TW301654B - - Google Patents

Description

A 6 B6 V. Description of the invention (f) _ The present invention relates to a compound that has affinity for the recipient of δ-QPiQid (anamorphine-like synthetic anesthetic). < 5 -QPiaid receptors are related to analgesia, immunity, circulation system (especially blood pressure), and the receptors have highly selective ligands. (ligand) can be used as analgesics, immunosuppressants, immune Enhancers, antihypertensive agents and other drugs. Printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) δ-opioid receptors have the above-mentioned various pharmacological effects, and compounds with high selectivity for this receptor are expected to be Used as analgesics, immunosuppressants, immune enhancers, and blood pressure lowering agents. However, with the exception of the Semenite compounds, complexes with high selectivity for delta receptors have not yet been discovered. The disadvantages of the Semenite compound are that it is not easy to pass through the blood brain gate and is easily decomposed by the Semena enzyme in the body, so it is difficult to develop the above-mentioned drugs. The reason for this is that people are eager to pursue. For agonists with high selectivity for S receptors (also known as agonists or agents, agents), antagonists. So far, Portghese et al. Have discovered a highly selective antagonist to delta-opioid, NT I (P.S. Portoghese e t a 1., J. Med. Chem., Vo 1. 31, No. 2, 1988). This NTI is a biological test. Unlike peptides, it can solve the problem of passing through the blood brain gate and being decomposed by the enzyme. However, since this NTI is synthesized using Naltrexone as a raw material, the manufacturing cost is high, and Naltrexone is synthesized by the anesthetic drug Thebaine, so it is difficult to obtain, There are really many problems. g In addition, the three receptor agonists are known to have DADLE, DPDPE and other winners, but the biological squad and the better selection have not yet been developed. The purpose of the present invention is to provide an inexpensive complex (agonist, antagonist) that can be expected to obtain the above-mentioned pharmacological effects on the S-accepted paper, which can be expected to obtain the national standard (CNS) A 4 standard (210x297 Mm) A6 _____B_6__ printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of invention-High affinity and selectivity, and its synthesis can be carried out without the use of anesthetics as its raw material. Through the blood-brain barrier, it is also highly stable to peptide enzymes. In order to achieve the above objectives, the present invention has the following configuration. The present invention is an indole derivative or a pharmacologically acceptable salt thereof. The vermiculite derivative can be represented by the general formula (1)

/ ν Η R4 ^^ or2 [In the formula, 1 ^ is an alkyl group having 1 to 5 carbon atoms, a cycloalkylalkyl group having 4 to 7 carbon atoms, a cycloalkenyl alkyl group having 5 to 7 atoms, and a master number 7 ~ 14 aralkyl group, trans alkenyl group with sulfo number 4 ~ 5, allyl group, furan-2-yl alkyl group with sulfo number 1 ~ 5, 晜 -2-yl alkyl group with 1 ~ 5 number , Ethoxycarbonyl, trifluoroethane gas carbonyl, benzyl gas glass, alkane groups with a number of 1 ~ 5, alkane carbonyl groups with a number of 7 ~ 14, arylcarbonyl groups with 2-furfural, thiophan-2-carbonyl, sulfone number 4 ~ 7 naphthenic carbonyl group, alkenyl carboxyl group with 3 to 8 or anisaldehyde; R * is hydrogen, alkyl group 1 to 3, benzyl or sulfone 1 to 5 alkylase; R3 is argon , Fluorine, gas, bromine, nitro, or alkyl groups of 1 to 5; hydrogen, alkyl groups of 1 to 5, benzyl or phenyl; Re is hydrogen, hydroxyl or alkyl groups of 1 to 5 Aldehyde base, and, the general formula (1) includes (+) hydrazone, (a) body, (±) body]. The size of this paper is based on the Chinese B House Standard (CNS) 4 specifications (210x297 g *) (please read the precautions on the back before filling this page)-Binding · Order · Line-A 6 B6 Ministry of Economic Affairs Central Standards Bureau Printed by Industrial and Consumer Cooperatives-V. Description of the invention (>)-Pharmacologically suitable salts can be exemplified as follows, namely: inorganic acid salts such as hydrochloride, sulfate, hydrobromide, phosphate, etc .; or, acetate , Organic acid salts such as lactate, methanesulfonate, P-toluenesulfonate, phthalate, fumarate, maleate, glutarate, and S silicate. Of course it is not limited to this. The 1 in the general formula (1) can be exemplified as follows: Di: methyl, ethyl, propyl, butyl, pentyl, ethylpropylmethyl, cyclobutylmethyl, ethylpentylmethyl, cyclohexylmethyl, cyclopentene Methyl, hexenylmethyl, allyl, 2-furanmethyl, 2-pyridyl, trans-2-butenyl, cyclopropylcarbonyl, 2,2,2-trichloroethoxy Carbonyl, ethyleneoxycarbonyl; 1? * Can be exemplified as follows: hydrogen, methyl, ethyl, propyl, benzyl, acetyl, propyl, butyl, pentyl; R3: hydrogen, fluorine, gas , Bromine, nitro, methyl, ethyl, propyl, butyl, pentyl; R * is: hydrogen, methyl, ethyl, propyl, butyl, pentyl, phenyl, benzyl; Ra is : Hydrogen, hydroxyl, acetaldehydeoxy, propyl gas, butyl gas, valeraldehyde, etc. Among them, the preferred ones are: R, methyl, cyclopropylmethyl, cyclobutylmethyl, allyl, 2-furanmethyl, cyclopropylcarbonyl, 2,2, 2-trifluoroethoxycarbonyl, ethylene Oxycarbonyl; R2 is hydrogen, methyl, acetaldehyde, benzyl; R3 is hydrogen, fluorine, chlorine, bromine, methyl; R * is hydrogen, methyl, benzyl; R * is hydrogen, hydroxyl, acetyl Oxygen and so on. In the compound of the general formula (1) of the present invention, 1 ^ is a methyl group and R2, R3, R *, Rs is a compound (Formula 2) which is named as follows, namely: 2-methyl-4act- (3-hydroxyphenyl ) -L, 2,3,4,4a, 5, ll, lla / 8 -octahydro-hexa H-indng [2, 3-g] isoquinoline. (Please read the precautions on the back before filling in this page) Install & Order-Line. This paper scale is used in the middle and sleepy home like standard (CNS) A 4 specifications (210x297 male dragon) -6-V. Invention description ( ) Η A 6 Β6

(Please read the precautions on the back before writing this page) According to the above nomenclature, the representative compounds of the present invention can be exemplified as follows, but of course not limited to these compounds, namely: 2-methyl-4aa (3-Hydroxyphenyl) -l, 2,3,4,4a, 5, ll, lla / G-octahydro-6H-indigo [2,3-g] isoquinoline, 2-methyl- 4aa- (3-methylphenyl) -1,2,3,4,4 &, 5,11,11 ug / 3-octahydro-6 {1-ind0dec [2,3-g] iso Quinoline, 2-allyl-4aa- (3-hydroxyphenyl) -1,2,3,4,4a, 5,11,113 / 3-octahydro-6}]-115 丨 Beta [2,3 -璟] Isosleep, 2-isopropyl-4aa- (3-methylphenyl) -1,2,3,4,43,5,11,113 / 5-octahydro-6 ^! -Ind Ocular [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -1,2,3,4,43,5,11,113 / 9-octa Hydrogen-6} 1-indo [2,31] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -1,2,3,4, 43,5,11,113 / 8-octahydro-6}]-ind 11 deca [2,3-carbo] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -1,2,3,4,43, 5,11,113 / 3-octahydro-6 ^ 1 -indino [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -l, 2,3,4 , 4a, 5, ll, lla / 3 -octazo-6H-B5 丨 Bite In addition, [2,3-g] the size of the different sleeping paper is used in the Chinese National Standard (CNS) A4 specification (210X297 public version-printed by the Employees ’Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs V. 3〇1C〇4 A6 a Description of the invention () Printed porphyrin, 2-phenylethyl-4aa- (3-hydroxyphenyl) -l, 2,3,4,4a, 5, ll, lla octahydro- [ 2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -1,2,3,4,43,5,11,11 / 3 / 3-octahydro-611 -Indino [2,3-g] isoquinoline, -2-methyl-4act- (3-hydroxyphenyl) -1,2,3,4, ", 5,11,1101 / 9-octa Hydrogen-6-methyl-indo [2,31] isoquinoline, 2-methyl-4 aa-(3 -methylphenyl) -1, 2, 3, 4, 4 a, 5, 11 , 11 a / 3 -octahydro-6-methyl-indo [2,3-g] isoquinoline, 2-chenpropylmethyl-4act-(3-hydroxyphenyl) -1,2, 3,4,4a, 5,11, lla / 3-octahydro-6-methyl-indolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methyl Gas phenyl) -1,2,3,4,43,5,11,113 / 9-octahydro-6-methyl-ind [1deco [2,3-g] isoquinoline, 2-benzyl Yl-4aa- (3-hydroxyphenyl) -1,2,3,4,4a, 5, ll, lla / 9-octahydro. 4-methyl-indazolo [2,3-g] isoquinoline, 2-benzyl-43〇 (-(3-methoxyphenyl) -1,2,3,4,43,5,11 , 11 & / 3-octahydro-6-methyl-indodo [2,3-g] isoquinoline, 2-phenethyl-4act- (3-hydroxyphenyl) -1, 2,3 , 4,4a, 5, ll, lla / 3-octahydro-6-methyl-p5Ug and [2,3 -g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -1,2,3,4,4 3,5,11,113; 9-octahydro-6-methyl-indoxo [2,3-§] isoquino, 2-allyl-4aa- (3 -Hydroxyphenyl) -l, 2,3,4,4a, 5, ll, lla / S-octahydro-6-methyl-indo- [2,3-g] iso-line ^ isopropyl- 4 a α-(3-methylphenyl) -l, 2,3,4,4a, 5, ll, lla) ^ k hydrogen-6-methyl-indox [2,3-g] isoquin Porphyrin, 2-methyl-4aa- (3-hydroxyphenyl) -9-methyl-1,2,3,4,43,5,11,1] ^ / 3-octahydro-6} 1-ind Benzo [2,3- |] isoquinoline, 2-methyl-4a〇t- (3-methoxyphenyl) -9-methyl-1,2,3,4, 4a, 5,11,113 / 3-octahydro-611-indo [2,3-2] isoquinoline, 2-benzyl- (please read the precautions on the back before filling in this page) Binding · Order 'Line · This paper is for standard use China National Standards (CNS) A 4 specifications (210x297 mm) 8 V. Description of invention () A 6 B6 Printed 48〇 (-(3-hydroxyphenyl) -9-methyl-1,2,3,4,4, 5,11,113 / 3-octahydro-6H- Indo [2,3-g] isobrinoline, 2-benzyl-4aa- (3-methoxyphenyl) -9-methyl-1,2,3,4,43,5,11,11 &; / 9-Octahydro-611- vermizo [2,3-g] isoquinoline,. 2-phenethyl-4act- (3-hydroxyphenyl) -9-methyl -1,2,3,4,43,5,11,113 call-octahydro-611-indagono [2. 3- 垤] isoquinine, 2-phenethyl-4aa- (3-methylphenyl) -9-methyl-1,2,3,4,4a, 5, ll, lla Ling-octahydro- 6H-indazolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4a〇t- (3-hydroxyphenyl) -9-methyl-1,2,3,4,4a , 5, ll, 11a lu-octahydro-6H-indazolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -9-methyl -1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline, 2-allyl-4aα- (3-hydroxyl Phenyl) -9-methyl-l, 2,3,4,4a, 5, ll, lla / Q-. Octahydro-6H-indino [2,3-g] isoquinoline, 2-allyl-4act- (3-methoxyphenyl) -9-methyl-1,2,3,4,43 , 5,11,113 / 8-octahydro-611-worm eye [2,3 · ^] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -9-methyl-1, 2,3,4,4a, 5,11,113 ling-octahydro-6-methyl-indo- [2,3_8] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -9-methyl-1,2,3,4,4 a, 5,11, 11a cold-octahydro-6-methyl-〇5 Shuo [2,3-g] isoquino, 2- Allyl-4a〇t- (3-hydroxyphenyl) -9-methyl-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-P? 丨Indo [2,3-g] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -9-methyl-1, 2,3,4,4a, 5, ll, lU Zhao-octahydro-6-methyl-l¾ 丨 Bg- [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aα- (3-hydroxyphenyl) -9-methyl-1, 2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-lumbo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3 -Methoxy (please read the precautions on the back before filling the nest page) Binding 'Thread · Line · The size of this paper uses the Chinese National Standard (CNS) A 4 specifications (210x297 g) 9 Staff consumption of the Central Bureau of Standards of the Ministry of Economic Affairs A6 _ B6_ printed by the cooperative Description ()-phenyl) -9-methyl-1,2, 3, 4, 4a, 5, 11, 11a / 3 -octahydro-6-methyl-indo [2,3-g] Isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -9-methyl-1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl-ind | ^ (〔2,3-dan) isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -9-methyl-1,2,3, 4,43,5,11,113 / 9-octahydro-6-methyl-di-112- [2,3-pyr] isosialin, 2-phenethyl-4aa- (3-hydroxyphenyl) -9-methyl-1,2, 3,4, 4a, 5, ll, lla lu-octahydro-6-methyl-indeno [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methylphenyl) -9-methyl-l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-6-methyl-05indo [2,3-g] isoquinoline, 2-methyl Yl-4aa-(3-hydroxyphenyl) -9-bromo-1,2,3,4,43,5,11,113 /?-Octahydro-611-indazolo [2,3-g] isoquinoline , 2-methyl-4aa- (3-methoxyphenyl) -9-bromo-1,2,3,4,43,5,11,11 & Lu-octahydro-611-ind 112 [2, 31] Isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -9-bromo-1, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-B5 | US benzo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -9-bromo-1,2, 3,4,4a, 5, 11, lla / 3 -Octahydro- 6H- Iso [2,3-g] isoquinoline, 2-phenethyl-4act- (3-hydroxyphenyl) -9-bromo-1,2,3,4,4 &, 5,11,113 / 3-octahydro-6 ^ indazolo [2,31] isoquinoline, 2-phenethyl-4ac (-(3-methylphenyl) -9-bromo-1,2,3,4, 43 , 5,11,113 / 5-Octahydro-6 {1-Indino [2,3- 苢] isoquinoline, 2-cyclopropylmethyl-4act- (3-hydroxyphenyl) -9-bromo- l, 2,3,4,4a, 5, U, lla / S-octahydro-6H-indPi [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3- Methyl phenyl) -9-bromo-l, 2,3,4,4a, 5, ll, lla; S-octahydro-6H-D? Dolo [2,3-g] isoquinoline, 2 -Allyl-4aa- (3-hydroxyphenyl) -9-bromo-1,2,3,4,43,5,11,113-octahydro-6 {1-ind118 [(Please first Read the precautions on the back and fill in the nest page) Binding · Order _ Line-This paper standard is universal Chinese National Standard (CNS) A 4 specifications (210x297 male dragon) 10 3u2C04 A 6 B 6 Employee Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs Print V. Description of Invention ()-.  2. 3-g] isoquinoline, 2-allyl-4aa- (3-methylphenyl) -9-bromo-1, 2,3,4,43,5,11,113 /?-Octahydro- 6} 1-Indo [2,3-2] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -9-bromo-1,2,3,4,4a, 5, ll , Lla / 3-octahydro-6-methyl-indDg- [2,3-g] isoquinoline, 2-methyl-4aa-(3-methylphenyl) -9-bromo-1,2 , 3,4,43,5,11,113 / 9-octahydro-6-methyl-ind HS- [2,3-g] isoquinoline, 2-allyl-4aa- (3-hydroxybenzene Group) -9-bromo-1,2, 3, 4, 4a, 5, 11, 11a / 3-octahydro-6-methyl-indeno [2,3-g] isoquinoline, 2-allyl Yl-4act- (3-methoxyphenyl) -9-bromo-1,2, 3,4,4a, 5, ll, lla / S -octahydro-6-methyl-indodecene [2, 3-g] Isoquinoline, 2-cyclopropylmethyl-4act- (3-hydroxyphenyl) -9-bromo-1,2,3,4,43,5,11,113 / 8-octahydro-6 -Methyl-11? 丨 Baso 〔2,3- 玨〕 _Iso_Lin, 2-Cyclopropylmethyl-4act- (3-methoxyphenyl) -9-bromo-1,2,3, 4,4a, 5,11,113 / 3-octahydro-6-methyl-indodecano [2,3-Ju] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -9- Bromo-1,2,3,4,4a, 5, ll, lla / G-octahydro-6-methyl-indolo [2,3-g] isoquinoline, 2-benzyl-4aa- ( 3-methylphenyl) -9-bromo-1,2,3,4,43,5,1 1,11 & / 3-octahydro-6-methyl-indo [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -9-bromo-1 , 2,3,4,4a, 5,11,11a Lu-octahydro-6-methyl-indolo [2. 3-g] isoquinoline, 2-phenethyl-4aa- (3-methylphenyl) -9-bromo-1,2,3,4,43,5,11,113 / 3-octahydro-6- Methyl-indazolo [2,3-glycoside] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -9-gas-1,2,3,4, 4a, 5,11, lla / S-octahydro-6H-d5 | US and [2,3-g] isoblister, 2-methyl-4aa- (3-methoxyphenyl) -9-chloro-1, 2,3, 4,43,5,11,113 / 8-octahydro-6} 1 -0¾ 丨 11decor [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -9 The paper size is used in Chinese National Standards (CNS) Grade 4 (210x297 male dragon) -11-(please read the precautions on the back before filling this page).  Order_ ^^ 1664 A 6 B6 Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention ()--Atmosphere-1. 2,3,4,43,5,11,113 / 3-octahydro-6} 1-worm 11 deca [2,3-ming] isoquinoline, 2-benzyl-4aa- (3-methyl gas Phenyl) -9-ammonia-1,2,3,4,4a, 5,11,113 / 3-octahydro-511-tonoquino [2,3-jun] isoquinoline, 2-phenethyl-4aa -(3-hydroxyphenyl) -9-chloro-l, 2, 3, 4, 4a, 5, ll, lla / S-octa. Hydrogen-6H-P51 ^ [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methylphenyl) -9-chloro-1,2,3,4,43,5 , 11,113 / 9-octahydro-6 {1-indazolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -9-gas-1, 2,3,4,43,5,11,113 ling-octahydro-611-indolo [2,3-min] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxybenzene Group) -9-nitrogen-1,2,3, 4,4 &, 5,11,113-octahydro-611-ind 11-deca [2,3-§] isoquinoline, 2-allyl-4aa -(3-hydroxyphenyl) -9-nitro-l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-6H-indAS- [2,3-g] isoquinoline, 2-allyl-. 4aa- (3-methoxyphenyl) -9-gas-1,2,3,4,43,5,11,113 / 8-octahydro-611-05 | Iso [2,3-g] isoquinine , 2-methyl-4aa- (3-pyridyl) -9-nitrogen-1,2,3,4,4a, 5, ll, lla0_octahydro-6-methyl-indazole (2, 3-g] Isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -9-gas-1,2,3,4, 43,5,11,113 / 3-octahydro-6-methyl -Ind 11 «(〔2,31〕 isoquino, 2-allyl-4aa- (3-hydroxyphenyl) -9-chloro-1,2,3,4,4a, 5, ll, lla ; S-octahydro-6-methyl-mama sor [2,3-g] isoquino, 2-allyl-4aa-(3-methyl gas phenyl) -9-atmosphere-1,2 , 3,4,43,5,11,113 / 3-octahydro-6-methyl-ind08 [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3- Hydroxyphenyl) -9-nitro-1,2,3,4,4a, 5,11, lla / 9-octahydro-6-methyl-indolo [2,3-g] isoquinoline, 2 -Cyclopropylmethyl-4aa- (3-methylphenyl) -9-chloro-1,2, 3, 4, 4a, 5, 11,1 la / S -octahydro-6-methyl-indene Showa (Please read the precautions on the back before filling in this page) This paper is used in China National Standards (CNS) A 4 specifications (210x297 g)-12-A6 printed by Beigong Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs B6_ V. Description of the invention ()-〔2,3-g〕 isoquine , 2-benzyl-4aa- (3-hydroxyphenyl) -9-gas-1,2,3,4,43,5,11,113zhao-octa-6-methyl-11? 丨 112 and 〔2,3- £. 〕 Isophthaloline, 2-benzyl-4act- (3-methylphenyl) -9-gas-1,2,3,4,4a, 5, ll, lla /?-Octahydro-6-methyl -Indo [2,3-g] isoquinoline, 2-phenethyl-4a〇c- (3-hydroxyphenyl) -9-gas-1,2,3,4,4a, 5, ll ， Lla / 3-octahydro-6-methyl-P? 丨 Floating [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methylphenyl) -9-ambient- 1,2,3,4, 4a, 5,11, lla / S-octahydro-6-methyl-P5 Shun- [2,3-g] isoquinoline, 2-methyl-4aa- (3 -Hydroxyphenyl) -7-fluoro-1,2,3,4,4 3,5,11,113 / 8-octahydro-6? 1-worm 11 deca [2,3-§] isoquinoline , 2-methyl-4aa- (3-methoxyphenyl) -7-fluoro-1, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indazolo [2, 3-g] isoquino, 2-benzyl-4aa- (3-hydroxyphenyl) -7-fluoro-1, 2,3,4,4a, 5, ll, lla / Q-octahydro-6H- D¾ 丨 ½ [2,3-g] isoquinoline, 2-benzyl-4aα- (3-methylphenyl) -7-fluoro-1,2,3,4,43,5,11,113 / 9 -Octahydro-6} 1-ind ^ [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -7-fluoro-1,2,3,4 , 43,5,11,118> 3-octahydro-6 [}-1 ^ 丨 biocclusion [2,3-§] iso-command, 2-phenethyl-4aa- (3-methoxyphenyl)- 7-fluoro-l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6H-indBg (〔2,3-g 〕 Isoquine. Porphyrin, 2-cyclopropylmethyl-4acc- (3-hydroxyphenyl) -7-fluoro-1,2,3,4,43,5,11,113-octahydro-6} 2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methylphenyl) -7-fluoro-1,2,3,4,43,5,11,113 / 3 -Octahydro-6} 1-worms 0 and [2,3-g] isomuline, 2-isopropyl- 4aa- (3-xiangphenyl) -7-fluoro-1,2,3,4 , 43,5,11,113 / 9-octahydro-61 ^ indo [2,3-min] isoquinoline, 2-allyl-4aa- (3-methylphenyl) -7-fluoro-1 , 2,3,4,4a, 5,11, (please read the precautions on the back before filling in this page) This paper uses Chinese National Standard (CNS) A 4 specifications (210X297 male dragon) -13-A6 B6 V. Description of the invention (printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs lla / 9-octahydro-6H-l «Ug and [2,3-g] isoquinoline, 2-methyl-4aa- (3- Hydroxyphenyl) -7-fluoro-1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl-indo [2,3-g] isoquinoline, 2 -Methyl-4aa- (3-methylphenyl) -7-fluoro-1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl-indo [2,3 -g] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -7-silver-1,2,3,4,4a, 5, ll, lla / 8-octahydro-6- Methyl-indozo [2,3-g] iso Quinoline, 2-allyl-4aa- (3-methylphenyl) -7-fluoro-1,2,3,4,4a, 5,11,113 /?-Octahydro-6-methyl- Indolo [2,3-quin] isoquinoline, 2-cyclopropylmethyl-4a〇t- (3-hydroxyphenyl) -7-fluoro-1,2,3,4,4a, 5, ll, lla Zhao-octahydro-6-methyl-indo [2,3-g] isoquinoline, 2-chenpropylmethyl-4aa- (3-methoxyphenyl) -7-fluoro- l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6-methyl-indo- [2,3-g] isoquinoline, 2-benzyl-4aa- (3- Hydroxyphenyl > -7-fluoro-1,2,3,4,43,5,11,1] ^ / 3-octahydro-6-methyl-indo [2,3-g] isoquine Porphyrin, 2-benzyl-4acc- (3-methylphenyl) -7-fluoro-1,2,3,4,43 ,. 5,11,118 / 3-octahydro-6-methyl-indoquinone [2,3-2] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -7-fluoro -1,2,3,4,43,5,11,113 / 8-octahydro-6-methyl-indolo [2,3-ming] isoquinoline, 2-phenethyl-4δα- ( 3-methyl gas phenyl) -7-fluoro-l, 2,3,4,4a, 5, ll, lla / 8-octahydro-6-methyl-hetero [2,3-g] iso Quinoline, 2-methyl-4a α-(3 -xiangphenyl) -9 -fluoro-1,2,3,4,4 a, 5, 11, 11 a / 3 -octahydro-6 Η -〇 5 Shun [2,3-g] isoquinoline, 2-methyl-4aa- (3-methylphenyl) -9-fluoro-1,2,3,4,43,5,11,118 / 3 -Octahydro-611-indolo [2,3-2] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -9-fluoro-1,2,3,4,4a, 5 , 11,118 / 3-octahydro-6! 1-115 丨 Isoquino [2,3-8] isoquinoline, 2-benzyl-14 (please read the precautions on the back before filling in this page) Printed A6 _B_6_ with the China National Standard (CNS) A4 specification (210x297 g *) Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs V. Description of invention ()-48〇 (-(3-methylphenyl) -9-fluoro -1,2,3,4,43,5,11,113 / 3-octahydro-6H-D5I ^ [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl ) -9-fluoro-1, 2, 3, 4,43,5,11,113 / 0-octahydro-6 hepatic indole [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -9-fluoro- 1, 2,3,4,43,5,11,113 / 3-octahydro-611-indo [2,3-ju] isoquinoline, 2-chenpropylmethyl-4act- (3-hydroxybenzene Radicals) -9-fluoro-1,2,3,4,4a, 5, ll, lla / 3-octahydro- δΗ-Βξ 丨 Beta [2,3-g] Iso-Lu, 2-cyclopropyl Methyl-4act- (3-methylphenyl) -9-fluoro-1,2,3,4,4a, 5, ll, lla / 9 -octahydro-6H-D? Bu eye and [2,3 -g〕 · Isosleep, 2-pyropropyl-4aa- (3-hydroxyphenyl) -9-fluoro-1,2,3,4,43,5,11,113 / 8-octahydro-6} 1 -Indo [2,3-g] isoquinoline, 2-allyl-4aa- (3-methylphenyl) -9-fluoro-1,2,3,4,43,5,11, 113> 3-octahydro-6} 1-ind02 [2,3-§] isoquinoline, 2-methyl-4 & 〇1- (3-hydroxyphenyl) -9-fluoro-1,2 , 3,4,4 &, 5,11, lla ^ S-octahydro-6-methyl-indeno [2,3-g] isoquinoline, 2-methyl-4a α- (3- Methylphenyl) -9-fluoro-1,2,3,4,43,5,11,113 > 3-octahydro-6-methyl-indo [2,3-g] isoquinoline, 2 -Allyl-4aa- (3-hydroxyphenyl) -9-fluoro-1,2, 3, 4, 4a, 5, 11,1 la / 3 -octahydro-6-methyl-indazolo [ 2,3-g] isoquinoline, 2-ene Yl-4act- (3-methoxyphenyl) -9-fluoro-1,2,3,4,43,5,11,113; 8-octahydro-6-methyl-indo 115 [2,3 -Dan] isoquinoline, 2-cyclopropylmethyl-4act- (3-hydroxyphenyl) -9-fluoro-1,2,3,4,43,5,11,113 / 3-octahydro-6- Methyl-indolo [2,3-ming] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -9-fluoro-1,2,3,4, 43, 5,11,113-octahydro-6-methyl-indo [2,3- 苕] iso-line, 2-benzyl-4aa- (3-hydroxyphenyl) -9-fluoro-1, 2,3,4,4a, 5, ll, lla (please read the precautions on the back before filling in this page) Binding-Order-This paper size is easy to use China National Standards (CNS) A 4 specifications (210x297) ¢ 15 A 6 B6 Printed by the Consumer Standardization Bureau of the Central Bureau of Economic Affairs of the Ministry of Economy V. Invention Instructions ()-.  / 3-octahydro-6-methyl-ind P2 [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -9-fluoro-1,2,3 , 4,4a, 5, ll, lla / S-octahydro-6-methyl-indeno [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -9-fluoro-1,2, 3,4,4 a, 5, 11, 11a zhao-octahydro-6-methyl-D? 丨 indo [2,3-g] isoquinoline, 2-benzene Ethyl-4act- (3-methylphenyl) -9-fluoro-1,2,3, 4, 4a, 5, 11,11a / 9 -octahydro-6-methyl-indo [2, 3-g] Isomorpholine, 2-methyl-4aa_ (3-xiangphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 9-octahydro-6} 1- 1) 5 bis- [2,3-Ju] isoquinoline, 2-methyl-4a〇t- (3-methoxyphenyl) -8-methyl-1,2,3,4,4a, 5, ll, lla / 9 -octahydro-6H-D5 | Dg & [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -8-methyl-1, 2,3,4,43,5,11,113 / 3-octahydro-611-in port? Benzo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 9 -Octahydro-6} 1-indo [2,31] isoquinoline, 2-phenethyl-4a «-(3-hydroxyphenyl) -8-methyl-1,2,3,4, 4a, 5, ll, lla / 3-octahydro 丨 Fonzo [2,3-g] isoquinoline, 2-phenethyl-4 & (^-(3-methoxyphenyl) -8-methyl -1,2,3,4,43,5,11,11 & / 3-octaqi- 6H-D5, bite [2,3-g] isosomal shower gel, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -8-methyl-1,2,3,4,4 &, 5,11,113 / 3-octahydro-6} 1-indazolo [2,3-g] iso Quinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 3-octahydro-611-11?丨 Eye [2,3-g] isoquinoline, 2-allyl-4a〇t- (3-hydroxyphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 8-octahydro-6} {-indoxo-2 [3,3-quin] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -8-methyl-1,2 , 3,4,4a, 5,11,113 Lu-octahydro-611-indo- [2,3- 纟] isoquinoline, 2-methyl- (Please read the precautions on the back before filling this page) This Paper-scale use of Chinese National Standards (CNS) A 4 specifications (210x297 mm) -16-A 6 Β6 V. Invention Bright() - .  Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy (-(3-hydroxyphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 3-octahydro-6- Methyl-indo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methylphenyl) -8-methyl-1, 2,3,4,4a, 5, ll, lla; S-octahydro-6-methyl-indolo [2,3-g ·] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -8-methyl- 1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl-ind [12- [2,3-g] isoquinoline, 2-allyl-4act- ( 3-methoxyphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl-indolo [2,3- &] isoquine Porphyrin, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -8, methyl-1, 2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl -Indo-Dodo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -8-methyl-1,2, 3,4,4a, 5,11,11a-octahydro-6-methyl-indolo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-xiangphenyl) -8-methyl-1 , 2,3,4,4a, 5, ll, llay8-octahydro-6-methyl-indo- [2,3-g] isoquinoline, 2-benzyl-43〇 (-(3-methyl Gas phenyl) -8-methyl-1,2,3,4,43,5,11,113-octahydro-6-methyl-indolo [2,3-g] isoquinoline, 2-benzene B -4aa- (3-hydroxyphenyl) -8-methyl-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-ll¾ 丨 B¾ [2,3 -g] isoquinoline, 2-phenethyl-4aα- (3-methoxyphenyl) -8-methyl-1,2, 3, 4,4a, 5, 11, 11a / 8 -octahydro- 6-methyl-051 benzo [2,3-g] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -9-nitro-1,2,3,4,43,5 , 11,113 / 3-octahydro-6} 1-tondo [2,3-§] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -9-nitro-1,2 , 3,4,4a, 5,11,113 / 3-octahydro-6} 1-indolo [2,31] isoquinoline, 2-benzyl-43〇 (-(3-hydroxyphenyl) -9 -Nitro-1,2,3,4,43,5,11,113 / 3-octahydro-6H-D5 Shun- [2,3-g] isoquinoline, 2-benzyl-4act- (3- Methoxy 17 (Please read the precautions on the back before filling in this page) The paper size is universal Chinese National Standard (CNS) flat 4 specifications (210X297 mm) A 6 B6 301C54 5. Description of invention ()-(please read the back first Please pay attention to this page and fill out this page) Phenyl printed by Beigong Consumer Cooperative of Central Bureau of Standards of the Ministry of Economic Affairs) -9-nitro-1,2,3,4,43,5,11,113 / 8-octahydro-611-ind Said 5 and [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -9-nitro-l, 2,3,4,4a, 5, ll , Lla / S-octahydro-6H-D5I B2 and [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -9-nitro-1,2, 3,4,4a, 5,11,113 / 3-Baqi-611-two | 11 dou [2,3-ming] isoquinine, 2-cyclopropylmethyl-4 & € ('-(3 di Hydroxyphenyl) -9-nitro-1,2,3,4,43,5,11, lla / S-octatrile, 6H-indoquino [2,3-g] isoquinoline, 2-ring Propylmethyl-4aa- (3-methylphenyl) -9-nitro-1, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-l , 3-g] isoquinoline, 2-allyl-4ac (-(3-hydroxyphenyl) -9-nitro-1,2,3,4,4a, 5, ll, lla / S-octa Hydrogen-6H-indP¾o [2,3-g] isoquinoline, 2-allyl-4act- (3-methoxyphenyl) -9-nitro-1,2; 3,4,43, 5,11,113 / 9-octahydro-61 {-indole 5 [〔2,3-ming〕 isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -9-nitro-1,2 , 3,4,4a, 5,11,113 / 3-octaqi-6-methyl-ton-bite [2,3- 纟] isosya_, 2-methyl-4a〇 (-(3-methyl gas benzene Group) -9-nitro-l, 2,3,4,4a, 5, ll, llayS-octahydro-6-methyl-acrido [2,3-g] isoquino, 2-allyl Yl-4 pattern 〇 (-(3-hydroxyphenyl) -9-nitro-1,2,3,4,43,5,11,113 / 9-octahydro-6-methyl-indo-PS [2, 3-g] isoquinoline, 2-ene Yl-4aa- (3-methoxyphenyl) -9-nitro-1,2,3,4,4a, 5, ll, lla-octahydro-6-methyl-indazol [2,3 -g] isoquinoline, 2-cyclopropylmethyl-4aα- (3-hydroxyphenyl) -9-nitro-1,2,3,4,4a, 5,11, lla / S-octahydro -6-methyl-ind02 [2,3-g] isoquino, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -9-nitro-1,2,3, 4,43,5,11,113 /?-Octahydro-6-methyl-indeno [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -9-benz Paper scales are printed in Chinese National Standard (CNS) Grade A (210x297 gongs). A6 _BJB__ is printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. 5. Description of invention ()-.  Nitro-1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl-Yo11deca [2,3-g] isoquinoline, 2-benzyl-4aa- ( 3-methoxyphenyl) -9-nitro-1,2, 3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-indolo [2,3-5] iso Quinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -9-nitro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl- Indeno [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -9-nitro-1,2,3,4,4 a, 5,11, lla / 9-octahydro-6-methyl-indigo [2,3-g] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -7-bromo-1,2,3 , 4,4a, 5, ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline, 2-methyl-4aα- (3-methylphenyl) -7- Bromo-1,2,3,4,43,5,11,113 / 0-octahydro-6 [1-indolo [2,3-g] isoquinoline, 2-benzyl-4aa- (3 -Hydroxyphenyl) -7-bromo-1,2,3,4, 43,5,11,113 / 8-octahydro-6} 1-indolo [2,31] isoquinoline, 2-benzyl- 4acx- (3-methylchlorophenyl) -7-bromo-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indoxo S [〔2. , 3-g] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -7-bromo-1,2,3,4,43,5,11,113 / 3-octahydro-611- Ind [^ benzo [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -7-bromo-1,2,3,4,43,5,11,113 Lu -Octahydro-6} 1-indolo [2,3-min] isoquinoline, 2-cyclopropylmethyl-4acc- (3-hydroxyphenyl) -7-JI-l, 2,3, 4,4a, 5,11,113 / 3-octahydro-611-indole [2,3-8] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methylphenyl) -7 -Bromo-1,2,3,4,4a, 5,11, lla; Q-octahydro-6Η-Βζ | Dolo [2,3-g] isoquinoline, 2-allyl-4aa-( 3-hydroxyphenyl) -7-bromo-1,2,3,4,43,5,11,113 / 3-octahydro-6! 1-worm eye [2,3-g] isoquinoline, 2-allyl-4acc- (3-methoxyphenyl) -7-bromo-1,2,3,4,43,5,11,113-octahydro-611-indolo [2,3 -(Please read the precautions on the back before writing this page) The size of this paper is printed in accordance with Chinese National Standard (CNS) # 4 (210x297 mm) 19 A 6 B6 Printed by Beigong Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs , Description of the invention ()-g] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -7-bromo-1,2,3,4, 4a, 5, ll, lla / 3-octa Hydrogen-6-methyl-P? 丨 Dan [〔2,3-g〕 iso Quinine, 2-methyl-4aa- (3-methylphenyl). -7-bromo-1,2,3,4,4a, 5,11, lla / 3-octahydro-6-methyl-aconizo [2,3-g] isoquinoline, 2-allyl -4act- (3-hydroxyphenyl) -7-bromo-1,2,3,4,4a, 5, ll, lla / S-octahydro-6-methyl-D¾ 丨 II¾ (2,3- g) Isoquinoline, 2-allyl-4aα- (3-methoxyphenyl) -7-bromo-1,2,3,4,43,5,11,113-octahydro-6-methyl- Indolino [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -7-bromo-1,2,3,4,43,5,11,113 / 9-octahydro-6-methyl-indoxo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -7-bromo-1,2 , 3,4,43,5,11,113 / 9-octahydro-6-methyl-indolo [2,3-layer • isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -7-bromo-1,2,3,4,4a, 5,11,113-octahydro-6-methyl-indoxo [2,3-ming] isoquinoline, 2-benzyl-4aa- ( 3-methoxyphenyl) -7-bromo-1,2,3,4,4a, 5, ll, lla / S-octahydro-6-methyl-indo [2,3-g] isoquine咻 、 2-phenethyl-4a〇c- (3-hydroxyphenyl) -7-bromo-1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl- Indo [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methylphenyl) -7-bromo-1,2, 3, 4, 4a, 5, 11, 11a / 3 -octahydro-6-methyl-indigo Bg (〔2, 3-g] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -7-amino-1,2,3,4,43,5,11,113 / 3-octahydro-6} 1-Ind ^^ [2,3-Team] isoquinoline, 2-methyl-4aa- (3-methylphenyl) -7-gas-1,2,3,4,4a, 5,11 , Lla> 9-octahydro-6H-D? Isoquino [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -7-gas-l, 2,3 , 4,4a, 5, ll, lla / S -octahydro-6H-indBdeco [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -7 -(Please read the precautions on the back before filling in this page) Installed · Yes.  This paper is printed on the Chinese National Standard (CNS) Grade 4 (210x297 gong), which is printed on the paper scale. Printed by the Employees Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A6 _B_6______ V. Description of the invention ()-.  Gas-1,2,3,4,43,5,11,113 / 9-octahydro-611-ind 112 [2,3-even] isoquinoline, 2-phenethyl-4aa- (3-hydroxybenzene Radical) -7-atmosphere-1,2,3,4,4a, 5,11,113 ling-octahydro-6} 1-11? 11dec [〔2,3-ming〕 isoquinoline, 2-phenylethyl Yl-43〇 (-(3-methylphenyl) -7-ambient-1,2,3,4,43,5,11,11 & / 3-octahydro-6H-indo [2,3 -g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -7-ambient-1,2,3, 4, 4a, 5, 11, 11a / 8-octahydro- 6H-indole '-[2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -7-chloro-1,2,3,4,43, 5,11,113 / 3-octahydro-6} 1-indazolo [2,3-g] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -7-nitrogen-1,2 , 3,4, 4 &, 5,11,113 / 3-octahydro-611-ind 11 $ and [2,31] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -7 -Chloro-l, 2,3,4,4a, 5, ll, llayS -octahydro-6H-indazolo [2,3-g] isoquinoline, 2-methyl-4aa- (3-hydroxy- Phenyl) -7-ambient-1,2,3,4,4a, 5,11, lla / 3 -octahydro-6-methyl-indolo [2,3-g] isoquino, 2- Methyl-4aa- (3-methoxyphenyl) -7-gas-l, 2,3,4,4a, 5, ll, lla0-octahydro-6-methyl-indo and [2,3- g] Isoquinoline, 2-allyl-4act- (3-hydroxybenzene ) -7-atmosphere-1,2,3,4,4a, 5,11,413 / 9-octahydro-6-methyl-1) 5 丨 11decor [2,3- 茶] isosalinate, 2-allyl-4act- (3-methylphenyl) -7-chloro-1,2, 3,4,4a, 5,11, lla / 3-octahydro-6-methyl-D? 丨Iso [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -7-chloro-1, 2,3,4,4a, 5, ll, lla / Q-octahydro-6-methyl-Il¾ 丨 D2 [2,3-g] isoquino, 2-cyclopropylmethyl-4a α- (3-methoxyphenyl) -7-chloro- l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl- ¾ 丨 lI¾ and [2,3-g] isol¾ command, 2-;! i ?: radical- 4acϊ- (3-xiangphenyl) -7-ambient-1,2,3,4, 4a, 5,11,1 la /?-Octahydro-6-methyl-indazole (please read the back side first Matters needing attention before filling this page) installed.  This paper uses the Chinese National Standard (CNS) A4 specifications (210x297 g *) 21 5. Description of invention (A6 B6 Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economics [2,3-g] isoquinoline, 2- Benzyl-4aa- (3-methylphenyl) -7-chloro-1, 2,3,4,4a, 5, ll, llay9-octahydro-6-methyl-indazolo [2,3- g] Isoquinoline, 2-phenethyl-4act- (3-hydroxyphenyl) -7-nitrogen-1,2,3,4,4a, 5,11,11 grain / 3-octahydro-6- Methyl_11? 丨 82 and. [2,31] Isosleep, 2-phenethyl-4acx- (3-methoxyphenyl) -7-chloro-1,2,3,4,4a, 5, ll, lla; S-octahydro _ 卜 methyl-B? Shuo [2,3-g] isosleep, 2-methyl-4aa_ (3-hydroxyphenyl) -7-methyl-1,2,3,4,4 and 5, 11,113 points-octahydro-611-indazolo [2,3-g] isoquinine, 2-methyl-4aa- (3-methoxyphenyl) -7-methyl-1,2,3 , 4,4a, 5, ll.  llayQ -octahydro-6H-indo [2,3-g] isoquino_, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -7-methyl-1, 2,3, 4,4a, 5, ll, lla /?-Octahydro-6H-indolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl)- 7-methyl-1,2,3,4, 43,5,11,113 / 9-octahydro-6. 11-ind [^ bi [2,3-layer] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -7-methyl-1, 2,3,4,4a, 5, ll, lla / S -octahydro-6H-indBg- [2,3-g] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -7-methyl-1,2 , 3,4,43,5,11,113 / 3-octahydro-6 {1-indazolo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -7 -Methyl-1,2,3,4,43,5,11,11 & / 8-octahydro-6} 1-indole 5 [〔2,3-ming〕 isoquinoline, 2-benzyl- 4aa- (3-methylphenyl) -7-methyl-1,2,3,4, 43,5,11,118 / 3-octahydro-6} {-ton 11deca [2,3- Once] Isosleep, 2-phenethyl-4aa- (3-hydroxyphenyl) -7-methyl-l, 2,3,4,4a. 5, ll, lla / 3 -octahydro-6H-D? Ilozo [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methylphenyl) -7-methyl -1,2,3,4,43,5,11,113 / 3-octahydro-6} 1-indo [2,3-g] isoquinoline, 2-methyl-4aa- (3-hydroxybenzene Base) -10- (Please read the precautions on the back before filling in this page) Binding · Threading · The paper size is easy to use Chinese a standard (CNS) A 4 specifications (210x297 male dragon) 22 A 6 B6 Central Ministry of Economic Affairs Printed by the Bureau of Standards and Employee Consumer Cooperatives V. Description of invention () —— Methyl-1,2,3,4,43,5,11,113 / 3-octahydro-6} 1-indazol [2,3- 苢〕 Isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -10-methyl-1,2,3, 4, 43,5,11,11 pattern / 3-octahydro-611- Indo [2,31] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -10-methyl-1,2,3,4, 4a, 5,11, lla / S-octahydro-6HHPdeca [2,3-g] isosal, 2-cyclopropylmethyl-4aa- (3-methylchlorophenyl) -10-methyl-1, 2,3, 4,4a, 5, ll, llajS-octahydro-6H-indeno [2,3-g] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -10-methyl- 1,2,3,4,43,5,11,113 / 9-octahydro-6} 1-ton bite [2,3-g] isosialin, 2 -allyl- 4aa_ (3 -methoxy Group) -10-methyl-1,2,3,4,43,5,11,113 / 9'-octahydro-611-indo [2,3-g] isoquinoline, 2-benzyl -4aa- (3-hydroxyphenyl) -10-methyl-1,2,3, 4,43,5,11,113 / 3-octahydro-61 indo [2,3-each] isosulfur Porphyrin, 2-benzyl-4act- (3-methoxyphenyl) -10-methyl-1,2,3,4,4a, 5,11, lla; S-octahydro-6H-indazolo [ 2,3-g] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -10-methyl-1, 2,3,4,4a, 5, ll, lla / S-octa Hydrogen-6H-indeno [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -10-methyl-1,2,3,4, 4a, 5, ll, lla / S-octahydro-6H-indo [2, 3-2] isoquinoline, 2-methyl-4 & «-(3-hydroxyphenyl) -8-bromo-1, 2,3, 4,43,5,11,113 / 9-octahydro-611-indolo [2,3-?] Isoquinoline, 2-methyl-4act- (3-methylphenyl) -8 -Bromo-l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-6H-0? 丨 [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa -(3-hydroxyphenyl) -8-bromo-1,2,3,4,43,5,11,113 / 8-octahydro-6} | -0? | D5 和 [2,3-g] Isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -8-bromo-1,2,3,4,4 &, 5,11,11 // 3-octahydro- 611-! 1? 丨 Squatting (2, (please read back Please pay attention to the details before filling out this page) Binding-The paper size used is Chinese National Standard (CNS) A4 specifications (210x297 male dragons) Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy Λ 6 Β6 V. Description of invention () -3-g] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -8-bromo-1,2,3,4,43,5,11,113 / 3-octahydro-611- Indo-8- [2,3-end] isoquinoline, 2-allyl-4aa- (3-methylphenyl) -8-bromo-1,2,3,4,4a, 5,11, lla / S-Octahydro-6H-D5 Shun [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -8-bromo-1,2,3,4 , 43,5,11,11 & / 3-octahydro-6} 1-indino [2,3-g] isoquinoline, 2-benzyl-4act- (3-methylphenyl) -8 -Bromo-1,2,3,4,43,5,11,11 & /?-Octahydro-6} 1-indo [2,3-1] isoquinoline, 2-phenethyl-4aa -(3-hydroxyphenyl) -8-bromo-1,2,3,4,4a, 5,11,113> 9-octahydro-611-ind112- [2,3- 豸] isoquinoline, 2 -Phenethyl-4acx-(3-methylphenyl) -8-bromo-1,2, 3, 4, 4a, 5, 11, 11a / 3 -octahydro-SH-indolo [2,3 -g] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -10-bromo-1,2,3,4,4 &, 5,11,113 / 3-octahydro-6} |- Indolo [2, 3-g] isoquinoline, 2- Yl-4aa- (3-methoxyphenyl) -10-bromo-1,2,3,4,43,5,11,11 pressure /?-Octahydro-611-ind115 [〔2,3- 客〕 Isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -10-bromo-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H- Indo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -10-bromo-1,2,3,4,4a, 5, ll , Lla / 3 -octahydro-6H-D? | BS and [2,3-g] iso_ leaching, 2-allylpropyl-4aa- (3-hydroxyphenyl) -10-bromo-1, 2, 3,4,43,5,11,113 / 3-octahydro-6} 1-indolo [2,3-g] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl)- 10 -Bromo-1,2,3,4,43,5,11,113 / 9-octahydro-611-indolino [2,3-ming] isoquinoline, 2-benzyl-4aa- ( 3-hydroxyphenyl) -10-bromo-1,2,3, 4,4a, 5,11,113 / 3-octahydro-61 indo [2,3-ming] isoquinoline, 2-benzyl- 4aa- (3-methylphenyl) -10-bromo-l, 2,3,4,4a, 5, ll, lla / 3-eight (please read the precautions on the back before filling in this page) -This paper scale uses the Chinese National Standard (CNS) A4 specifications (210X297 male dragon) -24-Printed by the National Standards Bureau of the Ministry of Economic Affairs, the Consumer Cooperative A 6 _B6_ V. Description of invention ()-Hydrogen-6H-Indira And [2,3-g] Quinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -10-bromo-1,2,3,4,4 &, 5,11,113 / 3-octahydro-611-ind》 8 And [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -10-bromo-1,2,3,4,43,5 ,. 11,113zhao-octahydro-6} 1-indhumo [2,3-min] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -8-gas-1,2,3,4 , 4a, 5, ll, lla / 3-octahydro-6H-indolo [2,3-g] isoquinoline, 2-methyl-4acc- (3-methylphenyl) -8-ammonia- 1,2,3,4,4 &,5,11,113; 0-octahydro-611 -1 >? Shun [2,3-ming '] isosleep shower, 2-cyclopropylmethyl-43 (_ (3-Xiangphenyl) -8-chloro-1,2,3,4,43,5,11,113 / 9-octahydro-611-indazolo [2,3-g] isoquinoline, 2-Cyclopropylmethyl-4aa- (3-methylphenyl) -8- 氱 -1,2,3,4,43,5,11,113 /?-Octahydro-61 indolo 〔2 , 3-Jun] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) 8-chloro-1,2,3,4,4a, 5, ll, lla /?-Octahydro-6H -IndBg [2,3-g] isoquinoline, 2-allyl-43〇 (-(3-methylphenyl) -8-ambient-1,2,3,4,43,5, 11,113 / 3-octahydro-6H-indo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -8-chloro-1,2,3, 4,43,5,11,113 / 9-octahydro-611-indaza [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) "8-gas -1,2,3, 4,43,5,11,113 / 9-octahydro-611-ind1! 5 and [2,3-§] isoquinoline, 2-phenethyl-4aa- (3-hydroxyl Phenyl) -8-chloro-1, 2, 3, 4, 4a, 5 ll, lla / 3 -octahydro-6H-indo [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methylphenyl) -8-nitro-1,2, 3, 4, 4a, 5, 11, 11a / 3 -octahydro-6H-indo [2,3-g] isoquino, 2-methyl-4ac (-(3-hydroxyphenyl) -10 -Chloro-l, 2,3,4,4a, 5, ll, llayS-octahydro-6H-inds p- [2,3-g] isoquinoline, 2-methyl-4aa- (3-methyl gas Phenyl) -10-Ambient-l, 2, 3, 4, 4a, 5, (please read the precautions on the back before filling in this page) Packing · This paper scale uses the Chinese National Standard (CNS) A4 specifications ( 210x297 Gonglong ·) 25 A6 _B6_ printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of the invention ()-ll, lla / 3-Baqi-6H-D§ 丨 Bite and [2,3-g] sleep abnormally Leaching, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -10-ambient-l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-indazolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aα- (3-methoxyphenyl) -10-ambient-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline, * 2-allyl-4aa- (3-hydroxyphenyl) -10-chloro-1,2,3,4, 43,5,11,11 & / 3-octahydro-6} 1-indazolo [2,3-ming] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -10 -Chloro-1,2,3,4 , 4a, 5, ll, lla> S-octahydro-6H-indo [2,3-g] isoquinoline, 2-benzyl-4a α-(3-hydroxyphenyl) -10-chloro- 1,2,3,4, 4a, 5, 11, 11a /?-Octahydro-6H-P? 丨 (1¾ and [2,3-g] iso-salary, 2-section base- 4aa_ (3-A Gas phenyl) -10-ammonia-1,2,3,4,43,5,11,113 / 8-octahydro-611-indazolo [2,3-g] isoquinoline, 2-phenethyl- 4aa- (3-hydroxyphenyl) -10-ammonia-1,2,3,4,4a, 5, ll, lla '/ 3-octahydro-6H-ind11¾ and [2,3-g] isoquin咻, 2-phenethyl-4aa- (3-methylphenyl) -10- 氱 -1,2,3,4, 43,5,11,113 Lu-octahydro-611-indho [2 , 3- 苕] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -8-fluoro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H -Indo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methylphenyl) -8-fluoro-1,2,3,4,43,5,11,113 / 8 -Octahydro-6} 1-indazolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -8-fluoro-1,2,3, 4,43,5,11,113 /?-Octahydro-6} 1-indo [2,3-2] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methylphenyl) -8-fluoro-1,2,3,4, 43,5,11,113-octahydro-6} 1-indole [2,3-§] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -8- -l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-l¾ 丨 ll¾ (2,3-g) isoquinoline, 2-allyl-4aα- (3- (Please read the precautions on the back before filling out this page) This paper standard is universal Chinese National Standard (CHS) A4 specifications (210x297 mm) Printed A6 _B6_ by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs V. Invention description ()- Methoxyphenyl) -8-fluoro-1,2,3, 4, 4a, 5, 11, 11a / 3 -octahydro-6H-indazolo [2,3-g] isoquinoline, 2-benzyl Yl-4aa- (3-hydroxyphenyl) -8-fluoro-1,2,3,4,43,5,11,113 / 9-octahydro-611-indo [2,3-ke] isoquinoline 、 2- 笮 基 -4act- (3-methoxyphenyl) -8-fluoro-1,2,3,4,4a, 5,11, lla / Q-octahydro-6H-indPS (2, 3-g] Isoquinoline, 2-phenethyl-4acc- (3-hydroxyphenyl) -8-fluoro-1,2,3,4,43,5,11,113 / 9-octahydro-6 } {-Indo [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -8-fluoro-1,2,3,4,4 &, 5 , 11,113-octahydro-611-indo [2,3-g] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -10-fluoro-1,2,3,4, 4a, 5, ll, lla; 3-octatri-6H-indazolo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methylchlorophenyl) -10-fluoro-1 , 2,3,4,4a, 5, ll, lla / S -Octahydro-6 Η-昭 -Bdec · and [. 2. , 3-g] iso pupil, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -10-fluoro-1,2,3,4,43,5,11,113 / 3-octa Hydrogen-6 ^ indole [2,3-g] isoquinoline, 2-cyclopropylmethyl-4a〇t- (3-methoxyphenyl) -10-fluoro-1,2,3,4 , 43,5,11,113; 8-octahydro-6 {1-indazolo [2,3-g] isoquinoline, 2-allyl-4act- (3-hydroxyphenyl) -10-fluoro- l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6H-indo [2,3-g] isoquinoline, 2-allyl-4aa- (3-methyl gas Phenyl) -10-fluoro-1,2,3,4,4a, 5,11,11 pressure / 3-octahydro-611-ind 11 deca [2,3- 豸] isoquinoline, 2-benzyl Yl-4aa- (3-hydroxyphenyl) -10-fluoro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-P5 | ng and [2,3-g] Isosialoline, 2-benzyl-4acx- (3-methoxyphenyl) -10-fluoro-1,2,3,4,43,5,11,113 / 8-octahydro-6} 1-1 ) §1 Bite [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -10-fluoro-1,2,3,4,43,5,11, 113 / 8-octahydro-6 ^ | bite [2,31] isoquinoline, (please read the precautions on the back before filling out this page) Binding · Order_ This paper is used in the national standard S (CNS) A4 specifications (210X297mm) 27 A 6 B6 Employee Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs Preparation V. Description of the invention ()-2-phenethyl-4aa- (3-methylphenyl) -10-fluoro-l, 2, 3, 4, 4a, 5, ll, lla / 3-octahydro- 6H-P5 丨 11¾ and [2,3-g] isocyanate, 2-methyl-4aa- (3-hydroxyphenyl) -7-nitro-1,2,3,4,43,5,11 , 113; 0-octahydro-6} {-indolo [2,3-g] isoquinoline, 2-methyl-4aoc- (3-methylphenyl) -7-nitro-1,2 , 3,4,43,5,11,113 / 3-octahydro-611-indo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl)- 7-nitro-1, 2,3,4,43,5,11,113 / 3-octahydro-61 ^ worm 1 ^-[2,3-name] isoquinoline, 2-cyclopropylmethyl -4aa- (3-methoxyphenyl) -7-nitro-1,2,3,4, 4a, 5, ll, lla / 3 -octahydro-6H-ind Ug and- [2, 3-g 〕 Isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -7-nitro-l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-ind Ug [〔2,3-g］ isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -7-nitro-1,2,3,4,43,5,11,113 / 3 -Octahydro-61 ^ -115 | Pi [〔2,3-g］ isoquinoline, 2-benzyl-4act- (3-hydroxyphenyl) -7-nitro-1,2,3,4, 43,5,11,11 & 6-octahydro-611-indolo [2,31] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -7-nitro-1 , 2, 3, 4 , 4a, 5,11,113 / 3-octahydro-61 indo [2,3-ming] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -7-nitro-l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6H-indBg- [2,3-g] isoquino, 2-phenethyl-4aα- (3-methoxyphenyl ) -7-nitro-l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6H-indo [2,3-g] isosalin, 2-methyl-4aa -(3-Phenyl) -8-nitro-1,2,3,4,43,5,11,113 / 3-octahydro-6? 1-ind "2 [〔2,31] isoquinoline, 2-methyl-4aa- (3-methylphenyl) -8-nitro-1,2,3,4, 43,5,11,11 &; 9-octahydro-6} 1-indolo [2,3- 纟] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -8-nitro-1,2,3,4,4a, 5,11, (please Please read the precautions on the back and then fill out this page) This paper standard uses the Chinese National Standards (CHS) A4 specifications (210x297 g) 28 Printed by the Ministry of Economic Affairs Bureau of Central Standards Staff Consumer Cooperative A6 _B6__ 5. Description of invention () _ lla / Q-octahydro-6H-indeno [2,3-g] isoquinoline, 2-cyclopropylmethyl-4 per〇 (-(3-methoxyphenyl) -8-nitro- 1,2,3,4,43,5,11,113 / 3-octahydro-6H-indeno [2,3-g] isoquinoline, 2-allyl-4act- (3-hydroxyphenyl)- 8-nitro-1,2,3,4,43,5,11,11 3 / 9-octahydro-6} 1-indo [2,3-g] isoquinoline, 2-allyl-4aa- (3-methylphenyl) -8-nitro-1,2 , 3,4,43,5,11,11 & / 3-octahydro-6 ^ 1-indo [2,31] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl)- 8-nitro-1,2,3,4,4a, 5,11,113-octahydro-611-ind [^ benzo [2,3-ming] isoquinoline, 2-benzyl-4aa- (3- Methoxyphenyl) -8-nitro-l, 2,3,4〆a, 5, ll, lla / 9-octahydro-6H-indo [2,3-g] isoquinoline, 2- Phenethyl-4aα- (3-hydroxyphenyl) -8-nitro-1,2,3,4,4a, 5, ll, lla) S-octahydro-6H-indolo [2,3- g] Isoquinoline, 2-phenethyl-4act- (3-methoxyphenyl) -8-nitro-1, 2, 3, 4, 43, 5, 11, 113 / 9-octahydro-611 -Indo [2,31] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -10-nitro-1,2,3,4, 4a, 5, ll, lla / 9 -Octahydro-6H-indolo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -10-nitro-1,2,3,4,4a , 5,11,11a / 3-octahydro-6H-ind11¾- [2,3-g] isoquinoline, 2-cyclopropylmethyl-4a α- (3-hydroxyphenyl) -10-nitro Yl-l, 2,3,4,4a, 5, ll, lla / 9-octahydro-611-11? 丨 eye [2,3 '^] isosialin, 2-cyclopropylmethyl-43 〇 (-(3-methoxyphenyl) -10-nitro -l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-D? 丨 lI¾ (2,3-g) isoquinoline, 2-allyl-4aα- (3 -Hydroxyphenyl) -l0-nitro-l, 2,3,4,4a, 5, ll, lla / Q-octahydro-6H-ind IIS- [2,3-g] isoquinoline, 2- Allyl-4acx- (3-methylphenyl) -10-nitro-1, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-indole [2,3 -g] Isoquinoline (please read the precautions on the back and then fill out this page) Installation · This paper uses the Chinese National Standard (CNS) A 4 specifications (210x297 male dragon) as the standard of the paper. 5. Description of the invention (Λ 6 Β6, 2 -Benzyl-4aa- (3-hydroxyphenyl) -10-nitro-l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6H-indo [2,3- g] Isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -10-nitro-1, 2, 3, 4, 43, 5, 11, 113; 9-octahydro-6H-ind And [2,3-g ·] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -10-nitro-1,2,3,4,43,5,11,113 / 3-octahydro-6 {1-ind11 «and [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methylphenyl) -10-nitro-1,2, 3,4,43,5,11,113 / 9-octahydro-611-ind [12benzo [2,3-ming] isoquino, 2-methyl-43 (!-(3-hydroxyphenyl) -113 / 9-Hydroxy-1,2,3,4, 4a, 5, 11,11a / 9-octahydrobiquino [2,3-g] isoquine Shower, 2-methyl-4a α-(3-methoxy concubine (please read the precautions on the back before filling in this page) Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 2,3,4,4a, 5, ll , lla / 3 -octazo-. .  6Η-〇ζ 丨 Dan [2,3-g] isosialyl, 2-cyclopropylmethyl-4aa- (3-benzyl) -113-hydroxy-1,2,3,4, 43,5,11,113> 0-octahydro-6} 1-ton B8iso [2,3-g] isobrin, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -lla / 3-Hydroxy-1,2,3,4, ", 5,11,113 / 3-octahydro-611-indo- [2,3-g] isosialin, 2-allyl-4aa- (3 -Epiphenyl) -11a / 3-hydroxy-1,2,3,4,43,5,11,113 / 3-octahydro-6} {-indolo [2,3-g] isoquinoline , 2-allyl-4aa- (3-methoxyphenyl) -lla / S-hydroxy-l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6H-D5U [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -lla / S-hydroxy-1,2,3,4,4a, 5,11,113 Lu-octahydro- 6 ^ 丨 Diazo [2,3-2] isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -lla / 3-hydroxy-1,2,3,4,4a, 5, ll, lla octahydro-6H-H5 丨 11¾ and [2,3-g] isosleep shower, 2-phenethyl-4aa- (3-hydroxyphenyl) -lla / 3-hydroxy-1,2,3 , 4,4a, 5, ll, lla / 3-octahydro-6H-indP¾ (2,3-g) isoquinoline, 2-phenethyl-4aa- (3-methoxybenzine paper scale Xiao Use the Chinese National Standard (CNS) Grade 4 (210x29? Gongxuan) -30-A 6 B6 Ministry of Economic Affairs Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards 5. Description of the invention ()-_ radical) -113 / 9-hydroxy-1,2,3,4,43,5,11,113 / 3-octahydro-61 indigo And [2,3-g] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -9-methyl-113 / 8-hydroxy-1,2,3,4,43,5, 11,113 / 9-octahydro-611-indino [2,3-g] isoquinoline, 2-methyl-4act- (3-methylphenyl) -9-methyl-11a / S -hydroxy- 1,2, 3,4, 4a, 5,11,1 la / 3 -octahydro-6H-indolo [2, 3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3 -Hydroxyphenyl) -9-bromo-113 / 8-hydroxy-1,2,3,4,43,5,11,113 / 3-octahydro-6 {1-indolo [2, 3-g 〕 Isoquinoline, 2-cyclopropylmethyl-4act- (3-methylphenyl) -9-bromo-11 & 3-hydroxy-1,2,3,4,4 3,5,11,113 / 3-octahydro-611-indino [2,3-g] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -9-ambient-113 / 9-hydroxy-1,2 , 3,4,4 ugly, 5,11,113 / 3-octahydro-6? 1-acrido [2, 3-g] isoquinine, 2-allyl-4aa- (3-methoxy Phenyl) -9-nitrogen-113 / 9-hydroxy-1,2,3,4,43,5,11,113 / 9-octatrile-6 ^ 1-indazolo [2, 3-g] isoquinoline , 2-benzyl-4aa- (3-hydroxyphenyl) -7-fluoro-11a lu-hydroxy-1,2,3,4,43,5,11,113 / 3- Hydrogen-6} 1- «丨》« and 〔2,31〕 isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -7-fluoro-lla / 3-hydroxy-1,2, 3,4,43,5,11,113 / 3-octahydro-6} 1-ind02 [2,31] isoquinoline, 2-phenethyl-4aa- (3-hydroxyphenyl) -9-fluoro -lla / S-hydroxy-1,2,3,4,43,5,11,113 / 3-octahydro-6} 1-indole [2,31] isoquinoline, 2-phenethyl -43〇 (-(3-methylphenyl) -9-fluoro-113 / 3-hydroxy-1,2,3,4,43,5,11,113 /?-Octahydro-611-indazole [2,3-Lu] isoquinoline, 2-methyl-43 «-(3-hydroxyphenyl) -8-methyl-113 / 3-hydroxy-1,2,3,4, 43,5, 11,11 & / 3-octahydro-6 ^ Embrino [2,3-§: 1 isoquinoline, 2-methyl-43 «-(3-methylchlorophenyl) -8-methyl-113 / 3-Hydroxy-1,2,3,4, (please read the precautions on the back before filling in this page) Binding · Book size General Chinese Standard (CNS) A 4 specifications (210x297mm) -31 -Printed by the Beigongxiaot Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention () 43,5,11,113 / 9-octahydro-611-indole [2,31] isoquinoline, 2-cyclopropyl Methyl-4aa- (3-hydroxyphenyl) -9-nitro-lla / 3-hydroxy-1,2,3,4,43,5,11,113 / 3-octahydro-611-indo (2 , 3-2] isoquinoline, 2- Cyclopropylmethyl -4aa. -(3-methylphenyl) -9-nitro-lla / 3-hydroxy-1, 2,3,4,43,5,11,113 / 3-octahydro-6} | -indolo [2, 31] Isoquinoline, 2-wall propyl-43〇 [-(3-pyridyl) -7-mo-113 / 3-pyridyl-1,2,3,4,4a, 5, ll, lla > 3-octahydro-6H-indo [2,3-g] isoquinoline, 2-allyl-4act- (3-methoxyphenyl) -7-bromo-lla / S-hydroxy- 1,2,3,4,4a, 5, ll, lla / 9-octahydro-6H-indo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl ) -7-fluoro-lla / 3-hydroxy-1,2,3,4, 43,5,11,113 / 3-octahydro-6 ^ 丨 115- [2,3-dan] isoquinoline, 2-benzyl -430- (3-methoxyphenyl) -7-fluoro-11 & / 9-hydroxy-1,2,3,4,4 &, 5,11,11 & / 3-octahydro-6} ^ Ind! 18- [2,31] isoquinoline; 2-phenethyl-4aa- (3-hydroxyphenyl) -7-chloro-11a / 3-hydroxy-1,2,3, 4,4a, 5, 11 , lla / S-octahydro-6H- vermiculo [2,3-g] isoquinoline, 2-phenethyl-4a «-(3-methoxyphenyl) -7-chloro-11 & / 3 ' -Hydroxy-1,2,3,4,43,5,11, 11a /?-Octahydro-6H-indino [2,3-g] isoquinoline, 2-methyl-4aa- (3- Hydroxyphenyl) -7-methyl-1101; 3-hydroxy-1,2,3,4,4 &, 5,11,11 & octahydro-6H-0? 丨 [2,3-g] iso Saliva, 2-methyl-4aa- (3-methylphenyl) -7-methyl-llaP-hydroxy-1,2,3,4,4a, 5,11,11a / 3-octahydro-6H -Indo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4a α- (3-hydroxyphenyl) -10-methyl-lla / S-hydroxy-1,2,3 , 4,4a, 5, ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4 & «-(3-methylbenzene Group) -10-methyl-113 /?-Hydroxy-1,2,3,4, 4 &, 5,11,11 & / 3-octahydro-61 ^ ind0 | and 〔2,3- 笤〕 Isoquinoline, 2-aryl (please read the precautions on the back before filling in this page) Installation · Line recognition from Rang ίΛ m Ψ 03 K ^: 燋 SiCNSl A 4 sister grid (210x297 g) 32 Central Ministry of Economic Affairs A6 _B6_ printed by the Standards Bureau employee consumer cooperative 5. Description of the invention ()-yl (3-methoxyphenyl) -8-bromo-llayS-hydroxy-l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-6H-ind11¾ And [2,3-g] isoquinoline, 2-benzyl-43〇 (-(3-hydroxyphenyl) -8-bromo-113-hydroxy-1,2,3,4,43,5, 11, 113 / 9-Octahydro-611-episo [2,3-§] isoquinoline, 2-benzyl-43〇1- (3-hydroxyphenyl) -10-bromo-lla / S- Hydroxy-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-pyc [2,3-g] isosleep shower, 2-section group- 4aa- (3-methoxyphenyl) -10-Bromo-lla / 3 -hydroxy-1, 2, 3,4, 4a, 5, 11, lla / 9 -octahydro-6H-indolo [2,3-g] isoquinoline, 2- Phenethyl-4aa- (3-hydroxyphenyl) -10-bromo-lla / S-hydroxy-1,2,3,4, 4 a, 5, 11,11a / 3 -octahydro-6H-B?丨 Ug- [2,3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -10-bromo-lla / S-hydroxy-1,2,3, 4,4a , 5, 11, lla / Q-octahydro-6H-indazolo [2,3-g] isoquinoline, 2-methyl-4aa- (3-hydroxyphenyl) -8-chloro-113 / 3 -Hydroxy-1,2,3,4,43,5,11,11per / 5-octahydro-6} 1 -indo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -8-chloro-11a / 3 -hydroxy-1,2, 3, 4, 4a, 5, 11, 11a / 9 -octahydro-6H-indeno [2,3-g Isoquinoline , 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -10-chloro-113 / 3-hydroxy-1,2,3,4,43,5,11,113 / 3-octahydro- 6} 1-Indo [2,3-g] isoquino_, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -10-chloro-llaP-hydroxy-1,2,3 , 4,4a, 5, ll, lla / 9-octahydro-6H-indazolo [2,3-g] isoquinoline, 2-allyl-4acx- (3-hydroxyphenyl) -8- Fluorine-llayS-hydroxy-1,2,3,4,43,5,11,113 / 9-octahydro-6? 1 -B? 丨 0decoc [2,3-g] isoquinone, 2- Allyl-4aa- (3-methylphenyl) -8-fluoro-11a / 3 -hydroxy-1,2, 3, 4, 4a, 5, 11, 11a / 3 -octahydro-6H-indazol And [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -10 (please read the precautions on the back and then fill out this page) China National Standards (CHS) A4 specifications (210x297 g; ¢) Printed by the Employees ’Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Α6 _Β6__ V. Description of invention ()--Fluoro-11a / 3 -Hydroxy-1,2, 3, 4 , 4a, 5, 11, 11a / 8 -octahydro-6H-tono [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -10-fluoro- 11a / 9 -hydroxy-1,2, 3,4,4a, 5, 11, 11a / 9 -octahydro-6H-indolo [2,3-g] isoquinoline, -2-phenethyl- 4aa- (3- Hydroxyphenyl) -7-nitro -113 / 3-hydroxy-1,2,3,4,43,5,11,113 / 9-octahydro-6} 1-115 | 3-g] isoquinoline, 2-phenethyl-4aa- (3-methoxyphenyl) -7-nitro-lla / S-hydroxy-1, 2, 3, 4, 4. a, 5, ll, llayS -octahydro-6H-05I indole 〔2. 3-g] isoquino_, 2-methyl-4aa- (3-hydroxyphenyl) -8-nitro-113 / 8-hydroxy-1,2,3,4,43,5,11,113 / ? -Octahydro-611-ton [1 and [2. 3-g] isoquinoline, 2-methyl-4aa- (3-methylphenyl) -8-nitro-113 / 9-hydroxy-1,2,3,4,43,5,11,113 / 3-octahydro-611-ind118 [[2. 3-g) Different command, 2-ring. Propylmethyl-4aa- (3-methoxyphenyl) -10-nitro-113 / 3-hydroxy-1,2,3,4,43,5,11,113 / 3-octahydro-6 } 1-Indo-2- (2,3-g) isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -10-nitro-113 / 5-hydroxy-1,2,3 ', 4,43,5,11,113 / 3-octahydro-61! -Indolo [2, 3-g] isoquinoline. The present invention also provides an intermediate for manufacturing the compound of the present invention represented by formula (1), that is, formula (101): (please read the precautions on the back before filling this page).  Η

