid-formamidine'H NMR ia DMSO: 8.42-8.44 (d, 1H, J = 4.69Hz ); 7.92-7.97 (m, 2H); 7.58 (s, 1H); 7.35-7.41 (t, 2H, J = 8.79Hz); 7.22 (s, 1H); 4.01-4.06 (t, 2H, J = 6.45 Hz); 2.84-2.85 (d, 3H, J = 4.69Hz); 2.28 (s, 3H); 2.25-2.28 (m, 4H); 2.11 (s, 3H); 1.91 (s, 2H); 1.75-1.84 (in, 2H); 1.36-1.48 (m, 4H); 0.84-0.86 (m, 2H) (M + H) + = 506.1 B 氺 氺 氺 435. 2- (4-Gas-phenyl) _5_ ( Pyrimazole 4-ylmethoxy) -benzofuran-3-guinic acid-formamidine 1H NMR in DMSO: 9.12 (s, 1H); 8.34 (d, J = 4.0 Hz, 1H); 7.92 (m, 2H); 7.79 (s, 1H); 7.57 (d, J = 8.8 Hz, 1H); 7.34 (t, J = 8.3Hz, 2H); 7.23 (s, 1H); 7.07 (ra, 1H); 5.25 (s, 2H); 2.82 (d, J = 3.5Hz, 3H) (M + H) + = 383.0 B &gt; 30 436. ^ 2- (4-air-benzyl) -6 &lt; 2-Hydroxy-ethenyl) -5-methoxy-benzofuran-3-carboxylic acid-formamidine'H NMR in CDC13: 8.20 (s, 1H); 7.87 (m, 2H); 7.45 (s, 1H); 7.22 (m, 2H); 5.77 (brs, 1H); 4.82 (s, 2H); 4.01 (s, 3H); 3.75 (brs, 1H); 3.00 (dt J = 4.8 Hz, 3H ) (M + H) + = 358.1 A &lt; 10 437. 5-Cyclopropyl-2- (4-amino-phenyl) -6- (methylsulfanyl-St-yl-fluorenyl-amino) -benzocran-3-metanoic acid-fluorene Lamine 1H NMR in DMSO: 8.39 (d, J = 4.40Hz, 1H); 7.95-7.90 (m, 2H); 7.81 (s, 1H); 7.39-7.33 (m, 2H); 7.13 (s, 1H) ; 3.22 (s, 3H); 3.14 (s, 3H); 2.82 (d, J = 4.40Hz, 3H); 2.33-2.24 (m, 1H); 0.96 (d, J = 8.35Hz, 2H); 0.79- 0.63 (mt 2H) (M + H) + = 417 A &lt; 1 438. 2- (4-Fluoro-phenyl) _5_hydroxy-6-[(2-hydroxy-propyl) -methyl-s-s-yl-amine] -benzyl_3_ complex Acid-formamidine 1H NMR in DMSO: 9.97 (s, 1H); 8.40 (brd, 1H, J = 4.10Hz); 7.92 (m, 2H); 7.55 (s, 1H); 7.35 (t, 2H, J = 8.79Hz); 7.09 (s, 1H); 4.72 (brs, 1H); 3.58-3.40 (m, 3H); 3.01 (s, 3H); 2.80 (d, 3H, J = 4.69Hz); 1.03 (d , 3H, J = 5.86Hz) (MH)-= 435 A 氺 氺 氺 -226- 88828.doc 200418452 Example number name NMRdata Mass Spec HCV pol -BB7 Κ ^ (μΜ) A = ^ 0.5 μΜ B = 05 to ^ 5.0 μΜ C = 5.0 to ^ 30 D = &gt; 30 μΜ replicon (μΜ) 439.2 2- (4-fluoro-phenyl) _6-[(2-benzyl-propyl) _ methanesulfonyl- Amine J-5-methoxy-benzofuran-3-carboxylic acid-formamidine ^ HNMRinDMSO: 8.41 (brd, 1H, J = 5.28Hz); 7.92 (m, 2H); 7.66 (s, 1H) ; 7.36 (t, 2H, J = 8.79Hz); 7.18 (s, 1H); 4.66 (brs, 1H); 3.89 (s, 3H); 3.56 (bnn, 3H); 3.00 (s, 3H); 2.82 ( d, 3H, J = 4.69Hz); 1.03 (d, 3H, J = 5.28Hz) (MH) * = 449 A 氺 氺 氺 440. 6-〇Ethyl 4-bilodine-2-yl) -5 -Ethyl-2- (4-fluoro-phenyl) &gt; benzofuran carboxylic acid-formamidine 1HNM RinCDCl3: (mixture of two enantiomers) 7.90 (m, 2H); 7.68 (s, 1H); 7.21 (s, 1H); 7.15 (m, 2H); 5.80 (brs, 1H); 5.20 (dd, J = 2.1 Hz, J = 8.4Hz, 1H); 3.85 (m, 1H); 3.65 (m, 1H); 3.20-3.40 (1H); 3.01 (d, J = 5.2Hz, 3H); 2.70-2.90, 2H); 2.30-2 JO, 1H); 1.80-2.10, 2H); 1.82 (s, 3H); 1.34 (t, J = 7.5Hz, 3H) (M + H) + = 409.1 A 氺 氺 氺 441. 2_ (4_ Gaso-phenyl) -6-methanesulfonylamino-5- (tetrahydro-furyl) -benzofuran-3-carboxylic acid-formamidine 1HNMRinDMSO: 9.15 (s, 1H); 8.44 (d , J = 4.40Hz, 1H); 7.94-7.89 (m, 2H); 7.62 (d, J = 4.40Hz, 2H); 7.39-7.34 (m, 2H); 5.21 (t, J = 7.47Hzt 1H); 4.06-4.03 (m, 1H); 3.82-3.80 (m, 1H); 3.08 (s, 3H); 2.82 (d, J = 4.40Hz, 3H); 2.45-2.41 (m, 1H); 1.98-1.94 ( m, 2H); 1.65 (m, 1H) (MH). = 431.0 A &lt; 1 442. 2- (4-Amino-phenyl) -5_methoxy-6- (tetrahydro-crean-3-yl) -benzoanan-3-carboxylic acid-methaneamine 1HNMRinDMSO : 8.34-8.36 (d, 1H, J = 4.69Hz); 7.90-7.95 (m, 2H); 7.53 (s, 1H); 7.33-7.39 (t, 2H, J = 8.79Hz); 7.10 (s, 1H ); 4.00-4.06 (t, 1H, J = 7.62Hz); 3.90-3,97 (m, 1H); 3.89 (s, 3H); 3.68-3.85 (m, 2H); 3.56-3.61 (t, 1H , J = 7.62Hz); 2.83-2.84 (d, 3H, J = 4.69Hz); 2.21-2.31 (m, 1H); 1.95-2.06 (m, 1H) (M + H) + = 370.0 A &lt; 1 443. 2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methoxymethyl-amino) -5-propoxy-benzofuran-3-carboxylic acid_fluorene Amidine 'HNMR in DMSO: 8.40 (d, J = 4.2Hz, 1H); 7.94 (dd, J = 8.8, 5.3Hz, 2H); 7.65 (s, 1H); 7.36 (t, J = 8.8Hz, 2H ); 7.19 (s, 1H); 5.94 (brs, 2H); 4.03 (t, J = 7.0Hz, 2H); 3.32 (s, 3H); 3.08 (s, 3H); 2.81 (d, J = 4.2Hz , 3H); 1.80 (sextet, J = 7.0Hzt 2H); 1.01 (t, J = 7.0Hz, 3H) (M + H) + = 465 A &lt; 1 44. 2- (4-Gas-phenyl) -5-hydroxy-6- (methanesulfonyl-methoxymethyl-amino) -benzofuran each carboxylic acid-methaneamine 1HNMRia DMSO : 10.08 (s, 1H); 8.40 (d, J = 4.4Hz, 1H); 7.92 (dd, J = 8.8, 5.7Hz, 2H); 7.53 (s, 1H); 7.35 (t, J = 8.8Hz, 2H); 7.12 (s, 1H); 4.92 (brs, 2H); 3.31 (s, 3H); 3.08 (s, 3H); 2.80 (d, J = 4.8Hz, 3H) (MH) '= 421 A &lt; 10 445. 2_ (4 · Gas · &quot; phenyl) -6_ methanesulfonylamino-5-propoxy-benzoanan-3-carboxylic acid-formamidine 1H NMR in CDC13: 7.82 (dd, J = 8.8 & 6.3Hz, 2H); 7.73 (s, 1H); 7.41 (s, 1H); 7.18 (t, J = 8.8Hz, 2H); 6.92 (s, 1H); 5.77 ( brs, 1H); 4.07 (t, J = 6.6Hz, 2H); 2.98 (d, J = 9.8Hz, 3H); 2.95 (s, 3H); 1.85 (sextet, J = 7.0Hz, 2H); 1.06 ( t, J = 7.0Hz, 3H) (M + H) &quot; = 421 A &lt; 1 446. 5- (4-Gasyloxy group) -2- (4-fluoroyl-phenylene) -6- (methanesulfonyl-methoxymethyl-amino) -benzo 4 1H NMR in DMSO: 8.40 (d, J = 4.6Hz, 1H); 7.93 (dd, J = 8.8, 5.3Hz, 2H); 7.88 (d, J = 8.2Hz, 2H); 7.75 (s, 1H); 7.71 (d, J = 8.2Hz, 2H); 7.37 (t, J = 8.8Hz, 2H); 7.31 (s, 1H); 5.33 (s, 2H); 4.94 ( brs, 2H); 3.31 (s7 3H); 3.04 (s, 3H); 2.81 (d, J = 4.6Hz, 3H) (MH) '= 536 A &lt; 1 227- 88828.doc 200418452 Instance number name NMRdata Mass Spec HCV pol -BB7 IC50O1M) A = μ, Μ B = 0 * 5 to 彡 5.0 · i / iM C = 5.0 to ^ 30 μΜ D = &gt; 30 μM replicon (μM) 447. —5_ (3-cyano-fluorenyloxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methoxy-amino-amino)- Benzo-3-carboxylic acid-formamidine'HNMRinDMSO: 8.40 (d, J = 4.4Hz, 1H); 8.00 (s, 1H); 7.90-7.80 (m, 4H); 7.75 (s, 1H); 7.62 (t, J = 8.0HzT 1H); 7.39 (t, J = 8.0Hz, 2H); 7.31 (s, 1H); 5.28 (s, 2H); 4.92 (brs, 2H); 3.31 (s, 3H); 3.04 (s, 3H); 2.82 (d, J = 4.4Hz, 3H) (M + H) + = 536 A &lt; 1 448.6 6- (1: cyclopropanecarbonyl-pyridine-2-yl) -2- (4-amino-phenyl) -5-isopropoxy-benzoanan-3-gui Acid-formamidine ^ NMRinCDCb: 7.84 (m, 2H); 7.34 (s, 1H); 7.18-7.23 (m, 3H); 5.74 (brs, 1H); 5.50 (d, J = 7.47Hz, 1H); 4.73 (septet, J = 5.72Hz, 1H); 3.85 (m, 1H); 3.82 (m, 1H); 2.99 (d, J = 4.84Hz, 3H); 2.22-2.43 (m, 1H); 1.92-2.00 (in, 2H); 1.79-1.80 (m, 2H); 1.40 (m, 6H); 0.85-1.01 (m, 4H) (M + H) + = 465 A 氺 氺 氺 1 449.2 2- (4- Carbyl-phenyl) -5_methoxyban [1,3,4] Hexajun-2-yl-benzyl-3-carboxylic acid-formamidine ^ NMRia CDC13: 8 ^ 1 (s, 1H); 8.11 (s, 1H); 7.91-7.87 (m, 2H); 7.54 (s, 1H); 7.26-7.20 (rat 2H); 5.80 (s, 1H); 4.04 (s, 3H); 2.99 ( cU = 5.4Hz, 3H) (M + H) + = 368 A 氺 氺 氺 450. 2- (4-fluoro-phenyl) each (methanesulfonyl-methoxymethyl-amine) -5- Pyridin-2-yl-benzopyran-3-carboxylic acid-formamidine 1H NMRinDMSO: 8.48 (m, 1H); 7.98-7.96 (m, 3H); 7.83 (m, 1H); 7.61-7.60 ( m, 1H); 7.42-7.36 (mt 3H); 7.13 (m, 1H); 3.16 (s, 3H); 3.08 (s, 3H); 2.66 (d, J = 3.96Hz, 3H) (M + H) + = 458.9 A 氺 * 氺 451.2 -(4-Fluoro-phenyl) -6-{[2- (4-fluoro-phenyl) -2-hydroxy-ethyl] -methyl-fe continuous group-amino group} · 5- Benzene-3 -metanoic acid-formamidine * H NMR in DMSO: 10.03 (brs, 1H); 8.42 (brd, 1H, J = 4.69Hz); 7.94 (m, 2H); 7.38 (t, 2H, J = 8.79Hz); 7.32 (m, 3H); 7.13 (m, 3H); 5.58 (m, 1H); 4.62 (m, 1H); 3.70 (brm, 2H); 3.01 (s, 3H); 2.82 ( d, 3H, J = 4.10Hz) (MH) '= 515 A 氺 本 氺 45. 5-methoxy-ί-phenyl-benzofuran-3-fatty acid-formamidine 氺 氺 氺 氺 氺 氺A &lt; 10 _ "453. 5-Hydroxy-2-phenyl-benzofuran-3-¾ acid-formamidine 氺 氺 氺 氺 氺 氺 C 氺 氺 氺 * Unless otherwise stated, all NMR and The 13C NMR spectra were all obtained through a Varian Mercury VX 300 spectrometer, with TMS as the reference index. ** Mass spectrum data is expressed by the mass-to-charge ratio of molecular ion of (M-Η) unless it is (M + H). * * * Show data not collected. 228-88828.doc 200418452 Table 3. Pharmaceutically acceptable salts of the selective compounds listed in Table 1. , _ Number 454.

Structure Name NMR Data * h3c—S〇2, n- CH, h3c / \

κ. 2_ (4-fluoro-phenyl) -5-isopropoxy-6-methanesulfonylamino-benzofuran-3-carboxylic acid-formamidine; potassium salt Ή in DMSO 8.18- 8.15 (br m, 1H); 7.87-7.81 (m, 2H); 7.28- 7.22 (1¾ 2H); 6.77 (s, lH); 4.57 (sept. J = 6.45 Hz, 1H); 2.78 (cU = 4.7Hz , 3H); 2.55 (s, 3H); 1.18 (d, J = 5.86 Hz, 6H) 455. CH,

2_ (4-Fluoro-phenyl) -5-isopropoxy-6-methane Continued-Acetylenyl-benzofuran-3-carboxylic acid-formamidine; sodium salt

lH NMR in DMSO 8.18-8.15 (br nou 1H); 7.87-7.81 (m, 2H); 7.28-7.22 (m, 2H); 6.77 (s, lH); 4.57 (sept. J = 6.45 Hz, 1H); 2.78 (d, J = 4.7Hz, 3H); 2.55 (s, 3H); U8 (d, J = 5.86 Hz, 6H) 456.

2- (4-Fluoro-phenyl) -6-pyranesulfonylamino-5-methoxy-benzofuran-3-carboxylic acid-formamidine; potassium salt 88828.doc 229- 200418452

88828.doc 230- 200418452

* Unless otherwise stated, all 4 NMR and 13C NMR spectra were obtained using a Varian Mercury VX 300 spectrometer, with TMS as the reference index. Chemical transfer and coupling constants are expressed in parts per million (ppm) and hertz (Hz), respectively. Example 464 Inhibition of viral RNA replication First, the antiviral activity of a representative compound of the present invention was evaluated in a human liver-derived cell line (Huh-7-Clone A) containing HCV replicon (BB7 sequence) (see Lohmann et al. Science 1999, 285: 110, 3; Blight KJ et al., Science 2000, 290: 1972-4; Pietschmann, T. et al., J. Virol. 2001, 73: 1252-1264; and Lohmann, V. Et al., J. Virol. 2001, 75. 1437-1449). The HCV replicon is a sub-viral viral RNA expressing the HCV protein required for its replication. These proteins include the non-structural proteins NS3, NS4A, NS4B, NS5A and NS5B. The replicon also contains foreign genes encoding 88828.doc -231-200418452 drug selection marker (neomycin phosphotransferase) to allow G41 8 (neomycin) to select cells containing replicons. After incubating replicon-containing cells at different compound concentrations for 72 hours, ELISA (enzyme-linked immunosorbent analysis) was used to determine the effect of compounds within the scope of the present invention on HCV NS5A protein production. COSTAR® 96-well cell culture plates are used, but other known cell culture plates can also be used. After incubation, the culture medium was removed from the tank, and the cells were fixed to the analysis plate with 0.05% glutaraldehyde. After 1 hour incubation, glutaraldehyde is washed off with phosphate buffered saline (PBS); non-specific antibody binding is blocked with a PBS solution such as SUPERBLOCK® reagent (blocking buffer). After 1 hour at 37 ° C, the blocking agent was wetted from the cells with PBS, and the primary monoclonal antibody was added to each compound-containing tank. Incubate the primary antibody at 37 ° C for 1 hour, and moisten it 3 times with PBS containing 0.02% Tween-20tm before adding secondary antibodies of wasabi peroxidase (HRP). HRP was incubated at 37X: for 1 hour and moistened several times, first with PBS / Tween-20TM, followed by PBS alone. In order to quantify peroxidase activity, 3,3 ', 5,5'-tetramethyl-p-diaminobiphenyl (TMB) was added to the culture plate, and after 30 minutes, it was read in an ELISA plate reader. The plate was read at OD 650 nm. The dose response of the compound was determined using a series of 8-dose dose curves to determine the 50% inhibitory concentration (EC5G value). A representative compound of the present invention shows a dose-dependent inhibition of the amount of NS5A in a cell. Table 2 shows the 50% effective concentration range (EC5Gs) of representative compounds within the scope of the present invention. The 50% effective concentration range of the preferred compound is about 30 micromoles or less, and the 50% effective concentration range of the better compound is about 5 micromoles or less, and the 50% effective concentration range of the best compound The ear concentration is about 0.5 μmol 88828.doc -232-200418452 or lower. Example 465 Inhibition of HCV NS5B targeted RdRp activity by viral RNA-dependent RNA polymerase (RdRp), a standard living organism using pure HCV NS5B protein derived from consensus sequences of patients infected with HCV genotype lb virus (BB7) Exochemical analysis is established and its characteristics are determined. (See Blight KJ et al., Science 2000, 290: 1972-4). The NS5B consensus sequence was selected and expressed in the form of a histidine tag (GSHHHHHH) fusion protein in E. coli; among them, the 21 amino acids at the carboxyl terminus were removed to increase solubility. In addition to evaluating its activity in a replicon analysis, this analysis was also used to evaluate the antiviral activity of a representative compound within the scope of the present invention as shown in Examples 1-453 in the foregoing table. The inhibitory activity of the compounds of the present invention can be measured as an IC5G value. The IC5G value represents the concentration of the compound when RdRp is inhibited by 50%. As a result of the analysis of the inhibition of RdRp activity of HCV, the result that NS5B protein is a substantial majority of the tested compounds revealed that the IC50 value ranges from &lt; 0.5 to about 30 micromolar concentration. The low concentration of these test compounds required to achieve 50% RdRp inhibition shows that the compounds of the present invention are effective in inhibiting RNA synthesis by the viral RdRp enzyme. Although the present invention has been illustrated and exemplified by preferred embodiments, other embodiments will be clear to those skilled in the art. Therefore, the present invention is not limited to the specific specific embodiments described and exemplified; moreover, modifications or changes can be made without departing from the spirit of the present invention, and its entire scope is deconstructed by the scope of the attached patent application. 88828.doc-233-

Claims (1)

200418452 Scope of patent application ... 1. A compound of the following formula ’ I where: represents a group selected from the group consisting of hydrogen, alkyl, halogen, and cyano R2 represents a group selected from murine, substituted or unsubstituted alkyl, substituted unsubstituted alkoxy, hydroxyl, cycloalkyl, cycloalkoxy, polyfluoroalkyl, polyfluoroalkoxy , A group consisting of a prime, an amine, a monoalkylamino, a dialkylamino, a cyano, a substituted or unsubstituted ethoxy group and a substituted or unsubstituted heterocyclic group; R3 represents a group selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkyloxy, alkenyl, halogen, #yl, polyfluoroalkyl, polyfluoroalkoxy, formate, and Group, carbonyl, oxal, lightly carbonyl, amine, substituted or unsubstituted monoalkylamino, dialkylamino, cyano, amido, alkoxyamido, substituted or Unsubstituted heteroarylamino, ethylsulfonamido, ureido, carboxyamido, sulfa, substituted amines, substituted or unsubstituted heterocyclic silanes, thiothio, Alkyl sulfenyl, alkylsulfonyl, alkylsulfonic acid and substituted or unsubstituted heterocyclic group and _〇 (CH2) -C (= 〇) -R7 group; FU represents 88828.doc 200418452 group selected from the group consisting of hydrogen, alkyl, hydrogen and alkoxy; Rs represents a group selected from the group consisting of Ci-CO group and cycloalkyl group; R6 represents an optional group A group consisting of a substituted or unsubstituted aryl group and a substituted or unsubstituted heteroaryl group; R7 represents a group selected from the group consisting of dialkylamino, substituted or unsubstituted arylamine, take Or an unsubstituted heteroarylamine group and a group consisting of a substituted or unsubstituted aryl group, the monoalkylamino substituent is one or more independently selected from cycloalkyl, hydroxyl, and alkoxy A group consisting of a substituted or unsubstituted heterocyclic group; 'the arylamino substituent and the heteroarylamino substituent are one or more groups independently selected from the group consisting of alkyl and alkoxycarbonyl A group of groups; the sulfonamide substituent is one or more independently selected from alkenyl, cycloalkyl, alkoxy, hydroxyl, halogen, polyfluoroalkyl, polyfluoroalkoxy, carboxyl, alkylcarbonyl, alkoxycarbonyl , Carboxamidine, a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group; the heterocyclic sulfonyl substituent is one or more independently selected from alkoxy A group consisting of an alkyl group and a boryl group; the alkyl substituent and the alkoxy substituent are one or more independently selected from the group consisting of alkenyl, amino, monoalkylamino, dialkylamino, and alkoxy , Cycloalkyl, hydroxyl, carboxyl, iS element, cyano, polyfluoroalkyl, polyfluoroalkoxy, hydrazine, tertiary amine, An acid group, a fluorenyl group, a oxenyl group, a vegetable group, a benzo [1,3] dioxo group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocyclic group. The group of the group; 88828.doc -2- 200418452 The heterocyclic group substituent is one or more independently selected from the group consisting of alkyl, amine, amido, early amino, amido-amino, and dihu Amine, Fe milk, Methoxy, Hydroxyl, Alkyl, Cycloalkyl, Compound, Ammonium, Halogen, Halo, Cyano, Polyfluoroalkyl, Polyfluorooxy, A group consisting of a fluorenyl group, an alkane group, a cycloalkylcarbonyl group, an alkoxycarbonyl group, a mercapto group, an oxy group, a substituted or unsubstituted aryl group, an aralkyl group, and a substituted or unsubstituted heteroaryl group The heteroaryl substituent is one or more independently selected from alkyl, amine, alkoxy, alkoxyalkyl, hydroxyl, hydroxyalkyl, cycloalkyl, carboxyl, carboxamidin, halogen, A group consisting of a polyfluoroalkyl group, a polyfluoroalkyloxy group, a dibasic acid group, a mirror group and an oxy group; the benzyloxy substituent is one or more independently selected from alkyl, alkoxy, poly Fluoroalkyl , A polyfluoroalkoxy group, a hydroxyl group, a carboxyl group, an alkoxycarbonyl group, a halogen group, a cyano group, a fluorenyl group, and a phenyl group; the aryl substituent is one or more independently selected from an alkyl group, Alkoxy, hydroxyl, halogen, polyfluoroalkyl, polyfluoroalkyl, cyano, amine, monoamine, diamine, amine, oxyalkyl, siamino, acid A base group of the group consisting of amine alkyl, carboxyl, alkanesulfonyl, alkoxycarbonyl, alkoxycarbonyl, fluorenyl, and heterocyclic groups, and pharmaceutically acceptable salts thereof; the limitation is that the formula does not Includes compounds selected from the group consisting of 5-methyllactyl-2-phenyl-benzoanan-3-leanine methyl blue cyanamide and 5-benzyl-2-phenyl-benzofuran-3-carboxylic acid Formamidine. 