Ο 3 Ο Λ (ΙΟΙ) This paper standard is used in the 0 National Standard (CNS) A4 specification (210x297 mm)

Printed by the Central Standards Bureau of the Ministry of Economic Affairs, M Industry and Consumer Cooperatives A 6 B6 V. Description of the invention ()-is hydrogen, 5 alkyl groups with 1 to 5 in number, cycloalkyl alkyl groups with 4 to 7 in sulfone, and 6 to 8 in sulfonate Cycloalkenyl alkyl, alkyl aryl groups with a number of 7 to 14, trans-alkenyl groups with a sulfonic number of 4 to 5, allyl, furan-2-ylalkyl, thio-2-ylalkyl, R1D7OCO (Here !? 1 () 7 is 2,2,2-triazaethyl, benzyl) or R1DeCO (here 1? 11) 8 is the alkyl group of sulfo number 1 ~ 5, the number of sulfo number 3 ~ 5 Cycloalkyl, cycloalkenyl with 5 to 7 carbons, phenyl, alkylaryl with 5 to 7 to 13, transalkenyl with 4 to 5 bases, vinyl, 2-11 furanyl, 2 -Hanyl), Rie3, R1D4, R1 () 5 are hydrogen, hydroxy, alkane oxy groups of 1 ~ 5 or alkoxy groups of 1 ~ 5; 1? 1.2 and 1? 1 () 3 or 1? 1. 4 and 1? 1 < > 5 can form an oxo group, R11) 3 can also be combined to form a 1,3-dioxolane ring; R1 [) S is hydrogen, hydroxyl , Alkyl groups with sulfo number 1 to 5 or alkoxy groups with sulfo number 1 to 5] isoquinoline derivatives, their pharmacologically acceptable salts, and methods for their production. '' The pharmacologically acceptable salts of the present invention can be exemplified as follows, namely: salts of inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid; acetic acid, lactic acid, oxalic acid, succinic acid, methanesulfonic acid, benzenesulfonic acid, toluene Among the isoquinoline derivatives shown in the general formula (101) of organic acids such as sulfonic acid, fumaric acid, maleic acid, tartaric acid, for example, the following are suitable: methyl, ethyl, propyl, cyclic Propylmethyl, cyclobutylmethyl, cyclopentenylmethyl, cyclohexenylmethyl, benzyl, phenethyl, phenylpropyl, trans-butenyl, allyl, B furan-2-ylmethyl Group, thio-2-ylmethyl group, 2,2,2-trichloroethoxycarbonyl group, benzyloxycarbonyl group, acetyl group, cyclopropyl carbonyl group, chlorobutene carbonyl cyclopentene carbonyl group, phenyl acetyl group, phenethyl acetyl group Base, trans-acryloyl group, propionyl group, 2-B furanyl group, 2-branched group; R " 2, Ri〇3, Ri〇4, r1D5, for example, it should be hydrogen , Hydroxy, Acetoxy, Methoxy, too ". Erbium ruler iii ffl Ψ Μ 03 Specifications (210x297 public goods) -35-(Please read the precautions on the back and fill in this page) Packing · Ordering- 5. Description of the invention (A 6 B6 Furthermore, 1? 1 !! and 1? 1 «13, and should preferably form an aero group, or r1D3 should be combined to form a 2,2-dimethyl-1,3-dioxolane ring, Rlos should be hydrogen, Hydroxyl group, methyl group, acetyl group ..., but not limited to this. Furthermore, the following general formula (l〇lb), (101c)

R

Ob (101c) (Please read the precautions on the back before filling in this page) (101b) [In the formula, RlDl, 2 is defined before [δ]] Derivatives of isoquinoline with keto group at 6-position and / or 7-position Good is better. In the compound of the general formula (101) of the present invention, R1D1 is a methyl group, R1Da · Rida is nitrogen and Ri. * Ridb is a compound of gas and Rioe is a methyl group. (106) Ding Quan Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs

(106) named 2-methyl-4aa- (3-methoxyphenyl) -6-aero-8a / 3-hydroxy1,2,3, 4,4 a, 5,6,7,8, 8a-decahydroisoquinoline. According to the above nomenclature, this paper standard uses the Chinese B Standard (CNS) A4 specification (210x297 mm) -36-A6 _ B6_ printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. The compounds of the present invention can be specifically exemplified as follows: 2-Chenpropylmethyl-4act- (3-methoxyphenyl) -6-fluoro-8a Lu-hydroxy-1,2, 3,4,4a, 5, 6,7,8,8a-decaisoquinoline, 2-benzyl-4aa-(3-methoxyphenyl)-€ -aero-8a; 8-hydroxy-1,2,3,4,4a , 5,6,7, 8,8a-decahydroisoquinoline, 2-phenethyl-4a〇t- (3-methoxyphenyl> -6-gaso-8a-hydroxy-1,2, 3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-allyl-43〇 (-(3-methylphenyl) -6-gaso-83 / 3- Hydroxy-1,2,3, 4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-methyl-4a〇t- (3-methoxyphenyl) -6,7- Difluoro-8 &amp; / 3-hydroxy-1,2,3,4,4 &amp;, 5,6,7,8,83-decahydroisoquinoline, 2-cyclopropylmethyl-4aa- (3 -Tolyl) -6,7-dioxo-8a / 3 -hydroxy-1,2, 3, 4, 4a, 5, 6, 7,8,8a-decahydroisoquinoline, 2-section Yl-4a〇t- (3-methylphenyl) -6,7-dioxo-8a / 3-keto-1,2,3,4,4a, 5,6,7,8,8a- Decahydroisoquinoline, 2-phenethyl-4aα- (3-Methylphenyl) -6, 7-difluoro-8a aza-hydroxy-1,2, 3,4,4 a, 5, 6, 7, 8,8a-decahydroisoquinoline, 2 -Allyl-4aa- (3-methoxyphenyl) -6,7 -dioxo-8a / 3 -hydroxy-1,2,3,4,4a, 5, 6, 7,8,8a- Decahydroisoquinoline, 2-methyl-4 &amp; £: (-(3-methylphenyl) -6,83; 3-dihydroxy-1,2,3,4, 43,5,6,7 , 8,83-decahydroisosal, 2-cyclopropylmethyl-43〇- (3-methylphenyl) -6,8a / 3-dihydroxy-1,2,3,4,4a , 5,6,7,8,8a-decahydroisoquinoline, 2-benzyl-4aa- (3-methylphenyl) -6,8a; S-dihydroxy-1,2,3,4, 4a, 5,6,7,8,8a-decahydroisoquinoline, 2-phenethyl-4acr- (3-methylphenyl) -6,8a / 3-dihydroxy-1,2,3, 4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-allyl-4aa- (3-methylphenyl) -dihydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-methyl (please read the precautions on the back before filling in this page). Packing: This paper size can be used in China National Standard (CNS) A4 specifications (210x297 male dragon) 37 A 6 B6 ^ 01C〇4 5. Description of the invention ()--4aa- (3-methoxyphenyl) -6,7,8a / S-trihydroxy-l, 2,3,4 , 4a, 5,6,7,8,83-decahydroisoquino, .2-cyclopropylmethyl-43〇 (-(3-methylphenyl) -6,7, 8a / Q-trihydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-benzyl-4a.a- (3-methoxyphenyl) -6,7,8a / 3-trihydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoline, 2-phenethyl-4aot- (3-methyl Gas phenyl) -6,7,8a / 3-trihydroxy-l, 2,3,4,4a, 5,6,7,8, 8a-decahydroisoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -6,7, 83 / 3-trihydroxy-1,2,3,4,43,5,6,7,8,83-decahydroisoquinoline, 2_ (2, 2,2-trichloroethane gas carbonyl) -43 «-(3-methoxyphenyl) -6-acetoxychloro-8a / 3-hydroxy-1,2,3,4, 4a, 5,6, 7,8,8a-decahydroisoquinoline, 2-benzylcarbonylcarbonyl-4aa- (3-methoxyphenyl) -6-acetoxy-8a / 3--hydroxy-1,2,3, 4 , 4 a, 5,6,7, 8, 8a-decahydroisoquinoline, 2-cyclopropylcarbonyl- "〇 (-(3-methoxyphenyl) -6-acetoxy-83 / 3 -Hydroxy-yl-1,2,3, 4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-phenylacryl-4act- (3-methoxybenzyl) -6- Acetyloxy-8a / 3 --Hydroxy-1,2,3, 4,4a, 5,6,7,8,3a -decahydroisoquinoline, 2-phenylethynyl_4aa- (3 -Methoxyphenyl) -6-acetylamino-8a / 3 -hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-propenyl Yl-4aa- (3-methoxyphenyl) -6-acetoxy-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7, 8,8a-decahydroisoquinoline, 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxyphenyl) -8a / 3-hydroxy-1,2,3,4 , 4a, 5, 6, 7,8,8a -decahydro-2,2-dimethyl-1,3-dichloro [4,5-g] isoquinoline, 2-benzyloxycarbonyl-4act- (3-methoxyphenyl) -8a / e-hydroxy-1,2,3,4,4a, 5, 6,7,8,8a-decahydro-2,2-dimethyl-1,3- Difluoro [4,5-g] isoquinoline, 2-cyclopropylcarbonyl-4ao :-( 3-methoxyphenyl)-8a / Q-hydroxy-1, 2,3,4,4a, 5,6,7,8,8a-decahydro-2,2-dimethyl-Taiyin recitation due to national regulations (CNS) V4 pole (210x297 public repair) -38-(Please read the back of the first (Notes and then fill out this page) Installation-Order-Printed by the Ministry of Economic Affairs Central Standards Bureau KX 工 消 # Cooperatives Printed by the Ministry of Economics Central Standards Bureau employee consumer cooperatives Fifth, the description of the invention ()-. 1,3 -dioxa [4 , 5-g] isoquinoline, 2-benzaldehyde- 4aa- (3-methylphenyl) -83 / 3-hydroxy-1,2,3,4,4 &, 5,6,7,8 , 8 ugly-decahydro-2,2-dimethyl-1,3-difluoro [4,5-g] isoquino, 2-phenylacetate-4aa- (3-methylphenyl) _8 Tongzhao--Sangji-l, 2,3,4,4a, 5,6,7,8,8a- + hydrogen-2,2-dimethyl-1,3-dioxo [4,5 -g〕 isoquine , 2-propenyl-43 «-(3-methylphenyl) -83 / 9-hydroxy-1,2,3,4,43,5,6,7, 8,8a-decahydro-2, 2-dimethyl-1,3-diazo [4,5-g] isoquinoline, etc .; of course, not limited to these. In addition, the compound of the present invention includes (+) body, (a) body and (soil) body. The compound of the general formula (1) of the present invention can be obtained by the following conditions. That is, the compound represented by the general formula 〇 can be simply placed in the amine derivative represented by the general formula ⑷ and a solvent, and then reacted in the presence of an acid catalyst (Figure 1) [here R *, R *, R3, R «, Re are defined as above]. As the solvent, alcohol-based solvents such as methanol and ethanol, fatty acid-based solvents such as acetic acid and propionic acid, and dipolar aprotic strip solvents such as DMF and DMSO can be used. Among them, yeast solvents are preferred, and ethanol is particularly preferred. The amine derivative represented by the general formula ⑷ can be a phenyl trap as an example. The Q acid catalyst can be inorganic acids such as hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, methanesulfonic acid, P-toluenesulfonic acid, acetic acid, formic acid, propionic acid, etc. Organic acids, among which hydrochloric acid, sulfuric acid and methanesulfonic acid are preferred. Of course, not limited to this. The reaction temperature can be considered in the range of 0 ~ 3 00t, of which the range of 25 ~ 150¾ is more feasible, and it is usually suitable for the implementation of 60 ~ 120t. Among the compounds represented by the general formula (1), the compound represented by the general formula (ί) in which R2 is hydrogen can be dissolved in a solvent by dissolving the compound represented by the general formula (1) in which Ra is methyl in a thiol (please read the notes on the back first Refill this page) This paper scale uses the Chinese a standard (CNS) A4 specifications (210x297 male dragon) -39-V. Description of the invention (A6 B6 exists to order it to react with the base, or make it with a price of 3 Obtained by reaction of boron compounds (where R3, R *, and R * are as defined above). When thiol and salt are used, the solvent S: using DMF, DMSO, HMPA and other dipolar aprotic inerts Among them, DMF is preferred. In addition, when using trivalent boron, halogen solvents such as dichloromethane, chloroform, and four-atmospheres are preferred, and methane gas is particularly preferred. Thiols can have a number of 1 ~ For example, the chain side chain of 10 is usually propylmercaptan. The base can be: t-butyrate, potassium ethoxide, potassium formate <t-butoxide, ethoxylation Ageing metal salts of alcohols such as sodium and sodium methoxide, hydrides such as sodium hydride and potassium hydride, and metal salts of ammonia such as aminated sodium, usually use t-butane in practice Potassium chloride can get quite satisfactory results. Examples of trivalent boron are: boron tribromide, boron trioxide, etc., especially boron tribromide is preferred. 6 The reaction temperature can be in the range of 0 ~ 300TC when using mercaptan. Among them, 50 ~ 20CTC is better, especially 100 ~ 160¾, and satisfactory results can be obtained; when trivalent boron is used, the reaction temperature can be in the range of -80 ~ 50 ° C. Especially preferably, it is 0 ~ 30C. General formula (S ) Compounds in which R, 1, 2 is methyl, and 1 to 8 is hydrogen can be synthesized according to the method of DM M. Z innernan et al. (J. Org. Chen. 1 989. 54, 1442). (Please read the precautions on the back and then fill out this page) Installation · Line · Printed by the Ministry of Economy, Central Bureau of Standards, Employee and Consumer Cooperatives of this paper standard for use a Standard (CNS) A 4 specifications (210x297 male dragon) 40 A6 B6 V. Description of invention (

R_

(3) ⑴ R, (Π) ODgDOC4 (1,) (Please read the precautions on the back before filling in this page) Pack. In the compound of general formula ⑴ in Figure 1, Ri is an alkyl group with a sulfo number of 2 ~ 5, Cycloalkylalkyl having a nitrate number of 3 to 6, Cycloalkenyl alkyl having a number of 5 to 7, Alkylaryl group, and trans-alkenyl, allyl, or furan-2-ylalkanes having a number of 4 to 5 Compounds with a base, 1 to 2 being methyl and R «being hydrogen ... can be obtained via the route shown in Figure 2. The first project is to transform the methyl group on the nitrogen of the ketone Ο into a carbamate using the general formula (9) in the presence of a salt group. In the formula Ο, Re represents vinyl or tri-gas Ethyl. The base uses a steric obstacle that does not react with the acid salt compound. For example, a proton adsorbent [proton sponge; 1,8-bis (dimethylamino sacrifice)], Huonixi base The solvent is preferably a halogen strip solvent such as dichloromethane, gaseous imitating, four-atmosphere, 1,2-dioxane, etc. Usually 1,2-dioxane is preferred. The reaction temperature can be -80 ~ 100 it, usually line &lt; printed by the Central Bureau of Standards of the Ministry of Economic Affairs, Beigong Consumer Cooperative, the paper scale is used in Chinese H home standard (CNS) A 4 specifications (210x297 male dragon) 41 A6 _B_6__ V. Description of invention ()-Economy The Ministry of Central Standards Bureau employee consumer cooperative printed at Ot: ~ room temperature can get satisfactory results. The second project uses the same as the first 圔 general formula ⑷ shown in the test to obtain the compound represented by the general formula (7) Engineering (reaction conditions, R *, R3 are the same as in Figure 1). The third engineering works of removing the protective group of nitrogen and converting it into a secondary amine When R6 is vinyl, hydrochloric acid-methanol can be used to easily add water for decomposition; the reaction is usually carried out at the reflux temperature of methanol. When R6 is trichloroethyl, it can be removed with zinc in the presence of an acid catalyst; the acid can be Taking acetic acid, hydrochloric acid, nitric acid, etc. as an example, acetic acid is usually used as a solvent and an acid catalyst to obtain quite satisfactory results; the reaction is carried out at a normal temperature. The fourth project orders the general formula (8) due to the presence of a base The process of reacting the compound shown with an acid salt to obtain an amide (10) (R7 represents an alkyl group with a number of 1 to 4, a cycloalkyl group with a number of 3 to 6, an alkenyl group with a number of 5 to 7 and an aromatic group) Allyl, trans 3-4 trans-alkenyl, vinyl, 2-furyl; R3 is as defined above. For the salt group, triethylamine, diisopropylethylamine, proton adsorbent, etc. can be used Tertiary amines, usually using triethylamine, can obtain quite satisfactory results. The solvent can be dihalomethane, chloroform, 1,2-dichloroethane, and other halogen strip solvents, among which digas methane is preferred. The reaction can be It is carried out in the range of -80 ~ 100, especially in the range of 0 ~ 3 () ¾. The fifth project is to return the amide The process of changing to amine. The reducing agent can be sodium boron hydride, lithium aluminum hydride, DAIBAL (diisobutylaluminum hydride), lithium boron hydride, etc., among which DAIBAL and lithium aluminum hydride are preferred. The solvent can be ether, THF, DME Ether, dioxane and other ether solvents, especially THF is preferred. The reaction is carried out in the range of -40 ~ 100 ° C, which is preferably in the range of 0 ~ 301. The sixth project is to remove the methyl and The process of transforming it into a hydrogen-based project. This condition is the same as that obtained when Ra in the compound of general formula (1) is hydrogen. 42 (Please read the precautions on the back before filling the nest page) The paper scale uses the Chinese National Standard (CNS) A4 specifications (210x297 mm) V. Description of invention (Η

(5) ⑴ A 6 B6

(6) Η R6〇 person 〇 Η A Η

RyCOCI FU ⑼ (IV factory (please read the precautions on the back before filling this page) 〇 Λ Η Η

(V)

R, (10) (11) Η Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (VI) R Guang

(11 ·) Figure 2 The paper scale uses the Chinese zero standard (CNS) A4 specifications (210x297 mm) -43-A6 _B6__ printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of invention ()- In the compound represented by the general formula (1), 1 is an alkyl group having a number of 2 to 5, a cycloalkyl group having a number of 3 to 6, a cycloalkenyl alkyl group having a number of 5 to 7, an alkylaryl group, and a sulfur number of 4 to 4. Compounds of 5 trans-alkenyl, allyl, B furan-2-ylalkyl, and Rs, 1-8 are hydrogen ... can be obtained through the route shown in Figure 3. The first project is the project to obtain the compound represented by Formula 6) (the definition of Rs is the same as before); the reaction conditions are the same as the first project in Figure 2. The second project is to remove the protective group of nitrogen and convert it into a secondary amine. When RB is vinyl, it can be easily hydrolyzed by hydrochloric acid-methanol, and the reaction is usually carried out at the reflux temperature of methanol; when 1-6 is trichloroethyl, zinc can be used in the presence of acid catalyst Reductive removal, acid can be exemplified by acetic acid, hydrochloric acid, nitric acid, etc., usually with acetic acid as a solvent and catalyst can get quite satisfactory results. The third project is the project of ordering the secondary amine (12) to react with the acid salt (9) to obtain the aldamine (13) in the presence of the base (the definition of 1 to 7 is the same as above); the base can use triethylamine, Tertiary amines such as diisopropylethylamine, proton adsorbents, etc., usually obtain satisfactory results if triethylamine is used; solvents can use halogens such as dichloromethane, gaseous imitation, 1,2-digasethane, etc. The strip solvent is usually dichloromethane; the reaction can be carried out at -80 ~ 100T, especially in the range of 0 ~ 3010. The fourth project is a project using the same reagent as shown in the general formula (4) to obtain the compound represented by the general formula ⑽ (R3 and R * are as defined above); the reaction conditions are the same as the second project in Figure 2. The fifth project is a project that converts the amide to a amine and the sixth project is a project that removes the methyl group and converts it to a hydroxyl group. The reaction conditions are the same as the fifth project and the sixth project in Figure 2 respectively. (Please read the precautions on the back before filling out this page) Binding · Order _ Line · This paper standard is universal Chinese S home standard (CNS) A 4 specifications (210x297 mm) 44 ΰ

66 AB V. Description of Invention (Η

Ο A Η

(II) (6) Η

RyCOCI (9), (ΠΙ) 〇 Λ

(Please read the precautions on the back before filling out this page) (12) (13) Install · 〇 Λ Η Η Order_

(V)

(10) (11) Η R7 production Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs (VI)

Figure 3 The paper size is free of Chinese National Standards (CNS) A 4 specifications (210x297 male dragons) A 6 B6 V. Description of invention (printed by Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the notes on the back before reading (Fill in this page) In the compound represented by the general formula ®, L is an alkyl group having a number of 2-5, a cycloalkylalkyl group having a number of 3-6, an alkenylalkyl group having 5-5 number, and an alkylaryl group , The number of 4 ~ 5 trans-alkenyl, allyl, furan-2-yl alkyl and 1? »Is methyl, R» hydrogen compounds can be obtained through the route shown in circle 4. First The project is to project the methyl carbamate of the nitrogen of acetate (14) under the salt with the amino acid ester represented by the general formula ®; Re can take vinyl, trifluoroethyl and the like as examples, especially three Gas ethyl is preferred; salt bases can be used that do not react with acid salts but have large steric obstacles, usually proton adsorbents, Huonixi salt bases, etc .; solvents can use dichloromethane, chloroform, tetrasulfonated sulfonate , 1,2-Difluoroethane and other halogen strip solvents, especially 1,2-Difluoroethane is preferred; the reaction can be performed in the range of -80 ~ 100C, usually around Ot ~ room temperature full The second project is a project to obtain the secondary amine (16) by removing the protective group of nitrogen with zinc in the presence of an acid catalyst; the acid can be exemplified by acetic acid, hydrochloric acid, sulfuric acid, nitric acid, etc., usually acetic acid It can be used as a solvent and a catalyst to obtain quite satisfactory results; the reaction is usually carried out at room temperature. The third project is to react the amine (16) with the acid salt represented by the general formula Ο to obtain the amide (17) (The definition of R7 is the same as above); the reaction is carried out under the same conditions as the third project in Figure 3. The fourth project is to convert the aldehyde amine into an amine and the ester into an alcohol to obtain the general formula (18). Examples of compounds are shown; the reducing agent can be exemplified by lithium aluminum hydride, DAIBAL (diisobutyl aluminum hydride), lithium hydride, etc., among which lithium aluminum hydride and DAIBAL are preferred; the solvent is ether, THF, DMF and other ethers The solvent is suitable, especially THF; the reaction can be carried out in the range of -40 ~ lQQt, especially in the range of 0 ~ 301C. The fifth project is the process of gasifying the yeast (18) to obtain the ketone (19) ; Gasification agent can include aluminate, potassium permanganate, and the Chinese National Standard (CNS) A4 specification (210X297 mm) -46-A6 B6 V. Description of the invention (DMSO-DCC, DMSO-oxalaldehyde ammonia, etc. as an example, of which DMSO-oxalaldehyde helium is particularly preferred; the solvent can use di-methane, atmosphere Imitate other halogen strip solvents, especially difluoromethane; the reaction can be carried out at -100 ~ 〇, which is better than -80 ~ · 5〇10. (5) (II) Ο (Please first Read the notes on the back and fill in this page) Ο

(15)

Η ⑴

(16) (9) (111)

. (IV) Binding-binding. (17) (V) (18) Figure 4 In the compound of formula ⑴! ^ Is a methyl group, and 1 to 8 is a hydroxyl group. The compound with a skeleton can be obtained from the following conditions (Figure 5). The first project is to enumerate the methyl group on the nitrogen of the enamine body (20) synthesized by the method of DH Zianner (J. Org. Chem. 1989, 54, 1442) with the general formula (21). Printed by the Central Standards Bureau employee consumer cooperative

(19) Η

This paper uses the National Standard (CNS) Grade A (210x297 mm) for the paper. 47 A6 _B6_ Printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention (1)-Coexistence of master esters in the base The process of down-conversion into a carbamate body; in formula (21) * Re is triethyl or benzyl, but triethyl is preferred; the base can be used without steric hindrance due to reaction with the acid salt Larger ones, such as proton-adsorbed skeletal and Huonixi bases, etc .; solvents such as dichloromethane, chloroform, tetrasulfonated sulfonate, 1,2-dichloroethane and other halogen-based solvents should be used, usually 1,2 -Dichloroethane; the reaction can be carried out at -80 ~ 100 ° C, usually satisfactory results can be obtained at about 0 ~ room temperature. The second project is a project in which the peracid acts on the urethane body (22) to form a ring gas; the peracid used is usually chlorinated benzoic acid. Satisfactory results can be obtained; the solvent can be dichloromethane , Gaseous imitation, tetrachloromethane and other halogen-based solvents, usually using two gas methane; the reaction can be carried out at a temperature of -80 ~ 50 ° C, usually at ~ room temperature to obtain satisfactory results. The third project is to restore the ring gas (23) to open the ring to form the hydroxyl group (24) at the bridgehead; the reduction agent is to use hydrogenated metal compounds such as sodium boron hydride, sodium cyanoborohydride. Satisfactory results can be obtained under acidic conditions such as sulfonic acid, especially when acetic acid is used as a solvent and sodium borohydride is returned; the reaction can be carried out in the temperature range of -80 ~ 5Q ° C, especially in 01C ~ room Satisfactory results can be obtained near Wen. The fourth project is a project to simultaneously restore the carbamate portion and acetate portion of the bridgehead hydroxyl group (24) to obtain the dihydroxyamine body (25); the reducing agents used may include lithium aluminum hydride and diisobutyl hydride For example, aluminum aluminum, lithium boron hydride, etc., among which lithium aluminum hydride is particularly preferred; the solvent can be ether strip solvents such as _, THF, DME, dioxane, etc., among which THF is particularly preferred; the reaction can be at -40C ~ 100t : The scope of implementation, especially in the vicinity of Gt ~ room temperature is better. The fifth project is to oxidize the second-stage hydroxyl group of the dihydroxyamine body (25) to form a hydroxyketone body (26) (please read the precautions on the back before filling out this page). Binding-Order ·-Line. This paper Standard General Chinese Standards (CNS) A4 specifications (210x297 gong) V. Description of invention () Λ6 B6 Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economy; gasification agents include chromic acid, potassium permanganate, DMSO -DCC, DMSO-oxalaldehyde atmosphere, etc., among which DMSO-oxalaldehyde atmosphere is particularly preferred; the solvent can be halogen strip solvents such as dichloromethane and ammonia, especially dichloromethane; the reaction can be at -100 Executed in the range of ~ 01, especially -80¾ ~ -50¾ is better. The sixth project for obtaining the indigo body (27) and the t-th project for obtaining the compound represented by the general formula (2 /) where Ra is hydrogen can be the same as those shown in the first project and the second project of Figure 1 Conditions are. In addition, in the compound of the general formula (1), R5 is a hydroxyl group and L is an alkyl group having a sulfo number of 2 to 5, an alkyl alkyl group having a sulfo number of 3 to 6, a reactive alkenyl group having an ash number of 4 to 5, and an allyl group. Compounds based on phenyl or furan-2-ylalkyl ... are obtained in the following way (Figure 6). The first project and the second project are to convert the 8a-hydroxy-carbamate body (24) obtained from the projects 1, 2, and 3 of Figure 5 into the amide body (29) through the secondary amine (28) Engineering; these projects can be done according to the methods of the second project and the third project in Figure 3, respectively. The third project is a project to change the aldamine acetate body (29) into a dihydroxyamine body (30); this project is the same as the fourth project in Figure 5. The fourth project is the same as the fifth project in Figure 5, which is the process of vaporizing the second-stage hydroxyl group of the dihydroxyamine body (30) into a ketone. Furthermore, the fifth process for obtaining the indole body (32) and the sixth process for obtaining the general formula (32〇) where Ri «is hydrogen are assumed to be the same as the conditions for the first and second processes in FIG. 1 (Please read the precautions on the back before filling in this page) This paper is used in a standard ah family standard (CNS) f 4 specifications (210x297 mm) 49 V. Invention description (r8〇c〇ci 0

66 AB

OAc (i)

OAc (U) (20) (22)

O

(23) (in) π

(24) (Please read the precautions on the back before filling out this page).