2. — a compound of the formula, 88828.doc 200418452 among them: R! Represents a group selected from the group consisting of hydrogen, alkyl, halogen and cyano; R2 represents a group selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, hydroxyl , Cycloalkyl, cycloalkoxy, polyfluoroalkyl, polyfluorinated oxy, 1¾, amine, monoamine, monophosphino, cyano, substituted or unsubstituted benzyloxy A group of a group consisting of a substituted or unsubstituted heterocyclic group; R3a represents a group selected from a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, an alkenyl group, a pixel, a hydroxyl group , Polyfluoroalkyl, polyfluoroalkoxy, formamyl, carboxyl, alkylcarbonyl, alkoxycarbonyl, hydroxyalkylcarbonyl, amino, substituted or unsubstituted monoalkylamino, dialkylamino, cyano Group, amido, alkoxyamido, substituted or unsubstituted heteroarylamino, ethenylamino, ureido, fluorenamide, sulfonamide, substituted sulfonamide, substituted or unsubstituted Substituted heterocyclic sulfonyl, alkylthio, alkylsulfinyl, hexane, alkylsulfonyl, alkylsulfonic acid and substituted or unsubstituted heterocyclic group with -〇 (c h2) -c (= o) -r7; R4 represents a group selected from the group consisting of hydrogen, alkyl, halogen and alkoxy; I represents a group selected from alkane (c "C6) R6 represents a group selected from the group consisting of a substituted or unsubstituted aryl group and a substituted or unsubstituted heteroaryl group; 88828.doc 200418452 R7 A group selected from the group consisting of a dialkylamino group, a substituted or unsubstituted arylamine group, a substituted or unsubstituted heteroarylamine group, and a substituted or unsubstituted aryl group; Alkylamino substituents are one or more groups independently selected from the group consisting of cycloalkyl, hydroxyl, alkoxy and substituted or unsubstituted heterocyclic groups; the arylamino substituent and the heteroaryl The amino substituent is one or more groups independently selected from the group consisting of alkyl and oxycarbonyl; the sulfonamide substituent is one or more independently selected from fluorenyl, cycloalkyl, alkoxy, hydroxyl, iS Element, polyfluoroalkyl, polyfluoroalkoxy, carboxyl, alkylcarbonyl, alkoxycarbonyl, carboxamidine, substituted or unsubstituted aryl and substituted Or a group of an unsubstituted heterocyclic group; the heterocyclic acid group substituent is one or more groups independently selected from the group consisting of an alkoxy group and a radical; the alkyl substituent And the alkoxy substituent is one or more independently selected from the group consisting of alkenyl, amine, monoalkylamino, dialkylamino, alkoxy, cycloalkyl, hydroxyl, carboxyl, autogen, cyano, polyfluoro Alkyl, polyfluoroalkoxy, ammonium amine, S &amp; amine, ammonium, ammonium, ammonium, ammonium, amido, substituted or unsubstituted A group of a group consisting of a substituted aryl group and a substituted or unsubstituted heterocyclic group; the heterocyclic group substituent is one or more independently selected from alkyl, amine, amidine, and monoalkylamino , Cycloalkenyl-alkylamino, dialkylamino, alkoxy, alkoxyalkyl, hydroxyl, hydroxyalkyl, cycloalkyl, carboxyl, carboxamide, halogen, haloalkyl, cyano, polyfluoro Alkyl, polyfluoroalkoxy, alkanesulfonyl, 88828.doc 200418452 alkylcarbonyl, cycloalkylcarbonyl, alkoxycarbonyl, thiol, oxy, substituted or unsubstituted aryl, aralkyl Groups of groups consisting of substituted or unsubstituted heteroaryl groups; Heteroaryl substituents are one or more independently selected from alkyl, amino, alkoxy, alkoxyalkyl, hydroxyl, hydroxyalkyl , A cycloalkyl group, a carboxyl group, a carboxamide, a halogen, a polyfluoroalkyl group, a polyfluoroalkyl group, an alkyl group, an alkyl group, and an oxygen group; the benzyloxy substituent is One or more independently selected from the group consisting of alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, hydroxyl, carboxyl, alkoxycarbonyl, halogen, cyano, fluorenyl and phenyl The aryl substituent is one or more independently selected from the group consisting of alkyl, alkoxy, hydroxyl, itin, polyfluoroalkyl, polyfluoroalkoxy, cyano, amino, monoalkylamino, and dioxane A group consisting of an amino group, an amine alkyl group, an alkoxyalkoxy group, an amine group, an amine group, a carboxyl group, an alkanesulfonyl group, an alkoxycarbonyl group, an alkoxycarbonyl group, a mercapto group, and a heterocyclic group; and Its pharmaceutically acceptable salt. 3. —a compound of the formula, — Among them: R1 represents a group selected from the group consisting of hydrogen, alkynyl, halogen and cyano; R2 represents a group selected from hydrogen, substituted or unsubstituted alkyl, substituted or 88828.doc -6- 200418452 Unsubstituted alkoxy, hydroxyl, cycloalkyl, cycloalkoxy, polyfluoroalkyl, polyfluoroalkoxy, halogen, amine, monoalkylamino, dialkylamino, cyano, A group of a group consisting of substituted or unsubstituted benzyloxy and a substituted or unsubstituted heterocyclic group; R3 represents a group selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted Alkoxy, fluorenyl, halogen, hydroxy, polyfluoroalkyl, polyfluoroalkoxy, formamyl, carboxyl, alkylcarbonyl, alkoxycarbonyl, hydroxyalkylcarbonyl, amino, substituted or unsubstituted Monoalkylamino, dialkylamino, cyano, amidino, alkoxyamido, substituted or unsubstituted heteroarylamino, ethylamino, aminomethyl, methylamino, aminomethyl , Continued amines, substituted sulfonamides, substituted or unsubstituted heterocyclic sulfonylsulfonyl, alkylthio, alkylthiosulfenyl, alkylsulfonyl, alkylsulfonic acid and Substituted or unsubstituted heterocyclic group and -0 (CH2) -C (= 0) -R7; fU represents a group selected from the group consisting of hydrogen, alkyl, halogen and alkoxy R5 represents a group selected from the group consisting of alkane (Ci-CO group and cycloalkyl group); R6a represents a group selected from substituted aryl group and substituted or unsubstituted heteroaryl group Base 7 represents a group selected from the group consisting of a dialkylamino group, a substituted or unsubstituted arylamine group, a substituted or unsubstituted heteroarylamine group and a substituted or unsubstituted aryl group The monoalkylamino substituent is one or more groups independently selected from the group consisting of cycloalkyl, hydroxyl, alkoxy and substituted or unsubstituted heterocyclic groups; 88828.doc 200418452 This The arylamine substituent and the heteroarylamine substituent are one or more groups independently selected from the group consisting of an alkyl group and an alkoxycarboxyl group; the sulfonamide substituent is one or more groups independently selected from an alkenyl group and a cycloalkane Group, alkoxy, hydroxyl, functional element, polyfluoroalkyl, polyfluoroalkoxy, carboxyl, alkylcarbonyl, alkoxycarbonyl, carboxamide, substituted or unsubstituted A group of a group consisting of a substituted aryl group and a substituted or unsubstituted heterocyclic group; the heterocyclic sulfonyl substituent is one or more members independently selected from the group consisting of an alkoxy group and a cyclic group The alkyl substituent and the alkoxy substituent are one or more independently selected from alkenyl, amine, monoalkylamino, dialkylamino, alkoxy, cycloalkyl, hydroxyl, carboxyl, halogen , Cyano, polyfluoroalkyl, polyfluoroalkoxy, ammonium, ammonium, ammonium, ammonium, ammonium, carboxyl, mirror, benzo [1,3] 2, a group consisting of a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group; the heterocyclic group substituent is one or more independently selected from alkyl, amine, and amine Base, monoalkylamino, cycloalkyl-alkylamino, dialkylamino, alkoxy, alkoxyalkyl, hydroxyl, hydroxyalkyl, cycloalkyl, carboxyl, carboxamido, halogen, haloalkyl , Cyano, polyfluorenyl, polyfluorinyloxy, alkynyl, alkylcarbonyl, cycloalkylcarbonyl, alkoxycarbonyl, mercapto, oxy, substituted or unsubstituted aryl, A group of a group consisting of an alkyl group and a substituted or unsubstituted heteroaryl group; the heteroaryl substituent is one or more independently selected from alkyl, amino, alkoxy, oxo, Base, benzyl, cyclamyl, sulfonyl, benzylamine, pixel, polyfluoroalkyl, polyfluoroalkoxy, alkylsulfonyl, mercapto and 88828.doc 200418452 oxygen ; M oxy substituents are one or more independently selected from alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, hydroxyl, carboxyl, alkoxycarbonyl, halogen, cyano, fluorenyl and The group of the group consisting of phenyl groups; 4. 5. The alkyl substituent is one or more independently selected from alkyl, alkoxy, hydroxyl, halogen, polyfluoroalkyl, polyfluoroalkoxy, cyano Group, amine group, monoalkylamino group, dialkylamino group, amine alkyl group, alkoxyalkoxy group, fluorenylamino group, fluorenylamino group, carboxyl group, alkanesulfonyl group, alkylcarbonyl group, alkoxycarbonyl group, thiol group The base of the group consisting of each group, and its pharmaceutically acceptable salts. The compound according to item 1 of the scope of application, wherein r5 is methyl. The compound according to item 1 of the scope of patent application has the following formula: Among them, R1, R3 and 4 are as previously defined, and Aik is an alkyl group and a pharmaceutically acceptable salt thereof. A compound of the formula Where: I represents a group selected from the group consisting of hydrogen, methyl and chloro; 88828.doc 200418452 h represents a group selected from hydrogen, methyl, ethyl, isopropyl, n-butyl, cyclopropyl, hydroxyl , Methylol, methoxymethyl, methoxy, trifluoromethoxy, difluoromethoxy, cyclopropylmethoxy, carboxymethoxy, cyanomethoxy, cyanomethylmethoxy, 1 -¾methyl-cyclopropylmethoxy, carbamoylmethoxy, methylaminemethylmethoxy, diethylaminemethylmethoxy, (4-ethoxycarbonyl-phenylaminemethyl) Fluorenyl) -methoxy, tert-butoxycarbonylmethoxy, ethoxy, 2-methoxyethoxy, 2-chloro-ethoxy, 2-carboxyethoxy, 2,2,孓 Difluoroethoxy, 1- (4-fluoro-phenyl) _ethoxy, 2-fluoro-phenyl) -2-oxy-ethoxy, 2- (4-methoxy-benzene ) -2_oxy_ethoxy, propoxy, isopropoxy, 2-oxy-propoxy, 2-hydroxy_propoxy, 3-hydroxy-propoxy, 2-hydroxy-2 -Methyl-propoxy, 3-bromo-propoxy, 3-ethoxy-propoxy, butoxy, 2-hydroxy-butoxy, cyclopentyloxy, fluorenylpropoxy, Cyano, chloro, fluoro , Methanesulfonic acid, benzyloxy, 2-phenylfluorenyloxy, 2-difluoromethoxy-benzyloxy, 3-methoxy-loweroxy, 3-methoxycarbonyl-benzyloxy, 3 -Carboxy-benzyloxy, 3-cyano-benzyloxy, 4-methoxy-benzyloxy, 4-fluoro-benzyloxy, 4-cyano-benzyloxy, 4-methoxycarbonyloxy Group, / μ carboxy-methyloxy, 4-carboxy-3-hydroxyoxy, 4-methanesulfonyl-fluorenyloxy, 3,4-difluoro-benzyloxy, 3,5-dimethoxy Methyl-fluorenyloxy, 2,2-dimethyl-4-oxy-4H-benzo [1,3] difluoren-5-ylmethoxy, 2,2-dimethyl-4-4-oxyl -411-benzo [1,3] difluorene-7-ylmethoxy, 2,2_dimethyl_4_oxy-4H-benzo [1,3] Nisakigen-6- Methoxy, 3-chloromethyl_ [1,2,4] thiadiazol-5-yloxy, 5-chloro- [1,2,4] thiadiazol-3-ylmethoxy , 5-chloro- [1,2,3] thiadijun-4-ylmethoxy, 5-p-tolyl- [i, 3,4p difluoren-2-ylmethoxy 88888.doc- 10- 200418452 group, 5- (3,5-dimethyl_isoxazole_4_yl number diazol_3-ylmethoxy, 5- (cyclopropylmethyl-amino)-[; 1, 2,4] fluoradiazolylmethoxy, 5-second β-butyl- [1,2,4] pyridazol-3-ylmethoxy 5- (4-methoxy-phenyl) · Π, 2,4] fluorenediazole_3-ylmethoxy, 5-diethylaminofluorenediazole_3-ylmethoxy, [丨, 3,4] pyrimidazol-2-ylaminemethylamidinomethoxy, 3,5-dimethyl-isoisonazol-4-yl, isoxazol-3-ylmethoxy, 3,5 -Dimethyl-isoindazol-4-ylmethoxy, 5-methyl-isoxazol-3-ylmethoxy, thiazolylmethoxy, thiazol-4-ylmethoxy, 2-methyl -Thiazole-4-ylmethoxy, 1-tetramethyl-2-yl-ethoxy, thiazole-2-ylaminomethylmethylmethoxy, (4,5-dimethyl-thiazole-2- Methylaminomethylmethyl) -methoxy, 4-chloro-1-methyl-1fluorene-pyrazol-3-ylmethoxy, 2-pyrazol-1-yl-ethoxy, 2- (3 , 5-dimethyl-pyrazol-1-yl) · ethoxy, 4-ethoxycarbonyl-pyrazol-2-ylmethoxy, 4-carboxy-pyrazol-2-ylmethoxy, 5 _Amino_4H- [1,2,4] triazol-3-ylmethoxy, thien-2-yl, furan-2-yl, 2-morpholin-4-yl-ethoxy, 3 -Hexahydro-1-Hydroxy-1-yl-propoxy, tetrahydro-crean-2-yl, 1-methyl-1H-tetramethyl-5-ylmethoxy, 1-methyl-1H- Imid-2-ylmethoxy, 1-Lee-1H-imid-2-ylmethoxy, 3H-Weijun-4-ylmethoxy, P specific bite A group consisting of 4-yl-methoxy, 6-bromomethyl-pyridin-2-ylmethoxy, and 2- (4-cyanohexahydropyridine-; μyl) -ethoxy ; R3 represents a member selected from the group consisting of hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, 1-hydroxy-ethyl, 1-acyl-2-methyl-propyl, 1-hydroxy-1-methyl-ethyl Base, formamidine, basal, acetyl, acetyl, acetyl, phenyl, phenyl, acetic, 2 ** acetyl-ethoxy, phenyl, dimethylenepentamine-1-yl, Acid amine, amine, methylamine, dimethylamine, ethylamine, diethylamine, 88828.doc -11- 200418452 isopropylamine, tertiary-butylamine, Ethyl-methyl-amino, 2-methoxy-ethylamino, cyclopropylmethyl-amino, 2,3-dihydroxy-propylamino, 1-methylamino-ethyl , Dimethylaminomethyl, 1-amino-1-methyl-ethyl, 2-amino-l-acyl-1-methyl-ethyl, acetateamino, 1-ethylamino Methyl-1-methyl-ethyl, (2-methyllactyl-ethyl) -methyl-amino, ethyl- (2-methoxy-ethyldonyl) -amino, 3-muryl- Propane-1-continued alkylamine, methylsulfonylamino, ethyl-methanesulfonyl- Amino group, isopropyl-methanesulfonyl-amino group, isobutyl-f-alkylsulfonyl-amino group, cyclobutyl-methanesulfonyl-amino group, ammonium-methanesulfonic acid group -Amine, Cyclopropylmethyl-methylsulfanyl-amino, (2-Cycloyl-ethyl) -methylsulfanyl-amino, (2- # methyl-propyl) -Methanesulfonyl-amino, (2-fluoro-ethyl) -methanesulfonyl-amino, 2- (4-fluoro-phenyl) -2- # to yl-ethyl] -formyl Burning acid-amino, methylol-cyclopropylmethyl) -methanesulfonyl-amino, (4-carboxy-fluorenyl) -methylsulfanyl-amino, amino-propyl Horizontal g-Amino, Amino-Acetyl-Methylmercapto-Amine, Ethyl-Methylsulfonyl-Amino, Methyl-Methylsulfonyl-Amino, Methanesulfonylamine Methyl-methyl, 1-methanesulfonylamino-1-methyl-ethyl, methyl-S &amp; yl-methylamino, 1- (methylalanyl-methyl-amino) -ethyl Methyl, methanesulfonyl-propyl-amino, methanesulfonyl- (2-methoxy-ethyl) -amino, methanesulfonyl- (2,2,2-trifluoro · ethyl ) _ Amino group, methylamino acid group- (2-oxy-propyl) -amino group, methylamino acid group_ (2_ di Gasomethoxy-ethyl) -amino group, methylsulfonyl- (4-methoxy-methylene group) _amino group, methanesulfonyl- (4-methoxycarbonyl-benzyl) -amine Methyl, methanesulfonyl-methoxymethyl-amino, methanesulfonyl-methylaminomethylmethylmethyl-amine, (methanesulfonyl-methyl-amino) -methyl, aminosulfonyl Fluorenyl, methylamine continued 88828.doc -12- 200418452 fluorenyl, dimethylaminesulfonyl, ethylaminesulfonyl, cyclopropylaminesulfonyl, cyclobutylaminesulfonyl, 3- Methanesulfonyl-phenyl, 4-methanesulfonyl-phenyl, phenyloxy, 1Η-ρ bis-4-yl, 2H-17 bis-3-yl, 1-methyl-3-yl , 2-methyl-2H-pyridyl-3-yl, 5-methyl-1H-p than 4--4-yl, 5-methyl-211_pyrazol_3-yl, 1,5-di Methyl-1H-pyrazol-3-yl, 2,5-dimethyl-2H-pyrazol-3-yl, 2,5-dimethyl-2H-pyrazol-3-ylamino, 3, 5-dimethyl-1H-pyrimidin-4-yl, 1,3,5-trimethyl-111-pyrazol-4-yl, isoxazol-3-yl, 5-methyl-isozazol -3-yl, 3-cyclopropyl-isoazazol-5-yl, 5-cyclopropyl-isoazazol-3-yl, 3,5-dimethyl-isoazin-4-yl, 3 , 5-Dimethyl-iso-4-ammonium-4-ylamino, 5-methoxy Iso-isozazol-3-yl, 5-ethoxymethyl-isoindazol-3-yl, 5-isopropoxymethyl-iso $ -3-yl, 5- # is methyl- Isoamidine-3-yl, 4- (2-ethenyl-ethyl) -isoazazol-3-yl, 3-methoxymethyl-5_methyl-isopurazol-4-yl ^ 5 -Methoxyfluorenyl-3-methylisoxazol-4-yl, 5-cyclopropyl-3-methoxymethyl-isoxazol-4-yl, 3-cyclopropyl-5- Methoxymethyl-isoxazol-4-yl, (3,5-dimethyl-isopurazol-4-ylmethyl) -methanesulfonyl-amino, 3-methoxymethyl- Isoxazol-5-yl, 3-methyl-isoxazol-5-yl, methanesulfonyl- (5-methyl-isoxazol-3-ylmethyl) -amino, thiazole-2- Methyl, oxazolyl-5-yl, methanesulfonyl-pyrimazol-2-ylmethyl-amine, methanesulfonyl-pyrimazol-4-ylmethyl-amino, methanesulfonyl- (2 -Methyl-pyrimazol-4-ylmethyl) -amino group, (4-multil-sep-2-enylmethyl) -methanesulfonic acid-amine group, (4-ethoxyl group) -p-supplied_2_ylmethyl) _ 'pit acid group-amino group, p-Hydro-3- group, p-Hydro-4- group, p-Hydro-4-ylamino group, 6-Amino radical-3-yl, methylphenidyl-pyridin-4-ylmethyl-amine, (6-bromoT-yl-pyridine 2-ylmethyl) -methanesulfonium 88828.doc -13-200418452 fluorenyl-amino, erlotin-1-yl, pyrrolidin-2-yl, erlotinyl, 3-# to 1-yl, p-pyrrolidine, 3-yl, p-pyrrolidine, 1-continuous acid group, oxy-pyrrolidine-3-yl, 1-ethyl-pyrrolidine- 2-yl, ι-acetic acid-1? Biloline-3-yl, 1-aminomethyl blue cyano-ρbiloline-2 -yl, methylcarbamic acid_ρbiloline-2-yl , 4-methylamine formamyl-5-oxy ^ biluozan: phenyl group, phenylene group-say ρGedian-2-group '1-methanyl group ρ Bilodian _ 2基 group, 1 -methylamino group-ergoline-3-yl group, 3-amino group -ρ ratio ρ group, 3-methylaromatic acid group-ρ ratio ρ group-1 group, lH-ρ bilo-2-yl, iH-p bilo-3-yl, 3-cyano-4- # to yl-2-oxy-2,5-dihydrobilo-1-ylmethyl , Sulfur-2-yl, furan-3-yl, (furan-3-ylmethyl) -amino, tetrahydro-sulfur-3-yl, (tetrahydro-sulfan-2-ylmethyl)- Amine group, [1,3,4] 17 