(25) (V)

(26) h2nn

(4) (VI) Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs

(27) (VII)

R, (27 ·) Figure 5 This paper size is free to use the Chinese standard (CNS) A 4 specifications (210x297)

Sul6〇4 A 6 B6 V. Description of invention ()

Ο A

OH

(Ο

RyCOCI (24)

n

OAc (III)

OH R wide

OH (IV) (Please read the precautions on the back before filling out this page) (29) (30) Pack ·

OH R3 R7 ^

Line (31) (32)

Printed by Beigongxiaot Cooperative of OH Ministry of Economics, Standards Bureau (VI) R7

r3 (32,) Figure 6 The paper size of the Chinese standard (CNS) A4 specification (210x297 mm) -51 V. Description of invention () A 6 B6 In addition, isoquinoline represented by the general formula (1Q1) Derivatives can be obtained through the following engineering, that is, in the presence of an appropriate base with chlorosulfonate acting on the general formula (102) CH〇. N.

R I 0 2B, R 0 3

R 0 4 (102) 0 5

R 0 6 [Ridz, Ri〇3, Ri. ·》, RiD5, Rids definition question L |] The enamine exemplified to form the general formula (1 〇3) α R, 〇2 R 丨 〇3_Ri 0, R. I 0 5 (103) (please first Read the precautions on the back and fill in this page) Installed &R; 0 ύ Printed by the Employee Consumer Cooperative of the Bureau of Standards, Ministry of Economic Affairs [Rl02, Ri〇3, Rl04, Rios, Rios, RlH7 Definition Questions] The urethane body, and then epoxidize the olefin portion to form the general formula (104) 〇 儿 R… ο N · .0 Rio

_R 10 3 1 R… R. 0 5 '(104) R.0 The paper standard is universal Chinese National Standard (CNS) A 4 specifications (210x297 public) -52 5. Description of invention () A 6 B6 [Ri02, Rl0 3. The definition of Ri〇4, Rioa, Ri〇6, Rl07 HU] epoxy body shown, and then under acidic conditions to return it to the general formula (101a)

(101a) [Rl. :!, Rl03, RlD4, RlOS, RlOS, Rl0 7 The same definitions] 4a α-allyl-8a / 3-hydroxydecahydroisoquinolines shown in this figure, the general formula (10 1 ) Compounds shown. The method for preparing the compound of the present invention, more specifically, can be carried out according to the following conditions. In the compound of the general formula (101b), if R1Ds is a methoxy group, specifically, it can be obtained under the following conditions (Figure 101).

OAc .⑴ 0

OAo (丨 I) (Please read the precautions on the back before writing this page) Binding · Order _ Line-Printed by the Employee Consumer Cooperative of the Bureau of Standards, Ministry of Economic Affairs R,

(104) 'OAc (in)

R η

This paper scale uses the Chinese National Standard (CNS) A 4 specifications (210 father 297 mm) -53-3ϋ! 6〇4 A 6 Β6 V. Description of invention ()

Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (l〇ld) (101b) 'Figure 101. The first project is to use the nitrogen masterbatch under the coexistence of the salt base. Chem., 54 144 2 (1 989)] The process of converting the methyl group on the nitrogen of the obtained enamine body (10 2) 'into the carbamate body (10 3) /. As the base, tertiary amines such as triethylamine, diisopropylethylamine, and proton adsorbents can be used. Among them, tertiary amines with large steric obstacles, such as proton adsorbents and diisopropyl, do not react with acid salts. Ethyl ethylamine, etc. are preferred; the solvent can be halogen strip solvents such as methane, gas imitation, tetrachlorinated sulfonate, 1,2-dichloroethane, etc., and ether solvents such as THF, DME, dioxane, etc. Halogen strip solvents, especially 1,2-difluoroethane; the reaction can be carried out at a temperature of -80 ~ 100t: usually, satisfactory results can be obtained around ~ room temperature. The second project is to transform the carbamate body (103) / into a ring-shaped air skeleton. The cyclic gasification agent used can be used for any reaction agent usually used for gasification, such as perbenzoic acid, m-chloroperbenzoic acid, peracetic acid, trifluoroperacetic acid and other peracids and peracid perhydrogen, especially It is m-gas substituted benzoic acid; the solvent can consider dichloromethane, gas imitation, four gasification halogen and other halogen-based solvents, benzene, toluene and other aromatic sulfonated hydrogen-based solvents, usually can use tooth-based solvents, especially two Gas methane; the reaction can be carried out at a temperature of -80 ~ 50¾, usually at 〇Ί〇 ~ room temperature. This paper scale is easy to use China B home standard (CNS) A 4 specifications (210x297 mm) -54-(please read first Note on the back and then fill out this page) Packing. Order-Line &lt; Printed by Beigong Consumer Cooperative of Central Bureau of Standards of the Ministry of Economic Affairs. A 6 B6 V. Description of invention ()-. You can get satisfactory results nearby. The third project is to restore the epoxy body (104) 'to open the ring to form a bridgehead hydroxyl group (10la)>. Reducing agents can be considered wherever they are commonly used in ring gas-based restitution, but it is better to use a reductive agent that is inactive to the carbamate and acetate parts and can only selectively revert epoxy groups, such as: Hydrogenated metal compounds such as sodium boron hydride, sodium cyanohydride, zinc boron hydride, sodium hydrogen cyanoborohydride, zinc boron hydride, etc. At this time, if the solution is adjusted to be acidic, better results can be obtained. The acid used may be inorganic acids such as hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, and acetic acid. Propionic acid, oxalic acid, methanesulfonic acid, benzenesulfonic acid, toluenesulfonic acid And other organic acids. Solvents can be considered ether ether solvents such as THF, ether, DME, halogen strip solvents such as dichloromethane and ammonia, methanol, ethanol and other alcohol solvents, acetic acid, propionic acid, butyric acid, etc. available organic acids, especially Satisfactory results can be obtained by using acetic acid as the solvent and acid catalyst and reducing with boron hydride. The reaction can be carried out at a temperature of -80 to 5010, and a satisfactory result can be obtained especially at around 01C to room temperature. The fourth project is a project of simultaneously reducing the carbamate portion and the acetate portion of the bridgehead hydroxyl group (10la ') to obtain a dihydroxyamine body (10ld). The reducing agent used can be considered as long as it is a commonly used metal hydride, such as lithium aluminum hydride, diisobutyl aluminum hydride, aluminum hydride, lithium boron hydride, diborane and other strong reducing metal hydride compounds, especially hydrogenation Aluminum lithium is preferred. If using lithium aluminum hydride, lithium boron hydride, diborane, etc., ether, THF, DME, dioxane and other ether strip solvents should be used, especially THF is preferred; in addition, diisobutyl aluminum hydride, hydrogenation In the case of aluminum, it is advisable to use aromatic hydrogen such as benzene and toluene. The reaction can be carried out in the range of -40TC ~ 10 (TC range, in particular (please read the precautions on the back before filling in this page). Installation-Line-55 A6 B6 5. Description of the invention (OC ~ around room temperature is better. No. The fifth project is the process of vaporizing the second-stage hydroxyl group of the dihydroxy amine membrane (IQ Id) into the hydroxy ketone body (101b). The oxidant can be considered as long as it is commonly used for the oxidation of the second-stage hydroxyl group. Chemical agent, permanganic acid strip gasifying agent, DMS0-DCC strip oxidizing agent, DMS0-grass air mist gasifying agent, etc., especially DMS0-grass gas strip oxidizing agent is preferred. The solvent can be considered dichloromethane, gas imitation It is suitable for halogen strip solvents, ether, THF, DME and other ether-based solvents, DMSO, DMF and other aprotic bipolar solvents. Among them, halogen strip solvents, especially dichloromethane are preferred. The reaction can be carried out in the range of -100C ~ 501C , When using DMS0-grass gas oxidant, -80X: ~ 50 ° C is preferred. In addition, compounds of general formula (101b) other than methyl are available under the following conditions (Figure 102). (Please Read the precautions on the back before filling in this page) Install &lt; Order '

R r \

(101a), Ο)

OH

OAc CO line. Printed by Beigong Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs

R

(lOlf) OAc. (ill)

R

OH

(101e) on (iv) The size of this paper is in accordance with the Chinese National Standard (CNS) A4 specification (210X297 g *) -56- A 6 B6 Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Invention Instructions ()- OHu〇a〇 ^^ OCI-la (1011)), Figure 10 2 The first project is the 8a / 3-hydroxycarbamate obtained from the first project, the second project, and the third project of Figure 1 The process of removing the nitrogen protecting group of the body (lola) and transforming it into a secondary amine (10 le). When L. When 7 is 2,2,2-trichloroethyl, this project can be carried out with zinc reduction in the presence of an acid catalyst. Acid can consider the use of inorganic acids such as hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid, and organic acids such as acetic acid, propionic acid, oxalic acid, methanesulfonic acid, benzenesulfonic acid, toluenesulfonic acid and the like. , Ether, THF, DME and other ether-based solvents, DMSO, DMF and other aprotic bipolar solvents, acetic acid, propionic acid, butyric acid and other organic acids can be used as solvents, usually acetic acid as an acid catalyst and solvent can be good Result. The reaction may be carried out at a temperature of -20 ° C to 150 ° C, preferably ~ 50C. In addition, when R1 &lt; &gt; 7 is a benzyl group, the protecting group can be removed under the conditions of hydrolysis. Catalysts Anyone who is commonly used in hydrodecomposition can consider using them, especially rake / sulfon and platinum catalysts. The hydrogen pressure can be considered in the range of 1 to several 10 atmospheres, but usually satisfactory results can be obtained at 1 atmosphere. As the solvent, alcohol-based solvents such as methanol and ethanol, ether strip solvents such as ether, THF, and DME, and aromatic sulfonated hydrogen-based solvents such as benzene and toluene can be considered. The second project is to order the second-level amine (l〇le) and acidify in the presence of the salt base (please read the precautions on the back and then fill out this page) Binding · Order-Line · This paper scale uses the Chinese national standard ( CNS) A4 specifications (210x297 mm) A6 B6 Printed by the Consumer Standardization Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. 5. Description of the invention ()-The process of reacting the substance or anhydride to obtain the amide body (lQlf). As the base, triethylamine, diisopropylethylamine, proton adsorption skull, etc. can be used. Tertiary amines and pyridine, dimethylaminopyridine, azole, etc .; when using acid salt for reaction, triethylamine and proton adsorbent can be used as the salt base to obtain quite satisfactory results. Solvents may consider the use of halogenated solvents such as diaminomethane, ammoniaform, tetrachlorinated sulfonate, 1,2-dioxane, ether solvents such as ether, THF, DME, and pyridine; Strip solvents, especially methane, are preferred; when acid drunk is used, it is preferred to use pyridine as both the base and solvent. The reaction can be carried out in the temperature range of -80 ^ ~ 1001C, in particular, it can hold satisfactory results in the vicinity of ~ room temperature. Secondly, the third project is to transform the acetamide acetate body (1Q1F) into a dihydroxyamine body (10lg). This project works in the same way as the fourth project in Figure 1. The fourth project is the same as the fifth project in Figure 1, which is the process of oxidizing the second-stage hydroxyl body (101g) to the ketone body (101b). In addition, 1 to 1. 1 is 2,2,2-triaminoethyl Gas carbonyl and 1? 1.2, 1? 1.3, 1? 1.4, = hydrogen compound (lola) '', and Rl () 1 is RlceCHa and R1 &lt;) 5 are all hydrogen- --- The compound (101 g) 'can also be obtained by the method of Evans et al. [DA Evans et. Al., J. Am. Chen. Soc., 102, 5955, (1980)] (102) ', as shown in Figure 103, obtained in the same way as the first project, the second project, and the third project in Figure 1. In addition, L can be obtained by the same reaction. 23. R1 &lt; &gt; 4. Various other compounds different from Rles. (Please read the precautions on the back before filling in this page) Binding · Binding-This paper uses the Chinese National Standard (CNS) A4 specifications (210x297 male dragon) -58- V. Description of invention (

r \ R, (1) 0

R (Chuan)

0H

(101e) 1 (V). A6 B6 0

As R, (Π)

(IV) rv

(Please read the precautions on the back before filling out this page)

R (VI).

OH

Printed by Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (101c) 'Figure 103 Using the isoquinoline derivative of the present invention as a synthetic intermediate, the indole derivative of the aforementioned general formula (1) can be prepared. Since the compound of the present invention is an antagonist with high selectivity to δ-contained, it can be used in complex 〇PiQid receptors (divided into ", 6, κ This paper scale is used in the trapped B standard (CNS) A 4 Specifications (210x297 mm) -59- A6 _B6_ printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Invention description ()-.) As a probe, it is very useful. That is, Opioid is related to the complex functions of gastrointestinal tract movement, kidney function, appetite, billion, gastric juice secretion, analgesia, circulatory organs, breathing, mental function, etc., but the detailed pharmacological effects of each subtype need to be further Exploring and investigating, and thus investigating and investigating, it is expected that the compound of the present invention having a very high selectivity for δ-accepted skeletons will be very useful. Furthermore, the delta-OpiQid receptor is related to analgesia, immunity, and circulation (especially blood pressure), and the ligand with high selectivity to this receptor can be used as an analgesic, immunosuppressant [used in organ transplantation (Kidney, liver, heart), skin graft, autoimmune diseases (rheumatic, various allergies, collagen diseases, osteoporosis and other refractory diseases), etc.), the possibility of blood pressure lowering agents and other drugs. Since the compound of the present invention has properties as a 5-receptor antagonist, it is particularly expected to be an excellent immunosuppressant in the above-mentioned diseases. When the compound of the present invention is used as an immunosuppressant in clinical practice, free bases or their salts, stabilizers, buffers, diluents, isotonic agents, preservatives and other excipients may be appropriately mixed. The dosage form can take various forms such as injection, capsule, seat, oral preparation and so on. The dosage can be appropriately determined according to the administration object, administration method, and symptom. If it is an injection, the range may be Q. 000 1 ~ U / day, and if it is an oral agent, it may be 01 ~ 10g / day. The content of the medicament containing the compound of the present invention may be in the range of 0.05 to 99%, preferably 0.5 to 20% in the case of injections, and 0.1 to 50% in the case of oral preparations. [Examples] The following examples illustrate the present invention in further detail. However, the present invention (please read the precautions on the back before filling the nest page) This paper standard uses the Chinese standard (CNS) A4 specification (210x297 Public ¢) A6 __B6_ V. Description of invention ()-. Not limited to this. Example 1 2-methyl-4aa- (3-methylphenyl) -1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indo [2,3- g) Isoquinoline 1

(Please read the precautions on the back before filling in this page) The print number of the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs will be 2-methyl-4aa- (3-methylchlorophenyl) -6-oxo-1,2, 3,4,4a, 5,6,7,8,83 / 3-decaisoquinoline 1611〇2 and phenylhydrazine 0.06411 | 1 were dissolved in 3nl of ethanol, and methanesulfonic acid 0.383 was added during heating and refluxing ml, stirring while refluxing for 1 hour. After the reaction mixture was cooled to room temperature, a saturated aqueous solution of sodium hydrogencarbonate was added under ice-cooling, and extraction was performed 3 times with an atmosphere of 10 mL. The combined organic layer was washed with 5b1 of saturated saline, dried and concentrated to obtain 25〇Bg of powder. Separate and purify with a chromatography tube [silica gel: methanol-aeroform-28% ammonia = 2.5: 97.5%: 0.1-5.0: 95.0: 0.1] to obtain 150 mg of the title compound (yield 73.5%). IR (KBr) cn-1: 3400, 2936, 1609, 1448 HMR (CDC 13) 500MHz 5: 1.98 (lH, b), 2.10 (1H, id), 2.32 (3H, s), 2.39 (lH, m) , 2.58 (1H, b), 2.65 (1H, t, J = 11.6Hz), 2.73 (lH, d, j = 12.2Hz), 2.87-3.06 (4H, m), 3.07 (lH, d, J = 15.9 Hz), 3.67 (3H, s), 6.61 (lH, m), 7.01-7.10 (5H, m), 7.20 (1H, b), 7.43 (lH, n), 7.65 (1H, brs) Mass (m / e): 346 (M *) set _ line-this paper standard is used in China National Standard (CNS) A4 specification (210x297 public goods) -61 &quot; A 6 B6 V. Description of invention ()-. 4-Nitrophenylhydrazine substituted phenylhydrazine to give 2-methyl-4aa- (3-methoxyphenyl) -9-nitro-1, 2,3,4,4a, 5, ll, lla / 8-octahydro-6H-¾ 丨 Bg and [2,3-g] isoquinoline; substituted with 3-nitrophenyl trap to give 2-methyl-4aa-(3-methylphenyl)- 8-nitro-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline and 2-methyl-4a α- (3-Methylphenyl) -10-nitro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indazolo [2,3-g] isoquinoline ; Replace with 2-nitrophenyl trap to get 2-methyl-4aa- (3-methylphenyl) -7-nitro-1,2,3,4,4a, 5, ll, lla / 3 -Octahydro-6H- Hg and [2,3-g] isoquinoline. Example 2 2-methyl-4aa- (3-hydroxyphenyl) -1,2,3,4,4a, 5, ll, lla / S-octahydro-6H-indolo [2,3-g 〕 Isoquinoline 2 (Please read the precautions on the back before filling out this page)

Line. The Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs printed 2-methyl-4act- (3-methylphenyl) -1,2,3,4,43,5,11 under the blanket of argon. 11 change / 8-octahydro-611- «| Dolo [2,3-§] isoquinoline 95.7rag and potassium-t-butoxide 93.1mg dissolved in 3®1 anhydrous DMF, add 1-propane After 0.08 ml of thiol, it was stirred at 1401C for 7.5 hours. Add 10ml of saturated aqueous solution of sodium bicarbonate, and extract 3 times with 30nl of gas: methanol = 5: 1 mixed solvent. The organic layers were combined, washed with 5 ml of saturated brine, dried and concentrated to obtain 100 mg of powder. Suspend the powder in methanol of lBll, add methanesulfonic acid to form methanesulfonate, and use the standard size of China National Standard (CNS) A4 (210x297mm) _62- Ministry of Economic Affairs Printed by the Central Standards Bureau staff consumer cooperative A 6 B6 V. Description of the invention ()-. Separation and purification of the analysis tube [Sephadex-LH-20; methanol] to obtain the methanesulfonate of the title compound 51.6ag (yield 43.5% ). IR (KBr) cm-1: 3400, 1586, 1466 NMR (DMSO-ds) 5 00MHz δ: 2.00 (1Η, π), 2.31 (3Η, s), 2.44-2.64 (3Η, π), 2.81 (3H, s), 2.81-2.90 (2H, m), 2.97 (lH, m), 3.10 (lH, d, J = 16.5Hz), 3.36-3.44 (2H, m), 3.61 (1Η, π), 6.53 (lH, m), 6.90-6.99 (4H, n), 7.04 (lH, t, J = 7.9Hz), 7.18 (1H, d, J = 7.9Hz), 7.34 (1H, d, J = 7.3 H z), 9.24 (lH, s), 9.53 (1H, brs), 10.46 (lH, s)

Mass (FAB): 333 (M * +1) Elemental analysis C2H〇. CH3S03

C HNS calculated value 64.4 6 6. 5 9 6.54 7.48 found value 64. 1 2 6. 3 1 6.25 7.3 3 The following is the same as 2-methyl-4act- (3-methoxyphenyl) -10-nitro- 1,2,3,4,48,5,11,113 / 3-octahydro-6} 1-indo [^ [〔2,3- 茶〕 isoquinoline substituted 2-methyl-4act- (3- Methoxyphenyl) -1,2,3,4,4a, 5,11,1 la / S-octahydroocta [2,3-g] isoquinoline, which gives 2-methyl-4 aa -(3-hydroxybenzene-10-nitro-l, 2,3,4,4a, 5, ll, lla / 3 octahydro-6H-05I PS and &lt; r2,3-g] isoquinoline; 2-methyl-4aa-(3-methoxyphenyl) -9-nitro-1,2,3,4,43,5,11,113 / 8-octahydro-61 {-indD5 [(2 , 3-g] isoquinoline substitution, you can get 2-methyl-4act- (3-hydroxyphenyl) -9-nitro-1,2,3,4,43,5,11,113 /?-Octa Hydrogen-611-Indox and the paper size of Chinese paper (CNS) A4 specifications (210x297 mm) are used happily (Please read the precautions on the back before filling out this page)

Α7 Β7 5. Description of the invention () [2,3-g] Isoquinoline; with 2_methyl-4acc-(3-methoxybenzyl) _8_ indeed -1, 2, 3, 4, 48, 5,11,113 / 3-octahydro-611-aconizo [2,3-8] isoquinoline substitution, you can get 2-methyl-4aa-(3-hydroxybenzyl) -8_nitro _1, 2,3,4,4,5,11,1131 / 3-octahydro-68-11? 1 indo [2,3-phanisoquinoline; 2-methyl-4aa- (3 -Methoxyphenyl) -7-nitro-1,2,3,4,4a, 5,11,1 la / 3 -octahad Hag D8 and [2,3-g] isoquinoline substitution; To give 2-methyl-4a〇t- (3-hydroxybenzyl) -7-nitro-l, 2,3,4,4a, 5, ll, / lla / 3-octahydro-6Η-ϋή | ® and [2,3-g] isoquinoline. Example 3 2 -methyl-4 a α-(3 -methoxyphenyl) -9 -methyl-1,2,3,4,4 a, 5, 11, lla / 3 -octahydrovolume [ 2,3-g] isoquinoline 3 Η

-------- ^ 装 ------ 訂 · —----- {, Bing (please read the precautions on the back before filling out this page) Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 2-methyl-4a〇t- (3-methoxyphenyl) -6-oxo-1,2,3,4,4a, 5,6,7,8,8a / 3-decahydroisoquine 250 ng of phenanthroline and 160-M of p-toluene hydrazine acid salt were dissolved in ethyl acetate of 3.1, methanesulfonic acid 〇.58b1 was added under heating and refluxing, and refluxing was conducted for 1 hour while mixing. The reaction mixture was cooled to room temperature * Under ice-cooling, add 10% of krypton carbonate and an aqueous solution, and extract 3 times of M10 · 1 of krypton. Combine the layer with water and wash it with saturated edible water, dry it, and get 40Oag powder. Μ chromatography tube [silica gel: methanol: chloroform: 28% ammonia solution = 2.5: 97.5: 0 · 1 ~ 5.0: 95.0: 0.1] This powder is applied to the Chinese national standard (CNS) A4 specification (210Χ 297 PCT) 64

i 'Description of the invention () Separation and purification will give you S compound 313eg (yield 94.9%) ° IR (KBr) cm-1: 3402, 2922, 1607, 1580 NMR (CDC13) 500MHz δ: 2.12 (1Η, b ), 2.25 (1H, m), 2.40 (1H, b), 2.42 (3H, s), 2.43 (3H, s), 2.60 (1H, i), 2.71-2.79 (2H, b), 2.86-2. 91 (3H, β), 3.03-3.〇8 (2H, n), 3.68 (3H, s), 6.62 (1H, b), 6.90 (1H, d, J = 8.6Hz), 6.97-6.98 (2H , a), 7.10 (2H, dd, J = 18.3Hz, 7.9Hz), 7.18 (1H, s), 7.81 (lB, s) Mass (丨 / e): 360 (M *) The same Mo- Toluazine HCl M replaces P-toluene hydrazine 'to give 2-methyl-4aa- (3-methylphenyl) -7-methyl-1,2,3,4,4a, 5, ll, lla) S- Octahydro-611-11¾dolo [2,3-g] isoquinoline. Example 4 2-methyl-4aa- (3-hydroxyphenyl) -9-methyl-1,2,3,4,4a, 5,11, llayS-octahydro-6H-indazol [2, 3-g] isoquinoline 4 I ------- 1 loaded ------ ordered I -.----- {t (please read the precautions on the back before filling this page) Ministry of Economic Affairs Printed by the Central Standards Bureau employee consumer cooperative

In the army of fi gas, 2-methyl-4acx- (3-methoxyphenyl) -9-methyl-1,2,3,4,4 &amp;, 5,11,118 / 8-octaoxy-68 -Indozo [2,31] isoquinoline 237mg and methyl-t-butoxide 333ng dissolved in 8b1 anhydrous DMF, add propane bromide 0.28 · 1. After stirring at 140 ° C for 4.5 hours, the mixture was cooled to room temperature. The DMF is removed under reduced pressure, and the carbon paper standard of IDbI is applied to the Chinese National Standard (CNS) A4 specification (210X 297 mm) 65 301CJ4 printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of the invention ()-. Sodium bicarbonate Saturated aqueous solution was extracted 3 times with 30B1 atmosphere: methanol = 5: 1 mixed solvent. The combined organic layer was washed with saturated brine, dried and concentrated to obtain 166 mg of powder. Suspend the powder in methanol of lnl and add toluenesulfonic acid to form tosylate salt. • Purify it with a chromatography tube [Sephadex, LH-20; methanol] to obtain 134 mg of the title compound as the methane hydrochloride salt. (Yield 46.1%). IR (KBr) cn-1: 3400, 2926, 2732, 1599 NMR (DMSO-ds) 5 0 0MHz 6: 2 .00 (1H, s), 2.33 (3H, s), 2.37 (3H, s), 2.51 -2.64 (3H, n), 2.8 1 (3H, s), 2.80-2.97 (3H, m), 3.06 (1H, d, J = 16.5Hz), 3.36 (2H, b), 3.61 (1H, d, J = 11.6Hz), 6.53 (1H, d, J = 7.9Hz), 6.80 (1H, d, J = 8.6Hz), 6.88 (lH, s), 6.92 (1H, d, J = 7.9Hz), 7.03 (lH, d, J = 7.9Hz), 7.06 (lH, d, J = 8.6Hz), 7.12 (1H, s), 9.24 (1H, s), 9.53 (1H, brs), 10.46 (lH, s)

Mass (FAB): 347 (M * +1) elemental analysis

CaH〇. CH3S03H 0.1 HaO C Η Ν S calculated value 64.87 6.85 6.30 7 .22 found value 64.62 7.04 6.16 7.53 The following same 2-methyl-4aa- (3-methylphenyl) -7- Methyl-1,2,3,4,43,5,11,113-octahydro-611-tono [2,3-ming] isoquinoline substituted 2-methyl-4aa- (3-methyl Oxyphenyl) -9-methyl-1,2,3,4,4a, 5,11,113 / 9-octahydro-611-indo [2,3-«] isoquinoline to give 2-methylbenzyl Paper-scale use Chinese Standards (CNS) Grade 4 (210X297) ¢ -66- (Please read the precautions on the back before filling out this page) Binding · Order · Thread-Beigong Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs Printed A 6 B6 5. Description of the invention ()-yl-43〇 (-(3-hydroxyphenyl) -7-methyl-1,2,3,4,4 in, 5,11,113 / 9-octahydrogen -6H-D? 丨 [1¾ and [2,3-g] isoquinoline. Example 5 2-methyl-4aa--(3-methoxyphenyl) -9-chloro-1, 2, 3, 4, 4a, 5, 11, lla / S -octahydro-6H-indazolo [2,3-g] isoquinoline 5 CH3d3g0cl. (5) • &amp; Dimethyl 2-methyl-4aa- (3 -Tolyl) -6-oxo-1,2,3,4,4a, 5,6,7,8,8a / S -decahydroisoquinoline 2 50 mg and 4-nitrobenzene hydrochloride Dissolve 180mg of hydrazide in 3ml Add methanesulfonic acid 0.6 π1 to the reflux while stirring for 1 hour. Cool the reaction mixture to room temperature, add 10 ml of a saturated aqueous solution of sodium hydrogenate under ice cooling, and extract three times with 10 ml of nitrogen simulant. Combine The organic layer was washed with saturated saline, dried, and concentrated to obtain 4 2 Omg powder skull. Chromatography tube [silica gel: methane: chloroform: 28% ammonia water = 2 · 5: 97.5: 0.1 ~ 5.0: 95.0: 0.1] This powder was separated and purified to obtain 3 15nig of the title compound (yield 90.4%). IR (KBr) cn-1: 3418, 2936, 1582, 1446 NMR (CDC13) 500MHz δ: 2.09 (1H, m), 2.23 (1H, π), 2.43 (3H, s), 2.51-2.02 (2H, m), 2.76 (1H, t, J = 11.6Hz), 2.82-2.91 (3H, m), 3.02 (lH, ffl), 3.09 (lH, d, J = 15.3Hz), 3.68 (3H, s), 6.63 (1H, dd, J = 7.9Hz, 2.4Hz), 6.95 (2 H, b), 7.02 (lH, dd, J = 8.5Hz, 1.8Hz), 7.10 (lH, t, J = (Please read the precautions on the back before filling out this page) Packing-line. The paper size is free to use China National Standard (CNS) A4 specifications (210X297) ) -67- A 6 B6 5. Description of the invention ()-. 7.9Hz), 7.15 (1H, d, J = 7.9Hz), 7.33 (1H, d, J = 1.8Hz), 8.13 (1H, brs) Mass (ai / e): 380 (M *) the following phase The same 3-amino substituted phenyl trap substituted 4-aminophenyl hydrazine to give 2-methyl-4aa- (3-methoxyphenyl) -8-ambient-l, 2,3,4,4a, 5 , ll, lla / S-octahydro-6H-indigo [2,3-g] isoquinoline and 2-methyl-4aα- (3-methoxyphenyl) -10-ambient-l, 2, 3,4,4a, 5, 11, 11 ^^ octahydro-6H-D5I quino [2,3-g] isoquinoline; take 2-gasophenylhydrazine to take 1 ^ 12-methyl-4act- (3-Methylphenyl) -7-ambient-1,2,3,4,43,5,11,113 / 3-octahydro-611-indo [2,3-g] isoquinoline. Example 6 2-methyl-4aa- (3-hydroxyphenyl) -9-gas-1, 2,3,4,4a, 5,11,11a /?-Octahydro-6H-P5 丨 Ug and [ 2,3-g] isoquine_ 6

(Please read the precautions on the back before filling out this page) Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs under the argon atmosphere -1,2,3,4,43,5,11,113 points-octahydro-6 {1-ind 11 Duo [2,3-2] isoquinoline 255mg and potassium-1-butane gasification 45 2ing After dissolving in DMF and adding 0.4 ml of 1-propanethiol, it was stirred at 1401C for 5.5 hours. The reaction mixture was cooled to room temperature. DMF was removed under reduced pressure, 5 ml of a saturated aqueous solution of sodium hydrogen nitrate was added, and extraction was performed with 30 ml of chloroform three times. The organic layers were combined and washed with saturated brine, dried, and concentrated to obtain 278 nig powder. Suspend the powder on the paper scale and use the Chinese National Standard (CNS) A4 specification (210x297 male dragon) -68- A 6 B6 V. Description of the invention ()-.lul of methanol, add methanesulfonic acid to make Methanesulfonate was formed and separated and purified by chromatography tube [Sephadex, LH-20; methanol] to obtain 100 mg of methanesulfonate of the title compound (yield 41.2%). IR (KBr) cm- ^: 3240, 1601, 1586, 1450 NMR (DMSO-d 6) 5 0 0MHz δ: 2.07 (1Η, t, J = 1 2.8Hz), 2.32 (3H, s), 2.53 (lH , M), 2.64 (2H, n), 2.79 (3H, s), 2.84- 2.9 7 (3H, m), 3.09 (1H, d, J = 15.9Hz), 3.35 (2H, m), '3.58 ( lH, d, J = 11.0Hz), 6.54 (1H, dd, J = 7.9 Hz, 1.8Hz), 6.90 (2H, m), 6.97 (1H, dd, J = 8.6Hz, 1.8Hz), 7.04 (lH, t, J = 7.9Hz), 7.20 (lH, d, J = 8.6Hz), 7.37 (1H, d, J = 1.9Hz), 9.28 (lH.s), 10. 03 (1H, brs), 10.86 (lH, s) Mass (FAB): 367 (Mf +1) Elemental analysis C 2 2 Η 2 3N3cr ch3 s〇3H2 c Η N Cl s calculated value 59.67 5.88 6.05 7.66 6.93 found value 59 · 78 5.93 6.24 7. 45 6. 63 (please read the precautions on the back before writing this page) Binding-Order _ Line · The Ministry of Economic Affairs Central Standards Bureau Beigong Consumer Cooperative printed the following with the same 2-methyl -4aa- (3-methylphenyl) -10-chloro-1,2,3,4,43,5,11,113zhao-octahydro-6? 1-indo [2,3-8] Isoquinoline substituted 2-methyl-4aa- (3-methoxyphenyl) -9-amino-1,2,3, 4,4a, 5, ll, lla / 3-octahydro-SH-P5IBS and [ 2,3-g] isoquinoline to give 2-methyl-4aa- (3-hydroxyphenyl) -10-gas-l, 2,3 , 4,4a, 5, ll, lla &gt; S-octahydro-6H-D? | Pg &amp; [2,3-g] isoquinoline; 2-methyl-4aa- (3-methylphenyl) -8-chloro-1,2,3,4,43,5,11,11 &amp; / 3-octahydro-6 [1-ind0? And [This paper scale uses Chinese National Standard (CNS) A4 specifications (210x297g *) -69-

V. Description of the invention () 2,3-g] isoquinoline substitution to give 2-methyl-4a α-(3-hydroxyphenyl) -8-gas-1,2,3,4,43,5, 11,11 &amp; 々-octahydro-611-indo31- [2,3-Dang] isoquinoline; M2-methyl-4aa- (3-methoxyphenyl) -7-chloro-1,2, 3,4,4a, 5,11,113 Zhao-octaqi-611-indolo [2,3-8] isoquinoline substitution, which gives 2-methyl-4aot-〇-hydroxyphenyl) -7 -Chloro-l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-6H-B5lDg and [2,3-g] isoquinoline. Example 7 2-methyl-4aa- (3-methoxyphenyl) -7-fluoro-1,2,3,4,4a, 5, 11, lla / S-octahydro-6H-〇? And [2,3-g] isoquinoline Ί (Please read the precautions on the back before filling this page) 1 Η

Order _ Printed by the Ministry of Economic Affairs Central Standards Bureau Employee Consumer Cooperative to print 2-methyl-4act- (3-methoxyphenyl) -6-oxo-1,2,3,4, 4a, 5,6,7, 8,8a / 3-Decahydroisoquinoline 250rog and 164 mg of 2-fluorophenylhydrazine hydrochloride were dissolved in 3 ml of ethanol, 0.6 ml of methanesulfonic acid was added to the heating and reflux, and the mixture was further refluxed for 1 hour while stirring. The reaction mixture was cooled to room temperature, 10 ml of a saturated aqueous solution of sodium hydrogencarbonate was added under ice cooling, and extracted three times with chloroform. The organic layers were combined, washed with 5ml of saturated brine, concentrated and dried to obtain 407g powder. Separated and purified by chromatography tube [silica gel: methanol: gas imitation: 28% ammonia = 2.5: 97.5: 0.1 ~ 50_: 95.0: 0.1] to obtain 120mg of the title compound (yield 36.1%). IR (KBr) cm-1: 3412, 2938, 1607, 1491 NMR (CDC1 a) 500MHz δ: 2.10 (1H, in), 2.20 (1H, m), this paper scale is applicable to China National Standard (CNS) A4 Specifications (21 ο X 297 mm) 70 C υ 3

66 AB V. Description of invention (2.41 (3H, s), 2.43 (lH, s), 2.60 (1Η, π), 2.76 (lH, t, J = 11.6Hz), 2.81-2.98 (4Η, ι), 3.05 (1Η.π), 3.13 (lH, n), 3.69 (3H, s), 6.64 (1Η, πι), 6.79 (lH, n), 6.96 (3H, n), 7.11 (lH, t, J = 7.9 Hz), 7.17 (lH, d, J = 7.9Hz), 8.04 (1H, brs)

Mass (m / e): 3 6 4 (M *) The following is the same as the 3-fluorophenyl trap instead of the 2-fluorophenyl trap to give 2-methyl-4aa- (3-methylphenyl) -8-fluoro-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6 {1-1 !? 丨 118 和 〔2,3- 纟〕 ISO_Lin and 2- Yl-43〇 (-(3-methoxyphenyl) -10-fluoro-1,2,3,4,43,5,11,113 (^ octahydro-611-ind »dece [2,3-g] Isoquinoline: 2-fluoro-4a α- (3-methylphenyl) -9-fluoro-1, 2,3,4,4a, 5, ll, lla is taken with 4-fluorophenyl trap / 3-Octahydro-6H-indo [2,3-g] isoquinoline ΰ Example 8 (please read the precautions on the back before filling this page)

) -7-Fluoro-l, 2,3,4,4a, 5, 8 Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs ch3n

⑴Under the envelope of argon gas, 2-methyl-4aa- (3-methoxyphenyl) -7-fluoro-1,2,3,4,4 &amp;, 5,11,113 / 9-octahydro- 6) 1-Indo [2,3-ming] isoquinoline 136ng and potassium-t-butoxide 126mg dissolved in 3ml of anhydrous DMF, add 1-propanethiol Q.lral and stir at 14Q ° C 3 hours. Copy the original paper standard with Chinese National Standard (CNS) A4 specifications (210x297 mm) -71- Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs A 6 B6 V. Description of invention ()-The mixture should be cooled to room temperature , DMF was removed under reduced pressure, 5nil saturated aqueous solution of sodium bicarbonate was added, and extraction was performed 3 times with 30ιπ1 gas. The organic layer was combined, washed with saturated saline, dried and concentrated to obtain 268Bg of powder. Purify this powder with a chromatography tube [sand waist: methanol: gas imitation-: 28% gas water = 5: 95: 0.1 ~ 10: 90: 0.1], suspend the resulting powder in 1ml of methanol, and add methanesulfonate The acid was used to make methanesulfonate, and the methanesulfonate was further purified by Sephadex tube [LH-20; methanol] to obtain the methanesulfonate of Sassafras compound 38.7nig (yield 23.1%). IR (KBr) cui-1: 3400, 15 99, 1400 NMR (DMSO-ds) 500MHz δ: 2.01 (1Η, m), 2.32 (3H, s), 2.46-2.57 (3H, m), 2.82 (3H, s), 2.89 (2Η.π), 2.97 (1H, n), 3.10 (1H, id), 3.35 (2H, m), 3. 6 2 (1H, d, J = 11. 6 ttz), 6.55 (1Η, πι), 6.80 (lH, ni), 6.8 9-6.9 9 (3 H, m), 7.04 (lH, n), 7.18 (1H, m), 9.2 7 (1H , S), 9. 54 (1H, brs), 11 · 0 9 (1H, s)

Mass (FAB): 351 (M * + 1) Elemental analysis C 2 2 Η 2 3N2〇F 'ch3 S03H2 c H NS Calculated value 61.86 6.09 6.27 7.18 Found value 61.77 6.12 6.35 7.43 The following is the same as 2-methyl-4a 〇t- (3-methylphenyl) -10-fluoro-1, 2,3,4,43,5,11,11 &amp; 0-octahydro-6} | -indolo [2,3-§ 〕 Iso-Porphyrin substituted 2-methyl-4a (3-methylphenyl) &gt; -7-fluoro-1,2, 3, 4, 4a, 5, the paper size is universal China National Standard (CNS) A 4 specifications (210x297 male dragon) (Please read the precautions on the back before filling in this page) Binding · Order _ A6 B6 Fifth, the description of the invention (ll, lla / 3-octahydro-6H-P5 Quinoline, 2-methyl-4 act- (3-hydroxyphenyl) -10-fluoro-1, 2,3,4,4a, 5, ll, lla / 9-octahydro-6H-indiig and [2,3-g] isoquinoline; 2-methyl-4aα- (3-methoxyphenyl) -9-fluoro-1,2,3; 4,43,5,11,113 / 9- Octahydro-611-indazolo [2, 3-g] isoquinoline substitution to give 2-methyl-4act- (3-hydroxyphenyl) -9-fluoro-1, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indolo [2,3-g] isoquinoline; with 2-methyl- "〇 (-(3-methylphenyl) -8-fluoro- 1,2,3,4,4 &, 5, 11,11a Zhao-octahydro-6H-indazoline (2, 3-g] isoquinoline substitution to give 2-methyl-4aot- (3-hydroxyphenyl) -8-fluoro-1, 2,3,4,4a, 5, ll, lla / SA hydrogen-6H- Indo- [2,3-g] isoquinoline. Example 9 2-methyl-4aa- (3-methoxyphenyl) -9-bromo-1,2,3,4, 4a, 5, ll , Lla / S -octahydro-6H-ind [1¾ and [2,3-g] isoquinoline 9 (please read the precautions on the back before filling in this page)

(9) Line-Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs, 5,6,7,8,8a; Q-decahydroisoquinoline 250mg and P-bromophenylhydrazine hydrochloride 255mg dissolved in To 3nl of ethanol, add 0.594ml of methanesulfonic acid to the heating and reflux, and reflux for further 1 hour while stirring. After the reaction mixture was cooled to room temperature, 1Qm 1 of a saturated aqueous solution of sodium hydrogencarbonate was added under ice-cooling, and extracted with 10 ml of acetone for 3 times. The organic layers were combined, washed with 5 ml of saturated saline, dried, and concentrated to obtain 474 ng of powder skull. To use chromatography tube [This paper scale is free to use China National Standard (CNS) A4 specifications (210X297 public)] -73- A6 printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs--_B_6___ V. Description of invention ()-_ Silicone : Methanol-Ambient-28% ammonia = 2.5: 97.5: 0.1 ~ 5.0: 95.0: 0.1] This powder was separated and purified to obtain the title compound of 348nig (yield 89.5%). IR (KBr) cm- 1: 34 1 2, 2 9 38, 1580, 1466, 1446 HMR (CDC 1 3) 5 0 0MHz 5: 2.09 (^, 0), 2.23 (1H, m), 2.43 (3H, s), 2.5 0-2. 5 3 (2 Η, π), 2.7 3-2.89 (4H, ι), 3.01 (lH.ni), 3.09 (1H, d, J = 15.3Hz), 3.68 (3H, s), 6.63 (1H, dd, J = 7.9Hz, J = 1.8Hz), 6.93-6.95 (2H, m), 7.09-7.16 (3H, n), 7.49 (lH, d, J = 1.8Hz), 8.21 (lH, brs)

Mass (m / e): 424 (M *) The following is replaced by 3-bromophenyl trap to 4-bromophenylhydrazine to give 2-methyl-4aa- (3-methoxyphenyl) -8-bromo -l, 2,3,4,4a ', 5, ll, lla / 9-octahydro-6H-indolo [2,3-g] isoquinoline and 2-methyl-4aa- (3-methyl Oxyphenyl) -10-bromo-l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-indo [2,3-g] isocyanate; The substitution of phenyl will give 2-methyl-4a〇t_ (3-methylphenyl) -7-bromo-1,2,3,4,43,5,11,113 / 3-octahydro-611- Indoline [2,3-g] isoquinoline. Example 10 2 -methyl-4 a α-(3 -xiangphenyl) -9 -mo-1,2,3,4, 4 a, 5,11, lla / S-octahydro-6H-indhu And [2,3-g] isoquinoline 10 Η (please read the precautions on the back before filling out this page)

The size of this paper is printed in Chinese National Standard (CNS) Grade A (210X297); -74- 3u16〇4 A6 B6 V. Description of invention () Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs under the envelope of argon Combine 2-methyl-4act- (3-methylphenyl) -9-bromo-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-611-indolino [ 2,3- |] isoquinoline 248.5mg and potassium-t-butoxide 296mg dissolved in 5ml of anhydrous 1) 11 ?, after adding 1-propanethiol 0.248111, stirring at 1401 [: 5.5 hours. The reaction mixture was cooled to room temperature. After distilling off the DMF, a saturated aqueous solution of sodium bicarbonate was added, and extracted 3 times with 20 ml of nitroform: methanol = 5: 1¾¾¾. The organic layers were combined, washed with IGbI saturated saline, dried and concentrated to give a powder of 2 08 nig. This powder was suspended in 1 ml of methanol. Methanesulfonic acid was added to form methanesulfonate, which was separated and purified by chromatography tube [Sephadex-LH-2 0; methanol] to obtain the title compound methanesulfonate 9 6ng (yield 32.4%). IR (KBr) cm-1: 3390, 1584, 1468 HMR (DMS〇-d 6) 5 0 0 MHz δ: 2.00 (1H, m), 2.33 (3H, s), 2.54- 2.68 (3H, ra), 2.82 (3H, d, J = 4.9Hz), 2.84- 2.98 (3H, n), 3.09 (lH, d, J = 15.9Hz), 3.33-3.44 (2H.b), 3.61 (1H, d, J = 12.2Hz), 6.54 (lH, dd, J = 7.9Hz, J = 1.8Hz), 6.87 (1H, s) 6.91 (lH, d, J = 7.9Hz), 7.04 (lH, t, J = 7.9Hz) , 7.08 (1H, dd, J = 8.5Hz, J = 1.8Hz), 7. 1 6 (1H, d, J = 8.6Hz), 7.52 (1H, d, J = 1.8Hz), 9.26 (lH, s ), 9.51 (1H, brs), 10.87 (lH, s) Mass (FAB): 411 (M * +1) Elemental analysis m 〇Br 'CH3S03H C H N Br S calculated value 54.44 5. 36 5.52 15.75 6.32 ( Please read the precautions on the back before filling out this page) 装 ·-线 · This paper is used in a national standard (CNS) A 4 specifications (210 &gt; &lt; 297 male dragon :) -75-

Fifth, the description of the invention () _ measured value 54. 24 5.58 5.37 15.35 6. 6 1 (please read the precautions on the back before filling this page) The following is the same as 2-methyl-4aa- (3-methoxyphenyl ) -10-Bromo-1 '2,3,4,43,5,11,113; 3-octahydro-6} 1-indo [2,3-8] isoquinoline substituted 2-methyl- 4a α-· (3-methylphenyl) -9-bromo-1,2,3,4,4a, 5, ll, lla; 8-octahydro-6H-indBg and [2,3-g] Isoquinoline gives 2-methyl-4 aa- (3-hydroxyphenyl) -10-bromo-1,2,3,4,4a, 5, ll, lla / S-octahydro-6H-indpg And [2,3-g] isoquinoline; 2-methyl-4aα- (3-methoxyphenyl) -8-bromo-1,2,3,4,43,5,11,11 company / 3-octahydro-611-indo [2, 3 ~ g] isoquinoline substitution to give 2-methyl-4aa- (3-hydroxyphenyl) -8-bromo-1, 2,3,4, 4a, 5, ll, lla; Q-octahydro-6H-D5IH2 and [2,3-g] isoquinine: 2-methyl-4act- (3-methylphenyl) -7-bromo-1 , 2,3,4,4a, 5, 11,11a /?-Octahydro-6H-indopodo [2,3-g] isoquinoline substitution to give 2-methyl-4act- (3-hydroxyl Phenyl) -7-bromo-1,2,3,4,4a, 5, ll, lla> 9-octahydro [2,3-g] isoquinoline. · Example 11

Printed by Beigong Consumer Cooperative of Central Bureau of Standards of the Ministry of Economic Affairs, 35 mg of sodium hydrogenate (60% mineral oil suspension) was washed with 2nl of anhydrous THF under argon and then suspended in 2ml of anhydrous hexamethylammonium phosphate (HMPA) , Drop 2-methyl-4aa- (3-methoxyphenyl) -1,2,3,4,4a, -76- in this paper, instead of using Chinese National Standard (CNS) A4 specifications (210 torr) 297 male dragon) V. Description of the invention (Λ 6 B6 5,11,113 / 3-octahydro_611-1151 entangled [2,31] isoquinoline 13811 ^ anhydrous HMPA 3nl solution, stirred at room temperature for 5 hours, Methane iodide 0.2b1 in anhydrous HMPA 4.8π1 solution was added dropwise to this reaction mixture. • It was further stirred at room temperature for 16 hours. 5nl of water was added to the reaction solution and extracted twice with ethyl acetate 10π1. The organic layers were combined Wash with saline • Dry, and concentrate to obtain 1.85g of oil. Use a chromatographic tube [silica gel: methanol: atmospheric imitation: 28% atmospheric water solution. = 2. 5: 97.5: 0.1 ~ 5.0: 95.0: 0.1] Separate and refine this oil to obtain 125ng of the title compound (yield 87.0%) (please read the precautions on the back before filling out this page) Beigong Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs IR (liquid film method) 011 ^ 2938, 1607, 1580, 1470 HMR (CDC 1 3) 5 0 0MHz δ: 2.23 (1Η, π), 2.33 (1Η, m), 2.47 (3H, s),-2.50 (lH, s), 2.74- 2.87 (3H, id), 2.95-3.02 (3H, m), 3.14-3. 17 (2H, n), 3.51 (3H, s), 3.69 (3H, s) , 6.65 (lH, m), 7.01-7.07 (3H, n〇, 7.11 (2H, n), 7.19 (lH, d, J = 7.9Hz), 7.44 (lH, d, J = 7.9Hz) Mass (jn / e): 360 (M *) Same as 2-methyl-4aa- (3-methoxyphenyl) -9-methyl-1,2, 3,4,4a, 5, ll, lla / 3 -Octahydro-6H-indolo [2,3-g] isoquinoline substituted 2-methyl-4aa- (3-methoxyphenyl) -1,2,3,4,4a, 5, ll, lla / S -octahydro-6H-indeno [2,3-g] isoquinoline to give 2-methyl-4; methoxyphenyl) -9-methyl-1,2,3,4,4a, 5,11, lla / 3 -octameric [2,3-g] isoquinoline; with 2-methyl-4acx-(3-methylphenyl) -8-methyl-1,2,3, 4,43,5,11,113 / 3-octahydro-611-ind | 18- [2,3-ming] isoquinoline substitution to give 2-methyl-4aa- (3-methoxyphenyl)- 8-Methyl-Τκίβ, ρΕεs-f ji Binding · Order _ This paper scale is easy to use Chinese S family standard (CNS) A 4 specifications (210X297; St) V. Description of invention (A 6 Β6 Ministry of Economy Central Standards Bureau Employee consumption cooperation Printed by the company 1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro- '© 1 ^ humo [2,3-6; 1 isoquinoline; 2-methyl-4acc -(3-methoxyphenyl) -7-methyl-1,2,3,4,4a, 5,11,113 Lu-octahydro-611-ind05- [2,3-2] isoxaline substitution, To give 2-methyl-4aa- (3-methylphenyl) -7-methyl-1,2,3,4,4a, 5,11, lla / 3-octahydro-6-methyl-ind 11¾ And [2,3-g] isoquinoline: 2-methyl-43〇 (-(3-methylphenyl) -9-chloro-1,2,3,4, ", 5,11,113 / 3-octahydro-6H-indazolo [2,3-g] isoquine_ substituted to give 2-methyl-4aa- (3-methoxyphenyl) -9-gas-1,2,3, 4,4a, 5,11,11a / 3-octahydro-6-methyl-indeno [2, 3-g] isoquinoline; with 2-methyl-4act-(3-methoxyphenyl) -8-nitrogen-1,2,3,4,43,5,11,113 / 3-octahydro-6 {1-indazolo [2,3-g] isoquinoline substituted to give 2-methyl -4acc- (3-methoxyphenyl) -8-amino-1,2,3,4,4a, 5, ll, lla / 3 -octahydro-6-methyl-indolo [2,3- g] Isoquinine; with 2-methyl-4act-(3-methylphenyl) -7-gas-1, 2, 3, 4, 4 &amp;, 5, 11, 11 lines / 3-octahydro- 611-Embrane 112 and [2,3-dan 3 isoquinoline substituted to give 2-methyl-4aa- (3-methoxyphenyl) -7-chloro-1,2,3,4,4a, 5, 11, 11a call-octahydro-6-A -Indo [2,3-g] isoquinoline; 2-methyl-4aa- (3-methylphenyl) -9-bromo-1,2,3,4,4a, 5, ll, lla / S-octahydro-6H- vermis US and [2,3-g] isoquinoline substituted to give 2-methyl-4aa- (3-methylphenyl) -9-bromo-1,2,3 , 4,4a, 5,11, lla / 9-octahydro-6-methyl-ind P5- [2,3-g] isoquinoline; with 2-methyl-4act-(3-methoxyphenyl ) -8-Bromo-1,2,3,4,4 &amp;, 5,11,113) 3-octahydro-6} 1-indo [2,3-g] isoquinoline to give 2- Methyl-4acx- (3-methylphenyl) -8-bromo-1, 2,3,4,4a, 5, ll, lla / S-octahydro-6-methyl-indodecene [2 , 3-g] isoquinoline; with 2-methyl-4a〇t- (3-methoxyphenyl) -7-bromo-1,2,3,4, (please read the notes on the back before filling in This page) Installed * tT_ This paper uses the Chinese National Standard (CNS) A4 specifications (210x297 mm) _ 78-A6 printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs ___B6___ V. Description of invention () _ 4a , 5, ll, lla called-octahydro-6H-indico [2,3-g] isoquinoline substituted to give 2-methyl-4aa- (3-methylphenyl) -7-mo-1 , 2,3,4,4a, 5,11, llayS-octahydro-6-methyl-indo [2,3-g] isoquinoline; with 2-methyl -4aa- (3-methylphenyl) -9-gas-1, 2,3,4,4a, 5, ll, lla / S-octahydro-6m | Bg and [2,3-g] isoquine Substitution of phenanthroline gives 2-methyl-4act- (3-methylphenyl) -9-fluoro-1,2, 3,4,4a, 5, 11, 11a / 9 -octahydro-6-methyl- Zhaodolo [2, 3-g] isoquinoline; with 2-methyl-4act- (3-methoxyphenyl) -8-fluoro-1,2,3,4,43,5,11,113 / 8 -Octahydro-6} | -indino [2,3-g] isoquine_ substituted to give 2-methyl-4act- (3-methoxyphenyl) -8-fluoro-1, 2,3, 4,43,5,11,11 &amp; Lu.-octahydro-6-methyl-indeno 112 [2,3 · ^] isoquinoline; with 2-methyl-4aa- (3-methylphenyl ) -7-fluoro-1,2,3,4,43,5,11,113 cold-octahydro-611-ind segment and [2,31] isoquinoline substituted to give 2-methyl-4aa- (3- Methoxyphenyl) -7-fluoro-1,2,3,4,4a, 5,11,11azhao-octahydro-6-methyl-〇5 | BS and [2,3-g] . If 2-cyclopropylmethyl-4aa- (3-methylphenyl) -l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6H-indus (2, 3-g] isoquinoline to give 2-cyclopropylmethyl-4 act- (3-methoxyphenyl) -l, 2,3,4,4a, 5, ll, lla / S-octahydro- 6-methyl-indazol [2,3-g] isoquinoline; using 2-cyclopropylmethyl-4aa-(3-methoxyphenyl) -9-methyl-1,2,3, 4,4a, 5,11,11a / 3-octahydro-SH-two | sacred [2,3-g] isosleep shower, to give 2-cyclopropylmethyl-4a〇t-(3-methoxy Phenyl) -9-methyl-l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6-methyl-indo [2,3-g] isoquinoline; use 2-cyclopropylmethyl-4aα- (3-methylphenyl) -8-methyl-1,2,3,4,4a, 5, ll, lla / β-octahydro-6H-l¾l indole 〔2,3-g〕 Isoquinoline, 2-cyclopropylmethyl-4aa-(3-methoxy (please read the precautions on the back before filling out this page) Standard (CNS) A 4 specifications (210x297 mm) A 6 B6 Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of invention ()-. Phenyl) -8-methyl-1,2,3, 4,43,5,11,11 &amp; / 3-octahydro-6-methyl-0? | PS and [2,3-g] isosialin; use 2-cyclopropylmethyl-4aa-(3 -Methylphenyl) -7-methyl-1,2,3,4,43,5,11,113 / 5-octahydro-611-indino [2,3-g] isoquinoline, 2-Cyclopropylmethyl-4aa-(3-methoxyphenyl) -7-methyl-1,2, 3,4,4a, 5, 11,11a Lu-octahydro-6-methyl-ind And [2,3-g] isoquinoline; using 2-cyclopropylmethyl-4aa- (3-methylphenyl) -9-nitro-1,2,3,4,43,5,11,113; 3-octahydro-61 ^ ind11deco [2,3-g] isoquinoline to give 2-cyclopropylmethyl-4aa- (3-methylphenyl) -9-chloro-1,2, 3,4,4a, 5,11,1 la / S -octahydro-6-methyl-indolo [2,3-g] isoquinoline; use 2-cyclopropylmethyl-4aa- (3 -Methoxyphenyl) -8-gas-1,2,3,4,43,5,11,113 / 9-octahydro-6} 1-indazolo [2,3-8] isosleep_, To obtain 2-cyclopropylmethyl-4a〇t- (3-methylphenyl) -8-nitro-1,2,3,4,4a, 5,11,11a-octahydro-6-methyl -IndHg [2,3-g] isoquinoline; using 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -7-ambient-1,2,3, 4,43,5 , 11,113 / 3-octahydro-611-ind118 [2,3-2] isoquinoline to give 2-cyclopropylmethyl-4aa- (3-methylphenyl) -7-nitrogen-1, 2,3,4,4a, 5, 11,113; 3-octahydro-6-methyl-indolo [2,3-name] isoquinoline; use 2-cyclopropylmethyl -4ac (-(3-methylphenyl) -9-bromo-1,2,3,4,4a, 5, ll, lla / S-octahydro-6H-indodecano [2,3-g 〕 Isoquinoline to give 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -9-bromo-1,2,3,4,4a, 5, ll, lla / 8 -octahydro- 6-Methyl-IndPg- [2,3-g] isoquinoline; use 2-Chenpropylmethyl-4aa- (3-methylphenyl) -8-bromo-1,2,3,4 , 4a, 5, ll, lla Lu-octahydro-6H-indazolo [2,3-g] isoquinoline to give 2-cyclopropylmethyl-4 act- (3-methylphenyl)- 8-tan-1, 2,3,4,4 & 5,11,113 / 9- octahydrobenzine standard 8 national standard (CNS) A 4 specifications (210 father 297 gong) -80- (Please read the precautions on the back before filling in this page) 装 · _ A 6 B6 ^ 〇1G〇4 Fifth, the description of the invention ()--6-methyl-indolo [2, 3-g] isoquinoline ; Using 2-cyclopropylmethyl-4a α- (3-methylphenyl) -7-bromo-1,2,3,4,4a, 5, ll, lla / 9-octahydro-6H-ind Indo [2,3-g] isoquinoline, to give 2-cyclopropylmethyl-4aα- (3-methylphenyl) -7-bromo-l, 2,3,4,4a, 5, ll, llayS-octahydro-6-methyl- «I benzo [2,3-g] isoquinoline; use 2-ethylpropylmethyl-4aa-(3-methoxyphenyl) -9-fluoro -1,2,3,4,43,5,11,113> 3- Hydrogen-611-indo [2,3-g] isoquinoline gives 2-cyclopropylmethyl-4act- (3-methylphenyl) -9-fluoro-1,2,3,4, 43,5,11,118-octahydro-6-methyl-indo [2,3-g] isoquinoline; using 2-cyclopropylmethyl-4aa-(3-methylphenyl) -8 -Fluoro-1,2,3,4,43,5,11,11 Kai / 8-octahydro-6} 1-indole 8 and [2, 3-g] iso-sleep, get 2-cyclopropyl Methyl-4aa- (3-methoxyphenyl) -8-fluoro-1,2,3,4,43,5,11 &gt; 118) 3-octahydro-6-methyl-ind , 3-Rong] isoquinoline; using 2-cyclopropylmethyl-4aa-(3-methoxyphenyl) -7-fluoro-1,2,3,4,43,5,11,113 / 9-octa Hydrogen-611-indodecino [2,31] isoquinoline to give 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -7-fluoro-1,2, 3,4,43 , 5,11,118 cold-octahydro-6-methyl-indo [2,3-2] isoquinoline Ο Example 12 2 -methyl-4 aa-(3 -xiangphenyl) -1, 2 , 3,4,4 a, 5, 11, 11 a / 3 -octahydro-6-methyl-indo [2,3-g] isoquinoline 12 (Please read the notes on the back before filling in This page) Outfit · Printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

This paper scale is used in the national standard (CNS) A4 specifications (210x297 male dragons) for the ease of use of the paper scale -81- Λ 6 B6 Printed by the Cooperative Society of the Central Standards Bureau of the Ministry of Economic Affairs V. Invention description ()-Under argon 2-methyl-4aa- (3-methylphenyl) -1,2,3,4,4 3,5,11,113 / 3-octahydro-6-methyl-indole [2,3- Ming] Isoquinoline 118 ng and potassium-t-butanol llOag are dissolved in 2η1 anhydrous DMF, 1-propanethiol is added to 0.11! 11. After the mixture was stored at 14010 for 3.5 hours, it was cooled to room temperature. DMF was removed under reduced pressure, 1 ml of saturated aqueous sodium hydrogensulfonate solution was added, and extracted twice with 20 ml of chloroform. The organic layers were combined, washed with saturated brine, dried and concentrated to obtain 120 mg of powder. Suspend this powder in methanol of Ini, add methanesulfonic acid to form methanesulfonate, and purify it with a chromatography tube [Sephadex, LH-20; methanol] to obtain 97.5 mg of the title compound as methanesulfonate ( Yield 67.7%). IR (KBr) cni- 1: 3 386, 29 3 6, 27 18, 1 60 1 NMR (DMS0-ds) 5 0 0MHz 5: 2. 0 6 (1H, m), '2. 3 2 (3 H , ill), 2.54-2.57 (2H, m), 2.65 (lH, m), 2.83 (3H, s), 2.85 (1Η, π), 2.90 (1Η, π), 3.00 (1Η, π), 3. 27-3 · 41 (3Η, π), 3.52 (3H, s), 3.63 (1Η, π), 6.55 (lH, dd, J = 7.9Hz, J = 1.8Hz), 6.94-6.9 9 (3Η, π), 7.04- 7.07 (2Η, m), 7.30 (1Η, d, J = 8.6 Hz), 7.37 (lH, d, J = 7.3Hz), 9.28 (1Η, $), 9.53 ( lH, brs) Mass (FAB): 347 (M * + 1) Elemental analysis C23HasNa〇.CH3S03H 0.5H2〇 C HNS calculated value 63.83 6.92 6.20 7.10 found value 63.87 7.05 6.61 7.40 The same as below 2-Methyl-4aa- (3-Methoxyphenyl) -9-Methyl- This paper scale is free to use Chinese National Standard (CNS) A4 specifications (210x297 male dragon) -82- (Please read the notes on the back first Please fill in this page again) </ S ^ lC〇4 Λ 6 B6 Printed by the Ministry of Economic Affairs Central Standards Bureau Beigong Consumer Cooperative. V. Invention Instructions () _ l, 2, 3, 4, 4a, 5, ll , lla / 3 -octahydro-6-methyl-indole 51- [2,3-g] isoquinoline substituted 2-methyl-4a〇t- (3-methoxyphenyl) -1,2, 3,4, 4a, 5, ll, lla-octahydro_6- -Indolo [2,3-g] isoquinoline to give 2-methyl-4aa- (3-hydroxyphenyl) -9-methyl-1, 2,3,4,4a, 5, ll, llazhao-octahydro-6-methyl-indox [2,3-g] isoquinoline; with 2-methyl-4aα- (3-methylphenyl) -8-methyl-l, 2 , 3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-indo [2,3-g] isosialyl substitution to give 2-methyl-4aa- (3-hydroxyl Phenyl) -8-methyl-1,2,3,4,4a, 5, 11,11 a / 9-octahydro-6-methyl-indo [2,3-g] isoquinoline; To 2-methyl-4act-(3-methoxyphenyl) -7-methyl-1,2,3,4,43,5,11,113 / 5-octahydro-6-methyl-indigo [ 2,3-g] isoquinoline substitution to give 2-methyl-4act- (3-hydroxyphenyl) -7-methyl-1,2,3,4,43,5,11,113 / 3-octahydro -6-methyl 2 indo [2,3-g] isoquinoline; 2-methyl-4aa- (3-methoxyphenyl) -9-bromo-1,2, 3,4,43 , 5,11,113 / 9-octahexa-6-methyl-indo [2,3- 纟] isoquinoline substituted to give 2-methyl-4aa- (3-hydroxyphenyl) -9-bromo- 1,2,3,4,4a, 5, 11, lla / 3 -octahydro-6-methyl-ind P2 [[3,3-g] isoquinoline; to 2-methyl-4aa- (3 -Methylphenyl) -8-bromo-l, 2,3,4,4a, 5, ll, lla cold-octahydro-6-methyl-indo [2,3-g] isoquinoline substitution To give 2-methyl-4aa- (3-hydroxyphenyl) -8-bromo-1,2,3,4,4a, 5, ll, lla / S-octahydro-6-methyl-1¾ 丨And [2,3-g] isoquinoline; 2-methyl-4act- (3-methoxyphenyl) -7-bromo-1,2,3,4,4 pattern, 5,11,11 / 3-octahydro-6-methyl-indazolo [2,3-g] isoquinoline substitution to give 2-methyl-4aa- (3-hydroxyphenyl) -7-bromo-1,2, 3,4,4 in, 5,11,113 / 3-octahydro-^^ yl-ind112 [2,3-g] isoquinoline; with 2-methyl_4aa-(3-methyl ^^ Base) -9- Atmosphere Scales (please read the precautions on the back before filling in this page). Binding · Thread-The paper size is in accordance with the Chinese Standard (CHS) A 4 specifications (210x297 degrees :) -83- V. Description of the invention () Α6 Β6 -l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-6-methyl-indigo Bg and [2,3-g] 2-methyl-4a〇t-(. 3-Xiangphenyl) -9-gas-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-D5 丨Isoquino [2,3-g] isoquinoline; with 2-methyl-4aa- (3-methylphenyl) -8-nitrogen-.1,2,3,4,4a, 5, 11,11a / 3-octahydro-6-methyl-tonne [2,3-g] isoquinoline substitution to give 2-methyl-4aa- (3-hydroxyphenyl) -8-gas-1,2, 3,4., 4a, 5, ll, lla / S-octahydro-6- -Indo [2,3-g] isoquinoline; 2-methyl-4act- (3-methylphenyl) -7-gas-1,2,3,4,43,5,11,118 ) 3-octahydro-6-methyl- (please read the precautions on the back before filling in this page) Indigo [2,3-g] isoquinoline printed by Beigong Consumer Cooperative of Central Bureau of Standards of the Ministry of Economic Affairs, Get 2- $ group-4a &lt; x- (3-hydroxyphenyl) -7-ammonia-1, 2, 3,4,4a, 5, 11, 11a6-methyl-indo (2,3-g 〕 Isoquinoline; 2-methyl-4aa- (3-methoxyphenyl) -9-fluoro-1,2,3, .4, 4a, 5,11, lla / S-octahydro-6- Methyl-indo- [2, 3-g] isoquinoline substitution to give 2-methyl-4aci, (3-hydroxyphenyl) -9-fluoro-1,2,3, 4,4a, 5 , ll, lla / 3 -octahydro-6-methyl-lumbe Bg diiso [2,3-g] isoquinoline; to 2-methyl-4aa- (3-methylphenyl) -8-fluoro -l, 2,3,4,4a, 5, ll, lla / 9-octahydro-6-methyl-D? 丨 Bg and [2,3-g] isoquinoline substituted to give 2-methyl- 4aa- (3-chlorophenyl) -8-fluoro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-indole [2,3-g 〕 Isoquinoline; 2-methyl-4a α-(3 -methoxyphenyl) -7 -fluoro-1,2,3,4, 4 a, 5, 11, 11 a / 3 -octahydro- 6-methyl-indazolo [2., 3-g] isoquinoline To give 2-methyl-4aa- (3-hydroxyphenyl) -7-fluoro-1,2,3,4,43,5,11,113) 9-octahydro-6-methyl-Yuan 112 and [2, 3-g] Isoquinoline. If using 2-cyclopropylmethyl-4aa- (3-methylphenyl) -1,2,3,4,4a, 5, 11, 11a / 3-octahydro-6-methyl-ind P5 In combination with [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa-(3-hydroxyphenyl)--binding · binding.-Line-This paper scale is used in China National Standards (CNS) A 4 specifications (210x297 g) -84- 301654 A6 B6 Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Invention Instructions ()-l, 2,3,4,4a, 5, ll, lla / 3- Octahydro-6-methyl-P5I benzo [2,3-g] isoquinoline; using 2-cyclopropylmethyl-4aa- (3-methylphenyl) -9-methyl-1,2 , 3,4,4 珏, 5,11,113 / 8-octahydro-6-methyl- vermizo [2,3-ming] isoquinoline • 2-cyclopropylmethyl-4aa- (3- Hydroxyphenyl) -9-methyl-l, 2,3,4,4a, 5, ll, llay9-octahydro-6-methyl-P5indo [2,3-g] isoquinoline; use 2-cyclopropylmethyl-4act- (3-methoxyphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl- Indo [2,3-Ren] isoquinoline gives 2-Chenpropylmethyl-4acc- (3-hydroxyphenyl) -8-methyl-1,2, 3, 4,4a, 5, 11,11a / 3 -octahydro-6-methyl-ind Bg and [2, 3-g] isoglucan; use 2-cyclopropylmethyl-4aa- ( 3-methoxyphenyl) -7-methyl-1,2,3,4,43,5,11,113 / 9-octahydro-6-methyl-indene [15! Bi [2,3-ming 〕 Isoquinoline to give 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -7-methyl-1,2,3,4,4a, 5, ll, lla0-octahydro-6- Methyl-¾ 丨 11¾ and [2,3-g] isoquinine; using 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -9-chloro-1,2,3,4, 4a, 5,11, lla / Q-octahydro-6-methyl-ind 11¾ and [2,3-g] isoquinolin, to give 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -9 -Ambient-1,2, 3,4,43,5,11,113 /?-Octahydro-6-methyl-indolo [2,3-rong] isoquinoline; use 2-cyclopropane Methyl- 4aa- (3-methoxyphenyl) -8-chloro-1,2, 3,4,43,5,11,113-octahydro-6-methyl-indolo [2, 3-§] Isoquinoline gives 2-cyclopropylmethyl-4aot- (3-hydroxyphenyl) -8-nitro-1,2,3,4, 4a, 5, ll, lla / 3-octa Hydrogen-6-methyl-〇5 丨 0¾ and [2,3-g] isosialin; using 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -7-chloro-1,2 , 3,4,43,5,11,11 &amp; Zhao-octahydro-6-methyl-indolo [2,3-end] isoquinoline, to give 2-cyclopropylmethyl-4a〇t- (3-hydroxyphenyl) -7-gas-1,2,3,4,4a, 5 (please Read the precautions on the back and then fill out this page) This paper uses the Chinese National Standard (CHS) A4 specifications (210x297 mm) 85- Λ 6 B6 Printed by the Central Bureau of Standards of the Ministry of Economic Affairs, the Consumer Labor Cooperative. )-, Ll, llayS-octahydro-6-methyl-indolo [2,3-g] isoquinoline •, using 2-cyclopropylmethyl-4aa- (3-methoxyphenyl)- 9-Bromo-1,2,3,4,4a, 5,11,11 &amp; / 3-octahydro-6-methyl-115,10-deca [2,3-jun] isoquinoline to give 2- Cyclopropylmethyl-4aa- (3-hydroxyphenyl) -9-bromo-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-indolo [ 2,3-g] isoquinoline; using 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -8-bromo-1,2,3,4,4a, 5,11, lla / 3-octahydro-6-methyl-indeno [2,3-g] isoquinoline to give 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -8-bromo-1,2 , 3,4,4a, 5,11,11a / 3-octahydro-6-methyl-ind Dg- [2,3-g] isoquinoline: using 2-cyclopropylmethyl-4aa- (3 -Tolyl) -7-bromo-l, 2, .3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-B? 丨 Pigolo [2, 3-g] Isoquinoline gives 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -7-bromo-1, 2,3,4,4a, 5, 'll, lla / S-octahydro-6 -A -Indeno [2,3-g] isoquinoline; using 2-cyclopropylmethyl-4act- (3-methoxyphenyl) -9-fluoro-1, 2,3,4,4a, 5, ll, lla / 9-A Hydrogen-6-methyl-indeno [2,3-g] isoquinoline, to give 2-chenpropylmethyl-4a «-(3-hydroxyphenyl) -9- Fluorine-1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl-indigo (2,3-g) isoquinoline; use 2-cyclopropylmethyl-4aa -(3-Methylphenyl) -8-fluoro-1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl-indo [2,3-g] isoquine Porphyrin to give 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -8-fluoro-1,2, 3,4,4a, 5, 11, 11a / 8-octahydro-6-methyl -»51 eye and [2,3- ^] isoquinoline; using 2-cyclopropylmethyl-43〇 [-(3-methylphenyl) -7-fluoro-1,2,3,4, 43,5,11,113 / 3-octahydro-6-methyl-indo [2,3-g] isoquinoline to give 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -7-fluoro-1,2, 3,4,4a, 5, 11, 11a / 3 -octahydro-6-methyl-indene (please read the precautions on the back before filling in this page) . This paper scale uses Chinese National Standard (CNS) A4 specifications (210X297 g *) -86- V. Description of invention () Λ6 B6 and [2,3-g] isoquinoline. Example 13 2-methyl-4aa- (3-methylphenyl) -8-methyl-1,2,3,4,4a, 5, ll, lla; 3-octahydro-6H-indeno [ 2,3-g] isoquinoline 13a and 2-methyl-4acx- (3-methoxyphenyl) -10-methyl-1, 2,3,4,4a, 5, ll, lla

/ 3-octahydro-6H-indDg [2,3-g] isoquinoline 13b Η CH3N

CH-,

(Please read the precautions on the back before filling this page) Outfit · Printed by the Consumer Labor Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (13 a) (13 b) 2-methyl-4aa- (3-methylphenyl) -6-Aero-1,2,3,4,4a, 5,6,7,8,8a decahydroisoquinoline 25 Ong and η-tolyl trap hydrochloride 16〇Bg dissolved in 3b1 ethanol, Methanesulfonic acid 0 · .594β1 was added to the reflux under heating, and the mixture was further refluxed for 1 hour while stirring. After the reaction mixture was cooled to room temperature, 10 mL of a saturated aqueous solution of sodium hydrogenate was added under ice-cooling, and extraction was performed three times with a 10 mL atmosphere. The organic layers were combined, washed with saturated brine, dried and concentrated to obtain 365 mg of oil. This oil was separated and purified using a chromatography tube [silica gel: methanol: gaseous imitation: 28% ammonia = 2.5: 97.5: 0.1 ~ 5.0: 95.0: 0.1] to obtain a mixture of the title compound of 313rag (yield 94.9%). IR (KBr) cn) -1: 3 3 9 0, 2898, 1 60 7, 1580, 14 6 2 NHR (CDC13) 500MHz δ: 1.98 (lH, m), 2.09 (1Η, π), 2.32 (3H, sX2), 2.38 (lH, m), 2.40 (3H, sX2), 2.53- 2.65 (Order-Line-This paper scale uses the Chinese National Standard (CNS) A 4 specifications (210X297)) -87- A 6 B6 5. Description of the invention 3H, m), 2.73 (1h, b), 2.85-2.96 (3H, π), 3.03 (1Η, π), 3.68 (3H, s), 6.61 (lH, m), 6.9 1 (1H, π), 6. 99-7. 10 (4H, m), 7.3Κ1Η, π), 7.47 (1Η, brsX2) Mass (π / e): 360 (Μ *) Ben Shi Example 14 2-A Yl-4aa- (3-hydroxyphenyl) -8-methyl-1,2,3,4,4a, 5, l 1,113 cold-octahydro-611-indodecano [2,3-2] iso Quinoline 143, and 2-methyl-4aa_ (3-hydroxyphenyl) _10_methyl-: ^ 2,3,4,43,5, 11, lla / 3-octahydro-6H-05 丨 11decand [2,3-g] isoquinoline 14b ch3n

ch3

(Please read the precautions on the back before filling in this page) Pack.-Order / Printed by Beigong Consumer Cooperative of Central Bureau of Standards of the Ministry of Economic Affairs (14 a) (14 b) 2-methyl-4aa- ( 3-Methoxyphenyl) -8-methyl-1, 2,3,4,43,5,11,113 /?-Octahydro-6} 1-indhao-8 [〔2,3- 茶〕 isoquinoline With 2-methyl_4aa- (3-methoxyphenyl) -10-methyl-1,2,3,4,4a, 5, 11,113 Lu-octahydro-6 »1-indazolo [2, 3-2] A mixture of isoquinoline 255.3 ng and potassium-t-butane vapor 4 7 7 ng was dissolved in 6 ml of anhydrous DMF. After adding 1-propanethiol 0.4 β1, the mixture was stirred at 140 ° C for 3.5 hours. The reaction mixture was cooled to room temperature, after distilling off DHF, 1 Gnl of a saturated aqueous solution of sodium hydrogensulfonate was added, and the mixture was extracted 3 times with 20® 1 gaseous simulation: methanol = 5: 1 mixed solvent. The organic layers were combined, washed with 1ml of saturated saline, dried and concentrated to obtain 401ing powder. Suspend the powder in 1ml of methanol and add methanesulfonate-line. Use the Chinese National Standard (CNS) A4 specifications (210X297 public goods) for the size of this paper. -88- A 6 B6 V. Description of the invention ()-acid The methanesulfonate was prepared and separated and purified by a chromatography tube [Sephadex, LH-20; methanol] to obtain the title compound methanesulfonate mixture 58ing (yield 18.5%). IR (KBr) c〇-1: 3400, 1601, 1586, 1462 NHR (DMS0-d6) 500MHz δ: 2.0 1 (1H, m), 2.31 (3H, sX2), 2.33 (lH, m), 2.50 (3H , sX2), 2.57 (3H, sX2), 2.78-2.97 (5H, b), 3.05-3'O8 (lH, n), 3.16-3.30 (2H, m), 3.60 (ΙΗ, η), 6.53 (1H , B), 6.79 (1Η, π), 6.89-6.99 (3H, n), 7.01-7.06 (1Η, πι), 7.21 (lH, m), 9.25 (1H, s X2), 9.65 (1H, brsX2), 10.38 (lH, sX2) Mass (FAB): 347 (Mf +1) elemental analysis' CaH〇.0.9CH3S03H. 0.1H * 0 C HNS calculated value 64.68 7.00 6.31 6.50 found value 64.50 6.93 6.62 6.47 (Please read the precautions on the back before filling in this page) Binding, Ordering, and -Line, Printed by the Ministry of Economic Affairs Central Standards Bureau Employee Consumer Cooperative Printed Reference Example 1 2- (2,2,2-Trichloroethane carbonyl) -4aa -(3-methylphenyl) -6-oxo-1,2, 3,4, 4a, 5, 6,7,8,8a; 3-decahydroisoquinoline 15

Dissolve 60ng of proton adsorbent in 2ml of anhydrous dihydrochloride under argon gas. The paper scale is printed in China National Standard (CNS) A4 specification (210Χ297 male dragon) -89- Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs A6 _B_6__ V. Description of the invention ()-_ Alkane, cool to 0 ° C, and add 2,3,2,2-trifluoroethyl azoate 0.03ml. In addition, 2-methyl_4aa_ (3-methylphenyl) -oxo-1,2,3,4,4a, 5,6,7,8,8a> 3-decahydroisoquinoline 5〇 Bg was dissolved in 0.5nl of anhydrous dichloroethane, then dropped into it, stirred at room temperature for 30 minutes, the dichloroethane was removed under reduced pressure, ethyl acetate 3Qid1 was added, washed with 1N hydrochloric acid, water, dried and concentrated to obtain 90mg of oil. This oil was purified by chromatography tube [silica gel; hexane / ethyl acetate (3: 1)] to obtain 73 mg of the title compound (+ yield 9 1.8%). IR (liquid film method) cm1: 1715, 1431, 1 2 4 3, 1125, 754, 717 NMR (CDC 1 3) 4 0 0MHz 5: 1.80 (1Η, m), 2.03 (lH, m), 2.13 (1Η, π〇, 2.26 (1Η, π), 2.31-2.43 (4H, m), 2.85 (1Η, π), 2.96 (lH, d, J = 13. 7Hz), 3.54 (lH, m) , 3.8'l (3H, s), 4.02 (1Η, π〇, 4.18 (1Η, ιπ), 4.71-4.81 (2H, m), δ.75 (1Η, π), 6.95-6.98 (2H, m), 7.25 (lH, m)

Mass (El): 4 3 3 (M〇 Example 15 2- (2,2,2-trichloroethane carbonyl) -43〇1- (3-methoxyphenyl) -1, 2,3,4 , 43,5,11,11 &amp; / 3-octahydro-61 indole pouch [2,3- 豸] isoquinoline 16

Under argon, 2- (2,2,2-triazaethoxycarbonyl) -4aot- (3-jiaben paper scale is used with Chinese sleepy standard (CNS) Jia 4 specifications (210x297 male dragon) -90- (Please read the precautions on the back before filling this page) Outfit · Printed by Beigong Consumer Cooperative of Central Standards Bureau of Ministry of Economic Affairs _BJ5_ V. Description of invention ()-. Gas phenyl) -6-oxo-1,2, 3,4,4a, 5,6, 7,8,8a; S-decahydroisoquinoline 100ng and phenyl trap 25 / u 1 were dissolved in 3ml of ethanol and heated at 80t :. Methanesulfonic acid 0.15b1 was added, and after stirring at 80 ° C for 40 minutes, it was cooled to room temperature. The yeast was removed under reduced pressure, 5 ml of sodium hydrogensulfonate planer and aqueous solution were added, and the mixture was extracted 3 times with 20 ml of gas. The organic layers were combined, washed with saturated brine, dried and concentrated to obtain 130 mg of oil. This oil was purified by chromatography tube [silica gel: hexane / ethyl acetate (3: 1)] to obtain 104 mg of crude crystals, which were recrystallized from ethyl acetate to obtain 60 mg of pure product, BP 197 ~ 198 t (yield 51.3%). IR (KBr) cm-1: 3410, 1707, 1441, 1245 1127, 752 NMR (CDC 13) 400MHz 5: 1.84 (1H, td, J = 13.ZHz, 3.9 Hz), 2.38- 2.4 6 (2H, m ), 2.88-3.03 (4H, m), '3.11 (1H, d, J = 14.7Hz), 3.48 (lH, m) 3.68 (3H, s), 4.11 (lH, m), 4.28 (lH, m) , 4.72-4.82 (2H, n), 6.65 (1Η, ιπ), 6.9 9-7.02 (2H, ra), 7.05-7. 14 (3H, m), 7.21 (1Η, π), 7.44 (1Η, π), 7.60 (1 Η, π) (Please read the precautions on the back before filling this page)

Mass (El): 5 06 〇T) Elemental analysis C 2 B Η 2QCl3H203 C Η Ν Cl calculated value 59. 13 4.96 5.52 20.94 found value 59.12 5. 14 5.54 20.70 The same, if using P-toluene trap instead of benzene Based on the well, 2- (2,2, 2-trifluoroethoxycarbonyl) -4aa- (3-methoxyphenyl) -9-methyl-1,2,3 Standard (CHS) A4 specifications (210x297 g) -91- A6 ___B6__ printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of invention () —. 4,43,5,11,113 /?-Octahydro-6 } 1-Indino [2,3-2] isoquinoline; using 111-tolyl trap to give 2- (2,2,2-trichloroethoxycarbonyl) -4 Oxybenzyl) -8-methyl-1,2,3,4,43,5,11,113 /?-Octahydro-611-8? | Conjugated [2,31] isoquinoline and 2- ( 2,2,2-trifluoroethoxycarbonyl) -4 £ 1〇 (-(3-methoxyphenyl) -10-methyl-1,2,3,4,43,5,11,113; 8 -Octahydro-6H-indolo [2,3-g] isoquinoline; using 〇-methylbenzyl hydrazine to give 2- (2,2,2-trifluoroethane gas carbonyl) -4aot- (3 -Methoxybenzyl) -7-methyl-1,2,3,4,43,5,11,118 / 3-octahydro-611-ind118 [2,3-rong] isobrazide; use 4-gas phenyl trap • Get 2- (2,2,2-triaminoethoxycarboxy) -4aa- (3-methylphenyl) -9-nitrogen-1,2,3,4,43,5,11, .113 / 3-octahydro-69-11 ^ indolo [2,3-g] isoquinoline; using 3-fluorobenzene · hydrazine to give 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-Methoxyphenyl) -8-chloro'-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-〇51tlS- [2,3-g] isoquinoline And 2_ (2 2, 2-triazaethoxycarbonyl) -43〇 (-(3-methoxyphenyl) -10-chloro-1,2,; 3 4,4a, 5, ll, lla / 3- Octahydro-6H-indazolo [2,3-g] isoquine; using 2-chlorophenylhydrazine, 2- (2,2,2-trichloroethoxycarbonyl) -43〇 (-(3_ Methoxyphenyl) -7-chloro-1,2,3,4,43,5,11,113 / 3-octahydro-6} 1__115 丨 | 12 and [2,3-g] isoquinoline; use 4-Bromophenyl trap, to get 2- (2,2,2-Ξ gas ethyl gas carbonyl)-"^-(3-methoxyphenyl) -9-bromo-1,2,3,4,4315, ll, lla / 3 -octahydro-6H-indazolo [2,3-g] isoquinoline; using 3-mophenylphenylhydrazine to give 2- (2,2,2-trichloroethoxycarbonyl)- 4aa- (3-methoxyphenyl) -8-mo-1,2,3,4,43,5,11,113 / 3-octahydro-6} 1-indazol [2 3-5] iso Quinoline and 2- (2,2,2-trifluoroethoxycarbonyl) -43〇 (-(3-methylphenyl) -1〇-mo-1,2,3,4, 43,5,11,113 / 9-octahydro-611-〇5 丨 1 ^ (Please read the precautions on the back before writing this page) Binding-Order.