dicrot-2-yl group, [1,2,4] slogan difluoren-3-yl group, 5-methyl- [1,2,4] 0 bijun -3_yl, 5-methyl- [1,3,4] Slogans dijun-2-yl, 5-trifluoromethyl- [1,2,4] Dijun-3-yl, morpholin-4-yl, 2,6-dimethyl-morpholin-4-yl, 2-morpholin-4-yl-ethylamino, morpholin- 4-contanoic acid group, mesylate- (2-morpholin_4-yl-ethyl) -amino group, thiomorpholin-4-yl, thiomorpholin-4-contanoic acid group, 1 _oxy_thiomorpholine-4-yl, 1,1-dioxy-1λ6_isop-sedad π_2-yl, 2-oxy_ Methyl-2-oxywazane &gt; 5-yl, π-Tetyl, 1Η-imidazol-4-yl, 1Η-imidazol-2-yl, 2,5-dioxy_imidazolidine_4 • Methyl, 4-methyl-2,5-dioxy-imidamine-4-yl, rhodamine-5 * · yl, 2,5-dimethyl-2Η- [1,2,4] tri Azol-3-yl, 2-methyl-2Η- [1,2,4] triazol-3-yl, 4Η- [1,2,4] triazol-3-yl, 5-methyl-2Η- [1,2,4] triazole-Hongji, iH-tetrazol-5-yl, 1-methyl-1fluorenyl-tetrazol-5-ylmethoxy, mesityl- (1-methyl- 1Η-tetra-12-s--5-ylmethyl) -amino group, 7T mouse p-pyridin-1-yl group, 4-fluoro group -14-88828.doc 200418452 hexahydropyridin-1-yl group, 4,4 -Difluoro-hexahydropyridin-1-yl, 3-hydroxy-hexahydropyridin-1-yl, 4-hydroxy-hexahydropyridin-1-yl, 4-hydroxy-hexahydropyridine-1-sulfonyl , 4- Carbamidyl-hexahydropyrimidin-1-yl, 4-methyl-hexahydropyrrolyl-1-yl and% chloro- [1,2,4] pyrimidazol-3-ylmethyl; R4 represents a group selected from the group consisting of hydrogen and methyl; Rs represents a group selected from the group consisting of methyl, ethyl, isopropyl, and cyclopropyl; and R6 represents a group selected from phenyl, 4-methyl-phenyl, 4-ethyl-phenyl, 4-methoxy-phenyl, 4-hydroxy-phenyl, 4-bromo-phenyl, 2-chloro-phenyl, 2- Gaso-phenyl, 4-fluoro-phenyl, 2,4-difluoro-phenyl, 3,4-difluorophenyl, odoryl-3-fluoro-phenyl, 3-chloro 4-Fluorophenyl, 4-chlorofluoro-phenyl, 2,4,5-trifluoro-phenyl, 3-fluoro-'methyl-phenyl, 'fluoro-3- Methyl-phenyl, 4-fluoro-3-hydroxy-phenyl, 2-ethoxy-4-fluorofluorophenyl, 3-trifluoromethyl-phenyl, 4-trifluoromethyl-benzene Methyl, cyano-phenyl, 4-amino-phenyl, 4- (ethylamidoamino-methyl) -phenyl 4-morpholin-4-yl-phenyl, 4-p-bilo Yodo-1-yl-phenyl, succin-2-ylfuran-3-yl, 3-methyl-furan-2-yl, pyrimin-2-yl, 5-chloro-thien-2-yl, Pyridyl and pyridin-3-yl; its limitations With the proviso that the formula does not include compounds selected from the group consisting of 5-methoxybenzyl-benzofuran-3-carboxylic acid formamide and 5-hydroxy-2-phenyl-benzopran-3-carboxylic acid Formamidine acid. The compound according to item 1 of the scope of patent application, which is selected from the group consisting of 2-pyran-3-yl-5-methoxy-benzofuran_3_carboxylic acid formamide; 88828. doc -15-200418452 2-phenyl-5-trifluoromethoxy-benzofurancarboxylic acid formamidine; 2_ (3,4-difluoro-phenyl) -5-methoxy_benzofuran -3_ formamidine carboxylic acid; 2- [4- (ethylamidoamino-methyl) _phenyl] -5-isopropoxy_benzofuran_3_ formamidine carboxylic acid; 2- ( 4-hydroxy-phenyl) _5_isopropoxy-benzofuran_3_carboxylic acid formamide; 2- (4-fluoroyl-phenyl) _5_isopropoxy_6-pyrrolidine― 丨—Methyl-benzofuran_3_carboxamide; 5-difluoromethoxy-2- (4-fluoro-phenyl) _benzofuran_3-carboxamide; 2- (4 -Fluoro-phenylisopropoxy-6- (2-methoxy-ethylamino) -benzofuran-3-carboxylic acid formamidine; 5-methyl-2-phenyl-benzofuran _3_ formamidine carboxylic acid; 5-methyl-2- (4-fluoroyl_phenyl) _benzofuran_3-formamide carboxylic acid; 2-phenyl-5- (2,2, 2-trifluoro-ethoxy) -benzofuran_3_carboxylic acid formamide; 2- (4-fluoroyl · phenyl) _5_methoxy-benzofuran_3_carboxylic acid form Amine; 6-bromo-2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamide; 5-methoxy-6-methyl-2- Phenyl-benzofuran-3-carboxylic acid formamide; 6- (3-Amino-pyrrolidin-1-yl) -2- (4-fluoro-phenyl) -5-isopropoxy- 2,3-dihydro-benzofuran-3-carboxylic acid formamide; 6-amino-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxy Formamidine acid; 6-Amino-2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamide; 6-Ethylamino-2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxyl 88828.doc -16- 200418452 formamidine acid; 2- (4-fluoro-phenyl) -5-iso Propoxy-6-methylamino-benzofuran_3-ammonium methylamine; 6-dimethylamino-2- (4-fluoro-phenyl) -5-isopropoxy- Benzofuran_3_ formamidine carboxylic acid; 2- (4-fluoro-phenyl) -5-isopropoxy-6-methanesulfonylamino-benzocaran-3-carboxylic acid formamidine Amine; 6-ethylamino-2- (4-fluoro-phenyl) _5 • isopropoxybenzofuran-3-carboxylic acid formamidine; 6-diethylamino-2- (4 -Fluoro-phenyl) -5-isopropoxy-benzofurancarboxylic acid formamidine; 2- (4-Fluoro-phenyl) -5-isopropoxy-6-morpholin-4-yl-benzofurancarboxylic acid formamide; 5-methoxy-4-methyl-2 -Phenyl-benzofuran_3_chloroacetic acid methylamine; 5-cyano-2-phenyl-benzocuran_3_metamic acid amine; 5-isopropoxy-2-pyridine- 4-methyl-benzofurancarboxylic acid formamidine; 6- (3,5-dimethyl-isoxazole_4_yl) _2_ (4_fluoro group · phenylmethoxy_benzofuran-3 -Formamidine carboxylic acid; 2- (4-fluoro-phenyl) -6- (methanesulfonylmethyl-amino) amino_methoxy_benzofuran-3_formamidine carboxylic acid ; 2- (4-fluoro-phenyl) -5- (4-methoxy_benzyloxymorpholine_4_yl_benzofuran-3-carboxylic acid formamide; 2- (4- Fluoro · phenyl) -6- [Methanesulfonyl 4-methoxy_benzyl) _amino] -5- (4-methoxy-benzyloxy) _benzofuran_3_carboxy Formamidine acid; 88828.doc -17- 200418452 5-ethoxy-6- (ethyl-methanesulfonamido_amino) fluoro_phenyl) _benzyfuran-3-carboxylic acid formamidine ; 2- (4-Fluoro-phenyl) _6_morpholine_4_ylaminothiazolylmethoxy) _benzyfuran-3-carboxylic acid formamide; 2_ (4-fluoro-benzene ) Isopropoxy [methanesulfonyl _ (2_oxy-propyl) -amino] -benzofuran-3-carboxylic acid formamidine; 2- (4-fluoroyl-phenyl) dongmodolin_4-yl-5 deca Oxazolyloxybenzobenzofuran-3-methanamide; 2- (4-fluoro-phenyl) isopropoxy (methanesulfonyl-thiazole-cardiomethyl-amino)- Benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) _6- (5- # is methyl-isoazazol-3-yl) -5-isopropoxy_benzene Aminopyridine-3-carboxylic acid carboxylic acid amine; 5-ethoxy_2_ (4-denyl-phenyl) -6- (methylpyridyl-methyl-amino) _benzofuran-3- Formamidine carboxylic acid; 4- [2- (4-fluoro-phenyl) -6_ (methanesulfonyl-methyl-amino) _3-methylaminomethyl-benzofuran_5_yl Oxymethyl] -2-hydroxy-arsinic acid; 2- (4-fluoro-phenyl) _6_ (5_hydroxymethyl-isohumazol-3-yl) -5-methoxybenzocran- Formamidine 3-chitoate; 2- (4-fluoro-phenyl) -6_ [; 4- (2-hydroxy-ethyl) -isoxazol-3-yl] -5-methoxy-benzene Benzofuran_3_carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6-[(2 • hydroxy-ethyl) · methanesulfonyl-amino] -methoxy-benzene Benzofuran-3-carboxylic acid formamidine; 5-cyclopropyl-2- (4-fluoro-benzene ) -6-[(2-Cyclo-ethyl) -methanesulfonyl-amino-amino] -benzofuran-3-carboxylic acid formamidine; 88828.doc -18- 200418452 5 -ethyl- 2- (4 -Gas-phenyl) -6-methylamino-benzyl-benzoanan-3_carboxylic acid formamidine; 5-ethyl-2- (4-fluoro-phenyl)- 6- (methanesulfonyl-methyl-amino) _benzofuran-3-carboxylic acid formamidine; 5-ethyl-2- (4 · fluoro-phenyl) -6-[(2- Hydroxy-ethyl) -methanesulfonyl-monoamino] -benzofuran-3-carboxylic acid formamidine; 6- (1-ethoxyl-pyrrolid-2-yl) -2- (4 -Fluoro-phenyl) -5 -methoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) _5_methoxy-6- (2-oxy -Sakitoyo- 5-yl) -benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-dongylbenzyl-1-methyl_ethyl) _5_methoxy-benzene Benzofuran-3-carboxylic acid formamidine; 2_ (4-fluoro_phenyl) _5_methoxy_6- (5-methyl- [1,2,4] pyridazol_3_yl) -Benzofuran-3-carboxylic acid formamide; 6- (3,5-dimethyl_isoxazole_4_yl) -2- (4-fluoro-phenyl) · 5_ (3_hydroxy · Propoxy) _benzofuran_3_carboxamide; 2- (4-fluoro-phenyl) _6_ (methane Fluorenyl_methyl_amino) _5_ (2_morpholin-4-yl-ethoxy) _benzoic acid ammonium formate; 5_ (diphenyl-2-yl-methoxy)- 2-Phenyl-benzoxan-3-carboxylic acid formamide; 5methoxy-2- (4-methoxy-phenyl) -benzoxan-3-3-chitoformamic acid form; 5 -Methyllactyl-2- (3-trifluoromethyl-phenyl) _benzofuran_3 side acid methylamine; 5-methoxy-2- (4-trifluoromethyl-phenyl) · Benzobenzofuran-3 methacrylic acid methylamine; 5-ethoxy-2-phenyl-benzoic acid-3-amino acid formic acid amine; 2- (2-fluoro group · phenyl> 5 -Methoxy-benzofuran_3_carboxylic acid formamide; 88828.doc -19- 200418452 5-isopropoxy-2-phenyl-benzofuran_3_carboxylic acid formamide; 5-butane Formamidine oxy-2-phenylbenzofurancarboxylic acid; Formamidine 2-phenyl-5-propoxy-benzofuran-3_carboxylic acid; 5-methoxy-2- (2, 4,5-trifluoro-phenyl) -benzofuran-3-carboxylic acid formamide; 5-methoxy-7-methyl-2-phenyl-benzofuran-3-chinoic acid Fluorenamine; 2- (4-fluoro-phenyl) -5- (2,2,2-trifluoro-ethoxy) _benzofuran_3_ formamidine carboxylic acid; 2- (4-fluoro -Phenyl) -5-isopropoxy-benzofuran_3-carboxylic acid Formamidine; 2- (2-chloro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine; 6-methoxy-2-phenyl-benzofuran-3 -Formamidine double acid; 2-furan-2-yl-5-methoxy-benzofuran-3-carboxylic acid formamide; 2- (3-fluoro-4-Tyl-phenyl)- 5-methoxy-benzofuran_3-carboxylic acid formamide; 2- (4-bromo-benzyl) -5-methoxy-benzofuran_3_-chinocarboxylic acid amine; 2- (4-Fluoro-3-methyl-phenyl) -5-methoxy-benzofuran-3-carboxamide; 2- (4-denyl-phenyl) -5-methoxy- 7-Methyl-benzofuran_3_carboxylic acid amine formic acid; 5-Rhamtyl-2- (4-fluoro-phenyl) -benzofuran-3-metanosylamine; 5-third -Butyl-2-phenyl-benzocaran-3-carboxylic acid methylamine; 5-chloro-2-p-methylalanyl-benzocaran-3-metamic acid amine; 2- ( 3-chloro-4-fluoro-phenyl) -5-methoxy-benzofuran-3_carboxylic acid formamide; m 88828.doc -20- 200418452 2- (cardiochloro-3-fluoro -Phenyl). 5_methoxy_benzoicronic acid, methenylamine; m'pan, J, 2- (4-fluoro-phenyl) -5-isopropoxy-6_ Methyl_benzofuran_3_carboxylic acid formamide; 3--3-carboxylic acid form 2- (4-fluoro -Phenyl) -5-isopropoxymethyl_benzofuranamine; 2- (4-fluoro-phenyl) -5_methoxy_6_fyl_benzofuran_3_carboxylic acid Formamidine; 5-fluoro-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid formamidine; 2- (4-ethyl-phenyl) -5-fluoro- Benzofuran_3-ammonium acetamidine; 5-ethyl-2-phenyl · benzofuran-3-chimamine methylamine; 2- (5-chloro · fluoren-2-yl ) -5-methoxy-benzofuran-3_carboxylic acid formamide; 5-hexylpropoxy-2-phenyl-benzofuran-3-metamic acid amine; 2- (5-chloro Methyl-fluoren-2-yl) -5-ethoxy-benzofuran-3-carboxylic acid formamidine; 5-methoxy-2-P cephen-2-yl-benzocran-3 -Ammonium formate; 5-Muryl-2-? Pyridin-3-yl-benzoanan-3 -pyridinamine; 2- (4-bromo-3-fluoro-phenyl) -5-isopropoxy_benzofuran_3_carboxylic acid formamide; 2- (2,4-difluoroyl-phenyl) -5-isopropoxy · benzofuran-3_carboxylic acid Formamidine 6-bromo-2- (4-fluoro-phenyl) -5-isopropoxy-benzofurancarboxylic acid formamidine; 5-methoxy-2- (4-morpholine -4-yl-phenyl) _benzofuran_3_carboxamide; 88828.doc -21-200418452 5,6-di Methoxy-2-phenyl-benzofuran-3-carboxylic acid formamidine; 5-isopropoxy-2- (4-p-bilopido-1-yl-phenyl) -benzylpyran Methylammonium double acid, 5-amino-2-p than yodo-4-yl-benzoanan-3-methyldonylamine; 2- [2- (4 -amino-dongyl) -6 -Methyl-3-methylcarbamic acid benzouran-5_yloxy] -propanoic acid; 6-acetamido-2- (4-fluoro-phenyl) -5 -isopropoxy Methylbenzyl-benzocaran-3-carboxylate; 2- (4-amino-phenyl) -5-isopropoxy-benzocaran-3-metanoformamide; 2- (4 -Fluoro-fluorenyl) -5 -isopropoxy-6- (2 -morpholin-4-yl · ethylamino) -benzofuran-3-carboxylic acid formamidine; 2- (4 -Fluoro * yl-phenyl) -5-isopropoxy-6-hexahydrop-pyridine-1-yl-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoroyl-winter ) -5,6-dimethoxy-benzoanan-3-methanamine; 2- (4-fluoro · phenyl) -5 -methoxy-6-morpholin-4 -Methylbenzamine-3-benzoic acid; 2- (4-bromo-dongyl) -5 -isopropoxy-benzobenan-3 -methanamine chitosan; 2- (4-Fluoro-3-phenyl-phenyl) -5-isopropoxy-benzoic acid 3-methaneformamide; 2- (4-amino -Mcyl) -5 -isopropoxy-benzoanan_3_methanoamine; 5-methoxy-2-pyridin-4-yl-benzofuran-3-carboxylic acid formamidine ; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (3-methanesulfonyl-pyrrolidinyl) -benzofuran-3-carboxylic acid formamide; 6-trimethylene Methylpentamine-1-yl-2- (4-fluoro-phenyl) -5-isopropoxy-benzo88828.doc -22- 200418452 formamidine furan-3-carboxylic acid; 2- ( 4-Fluoro-phenyl) -6- (3_hydroxy_pyrrolidine ― 丨 -propyl ^ isopropoxy-benzocaran-3-carboxylic acid formamide; 2- (4-fluoro- Phenyl) _5-isopropoxy_6_ (methanesulfonyl-methyl_amino) _benzocaran-3-carboxylic acid formamidine; 2- (4-amino-phenyl) _6- [(Furan_3_ylmethyl) _amino] _5_isopropoxy_benzopyran-3-carboxylic acid formamidine; 6 &lt; 2,3_dihydroxy-propylamino) -2- (4-fluoro-phenyl) -5-isopropoxy_benzofuran-3-carboxylic acid formamide; 2- (4 -Fluoro-phenyl) -5-isopropoxy-6-isopropylamino-benzocaran-3-carboxylic acid formamidine; 6- (cyclopropylmethyl-amino) -2- (4-Fluoro-phenyl) _5-isopropoxy_benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5 -methoxy-6-pyrrolidine 1-yl-benzoxanan_3_methanoxamine; 5-pentoxy-2- (4-airyl-dongyl) -6-morpholin-4-yl-benzopyran Acidic formamide; 5-hydroxymethyl-2-phenyl-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-isopropoxy-6- [(2-methoxy-ethylmethyl_amino] -benzofuran-3-carboxylic acid formamidine; 6-amino-5_ + oxy-2- (4-fluoro- winteryl) -Benzoxan-3 -formamidine mesitamine; 5-isopropoxy-2- (3-methyl-furan_2_yl) -benzofuran_3_carboxamide;- 23-88828. doc 200418452 2- (4-Fluoro-phenyl) -6-methanesulfonamido-5-methoxy-benzoanan-3-guidate formamidine; 2- (4-fluoro- Phenyl) -5-isopropoxy-6-[(tetrahydro-octane-2-ylmethyl) amino] •• benzocran-3-metanosamine; 2- (4- Fluoro-phenyl) -5-lightyl-6-morpholin-4-yl-benzoanan A formamidine; 5-cyclopropylmethoxy-2- (4-fluoro-phenyl) -6-morpholine-4-yl-benzosulfan-3 -amine carboxylic acid; 6-chloro-2- (4-fluoro-phenyl) -5-methoxy-benzofuran_ 3-Methylmethoxamine; 6- (2,5-dimethyl-2H-pyrazole-3_ylamino) _2_ (4_fluoroyl_phenyl) _5_ is propoxy-benzo Osan-3-methamidomethanamine; 2- (4-fluorofluoro-phenyl) -6-morpholin-4-yl-5- (p-pyridol-4-ylmethoxy) benzofuran Formamidine-3-carboxylic acid; 6-decanyl-2- (4-fluoro-phenyl) -5-isopropoxy-benzopyranoline; formamide; 5-methoxy-2 -Phenyl-benzofuran_3-carboxylic acid acetamide; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (pyridin-4-ylamino) _benzo Methane-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (4 · methyl-hexahydro Phenyl) -benzofuran-3-chiamate formamidine; 6- (3-chloro-propane-1-sulfonylaminofluoro-phenyl) cyclo-isopropoxy-benzo Furan-3-carboxylic acid formamidine; 6- (1,1-dioxy-1 λ isopyrimidin_2_yl) · 2_ (4_fluoroyl_phenyl) _5_ 88828. doc -24- 200418452 isopropoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6-ureido-benzopyran Formamidine-3-chioate; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (isopropyl-methylsulfanyl gf-amino-benzofuran-3-carboxylate Formamidine acid; (cyclopropylmethyl-methanesulfonyl-amino) -2- (4-fluoro-phenyl) -5_isopropoxy-benzofuran-3-carboxylic acid formamide; (2,6-dimethyl-morpholin-4-yl) -2- (4-fluoro-phenyl) _5 · isopropoxy-benzoxan-3-methanoate; 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (1H-tetrazol-5-yl) -benzocran-3-methanoic acid formamide; 2, (4_ Fluoro-phenyl) -6- (4-hydroxy-hexahydropyridin-1-yl) -5-isopropoxy-benzylfuran-3-carboxylic acid formamidine; 2-(4 -amino- Winter-based) -6- (3-Methino-7T mouse pbito-1-yl) -5-isopropoxy-benzylfuran-3-carboxylic acid formamidine; 2, (4-muryl- Phenyl) -5 -isopropoxy-6- (morpholin-4-continued): _ benzofuran-3-carboxylic acid formamide; 2, (4-fluoro-phenyl)- 5-isopropoxy-6-methylaminesulfonyl-benzofuran 3 -metanoic acid Acid amines; L dimethylamine sulfonamido-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-methanoic acid formamide; 2- (4-amino -Phenyl) -5 -isopropyllactyl-6- (propan-2-ylamino) -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl)- 5 -isopropoxy-benzoic acid-3,6_dipic acid 6-brew 88888. doc -25- 200418452 amine-3-formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy_6_pyrimidin-5-yl-benzoanan_3_metanoate Fluorenamine; 6-tert-butylamino-2- (4-fluoro-phenyl) -5-isopropoxy-benzocaran-3-carboxylic acid formamide; 2- (4- Fluoro-phenyl) -5-isopropoxy-6-aminosulfonyl-benzosulfan_3_membranate, 6-cyclobutylaminesulfonyl-2- (4- Fluoro-phenyl) -5-isopropoxy-benzoanan-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -6-furan-2-yl-5-iso Propoxy-benzofurancarboxylic acid formamidine; 2- (4-fluoro-phenyl) -6-galan-3-yl-5-isopropoxy-benzosulfan · 3_ ^ acid formic acid Amine; 2- (4-Fluoro-phenyl) -5-isopropoxy-6-pyridin-3-yl • benzofurancarboxylic acid formamidine; 2- (4-fluoro-phenyl)- 5-isopropoxy-6- (pyrrolidine-1-sulfonyl) _benzofuran-3-carboxylic acid formamidine; 6-cyclopropylaminesulfonyl-2- (4-fluoro- Phenyl) -5-isopropoxy_phenylsulfanylfuran-3-methanoformamide; 6-ethylaminesulfonyl-2- (4-fluoro-phenyl) -5-isopropoxy -Benzoan-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy _6_ vinyl - benzofuran carboxylic acid acyl amine; 2- (4-fluoro-phenyl) - _5_ isopropoxymethoxy - benzofuran carboxylic 88828 _3_. doc -26- 200418452 formamidine; 6- (3,5-dimethyl-isohumazol-4-yl) _2- (4-fluoro-phenyl) _5_isopropoxy-benzofuran- Formamidine 3-carboxylic acid; 2- (4-Gas-phenyl) -6-methyldonyl-5-methylpropanyl-benzo-anan-3-formamidine chitosan; 2-( 4-Gas-phenyl) -6- (6-Gas-p-Hydro-3-yl) -5-isopropoxy-benzofuran-3-carboxylic acid formamide; 2- (4- Fluoro-phenyl) -5-isopropoxy-6- (methanesulfonylamino-methyl) -benzofuran-3-carboxylic acid formamidine; 6- (cyclopentyl-methanesulfonyl) -Amino) -2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6 -[(2-hydroxy-ethyl) alkanesulfonylamino] -5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl)- 5-Hydroxy-6-methoxy-benzofuran-3-carboxylic acid formamide; 5-ethoxy-2- (4-fluoro-phenyl) -6-morpholine-4-yl- Benzofuran-3-carboxylic acid methyltetracycline; 5- (4-fluoro-etooxy) -2- (4-fluoro-phenyl) -6-morpholin-4-yl-benzofuran Formamidine-3-carboxylic acid; 