Printed by the Central Standards Bureau of the Ministry of Economic Affairs, M Industry and Consumer Cooperatives A 6 B6 V. Invented clever ()-and [2,3-g] isoquinoline; using 2-bromophenylhydrazine, 2- (2,2, 2-trihelium gas affinity group) -4act- (3-methoxyphenyl) -7-bromo-1,2,3,4,4a, 5, 11, lla / 3 -octahydro-6H-indB2 And [2,3-g] isoquinoline; using 4-nitrophenylhydrazine, to give 2- (2,2,2-triazide carboxy) -4aa- (3-methyl phenyl) -9 -Nitro-1,2,3,4,43,5,11,113 /?-Octa.hydrogen-611-〇5 丨 [1decor [2,3-g] isoquinoline; use 3-nitro Based on the basic stupid trap, 2- (2, 2, 2-tri. Nitrogen carbonyl) -4aa- (3-methylphenyl) -8-nitro-1,2,3,4,4a, 5 , Ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline and 2- (2,2,2-triaminoethoxycarbonyl) -4aa- (3-methoxybenzene Radicals) -10-nitro 3,4,4 &amp;, 5,11,11 ug / 3-octahydro-611-tonne [.2,31] isoquinoline; using 2-nitrophenylhydrazine, In order to get 2- (2,2,2-trifluoroethoxycarbonyl) -4aa_ (3-methoxyphenyl) -7-nitro-1,2,3,4,4 &amp;, 5,11,113 / 3 -Eight gas_6 [2,3-g] isoquinoline; using 1-methyl-1-phenyl trap to give 2_ (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methyl Oxyphenyl) -1,2,3 , 4,43,5,11,113 / 8-octahydro-6-methyl-indole 5- [2,3- forget] isoquinoline; using 1,1-diphenylhydrazine, 2- (2, 2,2-trichloroethoxycarboxy) -4ac {-(3-methoxyphenyl) -l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-6-phenyl, t Ning [2,3-g] isoquinoline. Example 16 2-cyclopropylcarbonyl-4act- (3-methylphenyl) -1,2,3,4,4a, 5, ll, lla / 3 -octahydro-6H-indeno '[2, 3-g] Isoquinoline 17 (Please read the precautions on the back before filling out this page) Binding · Ordering-This paper uses the Chinese National Standard (CNS) A 4 specifications (210x297; il :) • 93- A7 B7 V. Description of invention ()

Under argon, convert 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxyphenyl) -1,2,3,4,43,5,11,11 &amp; / 3 -Octahydro-611-11indo [2,3-g] isoquinoline 100 mg was dissolved in 2 ml of acetic acid, and 130 mg of zinc powder was added, and stirred at room temperature for 22 hours. After removing zinc by filtration and removing the acid under reduced pressure, 5 ml of a saturated aqueous solution of sodium hydrogen acid was added, extracted with K20 ml of chloroform three times, 6 combined organic layers, washed with saturated saline, dried and concentrated under argon Dissolve 50mg of the mixture in 5ml of anhydrous dichloromethane, add triethylamine 60wl and cyclopropane chloroform 35 // 1, and stir at room temperature Matters needing attention before filling this page) hours. Dichloromethane was removed under reduced pressure, 5 ml of a saturated aqueous solution of sodium hydrogen phosphate was added, and extraction was carried out 3 times with 20 ml of chloroform. The organic layers were combined, washed with saturated brine, dried and concentrated to obtain 65 mg of oil. This oil was purified by silica gel tube [silica gel; chloroform-chloroform / methanol &lt; 99/1)] to obtain 55 mg of crude crystals. This crude crystal was recrystallized from chloroform_hexane to obtain 37ing pure product, m.p.247 ~ 249 &quot; C (decomposition) (yield 46.9%). IRiKBrJcm-1: 3408, 3238, 1609, 1582, 1491, 1460 1255, 1228 NMR (CDC13) 500MHz δ: 0.75-0.78 (2H, m), 0.95-1.12 (2H, m)> 1.75-1.87 (2H, m), 2.37-2.48 (2H, m), 2.85 -3.30 (6H, m), 3.68 (3H, s), 4.05-4.72 (2H, br), 6.65 (1H, ιη), 7.01-7. 14 ( 5H, m), 7.22 (1H, d, J = 7.9Hz), 7.44 (1H, this paper scale is applicable to China National Standard (CNS) Α4 specification (210Χ297mm) 94 QPs A7 B7 V. Description of invention (d, J = 6.7Hz), 7.62 (lH, brs) Mass (El): 400 (M4) Elemental analysis CBeHaeNsOii CH calculated value 77.97 7.05 measured value 77.77 7.34 N 6.99 6.64 Ministry of Economic Affairs Central Standards Bureau employee consumption cooperation du printing the same as the following '' S use of gasified propylene to produce 2-propene brewing-4aa- (3_ methoxyphenyl) -1,2,3,4, 4a, 5,11, lla / 3-octahydro-6H-indole And [2,3-g] isoquinoline; using phenyl chloride, to give 2-phenyl acetyl-4act- (3-methoxyphenyl) -1,2,3,4,4 &amp;, 5,11, 113 / 3-octahydro-611-115 | Dolo [2,3-8] isoquinoline; use of phenylacetyl chloride to give 2-phenylacetoyl-4aa-(3-methoxyphenyl) ) _L, 2,3,4,4a, 5, ll, lla ^ 9 -octahydro-6H-Ιβ | indo [2,3-g] isoquinoline; With ethyl chloride, 2-ethano-4aa- (3-methoxyphenyl) -1,2,3,4,43,5,11,113 / 8-octahydro-611-indolo [2, 3-g] Isoquinoline; using propyl chloride to give 2-propanyl_4aa-(3-methoxyphenyl) -1,2,3,4,4a, 5,11, lla / 3-octa Hydrogen-6Η-ΙβΙ indo [2,3-g] isoquinoline; using butanyl chloride to give 2-butanyl-4aa-(3-methoxyphenyl) -1,2,3,4,43 , 5,11,11 &amp;; 8-octahydro-611-indazolo [2,31] isoquinoline; using 2-bromophene carbonyl chloride to give 2-thipancarbonyl_4aa-(3-methoxybenzene Radical) -1,2,3,4,43,5,11,11 &amp; / 3-octahydro-611-11indo [2,3-8] isoquinoline; using pentamethylene gas gives 2- Pentyl-4aa-(3-methoxyphenyl) -1,2,3,4,4 &amp; 5,11,118 / 3-octahydro-611-indolo [2,3- £] iso Quinoline; using 2-furfuryl chloride to obtain 2-furfuryl-4act- (3-methoxyphenyl) (please read the precautions on the back before filling this page)

J The size of this paper is applicable to China National Standard (CNS) Λ4 specification (210X297mm) -95-95

Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs V. Description of invention () -1, 2, 3, 4, 4 &amp; 5, 11, 113 Na-octahydro-611- vermido [2,3-Dang 〕 Isoquinoline; using cyclobutanecarbonyl chloride to give 2-cyclobutylcarbonyl-4aa-(3-methoxyphenyl) -1,2,3,4,4 pressure, 5,11,113 /?- Octahydro-6} 1-11 bow benzo [2,3-Rong] isoquinoline; using P-toluene gas, 2-P-toluene-4a〇t- (3-methoxyphenyl ) -1,2,3,4,43,5,11,11 £ 1 / 3-octahydro-6} 1-indolo [2, 3-g] isoquinoline; using xylene chloride, 2-xylyl-4aot- (3-methoxyphenyl) -l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-6H-B5 benzo [2,3-g 〕 Isoquinoline; using P-aniline brewing gas to obtain 2- (p-anisyl) -4 &amp; 〇 (-(3-methoxyphenyl> _1,2,3,4,43,5,11 , 11 &amp; cold-octahydro-611-indo [2,3-g] isoquinoline. If 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxybenzene is used Group) -7-chloro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6 ^ 1-indolo [2,3-8] isoquinoline substituted 2- (2 , 2,2-trifluoroethoxycarbonyl) -4aa- (3-methoxyphenyl) -1,2,3,4,4a, 5,11,11a / 3 -octahydro-6Η-Ι ^ 1indole And [2, 3-g Isoquinoline gives 2-cyclopropylcarbonyl-4 aa- (3-methoxyphenyl) _7_ gas-1,2,3,4,43,5,11,113 / 3-octahydro-611-ind Indo [2,3-8] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4act- (3-methoxyphenyl) -8-gas-1,2,3 , 4,4a, 5,11,11 a / 9 -octahydro-6Η-Ιβ | Dolo [2,3-g] isoquinoline, to give 2-cyclopropylcarbonyl-4act- (3-methoxybenzene Radical) _8_ gas-l, 2,3,4,4a, 5, ll, llayS-A hydrogen-611- verendolo [2,31:! Isoquinoline; use 2- (2,2,2-tri Gas ethoxylated base) -4aa_ (3-methoxyphenyl) _9 -chloro-1,2,3,4,4a, 5,11, lla / 9 -octahydro-6Η-ϋζ | Ι® 和 (2 , 3-g] isoquinoline to give 2-cyclopropylcarbonyl-4aot- (3-methoxyphenyl) -9-chloro-1, 2,3,4,4a, 5, ll, lla / 3- Octahydro-611- vermolo [2,31] isoquinoline; use of 2- (2,2,2-trichlorobenzine paper standard is applicable to China National Standard (CNS) A4 specification (210X297mm). ^ 1. 1 nm HI ^^ 1 ^^ 1 --- ^ m HI ^^ 1 In J 々 、? * (Please read the precautions on the back before filling in this page) r &gt;

Description of invention

Excerpt I A7 B7 Five Classics + ▲; [2,3-g] isoquinoline produced by the quasi-authorized shellfish consumer cooperation; use 2_ (2,2.2-trifluoroethoxycarbonyl) -4a〇t _ (3 Monomethoxyphenyl) -10-chloro-1,2,3.4,4a, 5, ll, lla / 3-octahydro-6H-lldolo [2,3-g] isoquinoline, giving 2-ring Propylcarbonyl-4aα- (3-methoxyphenyl) -l0-chloro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indazol [2,31] Isosialoline; use 2- (2,2,2_trifluoroethoxycarbonyl) -4aa_ (3-methoxybenzyl) _7_bromo_1,2,3,4,4a, 5, ll, lla / 3_A Hydrogen-6Η-Ι! ΖΙ is attached to [2,3-g] isoquinoline to give 2-cyclopropylcarbonyl-4act- (3-methoxyphenyl) -7-bromo-1,2,3,4 , 4 lines, 5,11,113 / 8-octahydro-611-1151 benzo [2,3-8] isoquineline, using 2- (2,2,2-trifluoroethoxycarbonyl) -4aa- (3-methoxyphenyl) -8-bromo-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-ll¾- [2,3 '^] isosleepoline, To obtain 2-cyclopropylcarbonyl-4aα _ (3_ methylphenyl) -8-bromo-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-6-oxo-indole [2,3-g] Iso-Porphyrin; use 2- (2,2,2-trichloroethoxycarbonyl) -4act- (3-methoxyphenyl) -9_ desert_l, 2,3,4, 4a, 5, ll lla / S-octahydro-611- 丨 跺 bi [2,3_g] isoprene's 2-cyclopropyl Xiang {yl-4aa-(3-methoxyphenyl) -9-bromo-l, 2 , 3,4,4a, 5, ll, lla / 3 -octahydro-6H -indolo [2,3-g] iso pupillin; use 2- (2,2,2-trifluoroethoxycarbonyl) -4aa- (3-methoxyphenyl) _10_ O-1,2,3,4,4a, 5, ll, lla / S -octahydro-6H-worm bites and [2,3_g] different leaching 2-Cyclopropylcarbonyl_4a α_ (3-methoxyphenyl)-1〇_ Ao_l, 2,3,4,4a, 5, ll, lla / 3-Afi _6} 1_mesh bite [ 2,3-g] isoquinoline * · Use 2- (2,2,2-trichloroethoxyl) -4aa- (3-methoxyphenyl) -7-code-1,2.3,4 , 4 Jue, 5,11, lla / 8-octacrota [2,3-g] isoquineline, to give 2-cyclopropylcarbonyl_4acr _ (3-methoxyphenyl) nitro-l, 2,3,4,4a, 5,11,11a This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (2 丨 297mm) _ --------- ^ installed ------ Order ------ 1¾ I (please read the precautions on the back before filling in this page) A7 B7_________ printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of the invention ()-(2,2,2-trichloro Ethoxycarbonyl) -4aa- (3-methylbenzyl) nitro-l, 2,3,4,4a, 5 , Ll, lla / 9-octahydro-6H-D§ | Indo [2,3_g] iso-line, to give 2-cyclopropylcarbonyl-4aa-(3-methoxyphenyl) nitro_1, 2 , 3,4,43,5,11,11 &amp; / 3-octahydro-611-〇51 indo [2,3-8] iso-lin; use 2- (2,2,2-trifluoroethoxy Carbonyl) -4aa- (3-methylphenyl) -9-nitro-1,2,3,4,48,5,11,113 / 9-octahydro-611-worm bite [2,3_8] isoquine Porphyrin to give 2-cyclopropylcarbonyl-4aa- (3-methylbenzyl) _9_nitro-1, 2,3,4,4 &amp;, 5,11,11 &amp; / 3-octahydro-611- 115 毈 [2,3_8] isoquinoline; using 2- (2,2,2-trifluoroethoxycarbonyl) -4aa- (3-methoxyphenyl) -1〇-nitro-1,2, 3,4,4 &amp;, 5,11,113 / 3-octahexa-6 ^ 1_indolo [2,3-g] isoquinoline to give 2-cyclopropylcarbonyl-4aa-(3-methyl Oxyphenyl) -10-nitro-1,2,3,4,48,5,11,11 &amp; / 3-octa-611-indolo [2, 3-8] isoquinoline; use 2 -(2,2,2-trichloroethoxyethyl)-"〇 {-(3-methoxyphenyl) -1,2,3,4,4a, 5, 11, 11a / 8 -octahydro- 6-methyl-indolo [2,3-g] isoquinoline to give 2-cyclopropylcarbonyl-4a〇 (-(3-methoxyphenyl) -7-nitro-1,2,3 , 4, 4a, 5, 11, 11a / 3 -octahydro-6H-indolo [2, 3-g] iso Lin. If using 2- (2,2,2-trifluoroethoxyethyl) -4a α- (3-methoxyphenyl) -7-methyl-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-D? Iloquino [2,3-g] isoquinoline and acryloyl chloride substituted 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3- Methylbenzyl) -1,2,3,4,4a, 5, ll, lla / Q-octahydro-6H-D5, indo [2,3-g] isoquinoline and cyclopropanecarbonyl chloride, in 2-propenyl-4aa- (3-methoxyphenyl) -7-methyl-1,2,3, 4,43,5,11,11 / 9-octahydro-611-indolo [ 2,3-§] isosialoline; use 2- (2,2,2-trifluoroethoxycarbonyl) _43 «_ (3-methoxyphenyl) -8- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) {Please read the precautions on the back before filling in this page) Order 98 Printed by the Consumer Standard Cooperation Bureau of the Ministry of Economic Affairs of the People's Republic of China V. Description of Invention () Methyl-1, 2, 3, 4, 43.5，11,113 /?-八 气 -611-11 bow | Isoquino [2,31] Isoquinoline and propylene amide gas, to obtain 2-propenyl-4aa- (3_methoxyphenyl) -8-methyl Yl_1,2,3,4,43,5,11,113 / 3-octahydro-611-〇511155 and [2,3-8] isoquinoline; use 2- (2,2,2-trichloroethyl Oxycarbonyl) -43〇 (-(3-methoxyphenyl) -9-methyl-1,2,3, 4,4a, 5, 11, lla / 9 -octakrypton-610¾ indolo [2,3-g] isoquinoline and acryloyl chloride to give 2-propenyl-4aa- (3-methoxyphenyl) _9_ Methyl-1,2,3,4,4a, 5,11,11a cold-octamarin-6 H-indo [2,3-g] isoquinoline; use 2- (2,2,2 -Trichloroethoxycarbonyl) -4aa_ (3-methoxyphenyl) -10-methyl-1,2,3,4,4a, 5,11, lla / 3 -octahydro-6H- vermido [ 2,3-g] Isoquinine and propylene aldehyde gas to give 2-propenyl-4aa- (3-methoxyphenyl) -10-methyl-1,2,3,4,4a, 5, ll , lla; S-octahydro-6H-H-dodo [2,3-g] isoquinoline; using 2- (2,2,2-trifluoroethoxycarbonyl) -4aa- (3-methoxy Phenyl) -7-gas-1,2,3, 4,4 &amp;, 5,11,11hexane / 3-octahydro-6 ^ indo [2,3-dang] isoquinoline and propylene amide gas To give 2-propenyl-4aa- (3-methoxyphenyl) -7-gas-1,2, 3,4,4 &amp;, 5,11,11 &amp; / 8-octahydro-611-indole And [2,3-Dang] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4a〇t- (3-methoxyphenyl) -8-gas-1,2, 3,4,43,5,11,113 /?-Octahydro-6} 1-115 3-methoxyphenyl)-8-chloro-1,2,3,4,4hexane, 5,11,113 / 9-octahydro-6} 1-indolo [2,3-lu] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aot- (3-methoxyphenyl ) -9-chloro-1,2,3,4,4 pressure, 5,11,113 / 3-octahydro-611-indazolo [2,3-g] isoquinoline and propene to produce chlorine to obtain 2-propene Acetyl-4aa- (3-methoxyphenyl) -9-gas-1,2,3,4,4 &amp;, 5,11,11 &amp; / 3-octahydro-61 ^ -indolo [This paper Applicable standards + National Standards (CNS) Α4 specifications (210X297mm) (Please read the precautions on the back before filling this page)

, 1T 99 yy-

Printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs-jL ... Invented and Produced () 2,3-8] Isoquinoline; use 2- (2,2,2-trifluoroethoxycarbonyl) -4 &amp; 0 (-(3-methoxyphenyl) -10-chloro-1,2,3,4,4 &amp;, 5,11,11 &amp; / 3-octahydro-611 -11¾dolo [2,3-g 〕 Isoquinoline and propylene are chlorinated to obtain 2-propenyl-4a α- (3-methoxycoryl) -10-chloro-1, 2,3,4,4a, 5, ll, lla / 9- Octahydro-6 ^ 5 丨 dolo [2,3-8] isoquinoline; using 2- (2,2,2-trifluoroethoxycarbonyl) -4aot- (3-methoxyphenyl) -7- Bromo_l, 2,3,4,4a, 5, ll, ll 3 / 3-octahydro_611-indolo [2,3-8] isoquinoline and propylene gas to give 2-propenyl -4aa- (3-methoxyphenyl) -7-bromo-1,2,3,4,4a, 5,11, lla / S-octadolo [2,3_g] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4 &amp; «-(3-methoxyphenyl) -8-bromo-1,2,3,4,4 &amp;, 5,11,113 / 3-octa Hydrogen-61 indolo [2,3-dang] isoquinoline and propylene acetyl gas to give 2-propenyl-4acx- (3-methoxyphenyl) -8-bromo-1,2,3,4 , 4 &amp;, 5,11,113 / 3-octahydro-611-indolo [2,3-8] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4 &amp; (2 -(3-methoxyphenyl) -9-bromo-1 , 2,3,4,43,5,11,113 / 8-octahydro-611- vermido [2,3-dang] isoquinoline and propylene gas to obtain 2-propenyl-4aa- (3- Methoxyphenyl) -9-bromo-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-611- verendolo [2,3-8] isoquine; use 2 -(2,2,2-trifluoroethoxycarbonyl) -43〇 (-(3-methoxyphenyl) -10-bromo-1.2,3,4,4 &amp;, 5,11,11 &amp; / 3- Octahydro-611-indolo [2,3-g] isoquinoline to give 2-propenyl-4act- (3-methoxyphenyl) _10-bromo-1,2,3.4,4 &amp;, 5 , 11,113 / 3-octahydro-611-indo [2,31] isoxaline; using 2- (2,2,2-trichloroethoxycarbonyl) -43〇 (-(3-methyl gas Phenyl) -7-fluoro-1,2,3,4,43,5,11,113 / 3-octahydro-61 ^ -0 rent 1 ^ and [2,3_ g] isoquinoline and allyl chloride ， Get 2-Acryloyl-4aa- (3-Methoxyphenyl) This paper standard is applicable to China National Standard (CNS) A4 specification (210X297mm) 1001 (please read the notes on the back before filling this page)

S01C04 at ,, _ B7_ V. Description of the invention ()) -7-Fluoro-1,2,3,4,4.5,11,11 &amp; / 3-octahydro-611-1151 indo [2,3 -g] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4acc- (3-methoxyphenyl) -8-fluoro-1,2,3,4,4, 5,11,11 &amp; / 3-octahydro-611-indolo [2,3-g] isoquinoline and acrylamide to give 2-propenyl-4a〇t- (3-methoxyphenyl ) -8-fluoro-l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-6H-n? | Indo [2,3-g] isoquinoline; use 2- (2 , 2,2-trichloroethoxycarbonyl) -4aa- (3-methoxyphenyl) -9-fluoro-1,2,3,4,4a, 5, ll, lla / 3-octaargon-6Η- Ιβ | Dolo [2,3-g] isoquinoline and propylene amide gas to give 2-propenyl-4 a α-(3 -methoxyphenyl) -9 -fluoro-1,2,3,4 , 4 a, 5, 11,11 a -octahydro-6H-ϋζ | dolo [2,3-g] isoquinoline; using 2- (2,2,2-trifluoroethoxycarbonyl) -4aa- (3-methoxyphenyl) -10-fluoro-1,2,3,4,4a, 5, ll, lla / S -octahydro-6H-indolo [2,3-g] isoquinoline and Propylene gas to get 2-propenyl-4aot- (3-methoxyphenyl) -10-fluoro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H- Vermolo [2,3-g] isoquinoline; using 2- (2,2,2-trichloroethyl Carbonyl) -43 «-(3-methoxyphenyl) -7-nitro-1, 2,3,4,43,5,11,113 Lu-octahydro-6! 3-8] Isoquinoline and acryloyl chloride to give 2-propenyl-4aa-(3-methoxyphenyl) -7-nitro-1,2,3,4,43,5,11,113 / 3-octahydro-6 ^ introduction of [2,31] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4act- (3-methoxyphenyl) -8- Nitro-1,2,3,4,43,5,11,113 / 3-octahydro-611-11, benzo [2,3-g] isoquinoline and propene are chlorinated to obtain 2-propenyl -4aa- (3-methoxyphenyl) _8-nitro-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-6} {-11? 丨 Biting [2,3- 8] Isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4 &amp; 〇 (-(3-methoxyphenyl) -9-nitro-1,2,3,4, 4a, 5,11, lla / 3-octahydrogen-This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) (Please read the notes on the back before filling out this page) Printed by the Industrial and Consumer Cooperative 101 Employees ’Consumer Cooperation of the Central Bureau of Standards of the Ministry of Economic Affairs. Du Printed A7 B7 Invention Theory ¥ ()

6H-B? | Dolo [2,3-g] isoquinoline and acryloyl chloride 'give 2-propenyl-4 act- (3-methoxyphenyl) -9-nitro-l, 2, 3,4,4a, 5, ll, lla / 9-A hydrogen-611- 丨 indo [2,3- £] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxyphenyl) -10-nitro-1,2,3,4,4a, 5, ll, lla / 3-octahydro [2,3-g] isoquinoline and propylene Brewing chlorine to get 2-propenyl_4aa- (3-methoxyphenyl) _1〇_nitro_1, 2,3,4,4 &amp;, 5,11,11hexane / 3-octahydrogen -611-11 bow 丨 Chromo [2,3- 纟] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxyphenyl) -1,2 , 3,4, 4 Jue, 5,11,118 / 3-octahydro-611-indolo [2,31] isoquinoline and propylene amide gas to give 2-propenyl-4act- (3-methoxybenzene Radical) -1,2,3,4,4a, 5,11,11 &amp; / 3-octahydro-6-methyl-indo [2,31] isoquinoline. Use 2- (2,2,2-trichloroethoxycarbonyl) -4aa_ (3-methoxyphenyl) -7-methyl-1.2,3,4,4 pattern, 5,11,113 / 3-octahydro- 611-Indino ^^ [2,31] isoquinoline and phenacyl chloride to give 2-phenacyl-4aa- (3-methoxyphenyl) -7-methyl-1,2,3,4, 43,5,11,11 &amp; / 8-octahydro-611-indolo [2,3-8] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aot- ( 3-methoxyphenyl) -8-methyl-1,2,3,4,4hexane, 5,11,11 & / 3-octagas-611-〇 引 1151bi [2,3-g] iso Quinoline and benzylidene chloride to give 2-phenylenyl-4aa- (3-methoxyphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 9-octahydro-611 «1Dolo [2, 3- §] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -43〇 (-(3-methoxyphenyl) -9-methyl- 1,2,3,4,4 pressure, 5,11,113; 3-octahydro-611- vermolo [2,3-g] isoquinoline and phenacyl chloride to give 2-phenacyl-4aot-( 3 -methoxyphenyl) -9-methyl-1,2,3,4,4a, 5, 11, 11a lu-octahydro-6H-indolo [2,3-g] isoquinoline; use 2- (2,2,2-Trichloroethoxycarbonyl basic paper standard universal Chinese national standard (CNS) A4 specification (2 丨 0X297mm) (please read the precautions on the back before filling this page) 1 Ding- &quot; 102 Α7 Β7, .21 η Description of the invention ()) 4 & 〇 (-(3_methoxyphenyl) -ίο-methyl-1, 2,3,4,4a, 5, ll, lla _ Octahydro-6H-P indole [2,3-g] isoquinoline and phenyl acetyl gas to give 2-phenyl acetyl-4act- (3-methoxyphenyl) -ΙΟ-methyl 1,2 , 3,4,4a, 5, ll, lla / 3-octahydro-6Η-Βζ | Isoquino [2,3-g] isoquinoline ', using 2_ (2,2,2-trichloroethoxycarbonyl ) -4act- (3-methoxyphenyl) _7_chloro_1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indolo [2,3-g] iso Quinoline and phenylchloride to give 2-benzyl-4aa_ (3-methoxyphenyl) gas_l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-B5I indole And [2,3-g] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4act- (3-methoxyphenyl) -8-gas-1,2,3, 4,43,5,11,1161 &gt; 3-octa-611-0 bow | 0 «Bomo [2,3-8] isoquinoline and phenacyl chloride to give 2-phenacyl-4aa- (3- Methoxyphenyl) -8-chloro-1,2,3,4,4a, 5,11,113 / 8-octahydro-611-indo [2,3-§] isoquinoline; use 2- (2 , 2,2-trichloroethoxycarbonyl) -43〇 {-(3-methoxyphenyl) -9-chloro-1, 2,3,4,43,5,11,113 / 9-octahydro-6} 11 Gong 丨 Stuck with [2,3-Dang] isoquinoline and benzene gas to get 2-benzene Yl-4aa- (3-methoxyphenyl) -9-chloro-1,2, 3,4,48,5,11,113 / 9-octahydro-6 {1-11 codolo [2,3-8 〕 Isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4 &amp; (1- (3-methoxyphenyl) -10-chloro-1,2,3, 4, 4a, 5, 11, lla; 9-octahydro-6H-05I benzo [2,3-g] isoquinoline and benzoyl chloride to give 2-phenyl acetyl-4aa-(3-methoxyphenyl) -10 -Chloro-1,2,3,4,4 &amp;, 5,11,11 &amp; / 3-octahydro-611- verazo [2,3-lu] isoquinoline; use 2- (2,2, 2-trichloroethoxyzyl) -4aa- (3-methoxyphenyl) -7-bromo-1,2,3,4,43,5,11,113 / 8-octa-6 ()-indole And [2,3-g] isoquinoline and benzene chloride, to give 2-phenacyl-4aa- (3-methoxyphenyl) -7-bromo-1,2,3,4,43,5, 11,11 &amp; / 3-octahydro-6 »1-indolo [2, ---------- 1 I ------, 玎 •-(Please read the notes on the back first (Fill in this page again) The paper standard printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 mm)

Printed by the Ministry of Economic Affairs, Central Bureau of Standards, Shellfish Consumer Cooperation V. Description of the invention () 3-Dang] isoquinoline; use 2- (2,2,2-trifluoroethoxycarbonyl) -4 &amp; (1- ( 3 -methoxyphenyl) -8-bromo-1,2,3,4,4a, 5, ll, lla / 3 -octahydro-6Η-〇ξ | indo [2,3-g] isoquinoline And benzene brewing gas, to obtain 2-phenyl acetyl-4a α-(3-methoxyphenyl) -8-bromo-1,2,3,4,43,5,11,11 Jue / 3-octahydro- 611-Vermolo [2,3-8] isoquinoline; using 2- (2,2,2-trifluoroethoxycarbonyl) -43〇 (-(3-methoxyphenyl) -9-bromo- 1,2,3,4,43,5,11,11 &amp; / 9-octahydro-6 {1 -0¾dolo [2,3-g] isoquinoline and benzene brewing gas to give 2-benzyl -4acc-(3-methoxyphenyl) -9-bromo-1,2,3,4,4a, 5, ll, lla / 3 -octahydro-6Η-0ξ | indo [2,3-g] Isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxyphenyl) -10-bromo-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6Η- ^ B5ί [2,3-g] isoquinoline and benzoyl chloride to give 2-phenyl acetyl-4a α- (3-methoxyphenyl) -10-bromo- 1,2,3,4,4a, 5,11, lla / 3-octahydro-611-indolo [2,3-8] isoquinoline; use 2- (2,2,2-trichloroethane Oxycarbonyl) -4act- (3-methoxyphenyl) -7-fluoro-1,2,3,4, 4a, 5, 11 , 11 a / 9 -octahydro-6Η-Βζ | Isoquino [2,3-g] isoquinoline and benzoyl chloride to give 2-phenyl acetyl-4act- (3-methoxyphenyl) -7- Fluorine-1,2,3,4,4a, 5, ll, lla / 8-octahydro-6H-B bowed 〖[2,3-g] isoquinoline; use 2- (2,2,2 -Trichloroethoxy pin group) -4aot_ (3 -methoxyphenyl) _8 -fluoro_l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-Dindo [ 2,3-g] isoquinoline and benzene chloride, to give 2-phenyl acetyl-4acx- (3-methoxyphenyl) -8-fluoro-1,2,3,4,4a, 5,1 1 , 1 la / 3 -octahydro-6H-B-indo [2,3-g] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxy Phenyl) -9-fluoro-1,2,3,4,43,5,11,11 &amp; / 3-octahydro-61 ^ indolo [2,31] isoquinoline and benzoyl chloride to give 2 -Benzyl-4aa- (3-methoxyphenyl) -9-fluoro-l, 2,3,4,4a This paper scale applies the Chinese National Standard (CNS) A4 specification (210X297 mm) (please read first (Notes on the back then fill this page)

J Order 104 ι86. 1.

1. Description of the invention (printed by A7 B7,5,11,113 Lu-octahydro-611-11 cited 5! And [2,3-8] isoquinoline by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs; use 2-( 2,2,2-Trifluoroethoxycarbonyl) -4aa- (3-methoxyphenyl) _10 ~ fluoro-1,2,3,4,4 &amp;, 5,11,11 &amp; / 9-octahydro- 6 ^ 11Introduction of isoquinoline [2,3_8] isoquinoline and benzene chloride to give 2-phenylacetate-4aa- (3-methoxyphenyl) _10_fluoro_1,2,3,4,43, 5,11,113 / 3-octahydro-6 ^ Bang Shuo [2,3-8] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3- Methoxyphenyl) -7-nitro-1,2,3,4,4a, 5,11, lla ^ S -octahydro-6Η-Ιβ | 跺 和 [2,3-g] isoquinoline and Benzene gas gives 2-phenylacetate-4act- (3-methoxyphenyl) -7-nitro-1,2,3,4,4 &amp;, 5,11,11 &amp; / 3-octahydro- 611-115 (Isoquino [2,3-8] isoquinoline; use 2- (2,2,2-trichloroethoxyethyl) -4aot- (3-methoxyphenyl) -8-nitro -1,2,3,4,4a, 5, 11, 1U / 3 -octahydro-6Η-ϋζ | indolo [2,3-g] isoquinoline and benzene chloride to give 2-phenylacyl_ 4aa- (3-methoxyphenyl) -8_nitro-1,2,3,4,4hexane, 5,11,113 / 9- 八 氲 _611-11? 丨 Hehe [2,3-8] Iso-Porphyrin; use 2- (2,2,2- Trichloroethoxycarbonyl) -43 (1-(3-methoxyphenyl) -9-nitro-l, 2,3,4.4a, 5, ll, lla / S-octahydro-6H-B¾B¾ 和 〔 2,3-g] isoquinoline and phenyl acetyl chloride to give 2-phenyl acetyl-4aα- (3-methoxyphenyl) -9-nitro-l, 2,3,4,4a, 5, ll , lla / S-octahydro-6 Ha-indo [2,3-g] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aot- (3-methoxyphenyl ) -10-Nitro-1,2,3,4,4a, 5,11, 11a / 3 -octahydro-611-11¾-indo [2,3-g] isoquinoline and benzyl chloride to give 2 -Benzyl-4aa- (3-methoxyphenyl) -10-nitro-1,2,3,4,4a, 5,11, lla / 3-octahydro-6H-D bowdo [ 2,3-g] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxyphenyl) -1,2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl- veroxolo [2,3-g] isoquinoline and phenoxychloride This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) (please (Read the notes on the back before filling this page)

105 tr. 1¾ 丄 id A7 B7 Fifth, the invention description (printed by the employee consumer cooperative of the Central Standards Bureau of the Ministry of Economic Affairs, obtained 2-phenyl acetyl-4act- (3-methylphenyl) -1,2,3,4, 4a, 5,11,1 lays -octahydro-6-methyl-indolo [2,3-g] isoquinoline; use 2- (2,2,2-trifluoroethoxycarbonyl) _4aa- ( 3-methoxyphenyl) -7-methyl-1,2,3,4,4 &amp;, 5,11,11 &amp; / 3-octahydro-611-indolo [2,3-8] isoquine Phenanthroline and phenethyl acetyl chloride to give 2-phenyl ethyl acetyl-4aa- (3_methoxyphenyl) -7-methyl-1, 2,3,4,43,5,11,113 / 8-octahydro- 611-Indo [2,3-name] isoquinoline; using 2- (2,2,2-trifluoroethoxycarbonyl) -43 «-(3-methoxyphenyl) -8-methyl- 1,2,3,4,4 &amp;, 5,11,11 &amp; / 3-octahydro-6 »1-indolo [2,3-g] isoquinoline and phenethyl chloride to give 2-benzene Acetyl-4act-(3-methylphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 3-octahydro-611-ind 1 «pyro [2.31] isoquin Porphyrin; using 2- (2,2,2-trifluoroethoxycarbonyl) -43〇 (-(3-methoxyphenyl) -9-methyl-1,2,3, 4, 4a, 5, 11 , 1 la / 3 -octahydro-6 Η-indolo [2,3-g] isoquinoline and phenethyl acetyl chloride to give 2-phenyl ethyl acetyl-4a cx- (3-methoxyphenyl) -9-methyl-l, 2, 3,4,4a, 5, ll, lla / 3-octahydro-611-indolo [2,31] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4acx- (3-methoxyphenyl) -10-methyl-1,2,3,4,4a, 5, II, lla / 3-octahydro-6H-a? | Dolo [2,3-g] iso Quinoline and styrene are used to produce 2-phenylethylacetate-4aa- (3-methylphenyl) -10-methyl-1,2,3,4,4 3,5,11,11 &amp; / 3-octahydro-611-11, benzo [2,3-8] isoquinoline; using 2- (2,2,2-trifluoroethoxycarbonyl) -43〇 (-(3-methoxybenzene Radicals) -7-gas-1, 2,3,4,4a, 5,11.lla / S-octahydro-6H-B entangled with [2,3-g] isoquinoline and styrene, In this way, 2-phenethylacetate-4a α-(3-methoxyphenyl) -7-chloro-1,2,3,4,43,5,11.113 / 9-octahydro-611-indolo [2 , 31] Isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4act_ (3-methoxyphenyl) This paper scale applies the Chinese National Standard (CNS) A4 specification (210 X 29? Mm ) (Please read the notes on the back before filling this page)-* Γ -106-

V. Description of the invention () A7 B7) -8-chloro-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-611-1151 indo [2,3-S] isoquine Phenanthroline and phenethyl chloride to give 2-phenylethyl acetyl-4a〇t- (3-methoxyphenyl) -8-chloro-1,2,3,4,4 &amp;, 5,11,11 &amp;) 3-octahydro-611-1? | 11deca [2,3-8] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -43 «-(3-methoxybenzene Radical) -9-gas-1,2,3,4,4a, 5, l 1,1 la / 3 -octahydro-611-0¾¾ and [2,3-g] isoquinoline and phenethyl chloride, To give 2-phenylethyl acetyl-4aot-(3-methoxyphenyl) -9-chloro-1,2,3,4,4 &amp;, 5,11,118 / 3-octahydro-611-11§ | [2,3-g] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxyphenyl) -10-chloro-1,2,3,4 , 4a, 5, ll, lla; S-octahydro-6H-indolo [2,3-g] isoquinoline and phenethyl chloride to give 2-phenethylacetate-4aa- (3-methoxy Phenyl) -10-chloro_l, 2,3,4,4a, 5, ll, lla / 3 -octahydro-611-1151 indo [2,3-2] isoquinoline; use 2- (2 , 2,2-trichloroethoxycarbonyl) -4aa- (3-methoxyphenyl) -7-bromo-1,2,3,4,4a, 5,1 l, lla / 3 -octahydro-6H -U5 丨 Dolo [2,3-g] isoquinoline and chloroacetin, to give 2-phenethylacetate-4act- (3-methoxyphenyl) -7-bromo -1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indolo [2,3-g] isoquinoline; use 2- (2, 2,2-trichloro Ethoxycarbonyl) -4 &amp; 〇 (-(3-methylphenyl) -8-bromo-1,2,3,4,43,5,11,11 &amp; / 9-octahydro-611-indolo [2,3-Ming] isoquinoline and phenethyl chloride to give 2-phenylethyl-4aa-(3-methoxyphenyl) -8-bromo-1,2, 3,4,4 &amp;, 5,11,113 / 3_octahydro-611-11indo [2,3-dan] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3-methoxy Phenyl) _9 -bromo-1,2,3,4,43,5,11,11 &amp; / 3-octahydro-611-〇introduction [2,3-dang] isoquinoline and phenethyl chloride , To get 2-benzyl acetyl-4aa-(3-methoxyphenyl) -9-bromo-1,2,3,4, 4a, 5, 11, lla / 3 -octahydro-6H-indolo 〔2,3-g This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) (please read the notes on the back before filling this page). Printed by the Ministry of Economic Affairs Central Standards Bureau Negative Work Consumer Cooperative 107 A7

V. Description of the invention () Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economics] Isoquinoline; using 2- (2,2,2-trifluoroethoxycarbonyl) -4a〇t- (3-methoxyphenyl) -10-Bromo-1,2,3,4,4a, 5,11, lla3 -octahydro-6H-ιβ 丨 indo [2,3-g] isoquinoline and phenethyl chloride 'get 2_foo Acetyl_4a〇t- (3-methoxyphenyl) -10-bromo-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-B¾ indo [2, 3-g] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4act- (3-methoxyphenyl) -7-fluoro-1, 2,3,4,4a, 5, ll, lla々-A Hydrogen-6H- vermolo [2,3-g] isoquinoline and styrene gas to obtain 2-phenylethyl acetyl-4act- (3-methoxyphenyl)- 7-fluoro-l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-B5 | II [2,3-g] isoquinoline; use 2- (2,2,2, 2-trichloroethoxyl) -43〇 £ _ (3-methoxyphenyl) _8_fluoro-1,2,3,4,4 ugly, 5, 11,113 cold-octahydro-6 ^? | 18 And [2,3-Dang] isoquinoline and phenethyl chloride, to obtain 2-phenethylacetate-4aa- (3-methoxyphenyl) -8-fluoro-1,2,3,4,4a, 5, 11, lla / 3 -octahydro-6H-D? | I® and [2,3-g] isoquinoline; use 2- (2, 2,2-trichloroethoxyxiang (yl) -4aa -(3-methoxyphenyl -9-fluoro-1,2,3,4,43,5,11,113 / 3-octa-611-115 丨 bite [2,3-8] isosialoline and phenethyl chloride to give 2-benzene Acetoyl-4aa- (3-methoxyphenyl) -9-fluoro-1.2, 3,4,4 &amp;, 5,11,113 / 3-octahydro-611-0indo [2,3-5] Isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4 &amp; «-(3-methoxyphenyl) -10_fluoro_1.2,3,4,43,5,11, 113 / 3-octahydro-6 ^ 8 items are combined with [2,3-8] isoquinoline and phenylethyl chloride to give 2-phenethylacetate-4aa-(3-methoxyphenyl) -1〇 -Fluoro-1,2,3,4,43,5,11,11 pressure-octahydro-611-ton 1 ^ (2,3 1) isoquinoline; use 2_ (2,2,2-tris Chloroethoxycarbonyl) -43〇- (3-methoxyphenyl) -7-nitro-1,2,3,4,4, 5,11,113 / 3-octahydro-611-indolo [2 , 3-g] isoquinoline and phenethyl chloride, to obtain 2-phenylethyl acetyl-4aot- This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) Fill in this page)

-108-A7 __B7__ —_____ printed by the Employees ’Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, 15th, Invention Instructions () (3-methoxyphenyl) -7-nitro-1,2,3,4,4a, 5 , 11,1 la / 3 -octahydro-6 HO? | 0g and [2,3-g] isoquinoline; use 2- (2,2,2-trichloroethoxycarbonyl) -4aa- (3- Methoxyphenyl) -8-nitro-1,2,3,4,4a, 5,11,11 a / 9 -octahydro-6H- vermolo [2,3-g] isoquinoline and benzene Acetyl chloride gives 2-phenylethyl-4aa- (3-methoxyphenyl) -8-nitro-1,2,3,4,4a, 5, ll, lla / S-octahydro-6H -U-indolo [2,3-g] isoquinoline; use 2- (2, 2,2-trifluoroethoxycarbonyl) -4act- (3-methoxyphenyl) -9-nitro-1 , 2, 3,4,43,5,11,11 &amp; / 3-octahydro-611-11? 1 indo [2,3-8] isoquinoline and phenethyl acetyl gas to give 2-phenyl ethyl acetyl -4act-(3-methoxyphenyl) -9-nitro-1,2,3,4,43,5,11,113 / 9-octahydro-611-indolo [2,3- £ 〕 Isoquinoline; using 2- (2,2,2-trifluoroethoxycarbonyl) -4aa- (3-methoxyphenyl) -10-nitro-l, 2,3,4,4a, 5, ll, lla; 8-octahydrodolo [2,3-g] isoquinoline and phenethyl chloride to give 2-phenylethyl acetyl-4aa-(3-methylphenyl) -10-nitro- 1,2,3,4,43,5,11,11 &amp; / 3-Eight -611-indolo [2,3-8] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -43〇 (-(3-methoxyphenyl) -l, 2 , 3,4,4a, 5, ll, lla / 3-octahydro-6-methyl- | l¾-indo [2,3-g] isoquinoline and phenylethyl chloride, to give 2-phenylethyl acetyl -4aα-(3-methoxyphenyl) -l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl-Bdolo [2,3-g] isoquine Example 17 2-Cyclopropylmethyl-4aa- (3-methoxyphenyl) -1,2,3,4,4a, 5, ll, lla; S-octahydro-6H-D5U5I and [ 2,3-g] Isoquinoline 18 This paper scale is in accordance with Chinese National Standard (CNS) A4 specifications (2〗 OX297mm) n-ml — ^ n nn HI — ^ ϋ · nv gas ^ Ί (please read the back first (Notes to fill out this page) -109-A6 ^ 〇1C〇4_2! Fifth, the invention description ()-

V

Lithium aluminum hydride 6Bg was suspended in 1 ml of anhydrous THF under argon, cooled to Ot :, and added 2-cyclopropylcarbonyl-4 a β-(3 -methoxyphenyl) -1,2,3, 4, 4a, 5, ll, lla々-octahydro-6H-indo [2,3-g] isoquinoline 20mg. After warming to room temperature and stirring for 1 hour, it was cooled to ΟΌ, and a saturated aqueous solution of ethyl acetate and sodium potassium tartrate was added. Over oil [After removing insoluble materials, ethyl acetate was removed under reduced pressure to obtain a 20 nig oil. This oily substance was purified with a chromatography tube [Silicon H; chloroform-methanol / 28% ammonia / aeroform (3: 0.1: 97)] to obtain 18 mg of the title compound (yield 93.2%). This compound was recrystallized from chloroform-hexane to obtain l〇Bg pure product (mP163.5 ~ 165.51C). IR (KBr) cm-1: 2928, 2900, 2842, 1607 1580 Ministry of Economic Affairs Central Standards Bureau #Cooperative, printed &amp; (please read the notes on the back before filling this page) NMR (CDC 1 3) 400HHz δ: 0.11 (2H, m), 0.52 (2H, m), 〇.91 (lH, m ), 1.99-2.10 (2H, m), 2.24-2.35 (2H, m), 2.38 ~ 2.41 (1H, m)> 2.58_2.67 (2H, m), 2.88-3.03 (4H, m), 3.07 (lH, d, J = 15.6Hz), 3.19 (lH, m), 3.67 (3H, s), 6.61 (7.01-7.10 (5H, ib), 7.20 (lH, m), 7.43 (1H, m), 7.66 (lH, brs)

Mass (m / e): 386 (M *) elemental analysis C "H3〇Nd

C Η N This paper is suitable for Sichuan National Standards (CNS) Grade 4 (210X297 mm) -110- Ministry of Economic Affairs Central Standard f- 局 员 消 # Cooperative Society Seal &quot; A6 _B6 V. Description of invention ()-. Calculation Value 80.79 7.82 7.25 Measured value 80.11 7.76 7.19 The following is the same, using 2-propenyl-4acx- (3-methylphenyl) -1, 2, 3, 4, 43, 5, 11, 113 / 3- Octahydro-6 (1-indolo [2,3-8] iso-line substituted 2-cyclopropylcarbonyl-4aot- (3-methylphenyl) -1,2,3,4,4a, 5 , 11,113-octahydro-611-ind 11-decano- [2,3-8] isoethroline to give allyl-4aot- (3-methylphenyl) -1,2,3,4 , 43,5,11,113; 3-octahydro-61 {丨 眹 [2,3-g] isoquinoline; using 2-phenylacyl-4aa- (3-methylphenyl) -1,2, 3,4,48,5,11,113 / 3-octahydro-611-indolo [2,3-pyr] isoquinoline to give 2-benzyl-4aa- (3-methyl gas. Phenyl) -1,2,3,4,4a, 5,11,113 cold-octahydro-611-ind'115- [2,3-8] isoquinoline; use 2-phenylethylaceto-4aa- (3 -Methoxyphenyl) -l, 2:, 3,4,4a, 5, ll, lla / 3-octahydro-6H-indolo [2,3-g] isoquinoline to give 2-phenylethyl Base-4act- (3-methylphenyl) .- 1, 2,3,4,48,5,11,113 / 3-octaargon-61 1-tono [2,3-g] isoquinoline; use 2-acetaldehyde-4act- (3-methylphenyl) -1, 2,3,4,48,5,11,113 points -Octahydro-6 ^ 1-indolo [2,33] isoquinoline to give 2-ethyl-4aot- (3-methylphenyl) -1,2,3,4,4a, 5,11 , 11a / 9 -octahydro-[[· 3ι] isoquinoline; using 2-propionaldehyde-4a a-(3-methylphenyl) * ~ l, 2,3,4,4a, 5, ll, lla &gt; 3-octa-gaso [2,3-g] isoquinoline, to give 2-propyl-4aot- (3-methylphenyl) -I, 2,3,4,43.5,11,113 ) 3-octahydro-611-indazolo [2,31] isoquinoline; using 2-butyryl-4aot- (3-methoxyphenyl) -1,2,3,4,4a.5, II, 113 cold-octahydro-611-1? Isoquino [2,3-8] isoquinoline to give 2-butyl-4 aa- (3-methylphenyl) _1,2,3,4 , 48,5,11,113 / 8-octahydro-611- (please read the precautions on the back before writing this page). Install · Order · Line · ―This paper is suitable for Chuanzhong® s (CNS) Ψ4 ( 210x297 ^^ :) -111- ^ 01064 A6 B6 V. Description of the invention () I. Indole [2,3-g] isoquinoline; use 2-copperyl-4aa-(3-methylbenzene Group) -1,2,3,4,43,5,11,113 /?-Octahydro-611-indazolo [2,3-g] isoquinoline to give 2-thienyl-4aa- (3-Methylphenyl) -1,2,3, 4.48,5,11,11 valley / 3-octahydro-611-〇5 丨 11dec [2,3-run] isoquinine; use 2 -Pentaldehyde-4act- (3-methoxyphenyl) -1,2,3.4,4a, 5,11,11a Lu-octahydro-6H-indolo [2,3-g] isoquinoline, In order to obtain 2-pentyl-4act-(3-methylphenyl) -l, 2,3,4,4a, 5, ll, lla / S -octahydro-6H-indopor [2,3-g 〕 Isoquinoline; using 2-furfuryl-4act- (3-methoxyphenyl) -I, 2,3,4,43,5,11,113 / 3-octahydro-611-indo [2,3 -8] Isoquinoline, 2-furanmethyl-4act- (3-methoxyphenyl) -1,2,3,4,4a, 5. Ministry of Economic Affairs China National Bureau of Standards Unemployment Cooperation Du Yinli (Please read the precautions on the back first, Cunqiwoben alfalfa) II, lla / 3 -octahydro-6H-H5I Bδ [2,3-g] isoquinoline; use 2-cyclobutyl kiyl-4aa- (3-Methylphenyl) -1,2,3,4,4a, 5,11,11a / 3_ octahydro-6H-indo [2,3-g] isoquinoline to give 2-cyclobutylmethyl Yl-4a α- (3-methylphenyl) -1,2,3,4,43.5,11,113 / 3-octahydro-611-indo [2,3-g] isoquinoline; use 2- (ρ-toluoyl) -4aa-(3-methoxyphenyl) -1,2,3,4,43,5,11,113 cold-octahydro-6 »1-ind 11-do [2, 3- g] isoquinoline, 2- (P-methylbenzyl) -4aa- (3-methoxyphenyl) -1,2.3,4.43,5,11,113 / 3-octahydro-611-indo [2,3-8] iso Quinoline; using 2- (P-anisaldehyde) -4aa- (3-methylphenyl) -1,2,3,4,43,5,11,113 / 3-octahydro-611-indazol [2 , 3-8] isoquinoline to give 2- (4-methoxybenzyl) -4aot- (3-methoxyphenyl) -1,2,3,4,4a, 5, ll, lla / S- Octahydro-6H-D? Isoquino [2,3-g] isoquinoline; using 2-U-anisyl) -4aa- (3-methylchlorophenyl) -l, 2,3,4,4a , 5, ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline, to give 2- (3-methoxybenzyl)-This paper scale is applicable to China National Standards (CNS) Xuan 4 specifications (21〇 father 297 public) -112- C〇4 Α6 Β6 V. Description of invention () Ministry of Economic Affairs Central Standardization Bureau employee consumption cooperation Du printed 43〇 (-(3-methylphenyl)- 1,2,3,4,43,5.11,113 / 3-octahydro-61 {-indazolo [2,3-g] isoquinoline; use 2-cyclopropylcarbonyl-4acx-(3-methyl Gas phenyl) -7-mo-1,2,3,4,43,5,11,113 /?-Octahydro-6 ^ 115 | ophthalo [2,3-g] isoquinoline, giving 2- Cyclopropylmethyl-4aa- (3-methylphenyl) -7-mo-1,2,3,4.43,5, '11, 113 / 5-octahydro-611-indolo [2,3 -8〕 Different_commanded; With 2-cyclopropyl-keto-4aa- (3-methylphenyl) -8_bromo-1,2,3,4,43,5,11,118; 9-octahydro-611-ind 115 (2, 31] Isoquinoline to give 2-cyclopropylmethyl-4acx- (3-methoxyphenyl) -8-bromo-1,2, 3,4,43,5,11,113 Lu-octahydro-611- 1151Dolo [2,3-8] isoquino ;; using 2-cyclopropylcarbonyl-4a〇t- (3-methylphenyl) -9-bromo-1,2,3,4, 43,5 , 11,113 / 3-octahydro.-611-indo [2,31] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl'yl) -9-mo- 1,2,3,4,4a, 5,11 l, lla / 5-octahydro-6H-indolo [2,3-g] isoquinoline; use 2-ethylpropylcarbonyl-4aa- (3 -Methylphenyl) -10-bromo-1,2,3,4,4a, 5,11,11a-octahydro-6H-indazolo [2,3-g] isoquinoline to give 2- Cyclopropylmethyl-4aot- (3-methylphenyl) -10-bromo-1,2,3,4,4a, 5, ll, lla / 9-octahydro-6H-indazol [2, 3-g] Isoquinoline. Use 2-propenyl-4a a-(3-methoxyphenyl) -7-methyl-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indolo [2,3-g] isoquinoline, to give 2-allyl-4acx- (3-methylphenyl) -7-methyl-1,2,3,4,43,5,11,118 / 3-octahydro-611-indolo [2,3-g] isoquinoline; using 2-propenyl-4a a- (3-methoxyphenyl) -8-methyl-1,2,3 , 4,43,5,11,113 / 8-octahydro-611-1151 indo [2,3-g] isoquinoline to give 2-allyl-4aot- (3-methylphenyl) -8- Methyl-1,2,3,4,43,5,11,113 / 3-octahydro-6 [1-indoxo [2,31] {Please read the precautions on the back before filling this page)- Installed • Ordered. Margin. This paper is suitable for the Chinese National Standard (CNS) f 4 specifications (210 father, 297 gong) -113 · V. Description of the invention (Institute of the Ministry of Economic Affairs, Central Standards Bureau, Employee and Consumer Cooperative A6 B6 Isoquinoline; using 2-acryloyl-4acx- (3-methylphenyl) -9-methyl-1,2,3,4,43,5,11,113-octahydro-611-ind Imagine [2,3-8 :) isoquinoline to give 2-allyl-4act- (3-methoxyphenyl) -9-methyl-1,2,3,4, 43,5,11 , 113 / 3-octahydro-611-indolo [2,31] isoquinoline; using 2-propenyl-4aa- (3-methylphenyl) -10-Methyl-1,2,3,4,4a, 5, ll, lla ling-octahydro-6H-D? Isoquino [2,3-g] isoquinoline to give 2-allyl -4aa- (3-methoxyphenyl) -10-methyl-1,2,3,4,4a, 5,11,11a Zhao-octahydro-6H-P? 丨 Pg 和 〔2,3-8 :] Isoquinoline; using 2-propenyl-4 act- (3-methylphenyl) -7-chloro-1,2,3,4,4a, 5,11, lla / 3-octa- 6H-indazolo [2,3-g] isoquinoline to give 2-allyl-4aa- (3-methylphenyl) -7-ambient-1,2,3,4,43,5, 11,113 / 0-octahydro-611-indyl [2,3-g] isoquinoline; using 2-propenyl-4acc- (3-methylphenyl) -8-chloro-1,2, 3,4,43,5,11,113 / 3-octahydro-61 {-indolo [2,3-8] iso-commanded to give 2-allylpropyl-4aa- (3-methylphenyl ) -8-chloro-1,2,3'4,43,5,11,113 /?-Octahydro-611-indazolo [2,31] isoquinoline; use 2-acryloyl-4aa- (3 -Methoxyphenyl) -9-gas-1,2,3,4,4a * 5, n, lla々-octahydro-6H-I? 丨 Dizzyl [2,3-g] isoquinoline 2-allyl-4aot- (3-methoxyphenyl) -9-gas-l, 2,3,4,4a, 5, ll, lla valley-octahydro-6H-indazolo [2,3 -g] isoquinoline; using 2-propenyl-4 aa- (3-methoxyphenyl) -10-gas-i, 2,3.4,4a, 5, ll, lla / 3-octahydro-6H -Indo [2,3-g] isoquinoline to give 2-allyl-4acc- (3-shenqiphenyl) -1〇-gas-1,2,3,4,43,5, 11,113 / 9-octahydro-611-1151 feed and [2,3-g] isobrazide; use 2-propionic enzyme-4aa- (3-methylphenyl) -7-bromo-1, 2,3,4.43,5,11,113 / 3-octahydro-611-inconjugation [National Standard of China (CNSVP4 Specification (210x297mm) —in

Printed by the Ministry of Economic Affairs of the Central Bureau of Standards and Technology of the Ministry of Consumer Affairs ^ A6 __B6 __ ^ Five 'Invention Description ()-. 2,3_g] Isosomal shower, get 2_ 似 propyl_4aa_ (3_ 甲 气 phenyl) -7- O-1,2,3,4,43,5,11,113 / 9-octahydro-611-indo- [2,3-8] isosporine; use 2-acryloylase-4aa- (3 -Methylphenyl) -8-bromo-1,2,3, 4,43,5,11,113 / 3-octahydro-611-indolo [2,3-8] isoquinoline to give 2 _ ene Propyl-4_aa- (3-methylphenyl) -8-bromo-1,2,3,4,4a, 5,11,1 la / 3 -octahydro-6H-P5 丨 benzo (2,3 -g] isoquinoline; using 2-propenyl-4aa- (3-methylphenyl) -9-bromo-1,2,3,4,4a, 5, ll, lla / 3-octahydro- 6H-indazolo [2,3-g] isoquinoline gives 2-allyl-4aa- (3-methylphenyl) -9-bromo-1,2,3,4,4a, 5, 11,11a / 3 -octahydro-6H-indigo [2,3-g] isoquinoline; using 2-propenal-4act- (3-methylphenyl) -10-mo-1,2 , 3,4,43,5,11,113 / 8-octa-611-indazolo [2,3-8] isoquinoline,-to give 2-allyl-4a α-(3-methoxy Phenyl) -10-bromo-1,2,3,4,43,5,11,113 ling-octahydro-611-indolo [2,31] isosialoline; using 2-acryloyl-4aot -(3-methoxyphenyl) -7-fluoro-1,2 , 3,4,4a, 5,11,118 Ling-Baqi-611-indo- [2,31] isosalinate, to obtain 2-isopropyl-4aa- (3-methoxyphenyl) -7 -Gas-1,2,3,4,4a, 5,11,11a / 9 -octahydro-6H-indo [2,3-g] isoporoline; use 2-propenyl-4 aa- (3-Methylphenyl) -8-fluoro-1,2,3,4,43,5,11,113 / 8-octaqi-6H-indigo [2,3-g] isoquinoline, giving 2 -Allyl-4aa- (3-methoxyphenyl) -8-fluoro-1,2,3,4,43,5,11,113 / 9-octagas-611-kehebi 〔2,3-g :] Isoquinoline; using 2-acrylic acid-4act- (3-methylphenyl) _9-gas-1,2,3,4.43,5,11,113 / 9-octahydro-611-1151 [2,3-g] isoquinoline, to give 2-allyl-4aot- (3-methylphenyl) -9-gas-1,2,3,4,43,5,11.113 / 3-octa Hydrogen-611-1151 eyes and [2.31] peculiar sleep shower; (please read the precautions on the back side before filling in this page) Interpretation) -115- A 6 B6 Printed by the Employees ’Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of invention () Use of 2-propenyl-4aa-(3-methoxyphenyl) -10-fluoro-1,2, 3,4,4a, 5,11,113 / 8-octa-611-115 | Dolo [2,3- 】 Isoquinoline, 2-allyl-4 &amp; «-(3-methylphenyl) -10-fluoro-1,2,3,4,4 &amp;, 5,11,114 / 3-octa Hydrogen-6H-indazolo [.2,3-g] isoquinoline. Use 2-propionaldehyde-4aa- (3-methylphenyl) -7-methyl-1,2,3,4, 4a, 5, 11,11a /?-Octahydro-6H-indBg and [ 2,3-g] isoquinoline to give 2-benzyl-4aa- (3-methoxyphenyl) -7-methyl-1, 2, 3, 4, 4a, 5, 11, lla / S- Octahydro-6H-indPg and [2,3-g] isoquinoline; use 2-propionyl-4aa- (3-methoxyphenyl) -8-methyl-1, 2,3,4, 43,5,11,113 / 3-octahydro-6} 1-indino [2,3-8] isoquinoline to give 2-benzyl-4aa-(3-methoxyphenyl) -8-methyl -1,2,3,4, 4a, 5, ll, lla / S-octahydro-6H-ind [2,3-g] isoquinoline; use 2-phenyl acetyl- 4 &amp; σ- (3- Methoxyphenyl) -4aa- (3-methylphenyl) -9-methyl-1,2, 3,4,43,5,11,11 &amp; / 9-octahydro-611-indolo [ 2,3-glycoside] isoquinoline to give 2-benzyl-4aa-(3-methoxyphenyl) -9-methyl-1,2, 3,4, 4a, 5,11, lla / 3- Octahydro-6H-indazolo [2,3-g] isoquinoline; using 2-phenylacyl-43〇 (-(3-methylphenyl) -10-methyl-1,2,3, 4,4 &amp;, 5,11,113 Lu-octahydro-6H-indolo [2,3-g] isoquinoline to give 2-benzyl-4aa- (3-methoxyphenyl) -10- Methyl-1,2,3,4,43,5,11,113 / 3-octahydro-6} 1-1) 5 丨 118- [2,3-g] isoquinoline; 2-phenyl acetyl -4acc- ( 3-methylphenyl) -7-chloro-1,2,3,4,43,5,11,113 called-octahydro-611-ind0 Rong [2,3-§] isoquinoline, in 2-benzyl-4aa-(3-methoxyphenyl) -7-gas-l, 2,3,4,4a, 5, ll, lla / 3 -octa-6H-indeno 〔2,3- g] Isoquine;; using 2-phenylacyl-4 &amp; 〇 &lt;-( 3-methylphenyl) -8-chloro-1,2,3,4,43,5,11,11 &amp; / 3 -Octahydro-6H-0? 丨 Isoquino [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methyl gas benzene (please read the precautions on the back before filling this page) · Order _ This paper scale uses the Chinese National Standard (CNS) A4 specifications (210x297 male dragons) 116 Printed A6 _B6__ by the Employees ’Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention ()-. Base) -8-chloro- 1,2,3,4,43,5,11,113 / 3-octahydro-611-ind ^ [2,3-g] isoquinoline: using 2-phenylacryl-4aa- (3- Methoxyphenyl) -9-amino-1, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-indeno [2,3-g] isoquinoline, giving 2- Benzyl-4a α-(3-methoxyphenyl) -9-nitro-1,2, 3, 4, 4a, 5, 11, lla; S-octahydro-6H-indBg (2, 3- g] Isoquinoline; using 2-phenylacryl-4aa-(3-methoxyphenyl) -10-chloro--1,2, 3,4,4a, 5,11, 11a / 9-octahydro- 6H-indhuo 〔2, 3-g] isoquino_, to give 2-benzyl-4aa- (3-methylphenyl) -1〇-gas-1,2,3,4,43,5,11,113 / 3-octahydro-611 -Indo [2,3-g] isoquinoline; using 2-phenylacryl-4act- (3-methoxyphenyl) -7-bromo-1,2,3,4,43,5,11 , 11 &amp; / 9-octahydro-6} 1-indino [2,3-§] isoquinoline, to give 2-benzyl-4act- (3-methoxyphenyl) -7-bromo-1, 2,3,4,4a, 5, ll, lla / S -octahydro-6H-indolino [2,3--g] isoquinoline; using 2-phenylacyl-4 &amp; 〇 (-(3 -Methoxyphenyl) -8-bromo-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-6H-ind 11¾- [2,3-g] isoquinoline to give 2- Benzyl-4aa- (3-methylphenyl) -8-bromo-1,2,3,4,4a, 5, 11,11a /?-Octahydro-6H-indazol [2, 3-g 〕 Isoquinoline; using 2-phenylacryl-4aa- (3-methoxyphenyl) -9-bromo-1,2,3,4,43,5,11,113 / 3-octahydro-6} 1-Indo [2,3-2] isoquino, to give 2-benzyl-43〇 [-(3-methoxyphenyl) -9-mo-1,2,3,4,43,5 , 11, lla / 3 -octahydro-6H-indazolo (2, 3-g) isoquinoline; using 2-phenylacetyl-48〇 [-(3-methoxyphenyl) -1〇-mo -1,2,3,4,43,5,11,113 /?-八 气-6Η-〇5 | Ι1δ and [2,3-g] isoquino, get 2-section group-4aa- (3-A Gas phenyl) -10- -1,2,3,4,43,5,11,11 Uzhaozhao-octahydro-6 ^ 丨 02 [2,3-g] isoquinoline; use 2-phenylacetyl-4aa- (3- Methoxyphenyl) -7-fluoro-1, 2, 3,4,48,5,11,113 / 3-octahydro-6H-¢ 41 and [2, 3-g] different (please read the notes on the back first (This page will be written on this page again.) Packed * This paper is used in accordance with Chinese National Standard (CNS) A4 specifications (210x297 g *) 117 S〇1C〇4 A 6 B6 Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs () ~ Quino, get 2-benzyl_4aa-(3-methylphenyl) -7-fluoro-1,2,3,4,4a, 5, ll, lla / 3-octahydro- and [ 2,3-g] isosomal shower gel; use 2-phenyl acetyl-4act- (3-methoxyphenyl) _8-fluoro-1, 2,3,4,4a, 5, ll, lla-octahydrogen -6H-l¾ | fl¾ and [_2,3-g] iso_ order to get 2-benzyl-4aot- (3-methoxyphenyl) -8-fluoro-1,2,3,4,43,5 , 11, 113 points-octahydro-611-indbito [2,3-g] isoblister; use 2_benzene awakenyl-4aa- (3-methoxyphenyl) -9-. Gas-1, 2,3,4,4 &amp;, 5,11,113 / 3-octa-611-indolo [2,3-2] isoquinoline to give 2-benzyl-4aa- (3-methoxyphenyl) -9-fluoro-1, 2,3,4,4a, 5, ll, lla &gt; 3-octahydro-6H-indo [2,3-g] isoquinoline; With 2-phenyl acetyl-4aa-(3-methoxybenzyl) -10-fluoro-1,2,3,4,4a, 5,11,11a Lu-octahydro-6H-indazolo (2 , 3-g] isoquinoline to give 2-benzyl-4a〇t- (3-methoxyphenyl)-: ^-·· ^, 2,3,4,44,5,11,113 ^ 3 ^, · -6 ^ 1 — 1 ^ 1 ^ and [2,3-g] isoquinoline. Use 2-phenylethylacetate-4a〇t- (3-methoxyphenyl) -7-methyl-1,2,3,4,43,5,11,118 / 3-octahydro-6} 1 -Indolino [2,3-g] isoquinoline to give 2-phenethyl-4aa- (3-methoxyphenyl) -7-methyl-1,2,3,4,4 technology, 5,11,113 /?-Octahydro-6} 1-ind11deco [2,3- |] isosleep shower; use 2-phenylethyl acyl-4-acx- (3-methoxyphenyl) -8 -Methyl-1,2, 3,4,48,5,11,113 / 3-octahydro-611-1)? 丨 115bi [2,3-2] isosleep_, to give 2-phenethyl-4aa -(3-methoxyphenyl) -8-methyl-1,2,3,4,4a, 5, ll, lla / S-octahydro-6H-indigo (2,3-g) isoquine Porphyrin; using 2-phenylacetaldehyde--4aa- (3-methoxyphenyl) -9-methyl-1,2,3,4,4a, 5,11,11a Zhao-octahydro-6H-ind 0decor [2,3-g] isoquinoline to give 2-phenethyl-4aa- (3-methylphenyl) -9-methyl-1,2,3,4,4a, 5,11 , lla / S-octahydro-6H-indolo [2,3-g] isoquinoline; use 2-phenylacetaldehyde-4a〇t- (3-methoxy (please read the precautions on the back before (Fill in this page) Installation · Line · This paper standard uses the Chinese National Standard (CNS) A 4 specifications (210x297 public 118 ^ Oic〇4 A6 B6 V. Invention description (Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Phenyl) -1〇-methyl-1,2,3,4,43,5,11,113 / 3-octahydro-611-ind08- [2,3-g] isoquinoline to give 2 -Phenethyl-4a〇t, (3-methylphenyl) -10_methyl-1,2,3,4,4 &amp;, 5,11,118 / 3-octahydro-611-indole [2,3-8] Isoquine; use 2-phenylethyl_S-4aa- (3-methoxyphenyl) -7-gas-1,2, 3,4,43,5,11,113 / 3- Octahydro-611-indodecano [2,3-§] isoquinoline to give 2-phenethyl-4a a-(3-methylchlorophenyl) -7-gas-1,2, 3,4 , 4a, 5, 11, llayS-octahydro-6H-indPg- [2,3-g] isoquinoline; using 2-phenylethylacetoyl-43〇- (3-methylphenyl) -8- Atmosphere-1,2,3,4,43,5,11,113 / 9-octahydro-6H-B? | Pg and [2,3-g] isoquinoline to give 2-phenethyl-4aa- (3 -Tolyl) -8-chloro-1,2,3,4,4 &amp;, 5,11,113 /?-Octahydro-61 ^ ind118 [2,3-g] isoquinoline; use 2- Phenylacetyl-4aa- (3-methylphenyl) -9-chloro-1,2,3,4,4a, 5,11, lla / S-octahydro-6H-B5I eye and [2, 3 -g] isoquinoline to give 2-phenethyl-4aa- (3-methoxyphenyl) -9-gas-1,2,3, 4,43,5,11,113 / 8-octahydro- 61] -Ind118 [2,3-2] isoquinoline; using 2-phenylacetaldehyde- 4aa- (3-methylphenyl) -10- -1,2, 3,4,4a, 5, ll, lla / 3-octazo-6H-d51BJ and [2,3-g] isosleep shower, to get 2-benzyl-43 € (-(3 -Methoxyphenyl) -1〇-atmosphere-1,2,3,4,43,5,11,113 / 3-octazo_6Η-ί3 | [^ 并 [2,3_g] isosalin; use this Naphthyl- 4a〇!-(3-Methylphenyl) -7-bromo-1,2,3, 4,4a, 5, 11,11a /?-Octahydro-6H-indazolo [2,3 -g] Isoquinoline to give 2-phenethyl-4a〇t- (3-methylphenyl) -7-bromo-1,2,3,4,43,5,11,113 /?-octa Hydrogen-6}}-ind ^ [2,3-ju] isoquinoline; using 2-phenethylol-4act- (3-methoxyphenyl) -8-bromo-1, 2,3,4 , 4 &amp;, 5,11,11 over / 3-octah-6} 1-indbito [2,3-ming] iso_shall give 2-phenethyl-4act-(3-methylphenyl) ) -8-Bromo-1,2,3,4,4a, 5, (please read the precautions on the back before filling in this page) 装 ·-訂 _ This paper standard uses Chinese Standards (CNS) A 4 Specifications (210x297 mm) 119 Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A6 _______B6___ V. Description of the invention ()-. Ll, lla; S-octahydro-6H-05 丨 0dec [2,3-g] Isoquinoline; use 2-phenylethyl acetyl-4aa- (3-methoxyphenyl) -9-bromo-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H- P5 The combination of [2,3-g] isoquinoline gives 2-phenylethyl-4ao [-(3-methylphenyl) -9-bromo-1., 2,3,4,43,5,11 , 113> 8-octahydro-611-indo [2,3-g] isoquinoline; using 2-phenylethyl acetyl-4act- (3-methylphenyl) -10-bromo-1,2 , 3,4,43,5,11,113) 9-octahydro-611- | 15 | Lando &amp; 2,3-g] isoquinoline, to give 2-phenethyl-4aa- (3-methylbenzene Radicals) -10-bromo-1, 2,3,4,43,5,11,113 points Hachi gas-611-115 | Iso [2,3-2] isodiffusion.; Using 2-phenylethyl acetyl -4a α-(3-Methoxybenzyl) -7-fluoro-1,2, 3,4,4a, 5, lUlla / 3-octahydro-6H-D? | B Deca 〔2,3-g 〕 Isoquinoline, to give 2-phenethyl-4aa- (3-methoxyphenyl) -7-fluoro-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H- D5 Shuo [2,3-g] isoquinoline; using 2-phenylacetaldehyde ^ laα-(3-methoxyphenyl) -8--1,2,3,4,43,5, 11,113 / 3-octahydro-6} 1-indolo [2,3-g] isoquinoline to give 2-phenethyl-4aa- (3-methoxyphenyl) -8-fluoro-1,2 , 3,4,43,5,11,113 Lu-octahydro-6 (1-indazolo [2,3- |]] isoquinoline; use 2-phenylethylaceto-4a α- (3-methoxybenzene Radicals) -9-fluoro-1, 2,3,4,4 and 5,11,11 and / 3-octahydro-611-ind 115! And [2,3-tin] isoquinoline to give 2- Styrene -4aa-(3-methylphenyl) -9-fluoro-1,2, 3,4,4a, 5, ll, lla / 3 -octa-6H-indazolo [2,3-g] iso Quinoline; using 2-phenylethyl acetyl-4aa- (3-methoxyphenyl) -10-fluoro-1,2,3,4,4a, 5,11, lla / S-octahydro-6H-ind Bg and [2,3-g] isoquinoline to give 2-phenethyl-4a〇t- (3-methylphenyl) -1〇-fluoro-1,2,3,4,43,5, 11,11 &amp; / 3-octahydro-6} 1-indolo [2, 3-g] isoquinoline. Example 18 (Please read the precautions on the back before filling the nest page) Binding · Binding-Thread · This paper scale uses the Chinese National Standards (CNS) A 4 specifications (210X297) "120 ^^ lC〇4 έ66 V. Description of the invention () _ 2-Cyclopropylmethyl-4a a-(3-hydroxyphenyl) -1,2,3, 4,4a, 5, 11, lla / 3 -octahydro-6H-B5I Iso [2,3-g] isoquinoline 19 Η

(19) The Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs printed 2-cyclopropylmethyl-4a a-(3-methylphenyl) -1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline 128mg (0.33 nmol), η-propanethiol 0.2ml (2..20mnol), potassium-t-butanol 225 ag (2.0niD〇l) dissolved in DMF, heated and stirred at 1251C. After 4 hours, η-propane thiolase 0.2 ml (2.2 ππο1), potassium-t-butoxide 2 25 mg (2 · 0 μο1) were added, and the mixture was further stirred at 125C for 4 hours. After cooling to room temperature, the reaction mixture was concentrated, a saturated aqueous solution of sodium bicarbonate was added to the residue, extracted with chloroform-methanol (3: 1), the organic layers were combined, washed with saturated brine, dried and concentrated to obtain a powder . This powder was separated and purified by chromatography tube [silica gel; chloroform: methanol: 28% ammonia water = 95: 5: 0.1 ~ 90: 10: 0.1] to obtain the title compound of 84ing. This compound was suspended in methanol, and methanesulfonic acid was added to make methanesulfonate, which was recrystallized from methanol-atmosphere to obtain 59 mg of pure compound methanesulfonate (mp> 25 0 ° C). IR (KBr) cm-1: 3390, 1586, 1046 NMR (DMSO-d6) 400MHz δ: 0.38 (2Η, br), 0.63 (2H, br), 1.07 (1Η, π,), 2.07 (1H , m), 2.31 (3H, s), 2.54 -2.65 (3H, m), 2.88-3.05 (5H1m), 3.11 (1H, d, J = 16.5Hz), 3.37 (lH.m), 3.51 (lll, m), 3.74 (lH, m), 6.54 (lH, m), 6.90-6.99 (please read the precautions on the back before filling in this page) Binding · Order-Line. This paper standard uses the Chinese Standard (CNS) ) A 4 specifications (210x297 male dragon) 121 V. Description of invention (A 6 B6 (4H, m), 7.04 (^, 1 ^ = 7.9112), 7.19 (1H, d, J = 7.9Hz), 7.34 ( 1H, d, J = 7.3Hz), 9.26 (lH, s), 9.38 (lH, br), 10.62 (lH, s Mass (FAB): 373 (M ++ 1) elemental analysis. M 2 S Η 2 8 N 2 〇 · C Η 3 S 0 3 H i C Η Ν 縕 綤 66.64 6.88 5.98 6.84 66.32 6.93 6.05 6.76 if inspection 丨 (please read the notes on the back before filling in this page) Printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs Prepare the same as below, using 2-benzyl-4act- (3-methoxyphenyl) -1,2,3,4,4 ^, 5,11,11hexane / 3-octahydro-6} 1- Indo [2,3-2] isoquinoline substituted V-cyclopropylmethyl-4a α-(3-methylphenyl) -1, 2, 3, 4, 4a, 5, 11, lla / S-octahydro-6H-indoxy [2,3-g] isoquinoline, to give 2-benzyl-4aa-(3-hydroxyphenyl) 1,2,3,4,43 , 5,11,113 / 3-octahydro-6} 1-11? Iloquino [2,3-g] isoquinoline: using 2-phenethyl-4aa- (3-methoxyphenyl)- 1,2, 3,4,43,5,11,113-octahydro-6} 1-indazolo [2,3-Ju] isoquinoline to give 2-phenethyl-4aa- (3-hydroxybenzene Group) -l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-indo [2,3-g] isoquinoline; use 2-ethyl-4aα- (3 -Methoxyphenyl) -l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-indflg and [2,3-g] isosalinate to give 2-ethyl- 4aa-(3-pyridyl) -1,2,3, 4,4a, 5, ll, lla / S -octahydro-6H-P51 P¾ ([2,3-g] isoquinoline; use 2- Propyl-4aa- (3-methylphenyl) -1,2,3,4,43,5,11,11 &amp; / 9-octahydro-6 eyes and [2,3-g] sleeping differently Leaching to obtain 2-propyl-4aa- (3-xiangphenyl) -1,2,3,4,43,5,11,113 / 3-octahydro-6} 1-indo [2,31 ] Isoquinoline · This paper scale is free to use Chinese National Standard (CNS) A 4 specifications (210x297 mm) 122-A 6 B6 Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Invention Instructions () —.; Used 2-butyl-4a α _ (3-methoxy Group) -1,2,3,4,4a, 5,11,1 la lu-octahydro-6H-ind 11¾- [2,3-g] isoquinoline. 2-butyl-4acc- (3 -Hydroxyphenyl) -1, 2, 3, 4 ^, 5, 11, 11a / 3 -octahydro-6H-ind 11¾ and [2,3-g] isoquinoline; make: ^^^-(3 -Tolyl) -1,2,3,4,4a, 5,11,113 / 3-octahydro-611- ^ 5 and [2,3-guer] isoquinoline to give 2-sleepyl-43 (2- (3-hydroxyphenyl) -1,2,3,4,41,5,11,113 / 3-octahydro-61 ^ P? 1 benzo [2,3-g] isoquinoline; use 2 -Pentyl-4aa- (3-methoxybenzyl) -1,2,3,4,43,5,11,113 /?-Octahydro-6} 1-indolo [2,3- 客] Isoquinoline gives 2-pentyl-4aa-(3-hydroxyphenyl) -1,2,3,4, 4a, 5, 11, lla / 3 -octahydro-6H-indazol [2,3 -g] isoquino_; using 2-B furanmethyl-4acx- (3-methylphenyl) _1,2,3 ,. 4,4a, 5, ll, lla / 3_octachloro_6H- D5 | Bg iso [2,3-g] isoquinoline gives 2-furanmethyl-4a〇t- (3-benzylphenyl) -1,2,3,4,43,5,11,113 / 5 -Octahydro-61 {-ind》 5 [〔2,3- 客］ isoquinoline; using 2-cyclobutylmethyl-4aot- (3-methoxyphenyl) -1,2,3,4,43, 5,11,11 &amp; 0-octahydro-611-〇5, benzo [2,3- 豸] isoquinoline, to give 2-cyclobutylmethyl-4a〇t- (3-hydroxybenzene Radical) -1,2,3, 4,4a, 5, 11,11a call -octahydro-6H-worm! ^ And [2,3-g] isoquino_; using 2- (4-tolylmethyl) -4aot- (3-methoxyphenyl) -1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-0? Shuo [2,3-g] isoquinoline to give 2- (4-tolylmethyl) -4a〇t-(3-hydroxyphenyl) -1 , 2,3,4,43,5,11,113 / 9-octahydro-611-indyl [2,3-g] isoquinine; use of 2-cyclopropylmethyl-4a〇t- (3 -Methylphenyl) -7-bromo-1,2,3,4,43,5,11,113 / 9-octahydro-611-indino [2,3-jing] iso-line, to give 2 -Cyclopropylmethyl-4a〇t- (3-hydroxyphenyl) -7-bromo-1,2, 3,4,43,5,11,113 Lu-octa-611-indo [2,3 -6] Isoquinoline; (please read the precautions on the back before filling in this page) This paper is in accordance with the Chinese Standard (CNS) A4 specification (210x297 mm) A6 printed by the Staff Consumer Cooperative of the Central Bureau of Standards ____B_6___ V. Description of the invention () _ Use of 2-cyclopropylmethyl-4aa-(3-methoxyphenyl 4,4a, 5,11,1U Zhao-octahydro-6HrD§ | Bg and [2,3- g] Isoquinoline to give 2-cyclopropylmethyl-4a a-(3-hydroxyphenyl) -8-bromo-1,2, 3,4,4a, 5,11, 1U / 3-octahydro -6H-indino [2,3-g] isoquinoline, using 2-cyclopropylmethyl-4 Phenyl) -9-bromo-1,2,3,4,4 ^, 5,11,11 &amp; / 3-octahydro-6H-indolo [2,3-g] isoquinoline to give 2- Cyclopropylmethyl-4aa- (3-hydroxyphenyl) -9-bromo-1,2,3,4,4a, 5, ll, lla / 9 -octahydro-6H-P5 3-g] Isoquine uses 2-cyclopropylmethyl-4aa- (3-methylphenyl) -1〇-bromo-1,2,3,4,43,5,11,113; 8-octa Hydrogen-6 {!-Indoxo [2, 3-g] isoquinoline to give 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -10-bromo-1,2,3, 4,43,5,11,113 / 5-octa-611-indo [2,3-2] isoquinoline, using 2-cyclopropylmethyl-4a a- (3-methylphenyl ) -7-nitro-1,2,3,4,4a, 5, ll, lla / S-octahydro-6H-ind "? [2,3-g] isoquinoline, to give 2-cyclopropane Methylmethyl-4aa-(3-pyridyl) -7-nitro-1,2,3,4,4a, 5,11,113 / 8-octahydro-611-indolo [2,3-2] Isoquinoline, using 2-cyclopropylmethyl-4a α-(3-methylphenyl) -8-nitro-1,2,3,4,4 a, 5, 11, lla / S-octa Hydrogen-6H-I? | PS and [2,3-g] isoxaline, to give 2-cyclopropylmethyl-4aa-(3- via phenyl) -8-nitro-1,2,3, 4,4a, 5,11,11a Lu-octahydro-6H-indeno [2,3-g] isoquinoline; use 2-cyclopropylmethyl-4act-(3-methoxybenzene ) -9-nitro-1,2,3,4,43,5,11,113 / 9-octahydro-611 -85 Shun [[2,3-g] isoquinoline, 2-cyclopropyl methyl Yl-4aa- (3-hydroxyphenyl) -9-nitro-1,2,3,4,43,5,11,113 / 9-octa-611-indolo [2,3-g] isoquine咻; using 2-cyclopropylmethyl-4acx- (3-methylchlorophenyl) -10-nitro-1, 2, 3, 4, 4 &, 5, 11, 113 / 3-octahydro-6 }}-Insights ((Please read the precautions on the back before filling out this page) Binding. Binding-Thread &lt; This paper size is used in China National Standard (CNS) A 4 specifications (210x297 g *) 124 Λ 6 Β6 Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs V. Description of the invention ()-. 2,3-g] isoquinolin, resulting in 2-cyclopropylmethyl_4aa-(3-hydroxyphenyl) -10- Nitro-1,2,3,4,48,5,11,113 / 3-octahydro-611-indo [2,3-2] isoquinoline. Using 2-benzyl-4a〇c- (3-methylphenyl) -7-methyl-1,2,3,4,43,5,11,113 / 3-octahydro-611-ind 112 (2 , 3-ming] isoquinoline, which gives 2-benzyl- 4aa_ (3-xiangphenyl) methyl_l »2,3,4,4a, 5, ll, lla / S -octahydro-6H-» 51 benzo [2,3-g] isoquinoline; using 2-benzyl-4 start (((3-methylphenyl) -8-methyl-1,2,3,4,43,5 , 11,113 / 3-octahydro-6H-Ρξ | Bδ and [2,3-g] isosomal shower to give 2-benzyl-4aa- (3-hydroxyphenyl) -8-methyl-1, 2,3,4,4a, 5, ll, lla0 -octahydro-6H-05I Dg and [2,3-g] isoquineline; use of 2-sulfanyl-4aa- (3-methoxyphenyl)- 9-Methyl-1,2,3,4,43,5,11,11 & 3-octahydro-6! ^ Ind118 [2,3- 笤] isoquinoline to give 2-benzyl- 4aa- (3-hydroxyphenyl) -9-methyl-l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-P? Shun Peng [2,3-g] Isoquinoline; using 2-benzyl-4 and 〇 (-(3-methoxyphenyl) -1〇-methyl-1,2,3,4,43,5,11,113 cold-octahydro- 6H-indolo [2,3-g] isoquinoline to give 2-benzyl-4aot- (3-hydroxyphenyl) _10-methyl-1,2,314,43,5,11,113 / 3-octazo-6 ^ 0? 丨 Land [2,3-g] isoquinoline; use 2-benzyl-4aa- (3-methoxyphenyl) -7-ammonia -1,2,3,4,43,5,11,113 / 9-octahydro-611-1151 eye and [2,3- 苕] isoquinoline, to give 2-sulfanyl-4a α-(3-hydroxybenzene Group) -7-atmosphere-1,2, 3, 4,4a, 5, 11, lla / S-octahydro-6H-P5lUg and Γ 2,3-g] isoquine; use 2-benzyl-48 〇 (-(3-Methoxyphenyl) -8-ambient-1,2,3,4,43,5,11,113 / 3-octahydro-611-115 Shunke [2,3-g] isoquine Porphyrin, to give 2-benzyl-4act- (3-hydroxyphenyl) -8-chloro-1,2,3,4,43,5,11,113 / 9-octahydro-6 {1-indazolo [2 , 3-ming] isoquinoline; use 2-benzyl-4a ot-(3-methylphenyl) -9-chloro-1,2,3, this paper uses China National Standard (CNS) A 4 specifications (210X297 male dragon) -125-one (please read the precautions on the back and then fill out this page) installed. Ύύ10〇4 V. Description of invention (Λ6 B6 Printed by the Employee Consumer Cooperative of the Ministry of Economic Affairs Central Standards Bureau 4,4玨 ， 5,11,114 / 3_ 八 气 _61! -115111decor [2,3-ming] iso_line 'is 2-section-43. (2- (3-xiangphenyl) _9_atmosphere- 1 * 2,3,4,43,5,11,113 Ling_ octahydro-6H-P5I cumulant [2,3-g] isoquinoline; use 2-benzyl-4aa- (3 -methylbenzene Radical) -1〇-aza-.1,2,3,4,43,5,11,113 / 9-octahydro-611-indo [2,3-g] isoquinoline, get 2_section base_ 4aa_ (3_perphenyl) _10_chloro_ 1,2,3,4,43,5,11,113 / 3_octahydro-611-worm mouth 2 and [2,3-2] is different; use 2 -Thousand-base ~ 4 aa _ (3 -methoxyphenyl) _ 7 -moor 1,2,3,4,4 a, 5, ll, lla / 3-octahydro Shun 〔2,3-g 〕 Isosomal shower, get 2-section base-Dougou ^-^-hydroxyphenyl bromide-1,2,3,4,43,5,11,113々 · ^, ®-^-ind HS [2,3-g] isoquinoline; using 2_benzyl-4aa_ (3_methoxyphenyl) -8-bromo-1,2,3,4,43,5,11,113 Lu-octahydro -6}}-ton Zhaobong [2,3-g] isoquino, get 2-section group_4a〇t- (3-xiangphenyl) -8-mo-1,2,3,4, 4a , 5, 11, lla / 3 -octahydro-6H-indazolo [2,3-g] isoquinine; use 2-benzyl_4act-. (3-methylphenyl) _9-mo-l ， 2,3,4,4a, 5, ll, lla-octahydro-δΗ-indwei [2,3-g] isosleep shower, to get 2-section group-4aoc- (3-xiangphenyl) -9-bromo-1 »2,3,4,43,5,11,1130-octahydro-611-115, eye [2,3-g] isoquinoline; use 2_section group_4aa_ (3 _Methoxyphenyl) _10_ Mo-1,2,3,4,43,5,11,113 points-octazo-6} 1-11? Shuzo [2,3-Dang] isoquinoline, 2- Benzyl-4aa- (3-hydroxyphenyl) -l〇-1,2,3,4,4a, 5, ll, llayS-octahydro And [2,3-g] isoquinoline; using 2-benzyl-43〇 (-(3-methylphenyl) -7-fluoro-1,2,3,4,4 &amp;, 5,11, 113 / 3-octahydro-6H-S5 dodo [2,3-g] isopyridin, to give 2-benzyl-4aa- (3-benzyl) -7-fluoro-1,2,3, 4,43,5,11,113 / 9-octahydro-611-indo [2,3-g] isoquinoline; using 2-benzyl-4aa- (3-methylphenyl) -8-fluoro- 1,2, (Please read the precautions on the back before filling out this page) Pack. -Line- This paper is used in the National Standards (CNS) A 4 specifications (210X297 Gongxu) 126 Employees of the Central Bureau of Standards of the Ministry of Economic Affairs Printed by the consumer cooperative A6 _B_6_ V. Description of the invention ()-_ 3,4,43,5,11,113 / 8-octahydro-6} 1-ind118 [2,3- 苢] isoquinoline, get 2- Benzyl-4a cc-(3-hydroxyphenyl)-&amp; -fluoro-1,2, 3,4, 4a, 5, 11, 11a / 9-octahydro-6} 1-indho [2, 3-dan] isoquinoline; use 2-sulfanyl-43〇 (-(3-methoxyphenyl) -9-fluoro-1,2,3,4,43,5,11,113 / 3-octa Hydrogen-611-indolo [2,3-g] isoquinoline to give 2-benzyl-4aa- (3-hydroxyphenyl) -9-fluoro-1,2,3,4,4 &amp;, 5 , 11,11 ugly /?-Octahydro-6} 1-ind3?-[2,31] isoquinoline; use 2-benzyl_4a〇 (-(3-methoxyphenyl) -10-fluoro -1,2,3,4,4a, 5,11,113 / 3-octahydro-611-indazolo [2,31] isoquinoline to give 2-benzyl-4act- (3-hydroxyphenyl) -10-fluoro-1,2,3,4 , 4a, 5, ll, lla / 3-A Hydrogen-6H-indo [2,3-g] isoquinoline; using 2-benzyl-4aa- (3-methoxyphenyl) -7-nitrate Yl-1,2,3,4,4 3,5,11,113 / 8-octahydro-.6} 1-ind 115- [2,3-g] isoquinoline to give 2-benzyl-4act- ( 3-hydroxyphenyl) -7-nitro-1,2,3,4,4 &amp;, 5,11,11 &amp; / 3-octahydro-611-indo [2,31] isoquinoline; use 2-benzyl-4aa- (3-methoxyphenyl) -8-nitro-1,2,3,4,4a, 5,11,113 / 3-octahydro-6} 1-indigo [2, 31] Isoquinoline to give 2-benzyl-4a α-(3-hydroxyphenyl) -8-nitro-1,2, 3, 4,4a, 5, 11, 11a / 3 -octahydro-6H -Indo [2,3-g] isoquinoline; using 2-benzyl-4aa-(3-methoxyphenyl) -9-nitro-1,2,3,4,43,5,11 , 113 / 3-octahydro-6 ^ 丨 118 and [2,3-g] isoquinoline to give 2-benzyl-4aa- (3-hydroxyphenyl) -9-nitro-1,2,3 , 4,43,5,11,113 / 9-octahydro-611-indo [2,3-0] isoquinoline; using 2-benzyl-4aa- (3-methoxyphenyl) -10-nitro -1,2,3,4, 43,5,11,113 /?-Octahydro-6} 1-indo [2,3-ming] isoquino, to give 2-benzyl-4aa- (3- Hydroxyphenyl) -10- Nitro-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indolo [2,3-g] isoquinoline: use 2-phenethyl-4aa- ( Please read the precautions on the back before filling out this page.) The size of this paper is based on the Chinese National Standard (CNS) A4 specifications (210x297 male dragons). 127 Printed A6 _B6_ by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs ()-_ (3-methoxyphenyl) -7-methyl-1,2,3,4,43,5,11,113 / 9-octahydro-611-indP5 [(3-, 3-g 〕 Isoquinoline, to give 2-phenethyl-4aa- (3-hydroxyphenyl) -7-methyl-1,2,3,4,43,5,11,113 / 8-octahydro-6} 1-Embrane 5, 5- [2,3-Lu] isoquinoline; use 2-phenethyl-4aa- (3-methoxyphenyl) -8-methyl-1, 2,3,4,43, 5,11,113-octahydro-6} 1-115 丨 Isoquinoline [2,3- 劤], 2-phenylethyl-4a α- (3-hydroxyphenyl) -8-methyl- 1,2, 3, 4, 4 a, 5, ll, lla / S-octahydro-6H-ind U5 [2,3-g] isoquinoline; use 2-phenethyl-4aa- (3- Methoxyphenyl) -9-methyl-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-dolo [2,3-g] isoquinoline, 2-phenethyl-4act- (| 3-hydroxyphenyl) -9-methyl-1,2,3, 4, 4 a, 5, 11, 11a / 3 -octahydro-6H-indolo [ 2,3-g Isoquinoline; using 2-phenethyl-4aa- (3-methoxyphenyl) -10-methyl-1,2,3,4,4, 5,11,11 & 3-octahydro- 6} 1-Indo [2,3-'g] isoquino-2-phenylethyl-4aa- (3-hydroxyphenyl) -10-methyl-1,2, 3,4,4a, 5 , ll, lla / S-octahydro-6H-indo S- [2,3-g] isoquinoline; use 2-phenethyl-4a α-(3-methoxyphenyl) -7-ambient- 1,2, 3, 4, 4a, 5, octahydro-6H-indo [2,3-g] isoquinoline, to give 2-phenethyl-4aa- (3-hydroxyphenyl) -7- Chloro-1,2,3,4,43,5,11,113; 8-octahydro-6H-indeno [2,3-g] isoquinoline; use 2-phenethyl-4aa- (3- Methoxyphenyl) -8-gas-1,2,3,4,43,5,11,11 &amp; / 3-octahydro-611-indazolo [2,3-g] isoquino, giving 2 -Phenethyl-4aa- (3-hydroxyphenyl) -8-chloro-1, 2,3,4,43,5,11,113-octahydro-611-indolo [2,3-min] iso Quinoline; using 2-phenethyl-4aa-(3-methoxyphenyl) -9-gas-1,2,3, 4,4a, 5, ll, lla / S-octahydro-6H-indPg And [2,3-g] isoquinoline, to give 2-phenethyl-4aa- (3-hydroxyphenyl) -9-gas-l, 2,3,4,4a, 5, ll, lla / 3 -Octahydro (please read the precautions on the back before writing this page) Packing-, ίτ_ line &lt; this paper scale is used in the country of China Standard (CNS) A4 specifications (210X297 gong) 128 A6 printed by the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs __B6_ V. Description of invention ()-. -6H-D5I BS and [2,3-g] isoquinoline ; Using 2-phenethyl-4aa- (3-methoxyphenyl) -10-gas-1,2,3,4,43,5,11,113 / 3-octahydro-6 (1-indolo [ 2,3-g] isoquinoline to give 2-phenethyl-4aa- (3-hydroxyphenyl) -10-chloro-1, 2,3,4,4, 5,11,11% / 3 -Octahydro-6-bumin 115- [2,3-tin] isoquinoline; using 2-phenethyl-4aa-(3-methoxyphenyl) -7-bromo-1,2,3,4, 4a, 5, ll, lla / S-octahydro-6H-indopolo [2,3-g] isoquinoline to give 2-phenethyl-4a α- (3-hydroxyphenyl) -7- Mo-1,2, 3, 4, 4a, 5, 11, 11a / 3 -octa »Hydrogen-6H-Indo [2,3-g] isoquinoline; use 2-phenethyl-4aa- ( 3-Methoxyphenyl) -8-mo-1,2,3,4,4a, 5, 11,1 layS -octahydro-6H-indigo [2,3-g] isoquino, to get 2 -Phenethyl-4aa- (3-hydroxyphenyl) -8-bromo-1,2,3,4,43,5,11,11 抆 / 3-octahydro-6} 1-indho [2 , 3-ming] isoquinoline; use 2-phenethyl-4act- (3-methoxyphenyl) -9-bromo-1,2,3,4,4a, 5,11,113 / 9-octahydro- 6} 1-two 丨 05 and [2,3-ming] iso salinate, get 2-phenylethyl -4aa- (3-hydroxyphenyl) -9-bromo-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-D? | Hg and [2,3-g] Isoquinoline; using 2-phenethyl-4aa- (3-methoxyphenyl) -10-bromo-1,2,3,4,43,5,11,113 / 9-octahydro-6} 1-ind 112 and [2,3-g] isoquinoline to give 2-phenethyl-4aa- (3-hydroxyphenyl) -10-bromo-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-6}]-indolo [2,3-ming] isoquinoline; use 2-phenethyl-4aa- (3-methylphenyl) -7-fluoro-1,2, 3, 4,43,5,11,113 / 8-octahydro-6 liver 0? Shun 〔[2,3-ming] isoquinoline, to give 2-phenethyl-4acc- (3-hydroxyphenyl)- 7-Fluoro-1,2,3, 4,4a, 5,11,11a yS -octahydro-6H-B? Isoquino [2,3-g] isoquinoline; use 2-phenethyl-4a α-(3-Methoxyphenyl) -8-fluoro-1,2,3, 4, 4a, 5, 11, 11a / 3 -octahydro-6H-Ο? 丨 跺 bi [2,3-g] Isoquinoline, 2-phenylethyl-4aa- (3-hydroxyphenyl) (Please read the precautions on the back before filling in this page) Binding · Ordering-This paper standard is used in China National Standard (CNS) A 4 Specifications (210x297 male dragons) 129 ^ 0tC〇4 A 6 B6 Printed by the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. 5. Description of the invention ()-. -8-fluoro-1, 2, 3, 4, 43, 5, 11, 113 call-Baji-611-ind 8 and [2,3-ming] isoquinoline; using 2-phenethyl-4a〇t- (3-methoxyphenyl) -9-fluoro-1,2, 3,4,43,5,11 , 11/3 / 3-octahydro-611-indole 2 [2,31; | isoquinoline, to give 2-phenethyl_4a〇c-(3-Xiangphenyl) -9-fluoro-1, 2,3,4,4a, 5,11,11 a / ϊ-octahydro-6H-indazolo [2,3-g] isoquinoline; use 2-phenethyl-4a α- (3-methyl Oxyphenyl) -10-fluoro-1,2,3,4,43,5,11,113 / 9-octahydro-6H-indo [2,3-g] isoquinoline to give 2-phenethyl -4aa- (3-hydroxyphenyl) -10-fluoro-1,2,3,4,4 &amp;, 5,11,11 & / 3-octahydro-611-ton [^ 和 〔2, 3-g 〕 Isoquinoline; using 2-phenethyl-4aa- (3-methoxyphenyl) -7-nitro-1,2,3,4,48,5,11,113 / 3-octahydro-6 {1 -Indo [2,31] isoquinoline to give 2-phenethyl-4a α-(3-hydroxyphenyl) -7-nitro-1,2, 3, 4, 4a, 5, ll, lla / S -octahydro-6H- «丨 conjugated [2,3-g] isoquinoline; using 2-phenethyl-4a α-(3-methylphenyl) -B-nitro-1, 2, 3,4,4a, 5,11,11a / 3-octahydro_611-115 丨 bite [2,3-ming] iso sleep shower to get 2-phenethyl-43〇 [-(3- Hydroxyphenyl) -8-nitro-1,2, 3,4,4a, 5, 11,11a / 8 -octahydro-6H-B5I BS [2,3-g] isoquinoline; use 2-phenethyl-4act- (3-methoxyphenyl) -9-nitro-1,2,3,4,4 &, 5,11,113 &gt; 3-octahydro-61! -Indzhao [ 2,3-g] isoquinoline. 2-phenylethyl-4act- (3-phenyl) -9-nitro-1, 2,3,4,43,5,11,11 start 0- Octahydro-6 ^ 丨 〇5 and [2,31] isoquinoline; using 2-phenethyl-4aa- (3-methylphenyl) -10-nitro-1,2,3,4, 43 , 5,11,113 / 9-octahydro-6} 1-ind115 [2,3- 苕] isoquinoline to give 2-phenethyl-4act- (3-hydroxyphenyl) -1〇-nitro -1,2,3,4,4a, 5, 11,11a / 3-octahydro-SH-indolo [2,3-g] isosomal shower. Example 19 (Please read the precautions on the back before filling in this page) Binding. Thread &lt; This paper standard is easy to use Chinese National Standards (CNS) A 4 specifications (210X297 mm) -130-Clear description issued% Five 66 ΛΒ 2-cyclopropylmethyl-4aa- (3-methylphenyl) -9-methyl-1,2,3,4, 4a, 5, ll, lla / S-octahydro-6H- Indolo [2,3-g] isoquinoline 20