2- (4-fluoro-phenyl) -5-isopropoxy-6-humazol-5-yl- Benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6- (4-light-hexahydrop-pyridine-1-sulfonyl) -5 · isopropoxy- Benzofuran-3-carboxylic acid formamidine; 6- (4,4-difluoro-hexahydrop-pyridine-1 · yl) _2_ (4-fluoro-phenyl) -5 -isopropyl 88828. doc -27- 200418452 oxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -6- (4-fluoro-hexahydrop-pyridine-1-yl) -5-isopropoxy_benzofuran-3-carboxylic acid formamide; 5--methoxymethoxy-2- (4-amino-phenyl) -6-morpholin-4-yl- Benzalan-3-carboxylic acid carboxylic acid amine; 5-fluorenylpentyloxy-2- (4-amino group-winteryl) -6-morpho 117 lin-4-yl-chrysene-3 ~ Formamidine carboxylic acid; 2- (4-fluoro-phenyl) -5-hydroxy-6-methanesulfonylamino-benzofuran-3-chitoic acid formamide; 2- (4-fluoro- Phenyl) -5-isopropoxy-6- (thiomorpholin-4-phenylmethyl) -benzofuran-3-carboxylic acid formamide; 2- (4-fluoroyl-phenyl)- 6- (3-hydroxy-pyrrolidin-1-sulfonyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoroyl-phenyl) -5- Isopropoxy-6-p than methyl-4-methyl-benzocaran-3-carboxylic acid formamide; 1 (4-fluoro-phenyl) -5-isopropoxy-6- (3 -Methanesulfonyl-phenyl) -benzopyran-3-methylacetamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (4-methane continued fluorene -Phenyl) _benzocrean-3-methanoic acid formamide; 5- (2-chloro-ethoxy) -2- (4 -Fluoro-phenyl) -6-morpholin_4-yl-benzocaran-3-carboxylic acid formamidine; benzyloxy-2- (4-fluoro-phenyl) -5-formyl Oxybenzoxanthene methylformamide; Amino-2- (4-fluoro-phenyl) -5-hydroxy-benzofuran_3_carboxylic acid formamide; 88828. doc -28- 200418452 5,6-bis-fluorenyloxy-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5 -isopropoxy-6- (5-trifluoromethyl- [1,2,4] diazol-3-yl) -benzofuran-3-carboxylic acid formamidine; [2- (4-Gas-phenyl) -5 -isopropoxy-3-methylcarbamic acid-benzoanan-6-yl] -hexahydropyrine-1-carboxylic acid sulfonamide; 2- ( 4-Fluoro-phenyl) -5-isopropoxy-6-thiomorpholin-4-yl-benzocaran-3-carboxylic acid formamidine; 2- (4-fluoroyl-phenyl ) -5-Isopropoxy-3-methylamine formamidine-benzofuran-6-quinic acid; 2- (4-fluoroyl-phenyl) -5-isopropoxy-6_ (1- Oxy-thiomorpholin · 4-yl) -benzofuran-3-carboxylic acid formamidine; {[2- (4-fluoroyl-phenyl) -5-isopropoxy-3-methyl Carbamoyl-benzofuran-6-yl] -methylsulfanyl-aminopyroxyacetic acid; 6- (cyclobutyl-methanesulfonyl_amino) _2- (4-fluoro-phenyl ) _5_isopropoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy_6_ [methanesulfonyl_ (2_? Fluorolin-4-yl-ethyl) _aminobenzofuran-3_carboxylic acid formamide; 2- (4-fluoro-phenyl) -5,6- Hydroxy-benzofuran_3-carboxylic acid formamide; 2- (4-fluoro-phenyl) _5_isopropoxy_6_ [methanesulfonyl_ (2_methoxy_ethyl)- Amine] -benzofuran-3-carboxylic acid formamidine; 6-loweroxy-2- (4-fluoroyl_phenyl) isopropoxy_benzofuran_3 • formamidine carboxylic acid; 6- (fluorenyl-methanesulfonyl-amino group) 2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamide; 88828. doc -29- 200418452 6-ethenyl-2- (4-fluoro-phenyl) _5_isopropoxy_benzofuran_3_carboxylic acid formamide; 2- (4-fluoroyl-benzene ) -5-isopropoxymethanesulfonamidoamino_benzofuran-3-carboxylic acid isopropylamine; 2- (4-fluoro-phenyl) -5-isopropoxymethyl 412.4 ] Pyridazol-3-yl) -benzocran-3 -chitoic acid methylglycine; 2- (4-fluoro-phenyl) -5-isopropoxymethanesulfonamido-benzene Benzofuran-3-carboxylic acid cyclopropanamine; 2- (4-fluoro-phenyl) -5-isopropoxy-6-methanesulfonylamino-benzofuran-3-carboxylic acid ethylamidine Amine; 2- (4-Fluoro-phenyl) -5- (2-methyl-p-sedino_4-ylmethoxy) -6-morpholin-4-yl-benzofuran_3_ Formamidine carboxylate; 2- (4-fluoro-phenyl) -6_ (1-hydroxymethyl-ethyl) -5-isopropoxy-benzocaran-3-carboxylic acid formamide; 5 -[5- (3,5-Dimethyl-isopurazol_4_yldiazole_3_ylmethoxy)]-2- (4-fluoroyl_phenyl) _6_morphol 4- 4-Methyl-benzoic acid-3-methylacidamine; 5- (5-tert-butyl-Π, 2,4] pyridazol-3-ylmethoxy) -2- (4 -Fluoro-phenyl) -6-morpholinyl-benzofurancarboxylic acid formamidine; 2- (4-amino ' ) -5-isopropoxy-6- [1,2,4] pyridazol-3-yl-benzoanan-3-carboxylic acid formamidine; 5- (5-Gasyl- [1 , 2,4] thiadiazol-3-ylmethoxy) -2- (4-fluoro-phenyl) -6-morpho f'4-yl-benzofuran-3-carboxylic acid formamide; 2- (4-Gasyl-benzyl) -6-morpholinyl_5_ (5_p-tolyl 88828. doc -30- 200418452 indoxazol-2-ylmethoxy) -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -6-hydroxy-5-methoxy_ Benzofuran-3-carboxamidine; 2- (4-fluoro-fluorenyl) -5- (1-methyl-1H-tetrafluoren-5-ylmethoxy) -6-morpholin -4-yl-benzocran-3-methanoic acid methylamine; 2- (4-fluoro-phenyl) -5- (3-methoxy-benzyloxy) -6-morpholin 4-yl-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoroyl- winteryl) -5methoxy-6- (1-fluorenyl-1H -tetramethyl-5-yl Methoxy) -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5 · [1- (4-fluoro-phenyl) -ethoxy] -6 _Morphine-4-yl-benzofuran-3-carboxylic acid formamide; 5_ (4 • cyano-benzylmethoxy) -2- (4-fluoro-phenyl) -6_morpho Phenyl benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5- [5- (4-methoxy-phenyl)-[ι, 2,4] $ Difluorenyl · 3_ylmethoxy] -6-morpho-4wood-4-yl-benzocrean-3-amine carboxylate; 2- (4-fluoro-phenyl) -6-morpho Porphyrin-4-yl-5- (2-oxy_propoxy) _benzyfuran-3-carboxylic acid formamidine; 5- (1-fluorenyl-1H-imidazol-2-ylmethoxy) ) -2- (4-fluoro-phenyl) -6_morpholin-4-yl-benzofuran-3-carboxylic acid formamidine; 5- (3,5-dimethyl-isoxazole 4-ylmethoxy) -2- (4-fluoro-phenyl) _6_ morpholin-4-yl-benzocaran-3-amine acid formate; 2- (4-fluoro-benzene ) -5- (5-methyl-isoxazol-3-ylmethoxy) morpholin-4-yl-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro- Phenyl) -5-isopropoxy-6-p-xen-2-yl-benzofuran 88828. doc -31-200418452 formamidine acid; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (1fluorene-pyrrole-2-yl) -benzofuran-3-carboxylic acid methyl ester Fluorenamine; 2- (4-fluoro-phenyl) -6- (isopropyl_methanesulfonyl-amino) methoxy_benzofuran-3-carboxylic acid formamide; 1 (4- Fluoro-phenyl) -6- (1-hydroxy-ethyl) -5_isopropoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5 -Isopropoxy-6-morpholin-4-ylmethyl-benzopyran-3-carboxylic acid formamidine; h (4-fluoro-phenyl) _6_hydroxymethyl_5_iso Propoxy-benzofuran_3_carboxylic acid formamide; 2_ (4-fluoro-phenyl) -5- (3H-imidazol-4-ylmethoxy) _6_morpholine_'yl- Benzofuran-3-methanoic acid formamidine; 2- (4-fluoro-phenyl) _5_ (2_methoxy_ethoxy) _6_morpholine_4_yl-benzofuran- Formamidine 3-carboxylic acid; 2_ (4-fluoro-phenyl) -5_isopropoxy_6_pyrazol_5_yl_benzyfuran_3_formamidine carboxylic acid; &amp; 5 Mono (4-chloro-1-methyl-1H-pyrazol-3-ylmethoxy) _2_ (4, fluoro-phenyl) morpholine_4-yl-benzofuran-3-carboxylic acid Formamidine; ^ (cyano-fluorenyl-methoxy) _2_ (4-fluoro-phenyl) _6_Morpholine_4_yl-benzofuran-3-carboxylic acid formamidine; 2 (4-fluoro-tolyl) _5_isopropoxy_6- (2H-p than Jun · 3- ) _Methylbenzylamine benzoic acid; 2- (4-fluoro-phenyl) _5_isopropoxy_6_ (2-methyl · 2Η, pyrazole_3_yl) _ 88828. doc -32- 200418452 benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (1-methyl-lH-p 3-yl) _benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (3-methyl-isoxazole-5 ) -Benzofuran-3-carboxylic acid formamidine; 6-[(5-chloro- [1,2,4] Homomono-3-ylmethyl) -formylamino-amino ] -2- (4-Fluoro-phenyl) -5 -isopropoxy-5-yl-benzoanan-3-formate methylformamide; 6- (3,5-dimethyl-iso Dijun-4-ylamino) -2- (4-fluoroyl-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoroyl-benzene ) -5 -methoxy-6-forman-3-yl-benzocaran-3-methanoic acid formamide; 6-dimethylaminomethyl-2- (4-fluoro-benzene Yl) -5-isopropoxy-5-yl-benzoanan-3-methylamine, 2- (4-fluoroyl-phenyl) -6- (1-hydroxy-2-methyl -Propyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-amino-phenyl) -5-isopropyllactyl-6- (liZ-p Than fluoren-4-yl) -benzocaran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6- [methanesulfonyl- (2-methoxy-ethyl) ) _ Methyl] -5-methoxy · benzofuran-3-carboxylic acid formamidine; 6- (3-cyclopropyl-isopurazol-5-yl) -2- (4-fluoroyl-phenyl) -5-isopropoxymonobenzofuran-3-carboxylic acid formamide; 2- (4-fluorofluoro-pentyl) -5 -isopropoxy-6- (3-methoxymethyl-iso β-fluoren-5-yl) -benzofuran-3-carboxylic acid formamide; 88828. doc -33- 200418452 2- (4-Fluoro-phenyl) -6-formaldehyde S1-based amino-benzoanan-3 -formamide methyl formamide; 2- (4-fluoro-phenyl ) -6- (1H-imidazol-2-yl) -5-isopropoxy · benzoxan-3-carboxylic acid formamidine; 6- (2,5-dimethyl-2H -17 specific bite -3-yl) -2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-methaneformamide; 6- (3,5 -monomethyl-llUls -4 -yl) -2- (4-fluoroyl-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoroyl-phenyl) -5 -Isopropoxy-6- (5-methyl-2H-erim-3-yl) _benzofuran-3-carboxylic acid formamide; 6- (1,5-dimethyl_1H-pyridine Azole_3_yl) -2- (4-fluoro-phenyl) -5_isopropoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) _5 _Isopropoxy-6-[(methanesulfonyl-methyl-amino) -methyl] -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl)- 5- (2_hydroxy_2_methyl-propoxymorpholine_4_yl-benzofuran_3_carboxylic acid formamide; 2- (4-fluoroyl-phenyl) -5_ (2- Hydroxymethyl-butoxy) _6_morpholine_4_yl-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl -5- (2_hydroxy-propoxy) -6_morpholinyl-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) _6-[(2-hydroxy -Propyl) _methanesulfonyl-amino] -5_ isopropoxy-benzofurancarboxylic acid formamidine; 2- (4-fluoro-phenyl) morpholinyl 5- (1-thiazole -2-yl-ethoxy) _benzobenan-3-carboxylic acid formamidine; 88828. doc -34- 200418452 6- (ethyl-methanesulfonyl-amino) _2- (4-fluoro-phenyl) isopropoxy_benzofuran-3-carboxylic acid formamide; 6- ( 3,5-dimethyl-1H-pyrazol-4-yl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamide; 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (5-methyl-1H-pyrazol-4-yl) -benzofuran-3-carboxylic acid formamide; 3- [ 2- (4-fluoroyl-phenyl) _3-methylaminomethylmethyl-benzofuran-5-yloxymethyl] benzyl methyl ester; 4- [2- (4-fluoroyl-phenyl) _3_methylaminomethylamido-benzofuran-5-yloxymethyl] benzic acid; 3- [2- (4-fluoroyl-phenyl) _3_methylaminomethylamido-benzofuran- 5-Methoxymethyl] benzyl acid; 6-Ethyl-2- (4-fluoro-phenyl) -5_methoxy_benzofurancarboxylic acid formamidine; 4- [2- (4 -Fluoro-phenyl) -3-methylaminomethylmethyl-6-morpholino-4-yl-benzofuran-5-yloxymethyl] -methylacetate; 3- [2- ( 4-Fluoro.phenyl). 3-methylamino formamidomorpholine. 4-. Benzofuran-5-yloxymethyl] -methylacetate; 2- (4-fluoro- Phenyl) _5_isopropoxy_6_ (1,3,5_trimethyl_ΐΗ_ρ 比 嗤 -4-yl) -benzene Cranan-3-metanoic acid amine; 2- (4-fluoro-phenyl) -5_isopropoxybenzyl-benzyl-benzoananthoxycarboxylic acid formamide; 6-cyano 2- (4-fluoro-phenyl) -5-methylchloro AJ 5 T lactyl · zaurofuran-3-carboxylic acid formamidine; 88828. doc -35- 200418452 4 [2_ (4-Fluoro-phenyl) _3_methylaminomethylamido-6_morpholine_4_yl-benzopfuran-5-yloxymethyl]- Arsenic acid; 3 · [2- (4-fluoroyl-phenylb 3-methylaminomethylforminomorpholine-4-yl_benzocran ~ 5-yloxymethyl] -arsenic acid; 2 -(4-Fluoro-phenyl) -5-isopropoxy-6- [methanesulfonyl group-methyl-1Η_tetrazol-5-ylmethyl) -amino] -benzocran _3_ formamidine methanoate; '({[2- (4-fluoro-phenyl) -5-isopropoxy_3_methylamine formamidine_benzo-6-yl] -Methylsulfonyl-Aminomethyl) _ acid acid purpose; 2- (4-fluoro-phenyl) _5_isopropoxy-6- [methanesulfonyl_ (2_methyl_ Thiazol-4-ylmethyl) -amino] -benzoicronic acid, methyltrisamine; 4-({[2- (4-fluoro-phenyl) -5-isopropoxy_3_ Methylaminomethylamidino_benzofuran-6-yl] -methanesulfonyl-aminomethyl) -benzyl acid; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (5-Methoxymethyl-iso $ xyl) -benzofuran-3-carboxylic acid formamide; 6- (5-cyclopropyl-isoxazol-3-yl) -2- (4-fluoro -Phenyl) -5-isopropoxy_benzofuran-3-carboxylic acid formamidine; 2- (4 -fluoro- ) _5_Hydroxypropoxy-6- (1-methylpyridinyl group than p_2_yl) -benzofuran_3_carboxylic acid formamidine; 6-ethylamidino-2- (4 -Fluoro-phenyl) -5-¾yl-benzofuran-3-chitoic acid methylamine; 6- (ethyl-methanesulfonyl-amino) -2- (4-fluoro-benzene Methyl) -5-methoxy-benzocrean-3-methanoic acid formamidine; 4- [2- (4-fluoroyl-phenyl) -5-methoxy-3-methylamine formamidine -Benzofuran-6-yl] -2-oxypyrrolidine-3-carboxylic acid formamidine; 88828. doc -36- 200418452 2- (4-fluoroyl-phenyl) _5-isopropoxy-6_ (4 ^ 1- [1,2,4] triazol-3-yl) -benzofuran-3- Formamidine carboxylic acid; 2- (4-fluoro-phenyl) _5-methoxy-6- (5-methoxymethyl-3-methyl-isoxazol-4-yl) -benzo Ammonium formate; 2- (4-fluoro-phenyl) _5_isopropoxy_6- [methanesulfonylmethoxy_benzyl) -amino] •• benzofuran-3- Formamidine carboxylic acid; 2- (4-fluoro-phenyl) -5-isopropoxy "6- [methanesulfonyl- (5-methyl-iso'-a-3-ylmethyl) _ Amine] -benzofurancarboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (5-methyl-isoxazol-3-yl) -benzene Benzofuran-3-carboxylic acid formamidine; 6-[(3,5-dimethyl-isopurazol-4-ylmethylhexylsulfonyl-amino group] -2- (4-fluoro- Phenyl) -5_isopropoxy_benzofurancarboxylic acid formamidine; 2- (4-fluoroyl-phenyl) _5-isopropoxy-6_ (methanesulfonyl-thiazolylmethyl- Amino group) -Benzeno-3-3 · amine acetic acid; 2-({[2- (4-Fluoro-phenyl) _5-isopropoxy-3-methylamine formamidine-benzene Ethyl-6-yl] -methanesulfonyl-aminomethylmethylzozole-4-carboxylic acid ethyl ester; 2- (4-Fluoro • phenyl) -5-hydroxy-6- (methanesulfonyl-methyl-amino) _benzofuran-3-carboxylic acid formamidine; ό- (allyl-methane Sulfonyl_amino) _5_alanyloxy_2_ (4-fluoro-phenyl) -benzocaran-3-methanoic acid formamidine; 6- (ethylamyl-methanesulfonyl_ Amine) _2- (4_fluoroyl_phenyl) _5_methoxy_benzofuran-3-carboxylic acid formamidine; 6-[(3,5-dimethyl-isopyrazolylmethyl) ) _Methanesulfonyl_amino] -2- (4-fluoro-phenyl) -5_methoxy_benzofuran_3_carboxylic acid formamidine; 88828. doc -37- 200418452 2- (4-fluoro-phenyl) -6- (methanesulfonyl-pyrimazol-4-ylmethyl-amino) _5_ methoxy-benzofuran-3-carboxylic acid Formamidine; 2-({[2- (4 -Gasyl-benzyl) -5-isopropoxy-3-methylcarbamate-benzopyran-6-yl] -formamidine S Lithium-amino} -methyl) -p-seta-n--4-acid; 5- (2,2-difluorenyl-4-oxy-411-benzo [1,3] -diyingen -5-ylmethoxy) -2- (4-amino-dongyl) -6-morpholin-4-yl-benzoanan-3-chitinate; 5- (2,2 -Dimethyl-4-oxy-411-benzo [1,3] -diginco-5-ylmethoxy) -6- (ethyl-methanesulfonyl-amino) -2- ( 4-Fluoro-phenyl) -benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6- (1H-imidazol-4-yl) -5-methoxy -Benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6 · (1fluorene-imidazol-2-yl) -5-methoxy-benzofuran_3_ Formamidine carboxylic acid; 6- (ethyl-methanesulfonyl-amino) -2- (4-fluoro-phenyl) -5-hydroxy-benzofuran-3-carboxylic acid formamide; 5 -Difluoromethoxy-2- (4-fluoro-phenyl) -6- (methanephenyl-methyl-amino) -benzofuran-3-carboxylic acid formamidine 2- (4-Fluoro-phenyl) _6_ (methanesulfanyl-pyridin-4-ylmethyl-amino) -5-methoxy-benzoanan-3-guinic acid amine; 2- (4-Fluoro-phenylhydroxy_1-methyl-ethylmethyl_benzofuran-3-carbinol methylamine; 6-acetoxyfluoro-phenyl) -5 -methyl- Benzene succinimidine · 3-ammonium chloroacetate; 5- (2,2_dimethyl-4_oxy-411-benzo [1,3] _Nisaki_-7-ylmethoxy 88828. doc -38- 200418452 -2- (4-fluoro-phenyl) -6_ (methanesulfonyl-methyl-amino) _benzofuran-3-carboxylic acid formamide; 2- (4-fluoro -Phenyl) -6- [1- (methanesulfonyl-methyl-aminoethyl] -5-methoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro -Phenyl) -5-methoxy-6- (1-methylamino-ethyl) -benzofuran-3-carboxylic acid formamidine; 4- [2- (4-fluoroyl-benzene ) -6- (methanesulfonyl-methyl-amino) _3-methylaminomethylmethyl-benzofuran-5-yloxymethyl] -benzoic acid methyl ester; 2- [2- (4 -Fluoro-phenyl) -6- (methanesulfonyl-methyl · amino) _3-methylaminomethylamidino-benzofuran-5-yloxymethyl] -methyl benzate; 6- [(2-fluoro-ethyl) _methanesulfonyl-amino group> 2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoroyl-phenyl) -6- [methanesulfonyl- (2,2,2-trifluoroethyl) -amino] _5_methoxy-benzofuran-3-carboxylic acid Formamidine; 2- (4-Fluoro-phenyl) -6- (1-methanesulfonyl-pyrrolidinyl) -5-methoxy-benzoanan-3-carbamic acid amine; 6 -(3-cyclopropyl-5-methoxymethyl-isoxazol-4-yl) -2- (4-fluoroyl-benzene ) -5-methoxy-benzofuran-3-carboxylic acid formamidine; 4- [2- (4-fluoroyl-phenyl) -6- (methanesulfonyl-methyl-amino) methyl Methylaminomethylamido-benzofuran-5-yloxymethyl] -benzyl acid; 3- [2- (4-fluoroyl-phenyl) -6- (methanesulfonyl-methyl-amino) Methylamine formamyl-benzofuran-5-yloxymethyl] -benzic acid; 2- (4-fluoro-phenyl) -5-methoxy-6- (5-methoxymethyl- Isozazol-3-yl) -benzofuran-3-carboxylic acid formamide; 88828. doc -39- 200418452 6- (3,5-dimethyl-isohumazol-4-yl) -2- (4-fluoro-phenyl) -5-hydroxy-benzofuran_3_carboxylic acid methyl ester Fluorenamine; 2- (4-fluoro-phenyl) -5 -methoxy-6- (5-oxy-pyrrolidin-3-yl) -benzofuran-3-carboxylic acid formamide; 2- (4-Fluoro-phenyl) -6- [methyl fe d g- (2-trifluoro ^ methoxy-ethyl) -amino] -5-methoxy-benzofuran- Formamidine 3-carboxylic acid; Formamidine 2- (4-fluoro-phenyl) -5 -methoxy-6- (1 Hp bihal-3-yl) -benzocaran-3-carboxylic acid Amine; 6- (3,5-dimethyl-isopurazol-4-yl) -2- (2-ethoxy-4-fluoro-phenyl) -5-methoxy · benzofuran -3-methanomethamine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _5_ (thiazole_4_ylmethoxy) -benzofuran- Formamidine 3-carboxylic acid; 2- (4-fluoro-phenyl) -6- (methanesulfonic acid-methyl-amino) _5- (2-methyl-thiazol-4-ylmethoxy) ) -Benzofuran_3_carboxylic acid formamide; 5- (3-chloromethyl- [1,2,4] thiadiazol-5-yloxy) -2_ (4-fluoro-benzene ) -6- (methanesulfonyl-methyl-amino) -benzofuran sulfonamide; 2- (4-fluoro-phenyl) -6-{[2- (4-fluoro -Phenyl) -2-yl-ethyl] -methanesulfonyl-amino group} -5-isopropoxy-benzoic acid _3_ leptate formamidine; 2- (4-fluoro -Phenyl) -5-methoxy-6- (2-methyl-2H- [1,2,4] -triazol-3-yl) -benzofuran-3-carboxylic acid formamidine; 5- (3,5-dimethyl-isoazazol-4-ylmethoxy) -2- (4-fluoroyl-phenyl) -6- (methyl k% S-S-methyl-amino ) _Benzauran_3_chitoic