〇: η ·-(Please read the precautions on the back before filling in this page) CH3 (20) Use 2- (2,2,2-trichloroethane gas carbonyl) -4aa-(3-methyl gas phenyl)- 6-Gaso-1, 2,3,4,43,5,6,7,8,83 / 3-decahydroisoquinoline 30〇11 ^ and 168 ng of P-tolyl trap hydrochloride, according to Examples 15 to 17 were subjected to the same reaction to obtain 60 mg of the title compound. IR (KB r) cnr ': 2922, 1605, 1580, H64. NMR (CDC 1 3) 400ΜΙΙζ δ: 〇. 10-0. 16 (211, m), 0.13 (111, m), 0.51-0.57 (211 , m), 2.02-2. 13 (211, m), 2.27- 2.40 (311, m), 2.42 (311, s), 2.55-2.67 (211, m), 2.83-3.06 (5ll.ni). 3 .18 (111, m), 3.67 (311, s), 6.60 (111, m), 6.89 (111 ^ (1, J = 8.6Hz, 1.2Hz), 7.00-7.02 (2H, m), 7.06-7.10 (2H, m), 7.26 (lH.s), 7.62 (lH, brs) Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs

Mass (m / e): 400 (M +) The same, using 3-methylphenyl trap instead of 4-methylphenylhydrazine to give 2-cyclopropylmethyl-4act- (3-methoxyphenyl) -8-methyl-1,2,3,4,4a, 5, ll, lla / S-octahydro-6H-indos (2,3-g) isoquinoline and 2-cyclopropylmethyl -4acx- (3-methylchlorophenyl) -1〇-methyl-1,2,3,4,4a, 5, ll, lla / 3 -octahydro-611-ind 1151 [2,3-g 〕 Isoquinoline; using 2-methylphenylhydrazine, 131 This paper scale is easy to use China Sleep Standard (CNS) A 4 specifications (210X297 public leakage) Λ 6 Β6 V. Description of invention ()-Get 2-cyclopropyl Ylmethyl-4 a α-(3-methylphenyl) -7-methyl-1,2, 3,4,4a, 5,11,11 &amp; / 3-octahydro-6} 1-worm eyes And [2,31: 1 isoquinoline. Example 2 0 2-cyclopropylmethyl, 43〇 (-(3-hydroxyphenyl) -9-methyl-1,2,3,4,4a, 5, ll, lla /?-6H-ind Naruto 〔2,3-g〕 isoquinoline 21

(Please read the precautions on the back before filling in this page) Printed by the Ministry of Economic Affairs, Central Standards Bureau Beigong Consumer Cooperative, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -9-methyl-1 , 2,3, 4,4a, 5, ll, lla / 3-6H-indole 2 (2,3-g) isoquinoline 105mg (0.26 miDol), η-propanethiol 0.27ml (2.98 nmol), potassium-t-butoxide 300mg (2.67M〇l) dissolved in 5ml of DMF, stored under 125 and stirred for 4 hours. After cooling to room temperature, the reaction mixture was concentrated, a saturated aqueous solution of sodium hydrogensulfonate was added to the resulting residue, and extracted three times with chloroform-methane (3: 1). The organic layers were combined, washed with saturated brine, dried and concentrated to obtain a powder. This powder was dissolved in methanol, methanesulfonic acid was added, concentrated, and separated and purified by chromatography tube [Sephadex, LH-20; methanol] to obtain The methanesulfonate salt of the pure title compound was 85% (yield 67.2%). IR (KBr) cm-1: 3270, 1657, 1586, 1460 Hass (FAB): 387 (H * + 1) same, use 2-cyclopropylmethyl-4a〇t- (3-methylphenyl ) -7-Methyl-1,2,3,4,43,5,11,113 / 9-Octahydro-611-Ind 115 [2,3-Rong] Binding-Binding · Thread · The size of this paper is easy to use in China Minjia Standard (CNS) A4 Specification (210X297 Axiom :) 132 Printed by the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Λ6 ___B6 _ V. Description of invention ()-Isoquinoline substituted 2-chenpropylmethyl-4aa- (3-Methoxyphenyl) -9-methyl-1, 2,3,4,43,5,11,113 / 8-octahydro-61 ^ ind 115 [bi [2,3-ming] isoquine Phenanthroline, to give 2-H-propylmethyl-4a α- (3-hydroxyphenyl) -7-methyl-1,2,3,4,4a, 5,11,11 &amp; / 3-octahydro-6 } 1-ind11dec [〔2,3-2］ isoquinoline; using 2-cyclopropylmethyl-4aa-(3-methylphenyl) -8-methyl-1,2,3,4 , 4a, 5, ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline, to give 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -8 -Methyl-l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indo [2,3-g] isoquinoline; using 2-cyclopropylmethyl- 4a α-(3-methoxyphenyl) -10-methyl-1,2,3, 4, 4a, 5, 11, llajQ-octahydro-6H-D5I Bg and 2, 3-g] isoquinoline. Reference Example 2 2-cyclopropylcarbonyl-4a α-(3-methoxyphenyl) -6-oxo-1,2,3,4, 4a, 5, 6, 7, 8,8a / S -dec Hydrogenisoquinoline 22 (22) 〇Me. Under argon, 2- (2,2,2-trifluoroethane carbonyl) -4a a-(3-methylphenyl) -6-gaso-1 , 2,3,4,4a, 5,6,7,8,8a / 3 -decahydroisoquinoline 3.28g dissolved in 5Qml of acetic acid, add zinc powder 4.9Qg, and stir at room temperature for 4 hours. After removing zinc by filtration and removing acetic acid under reduced pressure, 1N aqueous sodium hydroxide solution 3Qinl was added and extracted 4 times with 5Qral chloroform. Combine organic layers to saturate (please read the precautions on the back before filling in this page) Binding · Order-Line '

The paper scales are prepared in accordance with Chinese Standards (CNS) A4 specifications (210x297 male dragons) 133 B6 V. Description of the invention (washed with salt water, the dried and concentrated reaction mixture ^ 9 8g is dissolved in 50nl under argon Anhydrous digas methane. Add triethylamine 2.Ini and cyclopropane carbonyl nitrogen 0.9b1, and stir at room temperature for 3 hours. Wash with 1N hydrochloric acid, water, dry and concentrate to obtain 2.86g of oil. Chromatography tube [silica gel; gaseous imitation / ethyl acetate (9/1)] refined this oil to obtain 1.77g of the title compound (yield 75.3%). IR (liquid membrane method) cnr1: 2948, 1713, 1632 , 1582, 1450, 1245 EI-MS (m / z): 327 (Μ *) NMR (CDC 1 3) 400i1Hz δ: 0.72-0.81 (211, m), 0.96- 1.03 (211,0,), 1.72- 2.47 (9H, m), 2.76 (0.511, m), 2.97 (1H, d, J = 14. 2Hz), 3.07 (0.5H, in), 3.27 (0.5H, m), 3.75 (0.5 H, m) , 3.79 (3H, s), 4.01 (0.511, (11), 4.12 (0.5H, m), 4.33 (0.5H, m), 4.60 (0.5H, m), 6.75 (1H, dd, J = 8.3Hz, 2.ΟΗε), 6.9 · 5-7.01 (2H, m), 7.25 (1H, t, J = 8.3Hz) The same, using propylene acetyl chloride instead of cyclopropane carbonyl chloride to give 2-propenyl- 4a α-(3-A Phenyl) -6-oxo-1,2, 3, 4, 4a, 5,6,7,8, 8a / S-decahydroisoquine_ printed by the Consumer Labor Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs; Acyl chloride gives 2-benzaldehyde-4act- (3-methylphenyl) -6-aero-1,2,3,4, 4a, 5,6, 7,8,8a /?-Decahydro Isoquinoline; using phenethylacetoyl to give 2-phenylacetaldehyde-4aa- (3-methoxyphenyl) -6-oxo-l, 2,3,4,4a, 5,6,7, 8,8a / S-decahydroisoquinoline; use of acetonitrile gives 2-acetoyl-4a α-(3-methoxyphenyl) -6-gaso-1,2,3, 4, 4a , 5,6,7,8,8a /?-Decahydroisoquinoline; use of propyl chloride to give 2-propionyl-4a α-(3-methylphenyl) -6-oxo-1, 2, 3, 4, 4a, 5,6, 7,8,8a / S-134 (please read the precautions on the back and then fill in this page) This paper size is not in accordance with China Sleepy Standard (CNS) A4 Specifications (210x297 Male A 6 B6

V. Description of the invention () Decahydroisoquinoline; using butyraldehyde chloride to give 2-butyraldehyde-4act- (3-methylphenyl) -6-oxo-l, 2,3,4,4a, 5, 6,7,8,8a / 3-decahydroisoquinoline; using 2-thiophene carbonyl chloride to give 2-pyridinecarbonyl-4acc-(3-methylphenyl) -6-oxo-1,2 , 3,4,4a, 5,6,7,8,8a / 3-decahydroisoquinoline; using pentamethylene gas to give 2-pentanal_4a α-(3-methylphenyl) -6 -Oxo-1,2,3,4,4a, 5,6,7,8,8ayS-decahydroisoquinoline; using 2-furfural gas to obtain 2-furaldehyde-4aa-(3-methyl gas Phenyl) -6-aero-1,2,3,4, 4a, 5,6,7,8,8a Ji-decahydroisoquinoline: using cyclobutane carbonyl chloride to give 2-cyclobutane carbonyl -4a ct-(3-methoxybenzyl) -6-aero-1,2,3,4, 4a, 5, 6,7,8,8a / 3 -decahydroisoquinoline; use P-toluene Aldehyde chloride gives 2- (p-tolyl) -4act- (3-methoxyphenyl) -6-oxo-1,2,3,4,4a, 5,6,7,8,8a; S-decahydroisoquinoline; using xylaldehyde chloride to give 2-xylyl-4act- (3-methoxyphenyl) -6-oxo-1,2,3,4,4 a, 5 , 6,7,8,8a / 3 -decahydroisoquinoline; using P-anisyl gas to give 2- (p-anisaldehyde) -4a cr-(3-methylphenyl) -6-gas Generation-1,2,3,4,4a, 5,6,7,8,8a Lu-ten Isoquinoline. Example 2 1 (Please read the precautions on the back before filling in this page) Installation · Line · Printed by the Central Standards Bureau of the Ministry of Economic Affairs Beigong Consumer Cooperatives 2-cyclopropylcarbonyl-4aa-(3-methoxyphenyl)- 1,2, 3, 4,4a, 5,11, lla / 3 -octahydro-6-methyl-ind Pg- [2,3-g] isoquinoline 23

135 The size of the paper is used in the middle Η Gujia standard (CHS) A 4 specifications (210x297 male dragon) _B_6__ 5. Description of the invention ()-. (Please read the precautions on the back side before filling out this page) -Chenpropylcarbonyl-4a a-(3-methoxyphenyl) -6-aero-1,2, 3,4,4a, 5,6,7,8,8a / 3 -decahydroisoquinoline 185 mg and 1-methyl-1-phenyl trap 75W1 were dissolved in 3nl of ethanol and heated at 80T :. Methanesulfonic acid 0.37ib1 was added, and after searching and stirring at 801: 15 for 15 minutes, it was cooled to room temperature. The ethanol was removed under reduced pressure, a saturated aqueous solution of sodium hydrogenate was added, and extraction was performed 3 times with 20 nl of chloroform. The organic layers were combined, washed with saturated brine, dried and concentrated to obtain 33〇Bg of oil. Refine this oil by chromatography tube [silica gel; methane / ether (19/1)] to obtain 162mg of refined crystals. Recrystallized from ethyl acetate-hexane to obtain 141mg of pure product, m.P.131 ~ 132.5% (yield 60.2%). IR (KB r) cm'1: 1634, 1470, 1441, 1261, 1245, 1228, 735. EI-MS (m / z): 414 (H +), 157 NMR (CDC 1 3) 400MHz δ: 0.75-0.79 (2H, m), printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 0.95- 1.03 (2H, m), 1.76-1.89 (211, m), 2.38 (lH, m), 2.50 (1H, m), 2.80 ( 111, m), 2. 95-3. 06 (3H, m), 3. 22 (1H, d, J = 15. 6Hz), 3.40- 3.49 (lll, briti), 3.55 (3H, s), 3.69 (3H, s), 4.24-4.31 (lH.brm), 4.39-4.48 (lH, brm), 6.66 (111, m), 7. 03-7.08 (3H, m), 7.11-7.15 dm), 7.21 ( lH, d, J = 7.9llz), 7.45 (lH, d, J = 7.6 H z) The same, using 1, 1-diphenylhydrazine instead of methyl-1_phenyl trap to give 2-cyclopropylcarbonyl -4aa-(3-methoxyphenyl) -l, 2,3,4,4a, 5, 11, lla / 3 -octahydro-6-phenyl-ind 1 »Rong Buo [2,3-g] Isoquinoline; use 2-acryloyl-4act-(3-methylphenyl) -6-pyro-l, 2,3,4,4a, 5,6,7,8 136 for paper size China National Standards (CNS) A4 specifications (210X297 g) Printed by the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A 6 ___B_6_ V. Description of invention ()-., 8a / 9-decahydroisoquinoline substitution 2-cyclopropylcarbonyl-4acx-(3-methylphenyl) -6-fluoro-1,2,3,4,4a, 5,6,7,8,8a / 8 -decahydroisoquinoline , To give 2-propenyl-4 this 〇 (-(3-methoxyphenyl) -1,2,3,4,43,5,11,113; 9-octahydro-6-methyl-indole Pyro- [2,3-g] isoquinoline; use 2-benzaldehyde-4aot-(3-methylphenyl) -6-amino-1,2,3, 4, 4a, 5,6, 7,8,8a / 3 · -Decahydroisoquinoline, to give 2-phenylacryl-4a a- (3-methylphenyl) -1,2, 3, 4, 4a, 5, ll, llay9- Octahydro-6-methyl-D5 Isoquino [2,3-g] isoquinapan; using 2-phenylacetaldehyde-4a α-(3-methoxyphenyl) -6-gaso-1 , 2,3,4,4a, 5, 6, 7,8,8a / 3 -decahydroisoquinoline, to give 2-phenylacetoyl-4act-(3-methoxyphenyl) -1,2 , 3, 4, 4 a, 5, 11, 11a / 3-octahydro-6-methyl-indodec [2,3-g] isoquinoline. Example 22 2-cyclopropylmethyl-4aa- (3-methylphenyl) -1,2,3,4,4a, 5,11,11a / 3-octahydro-6-methyl-indole And [2,3-g] isoquinoline 24 (please read the precautions on the back before filling in this page) -install · order_ line &lt; Η

Under argon, 35 mg of lithium aluminum hydride was suspended in 5 ml of anhydrous THF, and cooled to 0 ° C. Another 2-cyclopropylcarbonyl-4a «-(3-methylphenyl) -1,2,3,4 , 4a, 5,11,113 / 9-octa-6-methyl-indo [2,3-ming] isoquinoline 150-Mu is dissolved in 2m 1 of anhydrous THF and dropped into it. Warm to room temperature and stir for 2 hours. This paper scale is used in China National Standards (CNS) A4 specifications (210x297 male dragon). 137 Printed by Beigong Consumer Cooperative of Central Standards Bureau of the Ministry of Economic Affairs. Cool to 0 ° C and add a saturated aqueous solution of ethyl acetate and sodium potassium tartrate. The insoluble material was removed by filtration and ethyl acetate was distilled off under reduced pressure to obtain 14Ong of oil. Purify this oil by a chromatography tube [silica gel; chloroform-chloroform / methanol (9 9/1)]. 13 lmg of the title compound was obtained. Recrystallize it from ethyl acetate to obtain 110ng pure product (bp 133 ~ 134C; yield 75.9%) 0 IR (KBr) cm- ': 3420, 1 601, H75, 138G, 1251, 7G4, EI- MS (m / ζ): / 100 (Η *), 157 Ν Μ R (CDC 1 3) 400MHz ί: 0.16-0.21 (211, m), 0.5G-0.61 (211, m), 1.02 (111 , m), 2.20-2.27 (211, m), 2.40- 2.50 (311, m), 2.70- 2.78 (211, ηι), 2.85 (1II, brd, J = 16.1 ΙΙζ), 3.00 -3.04 (2H, m), 3. 13-3. 18 (21l, m), 3. 31 (1H, m), 3. 51 (3Η, s), 3.68 (311,5), 6.63 (lH, m), 7.02-7. 14 (5! Ι, m), 7.19 (1II, d, J = 8.3Hz), 7.44 (111, d, J = 7.3IIz), the following uses the same 2-propenal Yl-4a α-(3-methylphenyl) -1,2,3,4,43,5,11,11 &amp; 0-octahydro-6-methyl-indo [2,3-ming] Isoquinol substituted 2-cyclopropyl glassy group-4aa-(3-methoxyphenyl) -1,2, 3,4, 4a, 5,11,113 / 3-octahydro-6-methyl- vermizo [2,3-Guest] isoquinoline to give 2-allyl-4aa- (3-methylphenyl) -l, 2,3,4,4a, 5, ll, lla / S-octahydro- 6-methyl-indeno [2,3-g] isoquinoline: using 2-phenenyl-4aa-(3-methoxyphenyl) -1,2,3,4,4a, 5, 11, lla / S -octahydro-6-methyl-indo [2,3-g] isoquinoline, to give 2-benzyl-4a〇t- (3-methylphenyl) -1, 2 , 3,4,43,5,11,113 / 3-octahydro-6-methyl-indo [2,31] isoquinoline; using 2-phenylethyl acetyl-4aa- (3-methoxy Phenyl) -1,2,3,4,4a, (please read the precautions on the back before filling out this page) Binding · Order-Line-This paper standard uses Chinese Standard (CNS) A 4 specifications (210x297 Male Dragon) 138

^ 〇16iS4_Ββ__ Fifth, the invention description ()-5, ll, lla / S-octahydro-6-methyl-D? I bite [2,3-g] isoquinoline to give 2-phenethyl-4aot -(3-Methylphenyl) -l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6-methyl- [2,3-g] isoquinoline. Example 23 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -1,2,3,4,4a, 5,11, lla / 3-octahydro-6-methyl-indazolyl [2,3-g] isoquinoline 25 ^ 0 (25) aMe 01! 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -i, 2,3,4 under argon , 43,5,11,113 / 3-octahydro-6-methyl-ind [18- [2,3-ming] isoquinoline 120mg, η-propanethiol 0.2ml, potassium-t-butane gas 2 3 0mg dissolved in 3ml of anhydrous DMF, stirred at 130 ° C. After 4 hours, η-propanethiol 0.2 ml of potassium-t-butane vapor 23Qng was added, and the mixture was further stirred at 13Q ° C for 2 hours, and then cooled to room temperature. The DHF was removed under reduced pressure, 5 ml of water was added, and extracted 3 times with 2Q ml of acetone. The organic layers were combined and washed with saturated saline, dried and concentrated to obtain 120 mg of powdered noodles. Suspend the powder in 3nl of formazan, add 20 W1 of methanesulfonic acid, and then add human DMF to dissolve it. DMF was removed under reduced pressure, ethyl acetate was added, and the solid was collected by filtration. This solid was recrystallized from methanol to obtain the title compound methanesulfonate (decomposed at 250 ° C) 74 mg (yield 51.4%). (Please read the precautions on the back before filling out this page)

, tT Printed by Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

66 AB Printed IR (KB r) cm-1 of the Staff Consumer Cooperative of the Central Bureau of Standards of Economy: 3410, 1601, 1474, 1212, 1170, 1042, 784, 555 FAB-MS (m / z): 387 (M + +1 ) NMR (DMS〇-d6) 500MHz 5: 0.36-0.41 (2H, m), 0.62-0.66 (2H, m), 1.07 (lH, m), 2.10 (lH, m), 2.30 (311, s), 2.56-2.67 (311,111), 2.85 (^^), 2.92 (lH, m), 2.98-3.08 (3H, m), 3.29-3.38 (2H, m), 3.53 (3H, s), 3.51-3.55 (lH .m), 3.75 (lH.m), 6.55 (lH, m), 6.94-6.99 (3 Hm), 7.03-7.07 (2II, in), 7.31 (lH, d, J = 7.9Hz), 7.37 (lH , D, J = 7.9H2), 9.25 (lH, s), 9,37 (lH.br) Elemental analysis C26H3〇N2 0-CH3 S03 Η · 0. 3 7 H 2 0 CH NS. Calculation value 66.28 7.16 5.73 6.55 '^ | 倳 値 66.27 7.18 5.69 6.65 The following is the same, using 2-benzyl-4aa- (3-methoxybenzyl) -1,2, 3, 4,43,5,11,113 / 3-octahydro- 6-Methyl-dimetho [2,3- &amp;] isoquinoline substituted 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -1,2, 3,4, 4a, 5 , 11, lla / S-octahydro-6-methyl-indo [2,3-g] isoquinoline, to give 2-benzyl-4 &amp; 〇 [-(3-perphenyl) -1, 2,3,4,43,5,11,113 / 3-octahydro-6-methyl-0? Shuzo [2,3-g] isoquinoline; With 2-phenethyl-4aa- (3-methoxyphenyl) -1,2,3,4,43,5,11,113 / 3-octahydro-6-methyl-indodo [2, 3 -Dan] isoquinoline, which gives 2-phenethyl-430- (3-hydroxyphenyl) -1,2,3,4, ", 5,11,113-octahydro-6-methyl-indene 1 ^ And [2,31] isoquinoline. (Please read the precautions on the back before filling in this page). Ϊτ_ This paper scale uses the Chinese National Standard (CNS) A4 specifications (210x297 male dragon). V. Description of the invention (A6 B6 Example 24 2-cyclopropylcarbonyl-4a α-(3-methoxyphenyl) -7-fluoro-1,2,3, 4, 4a, 5, ll, lla / 3 -octahydro- 6H-Indo [2,3-g] isoquinoline 26 〇

H

(26) (please read the precautions on the back before filling in this page) • Installed · Printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs under the argon gas, 2-cyclopropyl hydroxy-4a (((3- Oxyphenyl) -6-aero-1,2,3,4,4a, 5,6,7,8,8a / 9-decahydroisoquinoline 4 06mg and 2-fluorophenylhydrazine hydrochloride 267Bg dissolved in 5ml of ethanol, heated at 80 ° C. Add methanesulfonic acid 0.94ral, search at 8Q ° C for 30 minutes and then cool to room temperature. Add saturated aqueous solution of hydrogen oxalate to make it alkaline and extract with 5Gb1 of chloroform Three times. The organic layers are combined, washed with brine, dried and concentrated to obtain 684rag oil. Separated and purified by chromatography tube [silica gel: cyclohexane / ethyl acetate (2/1 ~ 1/1)] From this oily substance, 29 lmg of crude crystals were obtained, which were recrystallized from chloroform-cyclohexane to obtain 254 mg of the title compound m.P. 2 75 ~ 277 ° C (coloring started near 2 6 0 ° C) (yield 48.9%) • Ordered • • Green • This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210x297 mm) -141 A6 B6 Printed by the Consumer Consumer Cooperative of the Central Bureau of Economic Development of the Ministry of Economic Affairs V. Invention Instructions )-IR (KB r) cm & qu ot ;: 3252, 1619, 1581, 1460, 1249, 1228 El-MS (m / z): 418 (Μ *), 161 NMR (CDCI ") 400MHz 5: 0.76-0.79 (2H, m), 0.95 -0. Η (2! L, m), 1. 75- 1. 90 (211, m), 2. 35-2. 49 (211, m), 2.7 7-3.01 (411, m), 3.08- 3.25 (2ll, m), 3.69 (3ll, s), 3.97-4.74 (2H, brm), 6 * .67 (lll, m), 6.80 (1II, dd, J = 10.7llz, 7.8tlz), 6.96 (111, td, J = 7.8llz, 4.9llz), 7.00-7.19 (211, m), 7.14 (111, t, 7.8Hz), 7.19 (1H, d, J = 7.8Hz), 7.80 (1H, brs ), The following is the same, using 3-fluorophenylhydrazine to replace 2-fluorobenzylhydrazine to give 2-cyclopropylcarbonyl-4act-(3-methoxyphenyl) -8-fluoro-1,2,3, 4, .4 a, 5, 11, lla; 3-octahydro-6H-indo [2,3-g] isophenoline and 2-cyclopropylcarbonyl-4aa-(3-methylphenyl) -10-Fluoro-1,2,3, 4, 4a, 5, 11, 11a Zhao-octahydro-6H-indazol [2,3-g] isoquinoline; using 4-fluorophenyl trap 2-Cyclopropylcarbonyl-4aa- (3-methoxyphenyl) -9-fluoro-1,2,3,4,4a, 5, ll, lla / S-octahydro-6H-indimino 〔2 , 3-g] isoquinoline. Example 25 2- (2,2,2-trichloroethoxycarbonyl) -4aa-(3-methoxyphenyl) -7-fluoro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-d5 | US and [2,3-g] isoquinoline 27 (please read the precautions on the back before filling in this page). ¾. • Tagged--Green. This paper size applies to China National Standard (CNS) A 4 specifications (210x297 mm) -142-3υ16υ4 A 6 Β6 V. Description of invention (

CI3C and Η

(27) The Ministry of Economic Affairs, Central Bureau of Standards and Staff Employee Cooperative Printed 2- (2,2,2-trichloroethane gas carbonyl) -4aa-(3-methyl gas phenyl) -6-gas generation- under argon 1,2,3,4,43,5,6,7,8,88 / 3-decahydroisoquinoline 10 and 2-fluorophenylhydrazine hydrochloride 1.39g were dissolved in 40Π1 ethanol and heated at 80¾. Add methanesulfonic acid 4.6b1, stir at 80 ° C for 15 minutes and cool to room temperature. Ethanol was distilled off under reduced pressure, 1N sodium hydroxide aqueous solution was added to adjust it to test, and extraction was performed 4 times with 50 π 1 atmosphere. The organic layers were combined, washed with planing and brine, dried, and concentrated to obtain 4.1 lg of oil. This oil was separated and purified by chromatography tube [silica gel; diaminomethane / cyclohexane (1/1) -dichloromethane] to obtain 3.0 g of crude crystals, which were recrystallized from ethyl acetate to give 2. 08g of the title compound, m.P. 235 ~ 2 3 7 ° C (55.5%). IR (KB r) cm * 1: 3332, 1694, 1460, 1435, 1259, 1226, 1149, 1131, 1046, 777, 717 EI — MS (m / z): 524 (M +), 526, 161 NMR (CDC 1 3) 500MHz &lt; 5: 1 · 85 (1H, m), 2.39-2 · 46 (2H, m), 2. 88- 2.99 (411, m), 3. 14 (III, m), 3. 49 (1H, m), 3.69 (311, s), 4.10 (lH, m), 4.28 (111, brd, J = 13.4Ilz), 4.72-4.82 (211, m), 6.66 (111, m), 6 . 80 (III, dd, J = 11. Ollz, 7.91lz), 6.94-7.01 (311. m), 7.14 (111, t, J = 7.9llz), 7. 20 (111, m), 7.77 (1II, brd, J = 7.3llz) The size of the paper is used in the National Standard (CNS) A 4 specifications (210x297 male dragon) 143 (please read the precautions on the back before filling this page)

mci4 V. Description of the invention (Same, replace 2-fluorophenylhydrazine with 3-fluorophenyl trap to give 2- (2, 2, 2-trichloroethane carbonyl) -4aa-(3-methoxyphenyl ) -8-fluoro-1,2,3,4,4a, 5,11,11 &amp; / 3-octahydro-611-indolo [2,3-ming] isoquinoline and 2- (2,2 , 2-trifluoroethoxycarbonyl) -4act- (3-methoxyphenyl) -10-fluoro-l, 2,3,4,4a, 5,11,113 / 3-octahydro-611-indazol [ 2,3-ming] isoquine_; using 1 fluorophenyl hydrazine to give 2- (2,2,2-trifluoroethoxycarbonyl) -4a α-(3-methoxyphenyl) -9-fluoro- 1,2,3,4,4a, 5,11,11a-octahydro-6H-indpdeco [2,3-g] isoquinoline. Example 2 6 2-cyclopropylcarbonyl-4aa-( 3-methoxyphenyl) -7-fluoro-1,2,3,4,4a, 5, ll, llayS-octahydro-6H-indo [2,3-g] isoquinoline 26 (please first Read the legal matters on the back and fill in this yellow)-installed. 〇Η

(26) Order-line · Printed by the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs under argon gas 2- (2, 2,2-trigas ethoxycarbonyl) -4aa-(3-methyl »phenyl)- 7-fluoro-1,2,3,4,4 3,5,11,113 / 3-octahydro-611-〇5 &quot; deca [2, 3-g] isoquinoline 2.22g suspended in 40b1 acetic acid, 2.75 g of zinc powder was added and stirred at room temperature for 3 hours. After removing zinc by filtration and distilling off the acetic acid under reduced pressure, the solution was made alkaline with 1N sodium hydroxide aqueous solution and extracted three times with 50 ml of chloroform. The organic layers were combined, washed with saturated saline, and the dried and concentrated reaction mixture was suspended in 40 ml of diazomethane (1.70 g), and triethylamine was added to 1.20. 4 specifications (210X297 male dragon) -144-144 Printed A6 B6_ by the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. V. Invention description ().-.Ml and 0.57ml of cyclopropanecarbonyl chloride, stirred at room temperature for 2 hours Dichloromethane was distilled off under reduced pressure, 20 mL of ethyl acetate and 10 H of 1H aqueous sodium hydroxide solution were added, and the precipitated solid was collected by filtration to obtain 1.51 g of the title compound. Separately, the filtrate was separated into two layers and extracted three times with 2Qml · of gas. The organic layers were combined, washed with saturated brine, dried and concentrated to obtain 550 mg of oil. The oil was separated and purified by chromatography tube [silica gel; gaseous imitation] to obtain 180rag of the title compound (yield 95.6%). The various patterns are consistent with the compounds obtained in the examples. The following is the same, using 2- (2, 2, 2-trichloroethane gas glass) -4a α-(3-methoxyphenyl) -8-fluoro-1,2,3,4,43,5, 11,11 &amp; / 3-octahydro-611-ind (18- [2,3-g] isoquinoline substituted 2- (2,2,2-trichloroethane carbonyl) -43〇 (-(3- Methoxyphenyl) -7-fluoro-1,2,3,4,43,5,11,113 / 3-octahydro-6-indo [2,3-g] isoquino-2-cyclopropyl Carbonyl-4aa- (3-methylphenyl) -8-fluoro-1,2,3,4,43,5,11,11 and / 8-octahydro-611-indole 5 (〔2,3- g] Isoquinoline; using 2- (2,2,2-trichloroethoxycarboxy) -43 ^-(3-methoxyphenyl) -9-fluoro-1,2,3,4,43,5 , 11,113 / 9-octahydro-6 [1-indazolo [2,3-g] isoquinoline, to give 2-cyclopropylcarbonyl-4aa- (3-methylphenyl) _9-fluoro- 1,2,3,4,43,5,11,11 lines / 3-octaqi-611-0? | Decaquino [2,3-dan] isoquine uses 2- (2,2,2-tri Gas ethyl gas carbonyl) -4act- (3-methoxyphenyl) -10-fluoro-1,2,3,4,43,5,11,113 / 9-octahydro-611-ind112 [2, 3-g] Isoquinoline to give 2-cyclopropylcarbonyl-4aa- (3-methylphenyl) -10-fluoro-1,2,3,4,43,5,11,113 / 3-octa Hydrogen-6, indole 1 ^ [2,3-ming] isoquinoline. Example 2 7 2 -Cyclopropylmethyl-4aa-(3-methylphenyl) -7 -Fluorine-1,2,3,4,4a This paper scale uses the Chinese National Standard (CNS) A4 specifications (210x297 g)-145-(Please read the precautions on the back before filling the nest page) Install &lt; Line-3ύ1β〇4 A 6 Β6 V. Description of the invention (_)-., 5, 11, llayQ -octahydro-6H-P§ | H Duo [2, 3-g] isoquine_ 28

Printed by the Ministry of Economic Affairs Central Standards Bureau Employee Consumers Cooperative under 2-argon sulfonate 4-cyclopropylsulfo-4a〇t- (3-methylphenyl) -7-fluoro-1,2,3,4,4 Ugly, 5,11,113 / 8-octahydro-611-115 | 1! 2 and [2,33] isoquinoline 215Bg suspended in 20ml of anhydrous THF, cooled to 0T, 60ng lithium aluminum hydride was added. After warming to room temperature and stirring for 1 hour, it was cooled to 0 ° C, and a saturated aqueous solution of ethyl acetate and potassium sodium tartrate was added to filter out the insoluble materials, and ethyl acetate was distilled off under reduced pressure to obtain 210 ing of crude crystals. This crude crystal was recrystallized from chloroform monoether to obtain 17〇Bg of the title compound, β.P · 137 ~ 13910 (yield 81.8%) 0 IR (KB r) cm * 1: 2836, 1578, 1241, 1228, 1050, 779 EI-MS (m / z): 404 (Mf), 242 NMR (CDC 1 3) SOOMlIz δ: 0.07-0. 12 (211, m), 0.48-0.54 (211, m), 0.88 (111 , m), 1.97- 2.07 (211, m), 2.23-2.3 2 (211, m), 2.40 (111, m), 2. 54-2.65 (211, m), 2.89- 3.02 (411, m). 3. 10 (111.d, J = 15.9llz), 3.16 (111, m), 3.68 (311,5), 6.62 (lll, m), 6.78 (1ΙΙ, ί5ϋ, J = 7.911 z, 11.0 \\ z ), 6.94 (1II, td, J = 7.9llz, 4.91Iz), 7.02-7.04 (2II, n.), 7.09 (1II, l, J = 7.9! Lz), 7.19 (l II , d, J = 7.3llz), 7.80 (1H, brs) (Please read the precautions on the back before filling the nest page) Binding · Order · Thread · The paper size is free to use China National Standard (CNS) A4 specifications ( 210 X297 mm) 146 .A6 _B6__ 5. Description of the invention ()-The following is the same, using 2-cyclopropylcarbonyl-4aa- (3-methoxyphenyl) -8-fluoro-1, 2, 3, 4 , 43,5,11,11 and / 3-octahydro-61! -Indazolo [2,3-guest] isoquinoline substituted 2-cyclopropylcarbonyl-4aa-(3-methoxy Radical) -7-fluoro-1, 2,3,4,43,5,11,11 &amp; / 3-octahydro-6 {1-indigo [2,3- 豸] isoquinoline, giving 2- Cyclopropylmethyl-4aa- (3-methoxyphenyl) -8-fluoro-1,2, 3,4,4 a, 5, ll, lla / 8 -octahydro-6H-indPg (2 , 3-g] isoquinoline; using 2-cyclopropylcarbonyl-4act-(3-methoxyphenyl) -9-fluoro-1,2,3,4,4a, 5, ll, 11a Lu-octa Hydrogen-6H-indDg [2,3-g] isoquinoline to give 2-cyclopropylmethyl-4aa- (3-methylphenyl) -9-l, 2,3,4,4a , 5, ll, lla / S-octahydro-6H-05Idolo [2,3-g] isoquinoline; using 2-cyclopropylcarbonyl-4aa-(3-methoxyphenyl) -10-fluoro -1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-611-indolo [2,3-g] isosleepoline, to give 2-chenpropylmethyl-4acx- (3 -Methylchlorophenyl) -10-fluoro-1,2,3,4,4a, 5,11, lla / 3-octahydro-6H-inds PS [2,3-g] isoquinoline. Example 28 (Please read the precautions on the back before filling in this page) Binding · Ordering-Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 2-cyclopropylmethyl-4a α- (3-hydroxyphenyl) -7 -Fluoro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-ind Ug and [2,3-g] isoquine_29 Η

Under argon, 2-cyclopropylmethyl-4aa-(3-methylphenyl) -7-fluoro-1,2,3,4,43,5,11,11 &amp; zhao-octahydro-6 {1-Indox [2,3- &amp;] isoquine 147 This paper scale is used in the Chinese National Standard (CNS) A4 specification (210x297 g *) 3 ύ1β〇4 A6 B6 V. Description of the invention () Porphyrin 164nig, η-propane thiol 0.31 ml, potassium-t-butane vapor 35 nig dissolved in 51〇1 of anhydrous 〇 ^, 13 () &lt; 〇 was stirred for 4.5 hours. After cooling to room temperature, DMF was distilled off under reduced pressure, 5b1 water was added, and extraction was performed 3 times with 15 ml of acetone. The organic layers were combined, washed with saturated brine, dried and concentrated to obtain 155 mg of powder. This powder was suspended in 2b1 methanol, and 25w 1 of methanesulfonic acid was added to make methanesulfonate, which was separated and purified by chromatography tube [Sephadex, LH-20; methanol] to obtain 125Bg of crude crystals. This crude crystal was recrystallized from ethanol to obtain the potassium benzenesulfonate of the title compound (24024 decomposition) 51nig (yield 25.9%). (Please read the precautions on the back before filling out this page) IR (KB r) cin- 'printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs: 3180, 1601, 1460, 1330, 1210, 1046, 785 FAB-MS (m / z): 391 (M ^ + 1). NMR (DMS〇-dfc) 500MHz δ: 0.35-0.40 (2H, m), 0.62-0.67 (211, m), 1.06 (111, m), 2.07 (111 , m), 2.31 (3H, s), 2.55-2.67 (3ii, m), 2.89-3.07 (5H, ra), 3. 14 (1H, d, J = 15.8Hz), 3.38 (111, m), 3.51 (111, m), 3.73 (lH> m), 6.54 (lH, m), 6.81 (lH, dd, J = 11.6llz, 7.9Hz), 6.88-6.94 (3H, m), 7.04 (lH, t , J = 7.9Hz), 7.17 (111, d, J = 7.9Hz), 9.26 (lH, s), 9.39 (lH, br), 11.09 (111, s) elemental analysis' 0 C 2 5 Η 2 7 N 2 OF · CH 3 S 0 3 C Η NS it Calculated value 64.18 6.42 5.76 3.90 6.59 Long) 148 V. Description of the invention ()-. The following is the same, using 2-chenpropylmethyl-4acx- (3-methoxybenzene. ¾) -8-fluoro-1,2,3,4,43, 5,11,113 / 8-octahydro-611-indazolo [2,31] isoquinoline, substituted 2-cyclopropylmethyl-4aa- (3-methyl Phenyl) -7-fluoro_1,2,3,4,4 &amp;, 5,11, -113 / 3-octahydro-611- «| Momo [2,3-2] isoquinoline, giving 2 -Cyclopropylmethyl-4a〇t- (3-hydroxyphenyl) -8-fluoro-1,2,3,4,4a, 5,11,113 / 9-octahydro-6}}-indole And [2,3-Rong] isoquino_; using 2-cyclopropylmethyl-4act- (3-methylphenyl) -10-fluoro-1,2, 3,4, 4a, 5, 11, lla / 9-octahydro-6H- verazo [2,3-g] isoquinoline to give 2-cyclopropylmethyl-4xyl- (3-hydroxyphenyl) -1〇-fluoro-1 , 2,3,4,43,5,11,113 / 3-octahydro-6H-D5I cumulon [2,3-g] isoquinoline. Example 29 2-allyl_4aa-(3-methoxyphenyl) -1,2,3,4,4a, 5, 11,11a / 3 -octahydro-6H-indos [2, 3 -g〕 isoquinoline 30 (please read the precautions on the back before filling out this page)

(30) Line · Printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs under argon gas, 2- (2,2,2-trifluoroethane carbonyl) -4a α- (3-methoxyphenyl) -1, 2,3,4,43,5,11,113 / 5-octahydro-6} 1-indino [2,31] isoquinoline 130ng dissolved in 5b1 acetic acid, add 170mg zinc powder and stir at room temperature 2 hours. After removing zinc by filtration and distilling off the acetic acid under reduced pressure, 10 ml of a saturated aqueous solution of sodium hydrogensulfonate was added, and extracted 3 times with 3 ml of nitroform / methane (3/1). Combine the organic layer, wash with saturated saline, and dry the paper under argon using the Chinese National Standard (CNS) A4 specifications (210X297 gong) 149 Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A 6 B6 V. Description of the invention ()-_. The concentrated reaction mixture is dissolved in 100 ng of anhydrous DMF, 35 mg of sodium hydrogensulfonate and 23 «1 of allyl bromide are added, and heated to reflux for 30 minutes. After cooling to room temperature, the reaction solution was poured into 1 ml of water, and extracted 3 times with 3Gib1 atmosphere. The organic layers were combined, washed with saturated brine, dried, and concentrated to obtain 12〇Bg of oil. Separated and purified by chromatography tube [silica gel; acetone / methyl acetate (97/3)] to obtain 77 ng of crude crystals. This crude crystal was recrystallized with ethyl acetate to obtain 54 mg of the title compound, m.P. 188 ~ 189t: (yield 56.6%). IR (KB r) απ'1: 2930, 2838, 1609, 1578, 1460, 1294, 1238, 1042, 741 EI-MS (m / z): 372 (Μ *), 143 NMR (CDC 1 3) 500MHz 6 : 1.94-2.09 (2H, m), 2.39 (111, «,), 2.55-2.64 (2H, m), 2.80 (lH, m), 2.88-3.09 (7H, m), 3.68 (3 丨 丨, s ), 5.13-5.20 (2 &quot;, m), 5.9l (iH, m), 6.61 (lH, m), 7. (n-7.11 (5H, m), 7.21 (lH, m), 7.43 (lH, m), 7.58 (1H, brs) The following is the same, using 2- (2,2, 2-triazaethane carbonyl) _4a α-(3 -methylphenyl) -7 -methyl-1,2, 3,4,43,5,11,113 Ling-octahydro_511- | 1? |

Bg and [2,3-g] isoquinoline substituted 2- (2,2,2-triazaethoxycarbonyl) _4qi〇 (-(3_methoxybenzyl) _1,2,3,4,4 &amp;;, 5,11,113 / 5-octaqi ~ 6}]-11§ 丨 11¾ and [2,3-g] isoquine_, to give 2-allyl-4aa- (3-methoxyphenyl) -7-methyl-1,2,3,4,43,5,11,113 points-octahydro-61 &lt; -11§ | 115- [2,3-2] isoquinoline; use 2- (2 , 2,2-trichloroethoxycarbonyl) -4aa- (3-methylphenyl) -8-methyl-1,2,3,4,43,5,11,11 &9; octahydro- 6} 1-1) 5 丨 [1December (2,3 This paper standard uses the Chinese National Standard (CNS) A4 specification (210x297 male dragon> 150 (please read the precautions on the back and then write ) • ΤΓ. Line.