acid methylamine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl_methyl_amino) -5_ (3-methoxy- Benzyloxy) -benzofuran-3-carboxylic acid-formamide; 88828. doc -40- 200418452 2-(4-fluoro-phenyl) -5-hydroxy-6- (isobutyl-methanesulfonyl-aminobenzobenzofuran-3-carboxylic acid-methaneamine; fluorine -Phenyl) -6- (methanesulfonyl-methyl-aminomethoxy-monomethoxy) -benzoxan-3 -acid-methylamine; 2- (4-fluoro-benzene Group) _6_ (methanesulfonyl group_T group-amino group) _5 decapyridinylmethoxy group) -benzofuran-3-carboxylic acid-formamidine; 4-oxy-411_benzo [153] -bisphthyl-6-ylmethoxy) '2 _ (' fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _ Benzofuran-3-carboxylic acid formamidine; 6_ (cyclopropylmethyl-methanesulfonyl-amino group [2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3 -Carboxylic acid-methaneamine; ^ (4-fluoro-phenyl) -6- (methylamino-methylaminomethylamidomethyl_amino group> 5-methoxy-benzofuran _3_ Carboxylic acid-formamidine; 5-fluoro-2- (4-fluoro-phenyl) -6-methanesulfonylamino-benzofuran-chitoformate; Methanesulfonyl-amino) -5-fluoro-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid-formamidine; (4-fluoro-phenyl) formyl Burning g Yodo-3-yl) -5-methoxy, benzofuran-3-carboxylic acid-methaneamine; 5-ethyl-2- (4-fluoroyl-phenyl) -6- [methanesulfonyl -(2-methoxy-ethyl) -amino] benzofuran-3-metanoic acid-formic acid amine; 2- (4-fluoro-phenyl) _5_methoxy_6- (3- Methoxymethyl-5-methyl-isopyridin-4-yl) _benzofuran_3_carboxylic acid-formamidine; 5 · ethyl-6-[(2-fluoro-ethyl) -Methanesulfonylamino group 2- (4-fluoro group 88828. doc -41-200418452 phenyl) benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-propyl-amino) -5- Propoxy-benzofuran-3-carboxylic acid-formamidine; 5-ethyl-2- (4-fluoro-phenyl) -6- (1-hydroxy-1-methyl-ethyl) _ Benzofuran-3-carboxylic acid-formamidine; 6-Ethyl-5-ethyl-2- (4-airyl-winteryl) -Fenganan-3-chitoic acid-formamidine ; 4-Gas-6-ethylamino-2- (4-fluoro-benzyl) -5 -Cyclosyl-benzoanan-carboxylic acid-formamidine; Tishiishi buy red 4-chloro -6-ethylamino-2- (4-amino-phenyl) _3-methylaminomethane-benzofuran-5-yl ester; 5-ethyl-2- (4-fluoro- Phenyl) -6- (methylalanic acid-lacryl-4-ylmethyl group); phenyl] benzoanan-3 -metanoic acid-methanamine; 6- (5-cyclopropyl-3 -Methoxymethyl-isohumazol-4-yl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-formamidine; 6- (1 -Ethenyl-π-pyrrolidin-3-yl) -2- (4-fluoro-phenyl) -5 -methoxy-benzofuran-3-carboxylic acid-formamidine; 5- (3 , 4-difluoroyl-methyloxy) -2- (4-fluoroyl-phenyl) -6- (formyl-methyl-amino)- Benzofuran-3-carboxylic acid-formamidine; 5- (2-difluoromethoxy-fluorenyloxy) _2_ (4-fluoro-phenyl) _6_ (methanesulfonyl-methyl-amine) -Benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) _6_ (methanesulfonyl-methyl-amino) -5-propoxy_benzofuran-3 -Carboxylic acid-formamidine; 5-fluorenylpropoxy-2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _ 88828. doc -42- 200418452 benzofuran-3-carboxylic acid-formamidine; 6- (5-ethoxymethyl-isohumazol-3-yl) -2- (4-fluoro-phenyl) _5_ Formamyl_benzofuran-3-carboxylic acid-formamidine; 5-cyclopropylmethoxy-2- (4-fluoro-phenyl) -6- (f-alkylfluorenyl-methyl · amine 1-benzofuran-3-carboxylic acid-formamidine; 5- (3,5-dimethoxy-benzyloxy) -2- (4-fluoro-phenyl) _6- (methylbenzene continued Fluorenyl-methyl-amino) -benzocrean-3 -chicanic acid-formic acid amine; 2- (4-fluoro-phenyl) -5- (4-methanesulfonyl-benzyloxy)- 6- (methanesulfonyl-methyl-amino) -benzofuran-3-metanoic acid-formamidine; 2- (4-fluoro-phenyl) -5-hydroxy-6- [methanesulfonyl -(2-oxy-propyl) _amino] -benzofuran-3-carboxylic acid-formamidine; 2 · (4-fluoro-phenyl) _6- (methanesulfonylmethyl- Amine group) _5_ [2_ (4_methoxy-phenyl) -2-oxy-ethoxy] -benzocran-3-metanoic acid-formamidine; 5- (3 -enyloxy ) -2- (4-Fluoro-phenyl) -6- (formamylic acid-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 5- (4-cyano -Ethyloxy) -2- (4-fluoro-phenyl) -6- (methylsulfonyl-methyl-amino)- Benzofuran-3-acid-formamidine; 2- (4-fluoro-phenyl) -5_methoxy-6- (2fluorene- [1,2,4] triazol-3-yl)- Benzofuran-3-carboxylic acid-methaneamine; 4- {2- [2- (4-fluoro-phenyl) -6- (methanesulfonic acid-methyl-amino) -3 -methyl Ethylaminomethylamidino-benzofuran-5-yloxy] -ethylamidoaminobenzoic acid ethyl ester; 2- (4-fluoroyl-phenyl) -5- [2- (4-fluoroyl -Phenyl) -2-oxy-ethoxy] -6- (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 88828. doc -43- 200418452 6_ (benzyl-methanesulfonyl-amino) _2_ (4_fluoroyl_phenyl) _5-isopropoxy_benzofuran-3-carboxylic acid-formamidine; 4- Chloro-6- (ethyl-methyl-amino) -2- (4-fluoro-phenyl) -5-methoxy_benzofuran-3-carboxylic acid-formamidine, 4- Chloro-6-ethylamino-2 · (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid · methaneamine; 6-ethylamino-2- (4-Dunyl-phenyl) -5-hydroxy · benzofuran-3-carboxylic acid-methaneamine; 5- (3-bromo-propoxy) -6-ethylamino-2_ (4-fluoro -Phenylbenzofuran-3-chinoic acid-formamidine; 5-Allyloxy-6-ethylamino-2- (4-fluoroyl-phenyl) -benzocran_3_ji Acid-formamidine; 5- (3-ethoxy-propoxy) -6-ethylamino-2- (4-fluoro-phenyl) -benzocaran-3-carboxylic acid-formamidine Amine; 2- [4- (4-Fluoro_phenylmethoxy_3_methylaminomethylamidino-benzofuran-6-yl] -pyrrolidinecarboxylic acid; amine; 2- (4-fluoro Phenyl (methanesulfonyl-methyl-amino group 5_ (2_oxy_propoxy) &quot; benzobenzo-3-metanoic acid-formamidine; 2_ (4-fluoro- Phenyl) -5- (2-hydroxy-propoxy) _6_ (methanesulfonyl-methyl -Amine) -benzofuran acid-formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _5- (1_methyl-1H -Tetrafluoren-5-ylmethoxy) _benzocran_3_metanoic acid-formic acid amine; 2 (4_fluoroyl-fungyl) -6- (5-isopropoxymethyl-isonine Tween 3-yl) -5 -methoxy-benzofuran-3-carboxylic acid-formamidine; 88828. doc -44- 200418452 5- (5_diethylamino- [nqpyrimidazol-3_ylmethoxy) _2_ (4_fluoroyl_phenyl) -6- (methanesulfonyl-methyl -Amine) _benzofuran-3_carboxylic acid-formic acid amine; 5- [5- (cyclopropylmethyl-amino) 412,4] pyrimidazol-3-ylmethoxy] -2- (4-Fluoro-phenyl) -6- (methylpyridyl-methyl-amino) _benzoanan-3-metanoic acid-formic acid amine; 6- (2-amino-1-hydroxy- i_methyl-ethyl) _2- (4-fluoro-phenyl) isopropoxy · benzofuran-3-carboxylic acid-methaneamine; 6- (1 • amino-1-methyl- Ethyl) -2- (4-fluoro-phenyl) -5 -isopropoxy-benzoic acid_3_metanoic acid-formamidine; 2- [2- (4-fluoroyl-phenyl ) -5-methoxy-3-methylamine formamidine-benzofuran-6-yl] -pyrrolidine-carboxylic acid-formamidine; 6- (3,5-dimethyl-iso Oxazol-4-yl) -2- (4-fluoroyl-phenyl) -5-methoxy-monobenzo-3-quinoic acid-acetamidamine; 6- (3,5-monomethyl -Iso-p. Sit-4 -yl) -2- (4-Dentyl-phenyl) -5 -methoxy_ dongnaobitan-3 -chitoic acid-isopropyl amine; 6- (3,5 -Monomethyl-iso $ fluoren-4-yl) -2_ (4-fluoro-phenyl) -5-methoxy_benzofuran-3-carboxylic acid-cyclopropylhydrazone ; 2- (4-Gas-fungyl) -5-isopropyllactyl-6- (5-methyl-2-oxy-yinu-5-yl) -benzofuran_3_carboxy Acid-formamidine; [2- (4-fluoro-phenyl) -6- (formamidine-methyl-amino) _3-methylamine formamidine-benzofuran-5-yl Oxy] -tertiary-butyl acetate; 2- (4-fluoro-phenyl) _5-methoxy-6_ (5-methyl-2H- [1,2,4] trifluoren-3-yl l · benzofuran-3-carboxylic acid-formamide; 88828. doc -45- 200418452 6- (1-amino-1-methyl-ethyl) _2- (4-fluoro-phenyl) -5_methoxy-benzofuran-3-carboxylic acid-formamidine Amine; 6- (1-Ethylaminoamino-1-methyl_ethyl) -2- (4-fluoro-phenyl) -5-methoxybenzofuran-3-carboxylic acid-formamidine Amine; [2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _3-methylaminomethanyl-benzoan-5-yloxy]- Acetic acid; 6- (2,5-monomethyl-2H- [l, 2,4] trijun-3-yl) _2_ (4-fluorol-yl-phenyl) -5-methoxy-benzo Alan-3-metanoic acid-methdonamine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _5_ (thiazole_2_ylmethoxy) -benzo Furan-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -5-methoxy-6- (4-methyl-2,5-dioxy-imidazolidine-4- ) -Benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -6- (1-T-alkanesulfonylamino-1-methyl-ethyl) _5_ Methoxy-benzofuran-3-carboxylic acid-formamidine; 5- (6-bromomethyl-pyridin-2-ylmethoxy) -6-[(6-bromomethyl-pyridine-2- Methyl) -methanesulfonyl-amino] -2- (4-fluoro-phenyl) -benzofuran-3-metanoic acid-methanamine; 2- [2- (4-fluoro -Phenyl) -6- (methanesulfonyl-methyl-amino) -3-methylaminomethylmethyl-benzoxan-5-yloxymethyl] ^ azole Ethyl ester; 2- [2- (4-Fluoro-phenyl) -6- (methylsulfanyl-methyl-amino) -3-methylaminofluorenyl-benzofuran-5-yl Oxymethyl] -pyrimazole-4-carboxylic acid; 6-dimethylamino-2 · (4-fluoroyl-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-methyl Hydrazine; 5-dimethoxy-2- (4-fluoro-phenyl) -6- (methyl-S-blue-methyl-amino) _ 88828. doc -46- 200418452 benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro group_phenyl) _6- (formamidine group_methyl_amino group) _5_ (5-methyl group) _ Isoxazol-3-ylmethoxy) _benzofuran_3_carboxylic acid- ▼ fluorenamine; 5- (5-chloro- [1,2,3] fluorenediazole-4-ylmethoxy ) _2_ (4-fluoro-phenyl) 6- (methane% fluorenyl-methyl-amino) _benzofuran_3_carboxylic acid-fluorenylamine; 2- (4-fluoro group_benzyl ) _6- (methanesulfonic acid_methyl__amino) _5_ (1_methyl1H-imidazol-2-ylmethoxy) _benzofuran_3-carboxylic acid-formamidine; 5- (1-benzyl-1H-imidazol-2-ylmethoxy) _2_ (4-fluoro-phenyl (formamidine% methyl-methyl-amino) _benzofuran_3_carboxylic acid-formyl Hydrazine; 2- (2,4 · difluoroyl-phenyl) _6- (3,5 · dimethyl · isoindazole_4 • yl) _5_methoxy-benzobenzo-3-benzyl Acid-formamidine; 6- (3,5_dimethyl · isoxazole_4_yl) fluoro-phenyl) _5_ (pyrazol_4_ylmethoxy) -benzofuran-3-carboxy Acid-formamidine; 5- (5-amino_4H_ [1,2,4] triazol-3-ylmethoxy) -2- (4-fluorophenyl) -6- (methanesulfonyl) _Methyl-amino group> benzofuran_3_carboxylic acid_formamidine; 5- (4-amino-1-methyl _1H-pyrazole_3-ylmethoxy) _2_ (4_fluoroyl-phenyl) -6- (methanefluorenyl_methyl-amino) &gt; benzofuran_3_carboxylic acid · fluorenamine ; 2 (4-Fluoro_phenyl) _6_ (methanesulfonic acid_methyl-amine) _Jun -1--1-ethoxy) -benzocran_3_chinoic acid-formic acid amine; 2- (4-Fluoro-phenyl) _5_ (1H-imidazole_2_ylmethoxy (methanesulfonyl-methyl-amino) -benzofuran_3_carboxylic acid-methaneamine; 6 -(2,5-dioxy_imidazolidine_4_yl) _2_ (4_fluoroyl-phenyl) _5_methoxy_benzofuran-3-carboxylic acid-formamidine; 5- (3 , 5-dimethyl. Isoxazole_4-yl) _2- (cardiofluoro-phenyl) _6_methanesulfon 88828. doc -47- 200418452 fluorenylamino-benzofuran_3_carboxylic acid_formamidine; 2- (4-fluoro-phenyl) -6 &lt; Methanesulfonyl_methyl_amino group 5_ (1_oxazolyl-ethoxy) _benzofuran-3-carboxylic acid-formamidine; 6- (3,5-dimethyl- Isoxazol-4-yl) -2_ (4-fluoro-phenyl) _5_ (5_methyl_iso $ fluoren-3-ylmethoxy) _benzofurancarboxylic acid-formamidine; 6- (3,5-dimethyl-isopurazol-4_yl) -2- (4-fluoroyl_phenyl) _5_ (thiazole_2_ylmethoxy) -benzopyran-3-guinic acid- Ammonium formate; 6-Ethylfluorenyl-2- (4-fluoro-phenyl) _benzofuran_3-carboxylic acid-formamidine; 2- (4-fluoroyl-phenyl) -5- (2 -Hydroxy-2_methyl-propoxy) _6- (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 5-diethylamine formamidinemethyl Oxy_2- (4-fluoro-phenyl) (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 6- (3,5-dimethyl -Isoxazole_4_yl) _5_ethoxy-2- (4-fluoroyl-phenyl) -benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoroyl-phenyl ) -6- (methanesulfonyl-methyl-amino) -5-oxetazol-2-ylamine medonylmethoxy) -benzofuran_3_carboxylic acid-formamidine; 2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5-([1,3,4] fluorene 2-ylamine formamylmethoxy) _benzofurancarboxylic acid-formamidine; 5-[(4,5-dimethyl-pyrazol-2-ylamine formamyl) -methoxy ] —2- (4-Fluoro_winteryl) -6- (methyldonyl-methyl-amino) _benzopyranoic acid-methodamine; 5-cyclopropyl-2_ (4-fluoro -Phenyl) -6-methanesulfonylamino-benzofuran-3-carboxylic acid-fluorenamine; 5- [2- (4-cyano-hexahydrop-pyridine-1-yl) _ Ethoxy] _6- (3,5-dimethyl-iso88828.doc -48- 200418452 indazol-4-yl) -2- (4-fluoro-phenyl) -benzofuran-3-carboxy Acid-formamidine; 2- (4-fluoro-phenyl) -6-methylsulfonyl-amino-5-tephen-2-yl-benzofuran-3-carboxylic acid-formamidine ; 2- (4-Fluoro-phenyl) -6- (methylsulfonyl-methyl-amino) -5-methylaminomethylamidomethoxy-benzofuran-3-carboxylic acid -Formamidine; 2- (4-fluoro-phenyl) -5- (1-hydroxymethyl-cyclopropylmethoxy) _6-[(1-hydroxymethyl-cyclopropylmethyl)- Methanesulfonyl-amino] -benzofurancarboxylic acid-methaneamine; 6-diethylamino-5-ethmethoxy-2- (4-fluoro-phenyl) -benzoconan _3-carboxylic acid-formamidine; 5-amine formamylmethoxy-2- (4-fluoro-phenyl) -6- ( Alkyl fluorenyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 5- [2- (3,5- -methyl-p ratio-1-1-yl) -ethoxy Group] -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _benzofuran_3_carboxylic acid-formamidine; 2- (4-amino -Winter-based) -5 -keto-2 -yl-6-formylaminoamine-benzopyran-3-carboxylic acid-formamidine; 6- (3,5-dimethyl-isoamidine Azole_4_yl) -2- (4-fluoroyl-phenyl) -5- (1-methyl-1H-tetrazol-5-ylmethoxy) -benzofuran-3-carboxylic acid-methyl Hydrazine; 5-cyclopropylmethoxy-6- (3,5-dimethyl-isohumazol-4-yl) -2- (4-fluoro-phenyl) -benzofuran-3- Carboxylic acid-methanamine; 6- (3,5-dimethyl-isoxazol-4-yl) -5- (3,5-dimethyl-isoxazol_4-ylmethoxy)- 2- (4-Fluoro-phenyl) -benzoconan-3-metanoic acid-formic acid amine; 2- (4-fluoro-phenyl) -5-methoxy-6- (5-methyl -[1,3,4] pyridazol-2-yl) -benzofuran-3-carboxylic acid-formamidine; 88828. doc -49- 200418452 6- (3-cyano-4-hydroxy-2-oxy-2,5-dihydro-pyrrole-1-ylmethylfluoro-phenyl) -5-methoxy-benzene Benzene_3_metanoic acid_formic acid amine; 4-chloro-6- [ethyl- (2-methoxy_ethylamidoamino] _2_ (4-fluoro-benzyl) -5 -methyl Oxy-benzocaran-3-metanoic acid-formic acid amine; 6- (3,5-dimethyl-isoxazol-4-yl) · 2 _ ('fluoroyl_phenyl) -5_ (2_ Morpholine-4-ylethoxy) -benzocrean_3-carboxylic acid-methanamine, 6- (3,5-dimethyl-isoxazol-4-yl) -2- ( 4-Fluoro-phenyl) _5_ (3_hexahydropyridin-1-yl-propoxy) -benzocran-3-metanoic acid-formamidine; 2- (4-fluoroyl-phenyl) -5- (oxazol-4-ylmethoxy) _benzofuran_3_carboxylic acid-formamidine; 2- (4-fluoroyl-phenyl) -6- (2-¾yl-acetate ) · 5-methoxy-benzopyran-3-carboxylic acid-formamidine; 5-cyclopropyl-2- (4-fluoro · phenyl) -6- (methanesulfonyl-methyl -Amine) _benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoroyl-fungyl) _5-benzyl_6-[(2- | ^ yl-propyl) _methane Ji sheng sheng _ Amino] -benzoanan-3 -metanoic acid, methylamine; 2- (4-fluoro-phenyl) -6-[(2-light-propyl) -methanesulfonate -Amino group] _5_ methoxy-benzofuran-3-carboxylic acid-methaneamine; 6- (1-ethyldonylpyridin-2-yl) -5 · ethyl-2- (4- Fluoro-phenyl) _benzoanan-3 -metanoic acid-formic acid amine; 2- (4-fluorofluoro-phenyl) -6-methanesulfonic acid amino-5- (tetrahydro-squean) ) _ Benzofuran-3-carboxylic acid-methaneamine; 2- (4-fluoro-phenyl) -5-methoxy-6- (tetrahydro-furan-3-yl) -benzo Pyran-3-carboxylic acid-formamidine; 88828. doc -50- 200418452 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methoxymethyl-aminopropoxy-benzofuran_3-carboxylic acid-methaneamine; 2 -(4-Fluoro-phenyl) -5- mesityl-6- (methylpyridyl-methoxymethyl_amino) _benzofuran-3-carboxylic acid-formamidine; 2- ( 4-fluoro-phenyl) -6-methanesulfonylaminopropoxy-benzofuran-3-carboxylic acid-formamidine; 5- (4-cyano-benzyloxy) -2- ( 4-Fluoro-phenyl) -6- (methanesulfonyl-methoxymethyl-amino) -benzofuran-3-guinic acid-formic acid amine; 5- (3-pentyloxy)- 2- (4-Fluoro-phenyl) -6- (formamidine-S-S-methyl-methoxymethyl-amino) -benzofuran-3-metanoic acid-formamidine; 6- (1- Cyclopropanecarbonyl-pyrrolidin-2-yl) -2- (4-fluoroyl-phenyl) -5-isopropoxy-benzocaran-3-metanoic acid-methanamine; 2- (4- Fluoro-phenyl) -5-methoxy-6- [1,3,4] pyridazol-2-yl-benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro group -Phenyl) -6- (methanesulfonyl-methoxymethyl-amino) -5-thien-2-yl-benzocaran-3-metanoic acid-formic acid amine; and 2- (4-fluoro -Phenyl) -6 _ {[2- (4_fluoroyl-phenyl) _2_hydroxy-ethylmethane Bu 5-¾yl-benzocrean-3-acid-formamidine; and its medically acceptable salts. 8. The compound according to item 1 of the scope of patent application, which is selected from the group consisting of Group ·· 2- (4-Fluoro-phenyl) _5-methoxy_6_morpholin-4-yl-benzofuran-3-carboxylic acid-methanamine; 2- (4-fluoro -Phenyl) -5-isopropoxy-6-morpholino-4-yl-benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoroyl-phenyl) -5-iso Propoxy-51-88828. doc 200418452 6-methyl $% 1 cyanoamino-benzoanuronic acid_methanamine; 2_ (4-fluoro-phenyl) -5-isopropoxy-6-[(2-methyl Oxy-ethyl) _methyl-amino] _benzofuran-3-carboxylic acid-formamidine; 5_benzyloxy_2_ (4 • fluoro_phenyl) _6_morpholine-4 -Yl-benzofuran_3_carboxylic acid_methaneamine; 2_ (cardiofluoro_phenylphenyl 6 _ [(furan-3-ylmethyl) -amino] -5_isopropoxy_benzo Furan_3_carboxylic acid_formamidine; 6- (3,5_dimethyl-isohumazol-4-yl) _2_ (4-fluoroyl_phenyl) _5_methoxy-benzofuran- 3-carboxylic acid-formamidine; 5-cyclopropyl_2_ (4-fluoro group_phenyl ^-[(2-hydroxy-ethyl) _methanesulfonyl_aminobenzobenzofuran_3_ Carboxylic acid-formic acid amine; 6- (3,5_dimethyl-iso, fluorenyl 1) _2 ♦ fluoro group_phenyl) (3 per group-propoxy) _benzocran_3_chinic acid -Ammonium formate; and its pharmaceutically acceptable salts. 9.  10.  11.  12.   According to the scope of the patent application, the compound is in the form of a pharmaceutically acceptable salt. The compound according to item 9 of the scope of patent application, wherein the pharmaceutically acceptable salt is selected from the group consisting of hydrochloride, sulfate, acetate, lactate, sodium salt, potassium salt, hexahydroe lake or ammonium salt. The compound according to item 10 of the scope of Shen Qing's patent, wherein the pharmaceutically acceptable salt is unloaded salt or steel salt. The compound according to item 9 of the scope of patent application, which is selected from the group consisting of: 2 (4-fluoro-phenyl) -5-isopropoxy-6-methanesulfonylamino-benzo Furan 3- &amp; So-phosphonium amine, but salt; 2 (cardiofluoro-phenyl) -5-isopropoxy-6-methanesulfonylamino-benzofuran-3, carboxylic acid- Formamidine, sodium salt; 88828. doc -52- 200418452 2- (4-Fluoro-phenyl) -6-methanesulfonylamino-5-methoxy-benzoanan-3-carboxylic acid-formamidine, potassium salt; 2 -(4-Fluoro-phenyl) -6-formylaminobenzylamino-5 -methoxy-benzoanan-3-carboxylic acid-formamidine, sodium salt; 2- (4-fluoro -Phenyl) -5 -isopropoxy-6- (propan-2-ylfluorenylamino) _benzofuran-3-carboxylic acid-formamidine, potassium salt; 2- (4-fluoro -Phenyl) -5-isopropoxy-6- (propane-2-sulfoamidoamino) _benzofuran-3-carboxylic acid-amidoamine, sodium salt; 2- (4-fluoro group -Phenyl) -5-isopropoxy-6-methane difluorenylamino-benzocrean-3 -carboxylic acid-isopropylamine, desalting; 2- (4-fluoroyl-phenyl) -5-isopropoxy-6-methanesulfonylamino-benzocran-3-carboxylic acid-isopropylamidine, sodium salt; 2- (4-fluoro-phenyl) -5-iso Propoxy-6-methanesulfonylamino_benzofuran · 3-metanoic acid-amine acetate, potassium salt; and 2- (4-fluoro-phenyl) -5-isopropoxy-6_ Methylpyridinylamino-benzocrean-3 -chitoic acid-amine acetate, sodium salt. 13.   14.   A composition for preventing or treating a viral infection, the composition comprising a compound according to item 丨 of the scope of patent application 'and a pharmaceutically acceptable carrier vehicle in an amount sufficient to effectively reduce viral infectivity. A composition according to item 13 of the application, wherein the compound is selected from the group consisting of 2-furan-3-yl-5-methoxy-benzofurancarboxylic acid formamide; 2-benzene Methyl-5-difluoromethoxy-benzofuran_3_carboxylic acid formamide; 2- (3,4-difluoroyl-phenyl) _5_methoxy_benzofurancarboxylic acid formamide 88828. doc -53- 200418452 2- [4- (Ethylamido-methylphenylisopropoxy-benzofuran_3_ carboxylic acid formamide; 2- (4-hydroxy-phenyl) -5- Xylpropoxy-benzofuran gastric 3-carboxamidine; 2- (4-fluoroyl-phenyl) -5-isopropoxy-6-pyrrolidine "_yl_benzofurancarboxylic acid methyl Fluorenamine; 5-difluoromethoxy-2- (4-fluoro-phenyl) _benzofuran_3_carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-iso Propoxy-6- (2-methoxy-ethylamino) -benzofuran-3-carboxylic acid formamidine; 5-methyl-2-phenyl-benzofuran-3-chinic acid Formic acid amine; 5-methyl-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid gammaamine; 2-phenyl-5- (2,2,2-trifluoro- Ethoxy) _benzoxan-3-methanamine; 2- (4-fluoro-phenyl) -5-methoxy-benzoxan-3-aminocarboxylic acid amine; 6_ Bromo-2- (4-fluoro-phenyl) -5 -methoxy-benzoan-3-carboxylic acid carboxylic acid amine; 5-methoxy-6-methyl-2-phenyl-benzene Benzofuran-3-methanomethamine; 6- (3-Amino-pyrrolidin-1-yl) -2- (4-fluoro-phenyl) -5-isopropoxy-2,3 -Dihydro-benzofuran-3-carboxylic acid formamidine; 6-amino-2- (4-fluoro- Methyl) -5-isopropoxy-benzocaran-3-carboxylic acid formamidine; 6-amino-2- (4-fluoro-phenyl) -5-methoxy-benzofuran- Formamidine 3-carboxylic acid; 6-ethylamidoamino-2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamide; 88828. doc -54- 200418452 2- (4-Fluoro-phenyl) -5-isopropoxy-6-methylamino-benzofuran-3-carboxamidine; 6-methylamino 2- (4-Fluoro-phenyl) -5-isopropoxy_benzofuran_3_ formamidine carboxylic acid; 2- (4-fluoro-phenyl) -5-isopropoxy -6-Methanesulfonylamino-benzofuran-3-carboxylic acid formamide; 6-ethylamino-2- (4-fluoro-phenylisopropoxy-benzofurancarboxylic acid formamidine Fluorenamine; 6-diethylamino-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro- Phenyl) -5-isopropoxy-6-morpholinolin-4-yl-benzofuran-3-methonamine methanoate; 5-methoxy-4-methyl-2-phenyl-benzene 3-amino acid formic acid amine; 5-cyano-2-phenyl-benzoic acid methylformamide; 5-isopropoxy-2-eridin-4-yl-benzofuran _3_ Formamidine carboxylic acid; 6- (3,5-dimethyl-isoxazole_4_yl) _2_ (4_fluoroyl_phenyl) -5-methoxy-benzofuran-3 -Formamidine carboxylic acid; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl_amino) _5_methoxy-benzofuran-3-carboxylic acid formamide ; 2- (4-Fluoro-phenyl) -5- (4-methoxy-fluorenyloxy ) -6-morpholin-4-yl-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6- [methanesulfonyl_ (4-methoxy -Benzyl) -amino] -5- (4-methoxy-benzyloxy) _benzofurancarboxylic acid formamidine; 5 -ethoxy-6- (ethyl-methylsulfanyl) · Amine) -2- (4-fluoro-phenyl) -benzene 88828. doc -55- 200418452 benzofuran-3-carboxylic acid formamide; 2- (4-fluoroyl-phenyl) -6-morpholine-4 · yl-5- (thiazol-2-ylmethoxy) -Benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy [methanesulfonyl_ (2_oxy_propyl) -amino] Benzofuran-3-chinoic acid amine; 2- (4-fluoro-phenyl) -6-morpholine-4-yl (thiazolylmethoxy) _benzofuran-3-carboxylic acid methyl Fluorenamine; 2- (4-fluoro-phenyl) -5_isopropoxy (methanesulfonyl-thiazolylmethyl-amino) -benzofuran-3-carboxylic acid formamide; 2- (4 • Fluoro-phenyl) -6- (5- # Limethyl-iso-4-ammonium_3_yl) _5_isopropoxy_benzofuran-3-carboxylic acid formamidine; 5-ethyl Oxy-2--2- (4-fluoro-phenyl) -6- (methanesulfonyl_methyl-amino) _benzocaran-3-methanoic acid formamidine; 4- [2- (4 -Fluoro-phenyl) (methanesulfonic acid-methyl-amino) -3-methylcarbamic acid-benzofuran_5_yloxymethyl &gt; 2-hydroxy_benzoic acid; 2- (4-Fluoro-phenyl) _6_ (5_hydroxymethyl_isoindazole_3-yl) _5-methoxy_benzocrean-3 -amine acid formate; 2- (4-fluoro group -Phenyl) _6- [4_ (2-hydroxy-ethyl) _isohumazole-3 _Yl] _5-methoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) hydroxy-ethyl) _methanesulfonyl-amino group] _5-methoxy Methyl-benzofuran_3_carboxylic acid formamidine; 5-cyclopropyl_2- (4-fluoro-phenyl) -6-[(2-hydroxy-ethyl) -methanesulfonyl-amine Methyl] -benzofuran_3-carboxamidine; 5-ethyl-2- (4-fluoro-phenyl) -6-methylpyroxyamino-benzocaran-3- 88828 . doc -56- 200418452 mesylamine carboxylate; 5'ethyl-2- (4-fluoro-winteryl) -6- (methylbenzene g-methyl-amino-amino) _benzofuran-3 -Formamidine carboxylic acid; ethyl-2- (4-fluoro-phenyl) -6-[(2-light-ethyl) -methylsulfanyl-amino group; μbenzofuran-3 -Formamidine carboxylic acid; 6- (1-ethylamyl-pyrrolidin-2-yl) -2- (4-fluoro-phenyl) -5-methoxy-benzylfuran-3-carboxylic acid formamidine Fluorenylamine; (4-fluoro-phenyl) -5 -methoxy-6- (2-oxy-azendo-5-yl) -benzofuran-3-carboxylic acid formamide; 2- (4-Fluoro-phenyl) -6- (1-lightyl-1-methyl-ethyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine; 2- (4- Fluoro-phenyl) -5-methoxy-6- (5-methyl- [1,2,4] fluorenediazol-3-yl) benzofuran-3-carboxylic acid formamide; 6- (3,5-Dimethyl-isoxazol-4-yl) -2- (4-fluoro-phenyl) _5- (3-hydroxy_propoxy) -benzofuran-3-carboxylic acid Fluorenamine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5- (2-morpholine-4-yl-ethoxy) -benzo Formamidine furan-3-carboxylic acid; 5-(-Deryl-2-yl-methyllactyl) -2-phenyl. ; 5-methoxy-2- (4-methoxy-phenyl) -epiamino-3-amino acid formate; 5-methoxy-2- (3-trifluoromethyl-phenyl ) · Benzofuran-3-carboxylic acid formamide; 5-methoxy-2- (4-trifluoromethyl-phenyl) -benzofuran-3-carboxylic acid formamide; 5-ethoxy Methyl-2-phenyl-benzofuran-3-carboxylic acid formamide; 2- (2-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamide; 5 -Isopropoxy-2-phenyl-benzocran-3 -amine acid formate; 88828. doc -57- 200418452 5-butoxy-2-phenyl-benzofurancarboxylic acid formamidine; 2-phenyl-5-propoxy_benzofuran_3_carboxylic acid formamide; 5- Methoxy-2- (2,4,5-trifluoro-phenyl) _benzofuran-3_carboxylic acid formamide; 5-methoxy-7-methyl-2-phenyl-benzene Benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5- (2,2,2-trifluoro-ethoxy) _benzofuran-3_formamidine carboxylic acid Amine; 2- (4-fluoro-phenyl) -5-isopropoxy-benzofurancarboxylic acid formamidine; 2- (2-chloro-phenyl) -5-methoxy-benzo Formamidine furan carboxylate; 6-methoxy-2-phenyl-benzoic acid-3-methanoic acid methylamine; 2-amidan-2-yl-5-methoxy-benzofuran_ Formamidine 3-carboxylic acid; 2- (3-Fluoro-4-methyl-phenyl) -5-methoxy-benzofuran-3-metanoformamide; 2- (4-bromo -Phenyl) -5-methoxy-benzofuran_3_methanamine methanoate; 2- (4-fluoro-3-methyl-phenyl) -5-methoxy-benzofuran _3_ Formamidine carboxylic acid; 2- (4-fluoro-phenyl) -5-methoxy-7-methyl-benzocaran-3-methanamine formamidine; 5-chloro- 2- (4-Fluoro-phenyl) -benzofuran-3-carboxylic acid formamidine; 5-tert-butyl 2-Phenyl-benzocaran-3-methylformamide; 5-chloro-2-p-tolyl-benzocaran-3-methylformamide; 2- (3- Chloro-4-fluoro-phenyl) -5-methoxy gastric benzopyran-3-carbamate formamidine; 2- (4-chloro-3 -fluoro-phenyl) -5- Methoxy-benzoic acid-3-amino acid formic acid; 5-methoxymethyl-2-phenyl-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl ) -5-isopropoxy-6-methyl-benzoic acid-3-formamide methylformamide; 88828. doc -58- 200418452 2- (4-Fluoro-phenyl) -5-isopropoxy-7-methyl-benzocaran-3-methaneformamide; 2- (4-fluoro- Phenyl) -5-methoxy-6-methyl-benzofuran-3-carboxylic acid formamide; 5-fluoro-2- (4-fluoro-phenyl) -benzocran-3 -Formamidine chitoate; 2- (4-ethyl-phenyl) -5-fluoro-benzofuran-3-carboxylic acid formamide; 5-ethyl-2-phenyl-benzofuran_ Formamidine 3-carboxylic acid; 2- (5-chloro-thien-2-yl) -5-methoxy-benzofuran-3-carboxylic acid formamide; 5-xingpropoxy-2- Winteryl-benzoanan-3-metanosylamine; 2- (5-chlorosethen-2-yl) -5 -ethoxy-benzoanan-3-metanoic acid T acid amine; 5-Methoxy-2-p-cephen-2-yl-benzofuran-3-chimonate formamidine; 5-chloro-2-pyridin-3-yl-benzofuran-3-carboxylic acid $ Amine; 2- (4-bromo-3-fluoro-phenyl) -5-isopropoxy-benzoanan-3-methanoic acid formamide; 2- (2,4-difluoro -Phenyl) -5-isopropoxy-benzofuran_3_carboxylic acid formamide; 6-benzyl-2- (4-fluoroyl-phenyl) _5_isopropoxy-benzo Squeam_3_metamethamine; 5-methoxy-2- (4-morphol # _4-yl-phenyl) _benzoxan_3_stamate Amine; 5,6-dimethoxy-2-phenyl-benzofuran-3-metanoic acid carboxylic acid amine; 5-hexylpropoxy-2- (4-p-biloxo-1-yl-benzene ) _Benzocaran · 3_metamidine mesitamine; 5-dunyl-2 · ^ pylide-4-yl-benzocaran-3-chiamate formamidine; 2- [2- (4 -Fluoro-phenyl) -6-methyl-3-methylamine formamidine-benzofuranyloxy] -propionic acid; 88828. doc -59- 200418452 6acetamido-2- (4-fluoro-phenyl) -5-isopropoxy-benzoanan-3-chitoic acid formamide; 2β (4-amino- Phenyl) -5-isopropoxy-benzopyrancarboxylic acid formamidine; 2 · (4-fluoroyl-phenyl) -5-isopropoxy-6- (2-morpholin-4 -Yl-ethylamino) -benzoic acid-3-methylacetamide; 2- (4-fluoro-phenyl) -5-isopropoxy-6-hexahydropyridin-1-yl- Benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5,6-dimethoxy-benzofuran-carboxylic acid formamide; 2- (4-fluoro group -Phenyl) -5 -methoxy-6-morpholin-4-yl-benzocaran-3-methanoic acid formamide; 2- (4-bromo-phenyl) -5-isopropyl Oxy-benzoic acid methylformamide; 2- (4-fluoroyl-3- # presentyl-phenyl) -5-isopropoxy-benzoic acid_3_methanoic acid ; 2- (4-cyano-phenyl) -5-isopropoxy-benzoanan_3-methanoic acid formamide; 5-methoxy-2-pyridin-4-yl-benzo _3_ formamidine methanoate; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (3-methanesulfonyl-pyrrolidin-1-yl) -benzo Methane-3-carboxylic acid methylamine; 6-trimethylenepentamine-1-yl-2- (4-fluoro-phenyl) -5-iso Oxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6- (3-meryl-pyrrolidin_1_yl) -5-isopropoxy_ Benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy_6_ (methanesulfonyl_methyl-amino) _benzofuran-3 -Formamidine carboxylic acid; 2- (4-fluoro-phenyl) -6-[(furan-3-ylmethyl) -amino] -5-isopropoxy 88828. doc -60- 200418452 benzoic acid-3-dicarboxylic acid amine; 6- (2,3-dihydroxy-propylamino) -2- (4-fluoro-phenyl) -5-isopropoxy -Benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6-isopropylamino-benzofuran-3-carboxylic acid formamidine Fluorenamine; 6- (cyclopropylmethyl-amino) -2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamide; 2- ( 4-Fluoro-phenyl) -5-methoxy-6-p-Bilodoline-1-yl-benzyl-3-carbamate; 5-Wordoxy-2- (4- Fluoro >> yl-phenyl) -6-morpholin-4-yl-benzopyran-3 -methanamine mesitylate; 5-hydroxymethyl-2-phenyl-benzofuran-3-carboxylic acid Formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6-[(2-methoxy-ethyl) -methyl-amino] -benzofuran-3- Formamidine carboxylic acid; 6-amino-5-benzyloxy-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid formamide; 5-isopropoxy-2- (3-methyl-furan-2-yl) -benzofuran-3-carboxylic acid formamidine; 2- (4 -Gasyl- winteryl) -6-methyl-S-S-aminoamino-5-methyl Oxy-benzoanan-3-methanomethamine; 2- (4-fluoro-phenyl) -5-isopropoxy -6-[(tetrahydro-an-2-ylmethyl) -amino] -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-mer -6-morpholin-4-yl-benzocaran-3-methanamine; 5-cyclopropylmethoxy-2- (4-fluoro-phenyl) -6-morpholine- 4-methyl-benzofuran-3-carboxylic acid formamide; 88828. doc -61-200418452 6-chloro-2- (4-fluoro-phenyl) -5-methoxybenzofuran-3-carboxylic acid formamidine; 6- (2,5-monomethyl ratio Jun-3-ylamino) _2- (4-fluoroyl-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoroyl-phenyl) Morphine _4_yl-5_ (pbito-4-ylmethoxy) _benzopyran-3-carboxylic acid formamide; 6-cyano-2_ (4-fluoro-phenyl ) -5-Isopropoxy-benzoanan-3-methylacidamine; 5-methoxy-2-phenyl-benzofuran-3-carboxylic acid acetamide; 2- (4- Fluoro-phenyl) -5_isopropoxy-6- (pyridin-4-ylamino) -benzoanan-3-carboxylic acid formamidine; 2 (4 -muryl-dongyl) _5 _Isopropyllactyl ^-(cardiomethyl-hexachloro p ratio p well_1_yl) _ Benzofuran-3-carboxylic acid formamide; 6- (3-chloro-propane- 丨 _sulfonyl Amino group) _2_ (4-fluoro-phenyl) _5_isopropoxy-benzofuran_3_carboxylic acid formamide; 6- (1,1-dioxy_ia 6_isopyrimazole Pyridyl) -2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 2 (4-Gasyl- winteryl) isopropyllactylmethyl _Benzalan_ 3 _Metrazidine metabolite; 2- (4-fluoro-phenyl) _5 -Isopropoxy_6_ (isopropyl-methanesulfonyl-amino) -benzofuran-3-carboxylic acid formamidine; 6- (cyclopropylmethyl-methanesulfonyl-amine) _2_ (Cardiofluoro-phenyl) isopropoxy-benzofuran-3-carboxylic acid formamide; 6- (2,6-dimethyl_morpholine_4_yl) -2- (4- Fluoro_phenyl) _5_isopropoxy 88828. doc -62- 200418452 methyl-benzofuran-3-chitoic acid formamidine; 2- (4-amino group) -5 -isopropoxy-6- (1fluorene-tetra-5-yl) -benzene Benzene-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6- (4-boryl-hexahydroρ-pyridin-1-yl) -5 -isopropoxy- Benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6- (3-light-hexahydrop-pyridine-1-yl) -5-isopropoxy- Benzofuran-3-carboxylic acid formamidine; 2- (4-Gasyl-Methyl) -5-isopropoxy ^ -6- (morpholin p-4) -benzofuran Formamidine-3-carboxylic acid; Formaldehyde 2- (4-fluorofluorophenyl) -5-isopropoxy-6-methylamine-benzobenan-3-carboxylic acid formamide; 6-—Methylaminocontinyl-2- (4-amino-fluorenyl) -5-isopropoxy-benzoanan-3-metanoic acid formate; 2- (4-fluoro-benzene ) -5-isopropoxy-6- (propane-2-sulfoamidoamino) _benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5- Isopropoxy-benzoanan-3,6-dipicanoic acid 6-fluorenamine-3-carboxamide; 2- (4-fluoroyl-phenyl) -5-isopropoxy-6- Pyrimidin-5-yl-benzofuran_3_decanoate formamidine; 6-di-di-butylamino-2- (4 -Fluoro-phenyl) -5-isopropoxy-benzopyrrol-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6- Amino acid-benzoic acid_3_methaneformamide; 6-cyclobutylaminesulfonic acid-2- (4-fluoro-phenyl) -5 -isopropoxy-benzo bite 88828. doc -63- 200418452 formamidine-3-carboxylic acid; 2- (4-muryl-phenyl) -6-mauran-2-yl-5-isopropoxy-benzoanan-arsinic acid Ammonium formate; 2- (4-Fluoro-phenyl) -6-furan-3-yl-5-isopropoxy-benzofuran_3_-chimonic acid formamidine; 2- (4-amino- Phenyl) -5 -isopropoxy-6-shodo-3-yl-benzoylmethaneamine; 2-(4 -Gasyl-tolyl) -5 -Xyprolactyl-6- (p ratio bite_ 1 -continuous base) _benzyfuran-3-carboxylic acid formamidine; 6-cyclopropylaminesulfonyl-2- (4-fluoro-phenyl) -5-iso Propoxy-benzoanan-3 -methanoic acid melamine; 6-ethylaminesulfonyl-2- (4 • fluoro-phenyl) -5-isopropoxy-benzocran- Formamidine 3-carboxylic acid; 2- (4-fluoro-phenyl) -5-isopropoxy-6-vinyl-benzofuran-3-formamic acid 3-carboxylic acid; 2- (4-fluoro -Phenyl) -5-isopropoxy-6-methoxy-benzofuran-3-carboxylic acid formamide; 6- (3,5-dimethyl-isoxazole_4_yl) _2_ (4_Fluoro-phenyl) quinone_isopropoxy-benzocaran-3-metachloramine; 2- (4-fluoro-phenyl) -6-formylisopropyloxy Methyl_benzofurancarboxylic acid formamidine; 2- (4-fluoro · phenyl -6- (6-Fluoro-pyridin-3-yl) -5-isopropoxy · benzoic acid-3-amine acid formate; 2- (4-fluoro-phenyl) -5-iso Propoxy_6_ (methanesulfonamido_methyl) _ 88828. doc -64-200418452 benzofuran-3-carboxylic acid formamidine; 6- (cyclopentyl-methylamino-amino) -2- (4-fluoro-phenyl) -5-isopropyl Oxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro, phenyl) -6-[(2- mesityl-ethyl) -methanephenyl-amino] _5_ iso Propoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-hydroxy-6-methoxy-benzofuran_3-carboxylic acid formamide; 5-Ethyllactyl-2- (4-amino-phenyl) -6-morpholin-4-yl-benzoanan_3-methanomethamine; 5- (4-fluoro-benzyl (Oxy) -2- (4-fluoro-phenyl) -6-morpholin-4-yl-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) _5 _Isopropoxy-6-indazol-5-yl-benzofuran_3_Chloramic acid formamide; 2- (4-fluoroyl-phenyl) -6- (4-meryl-hexahydropyridine -1-continyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 6- (4,4-monomuryl-7T mouse? Bi Zheng-1-yl) _2- (4-Fluoro-phenyl) -5 -isopropoxy-benzoanan-3 -amine acid formate; 2- (4-fluoro-phenyl) -6- (4-fluoro-7T Chloro p ratio _1_ylisopropoxy_ benzofuran-3-carboxylic acid formamidine; 5-difluoro Oxy-2- (4-benzyl-phenyl) -6-morpholin-4-yl-benzopyran-3-carboxylic acid formamidine; 5-cyclopentyloxy-2- (4- Fluoro-phenyl) -6-morpholin-4-yl-benzofuran j-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5- # Pit-continued g-Amino-benzo-benzoan 88888. doc -65- 200418452 Carboxylic acid formic acid amine; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (thiomorpholine-4-sulfonamido) -benzene-3 -Formamidine carboxylic acid; 2- (4-fluoro-phenyl) -6- (3-hydroxy-pyrrolidin-1-sulfonyl) _5_isopropoxy-benzofuran-3-carboxylic acid Formamidine; 2- (4-fluoro ·· phenyl) -5-isopropoxy-6-pyridin-4-yl-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro -Phenyl) -5-isopropoxy-6- (3-methanesulfonyl-phenyl) -benzylfuran-3-carboxylic acid formamidine; 2- (4-fluoroyl-phenyl) -5-isopropoxy-6- (4-methanesulfonyl-phenyl) -benzofuran-3-carboxylic acid formamidine; 5- (2-muryl-ethoxy) -2- ( 4-Fanyl-phenyl) -6-morpholin-4-yl-benzoanan-3-methanoic acid formamidine; 6-fluorenyloxy-2- (4-fluoroyl-phenyl)- 5-methoxy-benzofuran-3-carboxylic acid formamidine; 6-amino-2- (4-fluoro-phenyl) -5-mercapto-benzoic acid_3_carboxylic acid formamidine Fluorenamine; 5,6-bis-fluorenyloxy-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5 -Isopropoxy-6- (5-trifluoromethyl- [ι, 2,4] humidazol-3-yl) -benzofuran-3-carboxylic acid Fluorenamine; [2- (4-fluoro-phenyl) -5-isopropoxy-3-methylamine methylamidino_benzofuran-6-yl] -hexahydropyrine-1-metanoic acid Fluorenamine; 2- (4-fluoro-phenyl) -5-isopropoxy-6-thiomorpholin-4-yl-benzoanan-3-carboxylic acid formamide; 2- (4 -Fluoro-phenyl) -5-isopropoxy-3-methylamine formamidine-benzofuran 88828. doc -66- 200418452 -6-carboxylic acid; 2- (4-fluoro- winteryl) -5-oxopropoxy-6- (1-oxy-thiomorpholin-4-yl) _benzo Furan-3-carboxylic acid formamidine; {[2- (4-fluoroyl-phenyl) -5-isopropoxy-3-methylamine formamidine-benzofuran-6-yl] formyl fe Continued S-S-yl-amino} -acetic acid; 6- (cyclobutyl-methanesulfonyl-amino) -2- (4-fluoro-phenyl) -5-isopropoxy-benzocran -3-Leptinic acid formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6- [methanesulfonyl- (2-morpholine-4-yl-ethyl) -Amine group] -Methylbendonamine-3-benzocaran-3-carboxylic acid; 2- (4-fluoro-phenyl) -5,6-dihydroxy-benzofurancarboxylic acid formamide; 2- (4 -Fluoro-phenyl) -5-isopropoxy-6- [methanesulfonyl- (2-methoxy_ethyl) -amino] -benzoxan-3-carbamate 6-benzyloxy-2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 6- (allyl-methanesulfonyl) Amine) _2- (4-fluoro-phenyl) _5_isopropoxy-benzofuran-3-carboxylic acid formamidine; 6-acetoxy-2- (4-fluoro-phenyl) &gt; 5-isopropoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5_ Propoxymethanesulfonylamino-benzoic acid-3-isopropylamine; -67- 200418452 2- (4-fluoroyl-phenyl) _5_isopropoxy_6_methanesulfonyl Amino-benzofuran'an-3-etanoic acid acedonylamine; 2- (4-fluoro-phenylmethyl ^ selazol-4-ylmethoxymorpholine-4-yl-benzofuran _3-methylformamide carboxylic acid; 2- (4 • fluoro-phenylhydroxy- ^ methyl-ethyl) _5_isopropoxy-benzofuran-3-carboxylic acid formamide; 5- [ 5- (3,5-dimethyl_isoindazole_4-ylpyridazolylmethoxy) -2- (4-fluoroyl-phenyl) _6_morpholin_4_yl-benzo Formamidine furan-3-carboxylic acid; 5- (5-third-butyl412,4] pyridazol-3-ylmethoxy) -2- (4-fluoro-phenyl) -6_ Morpholine-4-yl-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoroyl-phenyl) -5-isopropoxy-6- [1,2,4] fluorene Mazol-3-yl-benzofuran-3-carboxylic acid formamide; 5- (5-chloro- [1,2,4] thiadiazole-3-ylmethoxy) -2- (4- Fluoro-phenyl) -6-morpholinolin-4-yl_benzofuran-3-carboxylic acid formamide; 2- (4-fluoroyl-phenyl) -6-morpholin-4-yl -5- (5-p-tolyl- [1,3,4] oxadiazol-2ylmethoxy) -benzofuran-3-carboxylic acid formamidine ; 2- (4-Fluoro-phenyl) -6-¾yl-5 -methoxy-benzofuran-3-methanoate-amine; 2- (4-fluoro-phenyl)- 5- (1-methyl-1H-tetrazol-5-ylmethoxy) -6-morpholin-4-yl-benzofuran_3 · carboxylic acid formamide; 2- (4-fluoro group -Phenyl) _5_ (3-methoxy-benzyloxy) -6-morpholin-4-yl-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) _5methoxy-, (丨 -methyl-1H-tetrazol-5-ylmethoxy 88888. doc -68-200418452 methyl) -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5- [1- (4-fluoro "yl-phenyl) -ethoxy [Methyl] -6-morpholin-4-yl-benzofuran-3-carboxylic acid formamidine; 5- (4-amino-etomethoxy) -2- (4-amino-phenyl) -6 -morpholin-4 -yl-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -5- [5- (4-methoxy-phenyl) -[1,2,4] indoxazolylmethoxy] -6-morpholin-4-yl-benzofuran-3-carboxylic acid formamide; 2-(4-amino-phenyl) -6 -morpholin-4 -yl-5-(2-oxoyl-propoxy) -benzyfuran-3-carboxylic acid formamide; 5- (1-benzyl-1H-imidazole-2 -Methoxy) -2- (4-fluoro-phenyl) -6-morpholin-4-yl-benzofuran-3-methanamine; 5- (3,5-di Methyl-isoxazol-4-ylmethoxy) -2- (4-fluoro-phenyl) -6_morpholin-4-yl-benzofuran-3-carboxylic acid formamide; 2- ( 4-Fluoro-phenyl) -5- (5-methyl-isopurazol-3-ylmethoxy) -6-morpholine-4-yl-benzofuran-3-carboxylic acid formamidine ; 2- (4-Gasylphenyl) -5 -propanyloxy-6-ρ cejun-2 -yl-benzoanan-3 -methoxamine methylamine; 2- (4-gasyl -this ) -5 -Propanyloxy-6- (1Η-ρbilo-2-yl) -benzoxan-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -6 -(Isopropyl-methanesulfonyl-amino) -5-methoxy_benzoanan-3-amino acid formate; 2- (4-fluoro-phenyl) -6_ (1-hydroxy -Ethyl) -5-isopropoxy-benzocaran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-isopropoxy-6-morpholin- 4-ylmethyl-benzoic acid 88828. doc -69- 200418452 formamidine-3-carboxylic acid; 2- (4-fluoro-phenyl) -6-hydroxymethylisopropoxy-benzoxetine Amine; 2- (4-Fluoro-phenyl) -5- (3H-weijun-4-ylmethoxy) _6Wei, -fluorene, mayelin-4-yl-benzofuran_3_carboxy Formamidine acid; 2- (4-fluoro-phenyl) -5- (2-methoxy-ethoxy) &gt; 6-morpholine methobenzofuran-3-carboxylic acid formamide; 2 -(4-Gasyl-phenyl) -5 -isopropoxy-6_sulfan-5-yl-benzyl 3 methylformamide; 5- (4-chloro-1-methyl- lHw than Jun-3-ylmethoxy) -2- (4-fluoro-phenyl) -6-morpholin-4-yl-benzofuran-3-carboxylic acid formamidine; 5- (cyano -Methyl-methoxy) -2- (4-fluoro-phenyl) -6-morpholin_4_yl_benzofuran-3-carboxylic acid formamide; 2- (4-fluoro -Phenyl) -5-isopropoxy-6- (2H- ^ pyridol-3-yl) _benzoanan-3-methanoic acid formamide; 2- (4-fluoro-phenyl ) -5 -isopropoxy-6- (2-methyl-2Η-fluorenylpyridine-3 -yl) _benzofuran_3_carboxylic acid formamide; 2- (4-amino-benzene ) -5 -isopropoxy-6- (1-methyl-1H-1? Than fluorene-3 -yl) _benzofuran-3-chimonate formamidine; 2- (4-Fluoro-phenyl) -5-isopropoxy-6- (3-methyl-isopurazol-5-yl) -benzofuran-3-carboxylic acid formamide; 6- [(5-chloro- [1,2,4] pyrimidazol-3-ylmethyl) -methanesulfonyl-amino group] -2- (4-fluoro-phenyl) -5-isopropyl Oxy-benzofuran-3-carboxylic acid formamidine; 6- (3,5-dimethyl-isodiazol-4-ylamino) -2- (4-fluoro-phenyl) -5 -Different 88828. doc -70- 200418452 Propoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-methoxypyridin-3-yl-benzofuran-3- Formamidine carboxylic acid; 6-dimethylaminomethyl-2- (4 • fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamide; 2- ( 4-Fluoro-phenyl) _6- (1_hydroxy-2_methyl-propylisopropoxy-benzofuran-3_metamethylamine; 2- (4-fluoro-phenyl) ) -5-isopropoxy-6- (1H-pyrazol-4-yl) -benzofuran-3-methanoic acid formamidine; 2- (4-fluoroyl-phenyl) -6- [methane Sulfonyl- (2-methoxy-ethyl) _amino; | -5-methoxy-benzofuran-3-carboxylic acid formamide; 6- (3-cyclopropyl-isoxazole -5-yl) -2- (4-fluoroyl-phenyl) -5-isopropoxymonobenzofuran-3-carboxylic acid formamidine; 2- (4-fluoroyl-phenyl) -5 -Isopropoxy-6- (3-methoxymethyl-isoxazol-5-yl) -benzofuran-3-carboxylic acid formamide; 2- (4-amino-phenyl) -6 -Methylsulfonylamino-benzyl-3-benzylformamide; 2- (4-fluoro · • phenyl) -6- (1 //-imidazol-2-yl)- 5-isopropoxy-benzofuran-3-carboxylic acid formamide; 6- (2,5-dimethyl-2H-pyrazol-3-yl) -2- (4-Fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 6- (3,5-dimethyl-1H-pyrazol-4-yl) · 2- (4-Fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-isopropoxy- 6- (5-methyl · 2Η-pyrazol-3-yl)-88828. doc -71-200418452 benzofuran-3-carboxylic acid formamide; 6- (1,5-dimethyl-1H-pyrazol-3-yl) -2- (4-fluoro-phenylphenyl 5 _Isopropoxy_benzofuran_3_carboxamide; 2- (4-fluoro-phenyl) -5-isopropoxy-6-[(formamidine Amino) -methyl] -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5- (2-hydroxy-2-methyl-propoxy) _6_ Morpholine-4_yl-benzocrean-3-acid formate; 2- (4-fluoro-phenyl) -5- (2-hydroxy-2-methyl-butoxy) _6_? Fluoroline_4_yl-benzoxan-3 -amine acid formate; 2- (4-fluoro-phenyl) -5- (2-yl-propoxy) -6-morpholin_4 -Methyl-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6-[(2_ # Askyl-propyl) _methanesulfonate_amino] iso Propoxy-benzofuran-3-carboxylic acid formamide; 2- (4-Gasyl-phenyl) -6-morpholin-4-yl-5- (1-tetramethyl-2-yl- Ethoxy) _benzofuran-3-carboxylic acid formamidine; 6- (ethyl-tolueneSi-amino) -2- (4-fluoro-phenyl) -5-isopropoxy · Benzofuran-3-carboxylic acid formamidine; 6- (3,5 methyl-1H-etto-4-yl) _2- (4-fluoro-phenyl -5 -Methoxy_benzofuran-3-carboxylic acid formamide; 2- (4 -Gasyl- winteryl) -5 -isopropoxy-6- (5-methyl-1H -Ekou Sat-4 -yl) _benzofuran-3-carboxylic acid formamidine; 3- [2- (4- (fluoro-phenyl) -3-methylaminomethdonyl-benzoxan-5) Methyloxymethyl] methyl gallate; 4- [2- (4-Fluoro-phenyl) -3-methylaminomethylsulfanyl-benzo T? Furan-5-yloxymethyl 88828. doc -72- 200418452 yl] phosphonic acid; 3- [2- (4-fluoroyl-phenyl) -3-methylaminomethylamidino-benzofuran-5-yloxymethyl] noic acid S 6- Ethyl-2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid formamidine; 4- [2- (4-fluoro-phenyl) -3 -Methylaminomethylmethyl-6-morpholin-4-yl-benzofuran-5-yloxymethyl] -benzyl methyl ester; 3- [2- (4-fluoroyl-phenyl)- 3-methylamine formamyl-6-morpholin-4-yl-benzofuran-5-yloxymethyl] -benzoic acid methyl ester; 2- (4-fluoroyl-phenyl) -5- Isopropoxy-6- (1,3,5-trimethyl_1H-pyrazole_4-yl) -benzofuran-3-carboxylic acid formamide; 2- (4-amino-methyl ) -5 -Isopropoxy-6-p-pyrrolidine-2-yl-benzoanan-3_carboxylic acid formamide; 6-cyano-2- (4-fluoro-phenyl)- 5-methoxy-benzofuran-3-carboxylic acid formamidine; 4- [2- (4-fluoro-phenyl) -3-methylamine formamidine-6-morpholine-4- -Benzobenzo-5-yloxymethyl] -benzylic acid; 3- [2- (4-fluoroyl-phenyl) -3-methylaminomethylmethyl-6-morpholine-4- -Benzobenzo-5-yloxymethyl] -word acid; 2- (4-fluoroyl-phenyl) · 5-isopropoxy-6- [methanesulfonyl- (1-methyl -1H- Tetrazol-5-ylmethyl) -amino] -benzofuran-3-carboxylic acid formamide; 4-({[2- (4-fluoro-phenyl) -5-isopropoxy- 3-methylaminomethylamidino-benzofuran-6-yl] -methanesulfonyl-aminomethyl (methyl) -benzoic acid methyl ester; 2- (4-fluoro-phenyl) -5-isopropoxy -6- [methanesulfonyl- (2-methyl-thio 88828. doc -73-200418452 azole-4-ylmethyl) &gt; amino] -benzofuran-3 -carboxylic acid formamidine; 4-({[2- (4-fluoroyl-dongyl) -5- Isopropoxy-3-methylaminocarboxylic acid benzobenzo-6-yl] methylfedonyl-aminomethyl) _co-acid; 2- (4-fluoro-unyl) -5- Isopropoxy-6- (5-methoxymethyl-isostilbene-3-yl) -benzofuran-3-carboxylic acid formamidine; 6- (5-cyclopropyl-isoxazole-3 -Yl) -2- (4-fluoroyl-phenyl) _5-isopropoxy_ benzocrean-3-chinoic acid amine; 2- (4-fluoroyl-phenyl) -5-isopropyl Oxy-6- (1-methanesulfonyl-pyrrolidin-2-yl) -benzoic acid-3-amine acid formate; 6-ethynyl-2- (4-fluoro-phenyl) -5-Jinyl-benzocrean_3-methanoic acid methylamine; 6- (ethyl-methyl: yl-amino) -2- (4-denyl-phenyl) _5-methoxy_benzene Benzofuran-3-carboxylic acid formamidine; 4- [2- (4-fluoro-phenyl) -5-methoxy-3-methylamine formamidine_benzofuran-6-yl]- 2-oxopyridine-3-chimonate formamidine; 2- (4-fluoro-phenyl) -5-isopropoxy-6- (4Η- [1,2,4] triturate- 3-yl) -benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-methoxy-6- (5-methoxymethyl- 3-methyl-isoxazol-4-yl) -benzofuran-3-carboxylic acid formamide; 2- (4-fluoroyl-phenyl) -5-isopropoxy-6- [methanesulfonate Fluorenyl-('methoxy_benzyl) -amino] benzocarban-3-carbamate; 2- (4-fluoro-phenyl) -5-isopropoxy-6- [Methanesulfonyl- (5-methyl-isoxazol-3-ylmethyl) -amino] -benzofuran-chitoic acid formamidine; 2- (4-fluoro-benzyl) _5_iso Propoxy-6- (5-methyl-isoisopyridyl) _benzene 88828. doc -74- 200418452 benzofuran-3-carboxylic acid formamidine; 6-[(3,5-monomethyl_isoxazole_4_ylmethyl) _methanesulfonyl-amino group] -2- (4-Fluoro-phenyl) _5_isopropoxybenzofuran-3_methanamine methanoate; 2- (4-fluoro-phenyl) _5_isopropoxy_6- (methanesulfonate Fluorenyl-oxazolyl-methyl-amino) -benzofuran-3-carboxylic acid formamidine; 2 _ ({[2- (4-fluoroyl-phenyl &gt; 5-isopropyloxy_3 · Methylaminomethylsulfanyl-benzofuran-6-yl] -methanesulfonyl-aminomethylmethylxazole_4-carboxylic acid ethyl ester; 2- (4-fluoro-phenyl) _5_hydroxy_ 6_ (methanesulfonyl_methyl-amino group) benzofuran_3_carboxylic acid formamide; 6- (fluorenyl_methanesulfonyl-amino group) _5_allyloxy_2_ ( 4-Fluoro-phenyl) -benzofuran-3-carboxylic acid formamidine; 6- (ethylfluorenyl-methanesulfonyl_amino) -2 _ ('fluoroyl_phenyl) _5_methoxy Methyl_benzoican-3-methanoic acid formamidine; 6-[(3,5-dimethyl_isoxazole_4_ylmethylmethanesulfonyl_amino group] -2- (4- Fluoro-phenyl) -5-methoxy-benzosulfan_3_methanomethamine; 2- (4-fluoro-phenyl) _6_ (methanesulfonyl ^ selazol_4_yl Methyl_amino) _5_methoxy_benzene Furan-3-carboxylic acid formamidine; 2-({[2- (4-fluoro-phenyl) _5_isopropoxy_3_methylamine formamidine_benzofuran-6-yl] -Methanesulfonyl-aminomethylmethyl) thiazolyl_4-carboxylic acid; 5- (2,2-dimethyl-4-4-oxy_4H-benzo [1,3] -dioxine-5 -Methoxy) -2- (4-fluoroyl-phenyl) _6_morpholine_4_yl-benzofuran_3_carboxylic acid formamide; 5- (2,2-dimethyl _4-oxy_4H-benzo [1,3] _dioxen-5-ylmethoxy) -6- (ethyl-methanesulfonyl-amino) ('fluoro-phenyl> ; Benzofuran 88828. doc -75- 200418452 formamidine carboxylic acid; 2- (4'fluoro-phenyl) -6- (1fluoren-imidazol-4-yl) -5-methoxy-benzofuran-3-chinoic acid Ammonium amine; 2- (cardiofluoro-phenyl) -6- (1H-imidazol-2-yl) -5-methoxy · benzofuran-3-chinocarboxylic acid amine; 6_ (ethyl-methyl benzene) Acid group-amino group) -2- (4-fluoro-phenyl) -5- # ryl_benzobenzon-3-carboxylic acid formamide; 5-fluoromethoxy-2- (4 -Fluoro-phenyl) -6- (formyl-methyl-amino-l-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6- (Methanesulfonyl_pyridin-4-ylmethyl_amino) methoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-phenyl) -6- (1- Hydroxy-1-methyl_ethyl) _5-methyl_benzofuran-3-methanoic acid formamide; 6-ethylfluorenyl · 2- (4-fluoro-phenyl) -5-methyl- Benzofuran_3_carboxylic acid formamide; 5- (2,2-monomethyl-4-lactyl-4H-benzo [1,3] _jitsu-7-ylmethoxy) -2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro- winteryl) -6 -[1- (methanesulfonic acid_methyl-amino) _ethyl] _5_ methoxy-benzo -3-Amino acid formate; 2- (4 · fluoro-phenyl) -5-methoxy-6_ (丨 _methylamino_ethyl) _benzofuran-3-carboxylic acid formamidine ; 4- [2- (4-Fluoro-fluorenyl) -6- (methylsulfonyl-methyl-amino) -3-methylaminomethyl §1-yl-benzoxan-5-yl Oxymethylbuthic acid formazan; 88828. doc -76- 200418452 2- [2- (4-Fluoro_phenyl) -6- (methylalanyl-methyl_amino) _3_methylcarbamic acid-benzofuran-5-yl Oxymethyl] -methylacetate; 6-[(2-fluoro-ethyl) _methanesulfonyl-amino] _2_ (4-fluoro-phenyl) _5_methoxy-benzofuran- Formamidine 3-carboxylic acid; 2- (4-fluoro-phenyl) _6- [methanesulfonyl- (2,2,2_trifluoroethyl &gt; amino)] _ 5_methoxy «benzene Benzofuran_3_carboxylic acid formamidine; 2- (4-fluoro-phenyl) _6- (1_methanthanoic acid group_ahadian_2-yl) _5-methoxy-benzofuran Formamidine-3-carboxylic acid; 6- (3-cyclopropyl-5-methoxymethyl-isoxazole_4 • yl-phenyl) -5-methoxy-benzofuran_3_ Formamidine carboxylic acid; 4- [2_ (4-fluoro-phenyl) _6- (methanesulfonyl-methyl_amino) methylaminoformamyl-benzofuran-5-yloxymethyl ] -Acidic acid; 3- [2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _3-methylaminomethylamidino-benzofuran-5-yloxy Methyl] -benzoic acid; 2- (4-fluoroyl-phenyl) -5-methoxy-6- (5-methoxymethyl-isoninazol-3-yl) -benzofuran-3- Formamidine carboxylate; 6- (3,5-dimethyl · isozazol-4-yl) -2- ( 4-Fluoro-phenyl) -5-hydroxy-benzofuran-3-carboxylic acid formamide; 2- (4-fluoro-phenyl) -5-methoxy-6- (5-oxy -Pyrrolidin-3-yl) -benzofuran-3-carboxylic acid formamidine; 2- (4-fluoroyl-phenyl) -6- [methanesulfonyl- (2_trifluoromethoxy- Ethyl) -amino] -5 -methoxy-benzoanan-3 -chitoic acid methylamine; 2- (4-fluoro-phenyl) -5-methoxy-6- (1H- Pyrrol-3-yl) -benzofuran-3-carboxylic acid formamide; 88828. doc -77- 200418452 6 · (3,5-dimethyl-isoxazol-4-yl) -2- (2-ethoxyfluoro-phenyl) -5-methoxy-benzofuran _3_ formamidine chitoate; 2- (4-fluoro-phenyl) -6_ (methanesulfonyl-methyl_amino) _5_ (pyrimazole_4_ylmethoxy) -benzofuran- Formamidine 3-carboxylic acid; 2- (4-fluoro_phenyl) _6_ (methanesulfonyl_methyl_amino) _5_ (2_methyl_ Yuanjun_4-ylmethoxy) _ Benzofuran-3-carboxylic acid formamidine; 5- (3-chloromethyl- ^ 2,4] thiadiazole-5_yloxy) _2_ (4_fluoroyl_phenyl) -6- ( Formaldehyde &amp; | Monyl-methyl-amino) _benzoic acid methylamine; 2- (4-fluoro-phenyl) -6-{[2- (4-fluoro- Phenyl) -2- mesityl_ethyl] -methanesulfonyl-aminomethyl 5-isopropoxy-benzofuran-3-carboxylic acid formamidine; 2- (4-fluoro-benzene ) _5 · methoxy_6_ (2 · methyl-2H- [1,2,4] _triazol-3-yl) -benzopyran-3-carbamate formamidine; 5- (3 , 5 -monomethyl-isonine 11-s-4-ylmethoxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzo Methane-3-methanamine formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5- (3-methoxy -Benzyloxy) -benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -5-hydroxy-6- (isobutyl-methanesulfonyl-amino) _Benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5- (4-methoxy- Benzyloxy) -benzofuran-3-carboxylic acid-formamidine; 2-(4 -Gasyl- winteryl) -6-(Methionite-methyl-amino-amine) -5-( p-ratio-4_ylmethoxy) -benzofuran-3-carboxylic acid-formamidine; 5- (2,2-dimethyl-4-oxy-4H-benzo [1,3] -Dioxen-6-ylmethoxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzofuran 88828. doc -78- 200418452-3 'carboxylic acid formamide; 6_ (cyclopropylmethyl-methanesulfonyl_amino) -2-(' fluoro group_phenyl) _5_methoxy-benzofuran- 3-carboxylic acid-formamidine; 2- (fluorenylfluoro-phenyl) _6_ (methanesulfonyl-methylaminomethylamidomethyl_amino) 5-methoxy-aspartic acid · Methylamine; Fluoro-2- (4-fluoro · phenyl) -6-methanesulfonamido-benzofuran_3_carboxylic acid formamidine; 6_ (ethyl-methanesulfonyl-amine Group) _5_fluoro group_2_ (4_fluoro group-phenyl) _benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro group-phenyl) -6- (1_methanesulfonate Fluorenyl-pyrrolidinyl 5-methoxybenzofuran-3-metanoic acid-formamidine; 5-ethyl-2 · (4-fluoro-phenyl) -6- [methanesulfonyl- (2-methoxy-ethyl) -amino] benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -5-methoxy-6- (3- Methoxymethyl-5-methyl-isoxazol-4-yl) -benzofuran_3-carboxylic acid-formamidine; 5-ethyl-6-[(2-fluoro-ethyl) -Methanesulfonyl-amino] -2- (4-fluoro-phenyl) benzofuran_3-carboxylic acid-methaneamine; 2- (4-fluoro-phenyl) -6- (methyl Continued S-S-propyl-propyl-amino) -5 -propane -Benzylfuran-3-carboxylic acid-formamidine; 5-ethyl-2- (4-fluoro-phenyl) -6- (1-hydroxy-1-methyl-ethyl) -benzo Furan-3-metanoic acid-formamidine; 6-Ethyl-5-ethyl-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid-formamidine; 4-chloro Group-6-ethylamino) -2- (4-fluoro-phenyl) -5-hydroxy-benzofuran 88828. doc -79- 200418452 -3-carboxylic acid-formamidine; methanesulfonic acid 4-chloro-6-ethylamino-2- (4-fluoro-phenyl) -3-methylamine formamyl -Benzo-cran-5-yl ester; 5-ethyl-2- (4-fluoro-phenyl) -6- (methylsulfanyl-B-S-pyridin-4-ylmethyl_amino group ] Benzofuran-3-carboxylic acid-formamidine; 6- (5-cyclopropyl-3-methoxymethyl-isoxazol-4-yl) -2- (4-fluoro group · phenyl) -5-methoxy-benzofurancarboxylic acid-formamidine; 6- (1-ethylfluorenyl-pyrrolidin_3-yl) -2- (4-fluoro-phenyl) -5-methoxy -Benzofuran-3-carboxylic acid-formamidine; 5- (3,4-difluoro-benzyloxy) -2- (4-fluoro-phenyl) -6- (formyl _Methyl-amino) -benzofuran-3-carboxylic acid · amidamine; 5- (2-fluorofluoromethoxy-methyleneoxy) -2- (4-fluoro-phenyl)- 6- (formamidine-methyl-amino) -benzoanan-3 -acid-methanamine; 2- (4-fluoro-phenyl) _6- (methanesulfonyl-methyl -Amino) -5-propoxy-benzofuran-3-carboxylic acid-methaneamine; 5-allyloxy-2- (4-fluoro · phenyl) -6- (methanesulfonyl -Methyl-amino) _benzofuran-3-carboxylic acid-formamidine; 6_ (5_ethoxymethyl-isoxazole- 3 -yl) -2- (4-fluoroyl-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-formamidine; 5-cyclopropylmethoxy-2_ (4-fluoro -Phenyl) _6_ (methanesulfonyl-methyl-aminol. Benzofuran-3-carboxylic acid-formamidine; 5- (3,5-dimethoxy-benzyloxy) -2- (4-Fluoro-phenyl) &gt; 6- (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) ^ 5- (4-methanesulfonyl-benzyloxy) -6- (methanesulfonyl 88888. doc -80- 200418452 methyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -5-hydroxy-6- [methanesulfonyl -(2-oxy-propyl) -amino] -benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl) -Amino) -5- [2- (4-methoxy-phenyl) -2-oxy-ethoxy] benzofuran_3_carboxylic acid-formamidine; 5- (3-cyano -Fluorenyloxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 5- (4 -Cyano-benzyloxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 2 -(4-fluoro-phenyl) -5-methoxy · 6- (2Η- [1,2,4] triazol-3-yl) _benzofuran-3-carboxylic acid-formamidine; 4_ {2- [2- (4-Fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _3-methylaminomethylamidino-benzocrean-5-yloxy ] -Ethylamidoamino} -ethylacetate; 2- (4-fluoro-phenyl) -5- [2- (4-denyl · phenyl) -2-oxy-ethoxy]- 6- (formamylsulfonyl-methyl · amino) -benzofuran-3-metanoic acid-methdonamine; 6- (benzyl-methanesulfonyl- ) -2- (4-fluoro-phenyl) -5-isopropoxy-benzofuran-3-carboxylic acid-formamidine; 4-chloro-6- (ethyl-methyl-amine ) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-formamidine; 4-chloro-6-ethylamino-2- (4 -Fluoro-phenyl) -5-methoxy-benzofuran-3-carboxylic acid-formamidine; 6-ethylamino-2- (4-fluoro-phenyl) -5-¾yl -Benzoic acid-3-guinic acid-formamide; 88828. doc -81-200418452 5- (3-bromo-propoxy) -6-ethylamino-2- (4-fluoro-phenyl) _benzoxan-3-carboxylic acid-formamidine ; 5-Hydroxypropoxy-6-ethylamino-2- (4-fluoro-phenyl) -benzoπfuran_3_metanoic acid-formamidine; 5- (3-ethoxy -Propoxy) -6-ethylamino-2- (4-fluoro-phenyl) · benzofuran-3-carboxylic acid-formamidine; 2- [2- (4-fluoroyl-benzene ) -5-methoxy-3-methylamine formamidine-benzofuran-6-yl] -pyrrolidine-1-aminoacetamide; 2- (4-fluoro-phenyl)- 6- (formamidine-methyl-amino-)-5_ (2-oxy_propoxy) -benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-benzyl ) -5- (2-Protyl-propoxy) -6- (formamic acid_methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro -Phenylmethanesulfonyl-methyl_amino) _5_ (1_methyl-1H-tetrafluoren-5-ylmethoxy) _benzobenzoic acid_formic acid amine; 2- (4- Fluoro-phenyl) _6_ (5_isopropoxymethyl_isoxazole_3_yl) _5_methoxy-benzofuran_3_carboxylic acid-formamidine; 5- (5-di Ethylamino_π, 2,4] fluorenediazole_3_ylmethoxy) _2_ (4 · fluoro_phenyl) -6- (methanesulfonate -Methyl_amino) _benzofuran_3_carboxylic acid-formamidine; 1 5- [5-(% propylmethyl-amino) _ [1,2,4] thiadiazole- 3-ylmethoxy] -2- (4-fluoro-phenyl) -6_ (methanesulfonyl_fluorenyl-amino group> benzofuran-3-guinic acid-formic acid amine; ^ (2 persons [] Yl] 'yl + methylethylcardiofluorophenyl) isopropoxy-benzofuran_3_carboxylic acid_formamide; 88828. doc -82- 200418452 6- (1-amino-1-methyl-ethyl) -2- (4-fluoroyl_phenyl) _5_isopropoxy_benzofuran-3-carboxylic acid-methyl Hydrazine; 2- [2- (4-fluoro-phenyl) -5_methoxy_3-methylamine formamidine-benzofuran-6-yl] -pyrrolidine-1-carboxylic acid- Formamidine; 6- (3,5-dimethyl-isoxazol-4-yl-2- (4-fluoro-phenyl) _5_methoxy_benzofuran-3-carboxylic acid-ethyl Fluorenamine; 6- (3,5-dimethyl-isohumazol-4-yl) -2- (4-fluoro-phenyl) _5-methoxy_benzofuran-3-carboxylic acid-iso Promethazine; 6- (3,5_dimethyl-isoxazol-4-yl) «4_fluoro group_phenyl) -5_methoxy_benzofuran-3-carboxylic acid-cyclopropane Fluorenamine; 2- (4-fluoro-phenyl) _5_isopropoxy_6_ (5_methyl_2_oxy_oxazolidin-5-yl) _benzofuran-3-carboxylic acid -Formamidine; [2- (4-fluoro-phenyl) -6- (methanesulfonyl_methyl_amino) _3_methylamine formamidine-benzocran-5-yloxy -]-Acetic acid tertiary-butyrate; 2- (4 · fluoro-phenyl) -5-methoxy-6- (5-methyl_2H- [1,2,4] triazol-3- ) -Benzan-3-carboxylic acid-methaneamine; 6- (1-amino-1-methyl-ethyl) _2- (4-fluoro_phenyl) _5_methoxy_benzene and 3-3-carboxylic acid-formamidine; 6- (1-ethylamylamino_1-methyl-ethyl) -2- (4-fluoro-phenyl) methoxy-benzopyran -3 -Amino acid-formic acid amine; [2- (4-Fluoro-phenyl) -6- (methylalanyl-methyl-amino) _3-methylaminofluorenyl-benzofuran- 5-yloxy] -acetic acid; 6- (2,5-dimethyl-2H- [1,2,4] triazol-3-yl) _2- (4-fluoroyl-phenyl) _5_methoxy Benzo-benzofuran-3-carboxylic acid-formamide; 88828. doc -83- 200418452 2- (4-fluoro-phenyl) _6_ (methanesulfonyl-methyl_amino) -5_ (pyrimazole_2_ylmethyllactyl) -benzocran-3-benzyl Acid-formic acid amine; 2- (4-fluoroyl-phenyl) -5-methoxy-6- (4-methyl-2,5-dioxy-imidazol-4-yl) -benzofuran -3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -6- (1-methanesulfonylamino-; μ-methyl-ethyl) methoxy-benzofuran- 3-carboxylic acid-methaneamine; 5- (6-momethyl-pyramine-pyridine-2-ylmethoxy) -6-[(6-bromomethylpyridine-2-ylmethyl) -methane Sulfofluorenyl-amino] -2- (4-fluoro-phenyl) _benzofuran_3-quinic acid-formamidine; 2- [2- (4-fluoro-phenyl) -6- (Methanesulfonyl-methyl-amino) methylaminomethylmethyl-benzofuran-5-yloxymethyl] -pyrimazole-4-carboxylic acid ethyl ester; 2- [2- (4- Fluoro-phenyl) -6- (methanesulfonyl-methyl_amino) _3-methylaminomethanyl-benzo-cran-5-yloxymethyl] ^ Carboxylic acid; 6 -Dimethylamino-2- (4-fluoro-phenyl) -5-methoxybenzofuran-3-carboxylic acid-formamidine; 5-cyanomethoxy-2- (4-fluoro -Phenyl) -6- (methanesulfonyl_methyl_amino) _benzofuran-3-carboxylic acid- Fluorenylamine; 2- (4-fluoro-tolyl) -6- (methanesulfonic acid-methyl-aminomethyl_isoxazol-3-ylmethoxy) -benzofuran_3_ Carboxylic acid_methaneamine; 5- (5-chloro- [1,2,3] pyrimidazol-4-ylmethoxy) _2_ (4_fluoroyl-phenyl) -6- (methylbenzene% Sf group-methyl-amino group) _benzocran_3_metanoic acid-formic acid amine; 2- (4-fluoro group-phenyl) -6- (methanesulfonyl-methyl-amino group) -L-fluorenyl-imidazol-2-ylmethoxy) _benzofuran_3_carboxylic acid_formamidine; 5- (1-benzyl-1'-imidazol-2-ylmethoxy) _2_ (4- Fluoro-phenyl) _6_ (methyl 88828. doc -84- 200418452 burned donkey-methyl-amino) _benzofuran_3_carboxylic acid-formamide; 2- (2,4 · difluoro-phenyl) -6- (3, 5-dimethyl-isoiazole-4 · yl) -5-methoxy-benzofuran-3-carboxylic acid-formamidine; 6_ (3,5-dimethyl-isopurazol-4- ) -2- (4-fluoro-phenyl) -5-oxetazol-4-ylmethoxy) -benzofuran-3-carboxylic acid-formamidine; 5- (5-amino- 411- [1,2,4] triazol-3-ylmethoxy) _2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _benzofurancarboxylate Acid-formamidine; 5- (4-chloro-1-methyl_1H-pyrazol-3-ylmethoxy) -2- (4-fluoro-phenyl) -6- (methanesulfonyl) -Methyl-amino) _benzofurancarboxylic acid-formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methylamino) _5_ (2-pyrazole- 1 · ylethoxy) -benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -5- (1fluorene-imidazol-2-ylmethoxy) -6- (Methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 6- (2,5-dioxy-imidazolidine_4-yl) -2- (4- Fluoro-phenyl) -5-methoxy_benzofuran-3-carboxylic acid-formamidine; 5- (3,5-dimethyl-isoxazole) 4-yl) _2- (4-fluoro-phenyl) _6_methanesulfonyl_fluorenylamino-benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl)- 6- (methanesulfonyl-methyl_amino) thiazole—-2-yl · ethoxy) -benzofuranic acid · amine formate; 6- (3,5-dimethyl · isoxazole -4-yl) -2- (4-fluoro-phenyl) -5- (5-methyl_isopurazol-3-ylmethoxy) _benzofurancarboxylic acid-formamidine; 6- (3,5-Dimethylisoisnazole_4-yl) -2- (4-fluoro-phenyl)> 5- (thiazole_2_ylmethoxy) _benzofuran-3-carboxylic acid -Formamidine; 6-Ethyl-2 · (4-fluoro-phenyl) _benzofuran_3 • Metabolic acid_formamidine; 88828. doc -85-200418452 2- (4-Fluoro-phenyl) -5- (2-Ethyl-2 -methyl-propoxy) -6- (methylbenzene g-methyl-amino-amino ) -Benzofuran-3-metanoic acid-formamidine; 5-ethyl ethylamine methyldonylmethoxy-2- (4-fluoro-phenyl) -6- (methylsulfonylmethyl- Methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 6- (3,5 -monomethyl-iso-indo-4 -yl) -5 -ethoxy-2- (4 -Gas-phenyl) _benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -5- (Oxazol-2-ylamine formamylmethoxy) -benzofuran_3_metanoic acid-formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl) -Amino) · 5-([1,3,4] thia-fluoren-2-ylaminemethylamidinomethoxy) _benzocarbamic acid · methaneamine; 5-[(4,5 -Dimethyl-thiazole_2 · ylaminomethylmethyl) -methoxy] _2- (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) _benzofuran _3_carboxylic acid-formamidine; 5-cyclopropyl-2- (4-fluoro · phenyl) -6-methanesulfonylamino-benzofuran-3-carboxylic acid-formamidine; 5- [2- (4-cyano-hexahydropyridine_buyl) _ethoxybu 6- (3,5-dimethyl- Iodine-4-yl) -2- (4-fluoro group «winter group) _benzobenan_3_meta-acid-methanamine; 2- (4-fluoro-phenyl) -6-methane Sulfonyl_amino_5_pyrimin-2-yl-benzofuran-3-metanoic acid-formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-formyl) -Amino group) _5_methylaminomethylmethylmethoxy-benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoroyl-phenyl) _5- (1-hydroxymethyl_ Cyclopropylmethoxy) _6 _ [(丨 _Hydroxymethyl-cyclopropylmethyl) -methanesulfonyl group_amino group &gt; Benzoanan_3_metanoic acid-formamidine; 88828. doc -86-2 ^ 0418452 6-diethylamino-5-ethoxy-2- (4-fluoro-phenyl) -benzofuran-3-carboxylic acid-formamidine; 5-amine formamide Fluorenylmethoxy_2_ (4-fluoro-phenyl) -6- (methanesulfonyl-methyl-amino) -benzofuran-3-carboxylic acid-formamidine; 5_〇 (3 , 5-Dimethyl ^ pyrazole small ethoxy fluorenyl_phenyl) -6- (methanesulfonyl-methyl-amino) _benzofurancarboxylic acid-formamidine; 2- (4-Fluoro-phenyl) -5-furan-2-yl-6-methanesulfonylamino-benzofuran-3-guinic acid-formamidine; 6- (3,5-difluorenyl) _Isopurazol_4-yl) -2- (4-fluoro-phenyl) -5- (1-methyl-1H-tetrazol-5-ylmethoxy) -benzofurancarboxylic acid-methyl Amidoamine; 5-cyclopropylmethoxy-6- (3,5-dimethyl_isopurazol_4_yl) -2- (4-fluoro-phenyl) -benzocran-3 -Chloric acid-formic acid amine; 6- (3,5-dimethyl-isoxazole_4_yl) _5_ (3,5-dimethyl_isoxazole_4_ylmethoxy) -2- (4-Fluoro-phenyl) _benzofuran_3_carboxylic acid_formamide; 2- (4-fluoro-phenyl) -5-methoxy_6_ (5-methyl- [1 , 3,4] humidazol-2-yl) -benzoic acid-3-chinic acid-formic acid amine; 6- (3-cyano-4-hydroxy-2-oxy-2,5- Dihydro-pyrrole-1-ylmethyl) -2- (4-fluoro-phenyl) -5-methoxy-benzofuran_3-carboxylic acid · methaneamine; 4-chloro-6- [Ethyl- (2-methoxy_ethylfluorenyl) &gt; aminofluoro_phenyl) -5-methoxy-benzocrean_3_guinealyl-formamidine; 6- (3, 5-dimethyl-isoindazolyl) -2_ (4-fluoro-phenyl) -5- (2_morpholin-4-ylethoxy) _benzofuran_3-carboxylic acid_methyl Amidoamine; 6- (3,5-dimethyl-isoazazolyl) _2_ (4-fluoro. Phenyl) -5_ (3_hexahydropyridin-1-ylpropoxy) _benzofurancarboxylic acid_formamidine; 88828. doc -87.   200418452 2- (4-Fluoro-phenyl) _5- (thiazol-4-ylmethoxybenzobenzofurancarboxylic acid_formamidine; 2- (4-fluoro-phenyl) -6- (2 -Hydroxy-ethylamyl) _5_methoxy-benzofuran-3-carboxylic acid-methaneamine; 5-% propyl-2- (4-fluoro-phenyl) -6- (methanesulfonyl) -Methyl-amino-p-benzofuran-3-carboxylic acid-methaneamine; 2- (4-fluoro-phenyl) -5-¾yl-6-[(2- # Amino-propyl ) _Methanesulfonic acid group_amino group] -benzofuran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -6-[(2-hydroxy-propyl) _methane Sulfofluorenyl-amino] -5-methoxy-benzofuran-3-carboxylic acid-formamidine; 6- (1-ethylfluorenyl-pyrrolidin-2-yl) -5-ethyl-2- (4-Fluoro-phenyl) · benzofuran-3-carboxylic acid-methaneamine; 2- (4-fluoro-benzyl) -6-methylpyramine®-aminoamine 5- (tetrahydro- Crean-2-yl) _benzofuran-3-carboxylic acid-methaneamine; 2- (4-fluoroyl-phenyl) -5 -methoxy-6- (tetrahydro-crean-3- ) -Benzopyran-3-carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -6- (methylsulfonyl-methoxymethyl_amino) _5-propoxy Benzyl-benzopyran-3-metanoic acid-methdonine; 2- (4-fluoroyl-phenyl) -5-hydroxy-6- (methanesulfonate Fluorenyl-methoxymethyl_amino) _benzofuran-3-carboxylic acid-formamidine; 2- (4-fluorofluoro-tolyl) -6-methylsulfonylamino-5-propanyl Oxy-benzocaran-3-carboxylic acid-formamidine; 5- (4-cyano-benzyloxy) -2- (4-fluoro-phenyl) -6- (methylsulfanyl- Methoxymethyl-amino) -benzofuran-3-carboxylic acid-formamidine; 88828. doc -88-200418452 5- (3-cyano-etooxy) _2_ (4-fluoro-phenyl) -6- (methanesulfonyl-methoxymethyl-amino) -benzofuran_3 _Acetyl-methanamine; 6- (1-cyclopropanecarboxy-pyrrolidin-2-yl) -2- (4-fluoroyl-phenyl) -5-isopropoxy-benzofuran-3- Carboxylic acid-formamidine; 2- (4-fluoro-phenyl) -5-methoxy-6- [1,3,4] humidazol-2-yl-benzocran-3-carboxy Acid-formamidine; 2- (4-fluoro-phenyl) -6- (methanesulfonyl-methoxymethyl_amino) _5_P phenphen-2-yl-benzofurancarboxylic acid-formyl Hydrazine; and 2_ (4-fluoro-phenyl) _6_ji-2- (4-fluoro-phenyl) _2_hydroxy-ethyl] _methane ~ donyl-amino} _5_hydroxy-benzo Furan_3_carboxylic acid-formamidine; and pharmaceutically acceptable salts thereof. 15 · The composition according to item 13 of the scope of patent application, which further includes at least one supplementary agent selected from the group consisting of: · interferon, polyethylene glycol-based interferon, rabavirin, protease inhibition Agents, polymerase inhibitors, small interfering RNA compounds, antisense compounds, nucleotide analogs, nucleoside analogs, immunoglobulins, immunomodulators, hepatoprotective agents, anti-inflammatory drugs, antibiotics, antiviral agents and Anti-infective compounds. 16.  A pharmaceutical composition for preventing or treating a hepatitis C infection and a disease associated with such infection in a living host having the infection, comprising a therapeutically effective amount of a compound according to item 1 of the scope of the patent application. 17. The pharmaceutical composition according to item 6 of the patent application scope, wherein the living host is a mammal. U. The pharmaceutical composition according to item 16 of the application, wherein the living host is human. 88828. doc -89- 200418452 19.  20.  twenty one.  twenty two.  twenty three.  twenty four.   The pharmaceutical composition according to item 18 of the patent application park, wherein the compound is orally administered. The pharmaceutical composition according to item 19 of the application, wherein the oral dosage range of the compound is about 0. 05 to about 100 mg / kg. The pharmaceutical composition according to claim 16 in which the compound is administered orally 1 to 4 times a day. The pharmaceutical composition according to item 16 of the application, wherein the compound is combined with at least one other biologically active agent simultaneously or sequentially. The pharmaceutical composition according to claim 22 of the patent scope, wherein the other biologically active agent is selected from the group consisting of: interferon, polyethylene glycol interferon, rapavalin, protease inhibitor, polymerization Enzyme inhibitors, small interfering RNA compounds, antisense compounds, nucleotide analogs, nuclear analogs, immunoglobulins, immunomodulators, hepatoprotective agents, anti-inflammatory drugs, antibiotics, antivirals and anti-infective compounds . A pharmaceutical composition for preventing or treating a hepatitis C infection and a disease associated with such infection in a living host having the infection, comprising a therapeutically effective amount of a compound selected from the group consisting of: 5A Oxy-2-phenyl-benzofuran-3-carboxylic acid formamide and 5-hydroxy-2-phenyl-benzofuran-3-carboxylic acid formamide. 88828. doc -90- 200418452 柒. Designated representative map: (1) The designated representative map of this case is: (none) (II) Brief description of the component representative symbols of this representative map: 捌 If there is a chemical formula in this case, please disclose the best display invention Chemical formula of characteristics: 88828.doc