I A6 B 6 Printed by Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of the invention () -g] Isoquinoline to give 2-allyl-4aa- (3-methoxyphenyl) -8-methyl -1, 2,3,4,43,5,11,113 / 3-octahydro-6! 1-115 | 11-deca [2,3- 笤] isoquinoline: use 2- (2,2, 2-trifluoroethane carbonyl) -4aa-(3-methoxyphenyl) -9-methyl-1,2,3,4,43,5,11,113 / 3-octahydro-6 {1-ind1 ^ And [2,3- 笤:! Isoquinoline gives 2-allyl-4aa- (3-methoxyphenyl) -9-methyl-1,2,3, 4,4a, 5, ll, lla / S-octahydro-6H- P5I benzo [2,3-g] isoquinoline; use — 2- (2,2,2-trifluoroethanecarbonyl) -4aa-(3-methylphenyl) -10-methyl-1 , 2,3,4,43,5,11,11 &amp; / 3-octahydro-611-indoxo-8 [2,3-0] isoquinoline, to give 2-allyl-4aa- (3- Methylphenyl) -10-methyl-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-6} 1-indole [2,3-2] isoquinoline; Use 2- (2,2,2-trichloroethoxycarbonyl) -4a «-(3-methoxyphenyl) -7-gas-1,2,3,4,43,5,11,113 / 3-octa Hydrogen-6? 1-indazolo [2,3- &amp;] isoquinoline to give 2-allyl-4aa- (3-methoxyphenyl) -7-chloro-1,2,3,4 , 4a, 5,11, 11a /?-Octahydro-5H-ind [2,3-g] isoquinoline; use 2- (2,2,2-trichloroethane carbonyl) -4aα- (3- Methylphenyl) -8-chloro-l, 2,3,4,4a, 5, ll, lla / S-octahydro-6H-indPg- [2,3-g] isoquinoline to give 2- Allyl-43〇 (-(3-methoxyphenyl) -8-gas-1,2,3,4,4 &amp; 5,11,11 &amp; / 3-octa-6H-indo [ 2,3-g] isoquinoline; using 2- (2,2,2-trifluoroethyl chlorocarbonyl) -4 ugly [-(3-methoxyphenyl) -9-chloro-1,2,3 , 4,401,5,11 , 113 / 9-octahydro-6H-0? Isoquino [2,3-g] isoquinoline to give 2-allyl-4act- (3-methoxyphenyl) -9-chloro-1, 2,3,4,43,5,11,113 / 3-octahydro-6 {^ 11? 丨 eye [2,3-g] isoquinoline; use 2- (2,2,2-triaza Ethoxycarbonyl) -43 «-(3-methylphenyl) -10_chloro-1,2,3,4,43,5,11,113 / 3-octaqi-6 [{-indagonism [ 2,3-g] isoquinoline, to get 2-allyl-4aa- (3-methyl gas phenyl (please read the notes on the back before filling this page)

This paper uses the Chinese National Standard (CNS) A4 specifications (2) 0 X 297 male dragon) 151 Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs A 6 B6 V. Description of invention ()) -10-Ammonia-1 , 2,3,4,43,5,11,113 Lu-octahydro-611-indazolo [2,3-g] isoquinoline; using 2- (2,2,2-triethylethoxycarbonyl)- 43〇 (-(3-Methoxyphenyl) -7-bromo-1,2,3,4,43,5,11,113 Lu-octahydro-6} {-Indodecano [2,3-g] Isoquinoline gives 2-allyl-4-aa- (3-methylphenyl) -bumo-1,2,3,4,43,5,11,113 / 8-octahydro-6 »1- Ind 112 [2,3- 苕] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -43 «-(3-methoxyphenyl) -8'-bromo-1, 2,3,4,43,5,11,113 / 3-octahydro-611-ind 11 «^ [2,3-ming] Isoquino is given, and 2-pyridyl_4aa-(3-methoxyphenyl) is obtained 2,3,4,4 a, 5, ll, lla / 3 -octahydro-6H-indodece [2,3-g] isoquinoline; use 2- (2,2,2-trichloroethane Gas carbonyl) -4act-(3-methylphenyl) -9-bromo-1,2,3,4,43,5,11,113 / 9-octahexa-6} 1-0? 4dece [2, 3-Ju] isoquinoline to give 2-allyl-4aa- (3-methoxyphenyl) -9-bromo-1, 2,3,4,4a, 5, ll, ll 3 / 8-octa Hydrogen-6 ^ Indo [2,3-Ming] Quino; use 2- (2,2,2-trichloroethoxycarbonyl) -4aa-(3-methylphenyl) -10-bromo-1,2,3, 4,4a, 5, 11,11a /?-Octahydro-6H-indPg and [2,3-g] isoquino get 2-allyl_4 £ 1〇 (_ (3-methyl gas phenyl) _10_ desert _1, 2, 3 , 4,4 &amp;, 5,11,113 / 3_octahydro-611-indo [2,31] isosleepoline; use 2- (2,2,2-trifluoroethoxycarbonyl) -4act- (3-methoxyphenyl)-?-Fluoro-1,2,3,4,4a, 5, ll, lla; 3-octahydro-6H-indazolo [2,3-g] isocin, Obtained 2-allyl-4aa- (3-methylphenyl) -7-fluoro-1,2,3.4,43,5,11,113 / 3-octahydro-611-indapto [2,31] iso Quinoline; using 2- (2,2,2-trichloroethane carbonyl) -43 a- (3-methylphenyl) -8-fluoro-1,2,3,4,43,5,11, 113zhao-octahydro-6H-indazolo [2,3-g] isoquinoline to give 2-allyl_4a «-(3_methyl gas phenyl) -8-fluoro-1,2,3 , 4,43,5,11,113 call-octahydro-6} 1-indole 5 and [2 This paper standard is used in China National Standard (CNS) A4 specifications (210x297 mm) -152-(please first Read the precautions on the back and then write this page) Installation and thread. 4 J ΰ -42 ϋ 3

66 AB clearly stated that it was printed by the Beigong Consumer Cooperative of the Ministry of Economic Affairs, Standards Bureau, 31] isoquinoline; using 2- (2,2,2-trihelethoxycarbonyl) -43〇 (-(3- Methylphenyl) -9-fluoro-1,2,3,4,43,5,11,113-octahydro-611-115, decano [2,3-g] isoquinoline to give 2-ene Propyl-4act- (3-methylphenyl) _9-1,2,3,4,43,5,11,113-octahydro-611-indolo [2,3-2] isoquinoline; use 2- (2,2,2 ^ trichloroethoxycarbonyl) -43〇 (-(3-methoxyphenyl) -10-fluoro-1,2,3,4,43,5,11,113 / 8 -Octahydro-6} 1-indo [2,3- 苕 '·] isoquinoline, to give 2-allyl-4aa- (3-methylphenyl) -10-fluoro-1,2, 3,4,4a, 5, 11,11a-octahydro-6H-indo [2,3-g] isoquinoline; use 2- (2,2,2-trichloroethane carbonyl) -4aa -(3-methoxyphenyl) -7-nitro-1,2,3,4,43,5,11,113 Lu-octahydro-611-indo [2,3-tin] isoquine Df In this way, 2-allyl-4a α-(3-methylphenyl) -7-nitro-1,2,3,4, 4a, 5,11,113 / 3-octa-6-6 1-ind 0decor 〔2,3 ~ 8〕 isoquinoline; use 2- (2,2, 2-trichloroethoxycarbonyl) -4aa-(3-methylphenyl) -8-nitro-1,2 , 3, 4,4a, 5, ll, llay9-octahydro-6H-indo [2,3- g] Isoquinoline to give 2-allyl-4a α-(3-methoxyphenyl) -8-nitro-1,2, 3, 4,4a, 5, 11, lla / S-octahydro -6H- »5 | Pg and [2,3-g] isoquinoline; using 2- (2,2,2-trichloroethoxycarbonyl) -4aa-(3-methylphenyl) -9-nitro Group-1,2,3,4,4a, 5,11,113 / 3-octahydro-6} 1-indop [2,31] isoquino, to give 2-allyl-43〇 (-(3 -Methylphenyl) -9-nitro-1,2,3,4,43,5,11,113 / 3-octahydro-6 hepatic indole [2,31] isoquinoline; use 2- (2,2,2-triazaethoxyphile) -4aa _- (3-methylphenyl) -10-nitro-1, 2,3,4,4a, 5, ll, lla / 3-octa Hydrogen-6H-Embrane-8 [2,3-g] isoquinoline to give 2-allyl (((3-methoxyphenyl) -1〇-nitro-1,2,3,4 , 43,5,11,113 / 5-octahydro-6 H-ind DS- [2,3-g] isoquinoline: use 2- (2,2,2-triazaethane carbonyl (please read first Please pay attention to the back page and fill out this page). The size of this paper is in accordance with the Chinese National Standard (CNS) A 4 specifications (210x297 male dragon) -153-A 6 B6

V. Description of the invention (yl) -4aa-(3-methoxyphenyl) -1,2, 3, 4,4a, 5,11,11a / 3 -octahydro-6 Η-IND0decoc [2, 3-g] isoquinoline to give 2-allyl-4acx- (3-methylphenyl) -1,2,3,4,43,5,11,113-octahydro-6-methyl-indene Eye and [2, 3-g] isoquinoline. Example 30 2-allyl-4aa-(3-hydroxyphenyl) -1,2,3,4,4a, 5,11,11a xi-octahydro-6H-indeno [2,3-g] Isoquinoline 31 (31) (Please read the precautions on the back before filling in this page) Binding-Order _ Printed by the Central Standards Bureau of the Ministry of Economic Affairs β Industrial and Consumer Cooperatives under the argon gas to 2-allyl-4aa-(3 -Methoxyphenyl) -1,2,3,4, 43,5,11,113 / 3-octahydro-6 only-indo [2,3-8] isoquinoline 13〇1 ^ dissolved in 5ml Anhydrous DMF, η-propane thiol 0.35ng, potassium-t-butanol 390mg was added, and stirred at 130 ° C for 6 hours. After cooling to room temperature, DMF was distilled off under reduced pressure, 5 ml of water was added, and extracted 3 times with 20 ml of chloroform. The organic layers were combined, washed with saturated saline, separated by chromatography tube [silica gel; chloroform / methanol / 28% ammonia water (95/5 / 0.2)], refined and dried, and concentrated to obtain 130 mg of oily substance, giving 110 mg of powder . Suspend it in 1ml of formazan, add 22 ^ 1 of methanesulfonic acid to make methanesulfonate, separate and refine it by chromatography tube [Sephadex, LH-20; methanol] to obtain 130nig crude crystals Ethanol was recrystallized to obtain the title compound methanesulfonate (decomposed at 250 ° C) 67mg (yield 42.2%). This paper scale uses the Chinese National Standards (CNS) A 4 specifications (210 father 297 male jade) -154-A6 B 6 5. Description of the invention () IR (KB r) cm-1: 3416, 1601, 1460, 1212, 1160, 1042 FAB-MS (m / z): 3 5 9 (IV. + 1) NMR (D M S 〇-d6) 500Mllz δ: 2.03 (lll.m), .32 (3H, s), 2.54 -2.62 (3H, m), 2.87- -3.02 (311, m), 3.10 (1H, = 15.8 丨 lz), 3.30- 3.41 (2H, m), 3.61 (111, m), 3.79 (2H, m ), 5. 5.56 (2H, m), 5.92 (lH, m), 6.54 (11, dd, J = 7.9 Hz, 1.8 Hz), 6.89-6.94 (311, m), 6.98 (1 H, m) , '7.04 (1H, t, J = 7.9 IIz), 7. 18 (1H, d, J = 7.9 Hz), 7.33 (1H, d, J = 7.9 I! Z), 9.26 (lH, s), 9.64 (111, br), 10.61 (lH, s) elemental analysis CzdHztNz 65.44 6.60 6 • 08 7.02 The following is the same, use 2-allyl-4aa- (3-methoxyphenyl) -7-methyl-1,2,3,4,4a, 5,11, lla> Q -Octahydro-6H-indPg and [2,3-g] (Please read the precautions on the back before filling in this page) Dingxiang Central Bureau of Economics Industrial and consumer cooperatives printed isoquinoline substituted 2-allyl-4aa- (3-methoxyphenyl) -l, 2,3,4,4a, 5, ll, llayS-octahydro-6H-indBg and [2,3-g] isoquinoline to give 2-allyl-43〇 (-(3-benzylphenyl) -7-methyl-1,2,3,4 &gt; 4 &, 5,11, 11 ug / 3-octahydro-6H-indo [2,3-g] isoquinoline; using 2-allyl-4aa- (3-methoxyphenyl) -8-methyl-1,2 , 3,4,48,5,11,1130 -Octahydro-6H-indP and [2,3-g] isothiocyanate, to give the propyl propyl-4aa- (3-pyridyl) -8- Methyl-1, 2,3,4,43,5,11,113 / 3-octahydro-61 ^ indo [2,3-end; 1 isoquinoline on paper scale Chinese National Standard (CNS 4) Specifications (210x297 mm) A 6 B6 Printed by the Consumer Standardization Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (; using 2-allyl-4aa- (3-methoxyphenyl) -9-methyl -1,2,3,4, 43,5,11,113 Ling-octahydro-6} 1-ind112 [2,3-ming] isoquinoline, to give 2-allyl- 4act- (3 -Hydroxyphenyl) -9-methyl-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-ind Ug3 ^ (2,3-g] isoquinoline; use 2 -Allyl-4a 〇 (-(3-methylphenyl-)-1 ^^^^^ &quot;, 3,4., 43,5,11,113zhao-octahydro-61 ^ -ind And [2,3-g] isopyroline, to get 2--propyl-4acx- (3-via phenyl)-10-methyl-1, 2, 3, 4, 43, 5, 11, 113 ; 3-octahydro-6} 1-ind0-deco [2, 3-g] isoquino; use 2-allyl-4 a α-(3 -methylphenyl) -7 -gas-1 , 2,3,4,43,5,11,113 / 3-octahydro-611-ind "8- [2,31] isoquinoline, to give 2-allylpropyl-4aa- (3-pyridyl)- 7 -Gas-1,2, 3,4,4a, 5,11, lla / 3 -octahydro-6H-indo [2,3-g] isoquinoline; use 2-allyl-4 〇 &lt;-( 3-Methoxyphenyl) -8-ambient-1,2,3,4,43,5,11,113 / 9-octahydro-6H-indolo [2,3-g] Isoquinoline, which gives 2-allyl-4aa- (3-hydroxyphenyl) -8-chloro-1,2,3,4,43,5,11,113 / 8-octahydro-611-indo [ 2, 3-g] Iso-satisfaction: use 2-allyl-4aa- (3-methylphenyl) -9-chloro-1,2,3,4,43,5,11,113 / 3-octahydro _611-Indoxo [2,3-ming] isoquino is given, which gives 2-allyl-4aa- (3-benzyl) -9-chloro-1,2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indolo [2,3-g] isoquinoline; using 2-allyl-4 &amp; 〇 (-(3-methylphenyl) -1〇-gas -1,2,3,4,43,5,11,113 / 9-octahydro-6H-P5 | Dg and [2,3-g] isoquinoline to give 2-ene -4acx- (3-hydroxyphenyl) -1〇-atmosphere-1,2,3,4,43,5,11,113 / 3-octahydro-61ind05 [2,3-g] isoquinoline ; Using 2-allyl-4aa- (3-methoxyphenyl) -7-bromo-1,2,3,4,43,5,11,113 / 3-octahydro-611-indho [2, 3-Ming] Isoquinoline, 2-allyl-4aa-(3-hydroxyphenyl) -7-bromo-1,2, 3,4,4a, 5 This paper scale is used in China National Standard (CNS ) A 4 specifications (210X297 male dragon) -156-(Please read the precautions on the back before filling this page)

A 6 B6 printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of the invention (), ll, lla / S-octahydro-6H-D5 | Bg and [2,3-g] isoquinoline; 2-ene Propyl-4a α-(3-methoxyphenyl) -8-bromo-1,2,3,4,4a, 5, 11, 11a / 3 -octahydro-6H-indole [2,3- g] Isomorpholine, which gives 2-isopropyl-4aa- (3-hydroxyphenyl) -8-bromo-1,2,3,4,4a, 5, 11, 11a / 3 -octahydro-6H- Ind Ug and [2,3-g] isoquinoline; using 2-allyl-4aa- (3-methoxyphenyl) -9-bromo-1,2,3,4,43,5,11,113 / 3-octahydro-6! 1-ind118 [2,3-each] iso-quinoline to give 2-allyl-4aa-(3-hydroxyphenyl) -9-bromo-1,2, 3 , 4, 4a, 5, ll, lla / S -octahydro-6H-indo [2,3-g] isoquinoline; use 2-allyl-4aa- (3-methylphenyl)- 10-bromo-l, 2,3,4,4a, 5, ll, llajS-octahydro-6H-indazolo [2,3-g] isoquino, to give 2-allyl-4aa- (3 -Hydroxyphenyl) -1〇-bromo-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-6} 1-ind 115- [2,3-g] isoquinoline; use 2-allyl-4a〇t- (3-methoxyphenyl) -7-fluoro-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-6} 1-ind Conjugating [2,3-layer] isoquinoline to give 2-allyl-4acx- (3-hydroxyphenyl) -7-fluoro-1 , 2,3,4, 43,5,11,113 / 3-octahydro-6 ^ 丨 〇8- [2,3-ming] isoquinoline; using 2-allyl-4aa-(3-methylbenzene Group) -8-fluoro-1,2, 3,4,4a, 5, 11,11 a / 9-octahydro-6H-indazolo [2,3-g] isoquinoline to give 2-allyl Yl-4aa-(3-hydroxyphenyl) -8-fluoro-1,2, 3,4, 4a, 5, 11,11a / 3 -octahydro-6H-indopodo [2,3-g] Isoquinoline; using 2-allyl-4aa- (3-methoxyphenyl) -9-fluoro-1,2,3,4,43,5,11,113 / 3-octahydro-611-11? | Indo [2,31] isoquinoline, which gives 2-allyl-4aa- (3-hydroxyphenyl) -9-fluoro-1,2,3,4, 43,5,11,11 &amp; / 3 -Octahydro-6} 1-indole 5 [2,3-Ju] isoquinoline; use 2-allyl-4aa- (3-methoxyphenyl) -10-fluoro-1,2,3 , 4, 4a, 5,11, lla / 3-octahydro-6H-indeno [2,3-g] isoquinoline, to obtain 2-allyl-4a (please read the precautions on the back before filling in this Page) Install & Thread-This paper standard uses Chinese National Standard (CNS) A4 specifications (210x297 public goods) 157 I, V. Description of invention () 2, 3, 4, 4a, 5, 11, 11a / 3 -Octahydro-6H-indα- (3-hydroxyphenyl, Ministry of Economic Affairs Central Standards Bureau Beigong Consumer Cooperatives, printed the imprint [2,3-g] isoquinoline; using 2-allyl-4acc- (3 -A Phenyl) -7-nitro-1,2,3,4,43,5,11,113 / 9-octahydro-6 ^ indodecano [2,3-g] isoquinoline to give 2-allyl Yl-4act- (3-hydroxyphenyl) -7-nitro-1, 2, 3, 4, 4a, 5, 11, 11a lu-octahydro-6H- 禧 Bg and [2,3-1] iso Quinoline; using 2-allyl-4aa-(3-methoxyphenyl) -8-nitro-1,2, 3,4,4a, 5,11,113 / 3-octahydro-611-indazol [2,3-2] isoquinoline, to give 2-allyl-43 «-(3-hydroxyphenyl) -8-nitro-1,2,3,4,43,5,11,113 Hydrogen-6H-indog (2,3-g) isoquinoline; using 2-allyl-4aa- (3-methylphenyl) -9-nitro-1,2,3,4, 43,5,11,113 / 9-octahydro-611-ind Pg- [2,3-g] isoquinoline to give 2-allyl-4aa- (3-hydroxyphenyl) -9-nitro-1 , 2,3,4,43,5,11,113 /?-Octahydro-611-〇5 Shun- [2,3-g] isoquinoline; use 2-allyl-4act- (3-methoxy Phenyl) -10-nitro-1,2,3,4,43,5,11,113 / 9-octahydro-6} 1-indo [2,31] isoquinoline to give 2-ene Propyl-4act-(3-hydroxyphenyl) -10-nitro-1,2,3,4,4a, 5,11,113 / 5-octahydro-611-indazolo [2,31] isoquinoline ; Using 2-allyl-4aa- (3-methylphenyl) -1,2,3,4,4a, 5,11, lla ^ S-octahydro-6-methyl-indigo 2,3-g] isoquinoline. 2-allyl-4aa- (3-hydroxyphenyl) -1,2,3,4,43,5,11,113 / 9-octahydro-6-methyl -Indolo [2, 3-g] isoquinoline. Reference Example 3 2- (2,2,2-trichloroethane carbonyl) -43〇 (-(3-methoxyphenyl) -6-acetoxy-1,2,3,4,4a, 5 , 6,7,8,8a / 3 -decahydroisoquinoline 32 158 This paper scale uses Chinese National Standard (CNS) A4 specifications (210x297 g; «:) A 6 B6 ^ 1β〇4 () 〇

(Please read the precautions on the back before filling in this page) (32) OAc Dissolve 2.64g of proton adsorbent under argon in 64Qnl of anhydrous 1,2-digas ethane, cool to 0 ° C, add , 2,2-trichloroethyl chloroformate 1.35ral. 2-methyl-4aa- (3-methoxyphenyl) -6-acetoxy-1,2,3,4,4a, 5,6,7,8,8a / 3-decahydroisoquine 2.61 g of phenanthroline was dissolved in 15 ml of anhydrous 1,2-difluoroethane and dropped into it, warmed to room temperature, and stirred for 30 minutes. 1,2-Dichloroethane was distilled off under reduced pressure, 60nl of ethyl acetate was added, washed with 20ml of 1N hydrochloric acid and 2Qnil of saturated brine, dried and concentrated to obtain 4.14g of oil. Separate and refine this oil by chromatography tube [silica gel; cyclohexane / ethyl acetate (4/1)] to obtain 6 / 3-acetyl gas 950rag and 6α-acetyl gas and 6 / 3-acetyl oxygen The mixture of skulls is 2.41 mm (yield 85.3%). IR (liquid film method) an · 1: 1717, 1433, 1241, 1125, 1033, 71G EI-MS (m / z): 477 (Μ *), 479, 481 NMR (CDC 1 3) 500Hllz '6: 1.43 -1.49 (2H, m), printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 1.65 (111, td, J = 13.2112, 4.0112), 1.74 (111, m), 1.83 (111,0!), 1.96 (311 , s), 2.05 (111, brd, J = 14.3Hz). 2. 13-2. 19 (211, m), 2.4 7 (111, m), 2.60 (111, m), 3.58 (111, m) , 3.81 (311, s), 3. 95 (1II, m), 4.07 (111, tn), 4.39 (III, m), 4. .G8-4. 78 (211, m), G. 7 &lt; 1 ( 11 !, dd, J = 8. 1 112,2.2112), 6.99-7.05 (2ll, m), 7. 26 (1II, t, J = 8. 1 llz) This paper scale is free to use the Chinese National Standard (CNS) A 4 specifications (210x297 g *)-159-A 6 B6 3〇tC〇4 5. Description of the invention () Reference Example 4 2-cyclopropylcarbonyl-4aa-(3-methoxyphenyl) -6 / 3- Acetoxy-1, 2, 3, 4, 4a, 5, 6, 7, 8, 8a / 3-decahydroisoquinoline 33

(Please read the precautions on the back before filling in this page) Under argon, place 2- (2,2,2-trichloroethoxycarbonyl) -4aa-(3-methoxyphenyl) -6; 3-ethyl Acetyloxy-1,2,3,4,4a, 5,6,7,8,8a / 3 -decahydroisoquinoline 945mg dissolved in 2Qdi1 acetic acid, add zinc powder 1.3Qg, stir at room temperature for 24 hour. After removing zinc by filtration and distilling off the acetic acid under reduced pressure, a saturated aqueous solution of sodium hydrogensulfate was added to make it alkaline, and extracted with chloroform 5 Om 1 three times. Combine the organic layers, wash with saturated brine, dissolve the dried and concentrated reactant 5 70iog in 20 ml of anhydrous dichloromethane under argon, add 0.55 ml of triethylamine and Q.27 ml of cyclopropane carbonyl gas. Stir at room temperature for 2 hours. Wash with 1N hydrochloric acid and water, dry and concentrate to obtain 7 9 Qing oil. This oil was separated and purified by chromatography tube [δ evening gum: chloroform / ethyl acetate (9/1)] to obtain the title compound 4 30 ng (yield 58.6%). I R (liquid film method) cm-1: 1731, 1634, 1439, 1243, 1031

El—MS (m // z): 371 (M *) NMR (CDC 1 3) 400MHz δ: 0.69-0.78 (2H, m), 0.92- 1.00 (2H, m), 1.39- 1.50 (2H, m) , 1.63 (111, m), 1.69-1.8 This paper scale is printed and printed in China National Standard (CNS) A4 specifications (210X297 public). The R7 is printed by the Employee Consumer Cooperative of the Bureau of Standards of the Ministry of Economy

Η

301634 A7 2 (3H, m), l-96 (3H, s), 2.04-2.18 (311, m), 2.48 (111, m), 2.55-2.72 (11 !, br), 3.40-3.58 (111, br), 3.81 (3H, s), 4.01-4.43 (3H, m), 6.74 (lH, dd, J = 8.3llz, 2.0 \\ z), 7. 01-7. 06 (211, m), 7 -26 (111, t, J = 8.1 Hz) Reference Example 5 2-cyclopropylmethyl-4aa-(3-methoxyphenyl) -6/3 -residue-1,2,3, 4, 4a, 5, 6, 7, 8, 8a / 3-decahydroisoquinoline 34 (3〇

OH 190 mg of lithium aluminum hydroxide was suspended in 15 ml of anhydrous THF under argon, and cooled to 0¾. In addition, 2-cyclopropylcarbonyl-4aa-(3-methoxyphenyl) -6/8 -acetoxy-1,2,3,4,4a, 5,6,7,8,8a / 3 -430 mg of decahydroisoquinoline was dissolved in 5 ml of anhydrous THF, dropped into it, warmed to room temperature, and stirred for 2 hours. After cooling to zero, add a saturated aqueous solution of ethyl acetate and sodium tartrate. The insoluble matter was removed by filtration, and ethyl acetate was distilled off under reduced pressure to obtain the title compound of 360rag (yield 98.6%). IR (liquid desorption) a &quot; .1: 3340, 2942, 1607, 1580. 1241, 1075, 1052, 731 EI-MS (m / ζ): 315 (Μ *), 314 NMR (CDCI 3) 400MHz δ: 0.04-0.09 (211, m). China National Standard (CNS) A4 specification (210X297mm) --------- approved clothing ------ IT ------ ^ (please first Read the precautions on the back and fill in this page) 161 C〇4 A6 B6 V. Description of the invention () 0.44- 0.50 (211, ηι), 0.83 (1II, m), 1. 36-1. 42 (211, nt) , 1.64-1.86 (4Ii.ni), 1.93- 2.28 (611, m), 2.39 (111,0)), 2.68 (1II, t, J = 12. 0 llz), 2.76 (111, d, J = 11.2 llz), 2.92 (111, m), 3.31 (111, «0, 3.80 (3II, s), 6.69 (111, m), 7.Oi-7.05 (211, m), 7.21 (HI. L, J = 8. Ollz) Reference Example 6 2-cyclopropylmethyl-4a ct-(3-methoxyphenyl) -6 -aero-1,2,3 / 4,4a, 5,6,7,8, 8a / 3 -decahydroisoquinoline 35 Η

(35) (Please read the precautions on the back before writing this page) Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs, dissolving oxalaldehyde chloride ol lull in 5id1 anhydrous dioxane under argon and cooling to -55 it. In addition, 0.20ml of DMSO was dissolved in 0.5nl of anhydrous difluoromethane, which was added dropwise and stirred at -55 ° C for 5 minutes, then 2-cyclopropylmethyl-4aa- (3-methylphenyl) ) -6 / 9-Hydroxy-1,2,3, 4,4a, 5,6, 7,8,8a / 3 -decahydroisoquinoline 360mg dissolved in 2ral anhydrous dichloromethane and dripped into it. After stirring at -55 ° C for 15 minutes, 1.Oral trifluoroethylamine was added dropwise and the temperature was raised to room temperature. 5ml of water was added to the reaction solution, which was separated into two layers, and the organic layer was washed with saturated saline, dried, and concentrated to obtain 3 Qmg of oil. Separate and refine this oil by chromatography tube [silica gel; nitroform / methanol / 28% ammonia (98/2 / 0.1)] to obtain 290 mg of the title compound (yield 81.1%). Paper Scale Xiao uses the Chinese National Standard (CNS) standard 4 (210X297 gongjie) 162 V. Description of invention () A 6 B6 Printed by the employee consumer cooperative of the Bureau of Standards and Standards of the Ministry of Economic Affairs, reference examples 4 ~ 6, by 2- ( 2,2,2-triazaethoxycarbonyl) -4 3〇 (-(3-methylphenyl) -6〇 (-acetaldehydeamino-1,2,3,4,43,5,6, 7,8,8 &amp;; 8-Decahydroisoquinoline and 2- (2,2,2-trichloroethoxycarbonyl) -4aa-(3-methoxyphenyl) -6 Ling-Acetyl- A mixture of 12,3,4,43,5,6,7,8,83 / 9-decahydroisoquinoline 1.21g gives 2-cyclopropylmethyl-4act- (3-methylphenyl) -6 -Aero-1,2,3,4,43,5,6,7,8,83 / 9-decahydroisoquinoline 48〇1 ^ (yield 60.6%) 〇1 R (liquid film method) cm -丨: 2942, 1715, 1582, 1245, 1050,754 EI-MS (m / z): 313 (M +) NMR (CDC 1 3) 400MHz (ί: 0.06-0.12 (2H, m), 0.46-0.54 (2H, m), 0.87 (111, m), 1. 94-2. 11 (4 H, m), 2.24-2.54 (7H, m), 2.68 (^, 1 ^ = 11.7112), 2.84 (1II, m), 2.92 (lH, m), 3.05 (lH, m), 3.78 (3H, s ), 6.69 (lH, ni), 6.97-7.00 (211, m), 7.21 (III, t, J = 8.3ilz) According to Reference Examples 4 ~ 6, using propylene acetyl chloride instead of cyclopropyl chlorinated to give 2- Rare propyl-4aa- (3-methoxyphenyl) -6-oxo-1, 2,3,4,4a, 5,6,7,8,83 / 3-decahydroisoquinoline; use benzene Acetyl chloride, 2-benzyl-43〇 (-(3-methoxyphenyl) -6-oxo-1,2,3,4,4a, 5,6,7,8,8a / 9-dec Hydrogen isoquinoline; using styrene gas to give 2-phenethyl_4a α-(3-methoxyphenyl) -6-gaso-1, 2, 3, 4, 4 a, 5, 6, 7, 8, 8 a / 3 -decahydroisoquinoline Example 3 1 2-Cyclopropylmethyl-4aot- (3-methoxyphenyl) -9_fluoro-1,2,3, 4, 4a, 5, ll, lla / 3-八 氲 -6H-D51 2 and [2,3-g] isoquinoline 36 (please read the precautions on the back before filling in this page) Pack. Order_ This paper size Use the Chinese National Standard (CNS) A4 specifications (210x297 g). 5. Description of invention () Η

A6 B 6

F (36) The Ministry of Economic Affairs Central Standards Bureau employee consumer cooperative printed 2-cyclopropylmethyl-4aa-(3-methylphenyl) -6-gasoline-1,2, 3, 4 under argon , 4a, 5, 6, 7, 8, 8a / 3 -decahydroisoquinoline 32〇Bg and 4-fluorophenylhydrazine hydrochloride 195mg dissolved in 10ml of ethanol, heated at 80 ° C. Add 0.65 ml of methanesulfonic acid, and stir at 8Q ° C for 15 minutes, then cool to room temperature. The ethanol was distilled off under reduced pressure, 1N aqueous sodium hydroxide solution was added to make it alkaline, and extracted with 30 ml of chloroform. The organic layers were combined, washed with saturated saline, dried and concentrated to obtain 370 ng of powder. Separated and purified by chromatography tube [silica gel; chloroform / methanol (97/3)] to obtain the sample compound of 36% (yield 87.2%). IR (KB r) cm- ': 2898, 1607, 1580, 1489, 1460, 1294, 1238, 1044 EI-MS (m / z): 404 (M *), 242, 161 NMR (CDC 1 3) 400MHz 6 : 0.05-0.14 (211, m), 0-47 -0.56 (211, m), 0.90 (III, m), 1. 95-2.07 (2H, m), 2.22-2.32 (211, m), 2.39 ( 111, m), 2.53-2.64 (2! L, m), 2.87-2.99 (4H, m), 3.06 (1II, d, J = 16. lilz), 3. 15 (111, d, J = 8.8Kz ), 3.68 (3H, s), 6. 62 (111, m), 6.80 (111, td, 9.0Hz, 2.4Hz), 7. 00-7. 11 (511, m), 7.58 (111, brs) The following is the same, using phenylhydrazine to replace 4-fluorophenylhydrazine. 2-cyclopropylmethyl-43 «-(3-methoxyphenyl) -1,2,3,4.4 lines, 5,11, 11 &amp; / 3-Eight (please read the precautions on the back before filling in this page) Binding and Ordering-This paper standard uses the Chinese B Family Standard (CNS) A 4 specifications (210x297 mm) 164 A 6 B6 Central Ministry of Economic Affairs Printed by the Bureau of Standards and Employee Consumer Cooperative V. Description of the invention () Hydrogen-6H-D? Dioxa [2,3-g] isoquinoline; using 3-fluorophenylhydrazine, 2-cyclopropylmethyl- 4a α-(3-methylphenyl) -8-fluoro-1,2,3,4,4a, 5,11, g] isoquinoline and 2-cyclopropylmethyl-, 3,4, 4a, 5, ll, l.la / 3 -octahydro-6H-indeno [2,3-g] isoquinoline; using 2-fluorophenyl trap to give 2-cyclopropylmethyl-4a α -(3-methylphenyl) -7-fluoro-1, 2, 3,4,4a, 5, 11, 1Γ a / 3 -octahydro-6H-indPg (〔2,3-g〕 isoquine Porphyrin; using 4-methylphenylhydrazine to give 2-cyclopropylmethyl-4act-(3-methylphenyl) -9-methyl-1,2,3, 4,43,5,11, 11 &amp; / 3-octahydro-6} 1-ind115 [2,3-min] isoquinoline; using 3-methylphenylhydrazine to give 2-cyclopropylmethyl-4aa- (3-methyl Oxyphenyl) -8-methyl-1,2,3,4,43,5,11,113 / 9-octahydro-61 oxo- [2,3-g] isoquinoline and 2-cyclopropyl Methylmethyl-4a〇t- (3-methoxyphenyl) -10-methyl-1,2,3,4,4a, 5,11,1 la / 9-octahydro-6H-indazolo [ 2, 3-g] isoquinoline; using 2-methylphenylhydrazine. 2-cyclopropylmethyl-4acc- (3-methylphenyl) -7-methyl-1,2,3, 4,43,5,11,113 / 3-octahydro-611- vera [2,3-g] isoquinoline; using 4-chlorophenylhydrazine to give 2-cyclopropylmethyl-43〇 (- (3-Methoxyphenyl) -9-atmosphere-1,2,3,4,43,5,11,113 / 9-octahydro-6Η-0ζ 丨 Momo [2,3-g] isoquinoline: use 3-nitrophenyl trap to give 2-cyclopropylmethyl-4aa- (3_ A Phenyl) -8-chloro-1,2,3,4,4a, 5,11,11 a / Q-octahydro-6H-indazolo [2,3-g] isoquinoline and 2-cyclopropyl Ylmethyl-4 3〇- (3-methylphenyl) -10-gas-1,2,3,4,4 pattern, 5,11,11 & / 9-octahydro-6H-indolo [ 2,3-g] isoquinine; using 2-gas phenyl trap to give 2-cyclopropylmethyl-4aa- (3-methylchlorophenyl) -7-ambient-1,2,3,4, 4a, 5,11,11 a / 3-octahydro-6H-indoquino [2,3-g] isoquinoline; use 4-bromophenylhydrazine lla / 3 -octahydro-6H-indolo 4aa-(3-methylphenyl)

(Please read the precautions on the back before filling in this page) Binding-Order-This paper is used in China National Standard (CNS) A4 specifications (210x297 public goods). A6 __B6_ printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs Description of the invention () to give 2-cyclopropylmethyl-4a α-(3-methylphenyl) -9-gas-1, 2, 3,4, 4a, 5,11,11 &amp; / 3-octa Hydrogen-6 {1-ind11duo [2,3-ming] isoquinoline; using 3-bromophenyl trap to give 2-cyclopropylmethyl-4a α-(3-methoxyphenyl)- 8-ambient-1, 2,3,41,43,5,11,113 / 3-octahydro-611-indodec [2,3-min] isoquino and 2-cyclopropylmethyl-4a a -C3-Methoxybenzyl) -10-fluoro-1,2, 3,4,4a, 5, ll, lla / S -octahydro-6H-B5I iso [2,3-g] isoquinoline; Use of 2-bromo '· phenylhydrazine to give 2-cyclopropylmethyl-4aa- (3-methylphenyl) -7-gas-1,2,3,4,43,5,11,113zhao-8 Hydrogen-6} 1-115 丨 hetero [2,31] isoquinoline .; using 4-nitrophenylhydrazine to give 2-cyclopropylmethyl-4a «-(3-methylphenyl) _9 -Chloro-1,2,3,4,43,5,11,113 / 9-octahydro-6} 1-0? | 11deca [2,3-§] isoquinoline; use 3-nitro Phenylhydrazine to give 2-cyclopropylmethyl-4a α-(3-methylphenyl)- 8-chloro-1,2,3,4,43,5,11,113 / 9-octahydro-6}}-indazolo [2,3-g] isoquinine and 2-cyclopropylmethyl-4aa -(3-methoxyphenyl) -10-fluoro-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-6 ^ dolo [2,3-g] isoquinoline; Using 2-nitrophenylhydrazine, 2-cyclopropylmethyl-4 acx- (3-methoxyphenyl) -7-chloro-1, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indus [2,3-g] isoquinoline: use of methyl-buphenyl trap to give 2-cyclopropylmethyl-4act- (3-methylphenyl) -1 , 2,3,4,4a, 5,11,11 a / 3-octahydro-6-methyl-indolo [2, 3-g] isoquinoline. Example 3 2 2-cyclopropylmethyl-4act-(3-hydroxyphenyl) -9-fluoro-1,2,3,4,4a, 5,11, lla / S -octahydro-6H-ind And [2, 3-g] isoquinoline 37 (please read the precautions on the back before writing this page). Binding-Thread-This paper standard is used in China National Standard (CNS) Grade 4 (210x297 public goods) ) Ββ.

-V.J • Z i A7 B7 5. Description of invention (

. (37) OH Ministry of Economic Affairs Central Standards Bureau employee consumer cooperative printed and polymerized 2-cyclopropylmethyl-4aa- (3-methoxyphenyl> -9-fluoro-l, 2,3,4 under argon , 4a, 5, ll, lla / 9 -octahydro-6H-B-indo [2,3-g] isoquinoline. 250mg dissolved in 6ml of anhydrous DMF, add potassium-t-butoxide 350mg and N -Propane thiol 0.31ml * Stir at 150 ° C for 3 hours. After cooling to room temperature, remove the DMF from the reduced pressure box, add 10ml of water, and extract 3 times with M30ml of chloroform / methanol (3/1). Combine Organic calendar, washed with saturated brine, dried and concentrated to obtain 220 mg of powder. Suspend the powder in 2 ml of methanol, add 40 ml of methanesulfonic acid to make methanesulfonate, M chromatography tube [ Sephadex, LH-20; methanol] Separation and purification to obtain methanesulfonate (decomposition of 245t) 199mg (yield 66.2%) of the Sassafras compound. IR (KB r) or 1: 3392, 1586, 1477, 1249, 1173, 1049, 790F AB-MS (m / ζ): 391 (Η * +1) NMR (DMSO-dt,) 500ΜΠζ δ: 0.35-0.41 (2li, m), 0.Gl-0.65 (211, m), 1.07 (111, m), 2.07 (111,11,), 2.31 (311s), 2.53-2.G7 (3li, m), 2.87-3.06 (511, ™), 3. 12 (1II, d , J = 1 .51lz), 3.48 (111, m), 3.51 (111, m), 3.72 (111, m), G.54 (lll, m), G.80 (111, Ld, J = 9. 2llz, 2.4llz ) .6.22 (lil.brs), C. 93 (1II, brd, J = S-6llz), 7.04 (111, LJ = 7.9IIz), 7.09 (1II, (3 d, J = 9. 8liz, 2.4 llz) This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) (please read the precautions on the back and then fill out this page) Order-167-A 6 B6 V. Description of invention () 7. 17 ( 111, dd, J = 8.5llz, 4.3Hz), 9.26 (111, s),, 9.40 (111, brs) 10.73 (111, s) Elemental analysis C 2 5 Η 2 7 Ν τ OF • C II 3 SO CHNF s ^ 十 箅 値 64. 18 C. 42 5.76 3.90 6.59 実 渤 値 63.91 6.61 5.91 3.91 6.57 (please read the precautions on the back before filling in this page) Example 3 3 2-cyclopropylcarbonyl-4aa-(3- Methoxyphenyl) -7-chloro-1,2,3,4,4a, 5,11,1 la / 3-octahydro-6H-indazolo [2,3-g] isoquinoline 38

The Ministry of Economic Affairs, Central Bureau of Standards and Staff Cooperative Society printed 2-cyclopropyl-yl-4a «-(3-methoxyphenyl) -6-oxo-l, 2,3,4,4a under argon , 5,6,7,8,8a / S-decahydroisoquinoline 52〇rog and 2-chlorophenyl sulfate 360mg dissolved in 10ml of ethanol, heated to 80 ° C. After adding methanesulfonic acid 1.Qml and stirring at 8G ° C for 15 minutes, it was cooled to room temperature. The precipitated crystals were collected by filtration to obtain 480 mg of the title compound (yield 66.1%). IR (K.Br) cm '': 3284, 1615, 1578, 1493, H60, 1257, 1234, 1052, 878, 775 This paper scale is free to use the Chinese National Standard (CNS) standard 4 (210x297 male dragon) 168 V 3. Description of the invention () A 6 B6 EI-MS (m / z): 434 (M +), 432, 177 NMR (CDC 1 3) 400MHz 6: 0.75-0.80 (2H, m), 〇.96-l.〇 5 (2H, m), 1.74- 1.88 (2H, m), 2.34-2.49 (211, m), 2.75-2.99 (411, m), 3.10-3.28 (2H, m), 3.70 (3H, s), 4.04-4.75 (2H, brm), 6.67 (lH, m), 6. 97-7.05 (311, m), 7.08 (lil.brd, J = 7.9Hz), 7. 14 (1H, t, J = 7.9llz), 7.33 (1H, d, J = 7.6Hz), 7.85 (1H, brs) The following is the same, replacing 2-chlorophenylhydrazine with 4-gas phenyl to give 2-cyclopropylcarbonyl- 4aa-(3-methoxyphenyl) -9-chloro-1,2, 3,4,4a, 5, 11, 11 a / 3 -octahydro-6H-.D? g] Isoquinoline; using 3-aminophenyl trap. 2-cyclopropylcarbonyl-4acx-(3-methylphenyl) -8-chloro-1,2,3,4,4a, 5,11,113 / 3-octahydro-611-ind118 [2,3-0] isoquinoline and 2-chenpropylcarbonyl-4aa-(3-methylphenyl) -10--1,2,3,4 , 4a, 5,11, lla / S-octahydro-6H-P5 丨 UJ [2,3-g] isoquinoline. Example 34 2-cyclopropylmethyl-4a «-(3-methylchlorophenyl) -7-gas-1,2,3,4,4a, 5, ll, lla / 9-octahydro-6H- IndPg and [2,3-g] isoquinoline 39 (please read the precautions on the back before filling in this page). Installed. Line. Printed by Beigongxiaof Cooperative, Central Bureau of Standards, Ministry of Economic Affairs

fV Ν

Lithium aluminum hydride llOnig is suspended in lGml of anhydrous THF under argon, and the paper size is free to use the Chinese National Standard (CNS) A4 specification (210X297 male dragon) 169 V. Description of invention () A 6 B6 Sample 2, Printed by the Ministry of Economic Affairs Central Bureau of Standards' Staff Consumer Cooperative to 01. In addition, 2-cyclopropylcarbonyl-4aa- (3-methoxyphenyl) -7 ^ 3,4,43,5,11,113 called-octahydro-611- | 15 | Mix [2,31] Isoquinoline 400rag was suspended in 10Bl of anhydrous THF and dropped into it, warmed to room temperature, and stirred for 2 hours. After cooling to 0 ° C, a saturated aqueous solution of ethyl acetate and potassium sodium tartrate was added. The insoluble material was removed by filtration, and ethyl acetate was distilled off under reduced pressure to obtain 44 mg of oil. Separate and refine this oil by chromatography tube [silica gel; chloroform / methanol (98/2)] ^ to obtain 390nig crude crystals. This crude crystal was recrystallized from ethyl acetate to obtain 256 mg of pure product (m.p_96 ~ 98 ° C; yield 6 6.196). IR (KB r) cur1: 2906, 1607, 1578, 1491, 1460, 1243, 1052, 777 EI-MS (m / z): 420 (IT), 422, 242 NMR (CDC 1 3) 500Mllz 6: 0.08 -0.14 (2H, m), 0.50-0.56 (2H, m), 0.90 (lH, m), 1.99-2.08 (2H, m), 2.24-2.34 (2H, m), 2.41 (III, m), 2.57 -2. 67 (2H, m), 2.91-3.03 (4H, m), 3.13 (1H, d, J = 15.9Hz), 3. 17 (111, br d, J = 9.2 Hz), 3.69 (3H, s), 6.62 (1ΙΙ, πι), 6.98 (1 H, t, J = 7.9Hz), 7.01-7.07 (3H, m) 7.10 (111, t, J = 7.9llz), 7.32 (lH, d , J = 7.9llz), 7.81 (lll, brs) The same below, with 2-cyclopropylcarboxy-4aa- (3-methoxyphenyl) -8-chloro-1,2,3,4,43, 5,11,113 / 3-octahydro-6} 1-indo [2,3-2] isoquinoline substituted 2-cyclopropylcarbonyl-4a α-(3-methoxyphenyl) -7- Nitrogen-1, 2,3,4,4 &amp; 5,11,113 / 3-octahydro-6} 1-11? Shun- [2,3-Rong] isoquinoline gives 2-cyclopropyl Methyl_4a α-(3-methylphenyl) -8-gas-1,2, 3, 4, 43,5,11,113 / 3-octahydro-611-indazol [2,3-8] Isoquinoline; use (please read the precautions on the back before writing this page) Binding · Binding-Line 'This paper uses Chinese National Standards (CNS) 4 Specifications (210X297 male dragon) 170 5. Description of the invention (A 6 B6 2-cyclopropylcarbonyl-4aa-(3-methylphenyl) -9-chloro-1,2,3,4,4 a, 5 , 1 l, lla / 3-octahydro-6H-indDg [2,3-g] isoquinoline to give 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -9-chloro -l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-indog (2,3-g) isoquino; using 2-cyclopropylcarboxy_43. -(3-methylphenyl) -10-chloro-1,2,3,4,43,5,11,113 / 3-octahydro-6H-indng [2,3-g] isoquinine To give 2-cyclopropylmethyl-4aa- '' (3-methoxyphenyl) -10-nitro-1,2,3,4,43,5,11,113 / 3-octahydro-61} -Indo [2,3-g] isoquinoline. Example 35 2-cyclopropylmethyl-4aa-(3-hydroxyphenyl) -7-nitro-1,2,3,4, 4a, 5, ll, lla / 3 -octahydro-6H-P? | B Duo 〔2,3-g〕 isoquinoline 40 Η

W) The Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs printed 2-cyclopropylmethyl-4act- (3-methylphenyl) -7-nitrogen-1,2,3,4,43 under argon , 5,11,113 / 3-octahydro-611-〇5 ^ 2 [2,3-2] isoquinoline 2 70 mg dissolved in 6nl of anhydrous DMF, adding potassium-t-butoxide 4 0 0ng and η -0.36 ml of propane thiol, stirred at 150 ° C for 2.5 hours. After cooling to room temperature, DMF was distilled off under reduced pressure, 5 ml of water was added, and extracted with 30 ml of chloroform / methanol (3/1). Combine the organic layers. Wash with distilled water and brine, dry, and concentrate to obtain 230 mg of powder. Suspend this powder in 2m 1 of methanol and add methanesulfonate (please read the notes on the back before filling this page)

The standard of this paper is the general Chinese National Standard (CNS) A4 specification (210X297 g) 171 A 6 B6 V. Description of the invention () Acid 4〇wl is made into the salt of formic acid, using chromatography tube [Sephadex, LH-20 ; Methanol] separation and purification to obtain 260ng of crude crystals. Recrystallized from methanol to obtain the tosylate salt of the title compound (26〇10 decomposition) 14911 ^ (yield 46.2%). IR (KB r) an '': 3320, 1599, 1460, 1201, 1164, 1042, 772 FAB—MS (m / z): 407 (H + +1) NMR (DMSO-d6) 400Mllz δ: 0.35-0.40 ( 211, m), 0.61-0.66 (211, m), 1.06 (lll, m), 2.06 (lli, m), 2.30 (31l, s), 2.54-2.68 (3ll, rn), 2.86- 3.06 (5ll, m), 3.20 (1II, br d, J. 16. 1II, 3.37 (1II, m), 3.52 (111, m), 3.73 (111, m), 6.54 (1II, m), 6.88 (lli.m) , 6.92-6.97 (2H, m), 7.02-7 .07 (211, m), 7.33 (1II, d, J = 7.8llz). 9.27 (lii, s), 9.38 (111, brs), 10.97 (111 , s) Elemental analysis CZ 5 Η 2 7 Ν 2 0 C 1 · C Η 3 S 0 3 Η • 0. 2 Η 2 0: t LT (DC Η Ν Cl S calculation value 61.64 6.25 5.53 7.00 6.33 measurement value 61.46 6.25 5.56 7.14 6.26 The following is the same, using 2-cyclopropylmethyl_4a a-(3-methoxyphenyl) -8-chloro-1,2,3,4,43'5,11,113; 3-octahydro_6} ^ _ indzhao [2,3_2] isoquinoline substituted 2-cyclopropylmethyl-4a〇t- (3-methylphenyl) -7-ambient-1, 2, 3,4,43,5,11,113 / 3-octahydro-6} ^ indazolo [2,3 -2] isosialoline to give 2-cyclopropylmethyl-4aa-(3-hydroxybenzene Base) _8_nitrogen—jl 2 3 4 4 5 (please read first Read the precautions on the back and then fill out this page) Binding-Order--Line. Printed by the Staff Consumption Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs. The paper standard is used in China National Standard (CNS) Grade 4 (210x297 public goods). 172 V. Inventions Description (A 6 B6 Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs, ll, lla / 9-octahydro-6H-indino [2,3-g] isoquinoline; 2-cyclopropylmethyl- 4aa- (3-methylchlorophenyl) -9-chloro-1,2,3,4,4a, 5,11,11 a / 3-octahydro-6H-indBg (〔2,3-g〕 iso Quinoline to give 2-cyclopropylmethyl-43〇 (-(3-hydroxyphenyl) -9-ambient-1,2,3,4,43,5,11,113 / 3-octahydro-6H-ind Indo [2,3-g] isoquinoline; using 2-cyclopropylmethyl-4a〇c- (3-methylphenyl) -10-chloro-1,2,3,4,4 &amp;, 5,11,113 / 3-octahydro-611- · D? | Ug [2,3-g] isoquinoline to give 2-cyclopropylmethyl-4a〇c- (3-hydroxyphenyl) -1〇-chloro-1,2,3,4,43,5,11,113 / 3-octahydro-6} 1-indolo [2,3 -g] isoquinoline. Reference Example 7 (±) -2-methyl-4act-(3-methoxybenzyl) -6-oxo-1,2,3,4, 4a, 5,6,7,8,8a / S- The optical division of decahydroisoquinoline (+)-di- (P-tolyl) -D-tartaric acid and (一) -di- (P-tolyl) -L-tartaric acid 41,42 will ( Soil) -2-methyl-4aa- (3-methoxyphenyl) -6-oxo-1,2,3, 4,4 &amp;, 5,6,7,8,83 / 3-decahydroiso Quinoline 3.13 tea and (+)-bis-({)-tolualdehyde) -D-tartaric acid 4.6 8g were dissolved in methanol and concentrated to crystallize it. Add methanol to this salt, heat and dissolve and add (一) -2-methyl-4aa-(3- | ^ phenyl) -6-oxo-1,2, 3, 4, 4a, 5,6, 7,8, -Decahydroisoquinoline- (P-tolyl) -D-tartrate crystalline seed, left at room temperature all day and night. The precipitated crystals were collected by filtration, and the resulting crystals were further recrystallized in the same manner to obtain 1.65 g of crystals. The crystals of this salt were suspended in 1N hydrogenated sodium of 15ral, and extracted twice with 25 ml of ethyl acetate. Wash the organic layer with a saturated vaporized sodium aqueous solution, and then dry with anhydrous sodium sulfate (please read the notes on the back before filling in this page). This paper is used in the Chinese National Standard (CNS) A 4 specifications (210x297 public ) 173-A6 ______B6_ printed by the Ordnance Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of the invention () After concentrating, obtain 0.68g of (-)-2-methyl-4aa- (3-methylphenyl) -6-oxo-1,2,3,4,4a, 5,6,7,8,8a / 3-decahydroisoquinoline (yield 43.5¾). The crude crystals were recrystallized (ethyl acetate / η-hexane) to obtain 0.45 g of needle-like crystals (π.PP. 91.3 ~ 91.8 ° C). Next, 4_28g of the concentrate of the mother liquor obtained by the above division was suspended in 40 ml of 1H sodium hydroxide, and extracted twice with 50nl of ethyl acetate. The organic layer was washed with a saturated aqueous solution of sodium fluoride, dried over anhydrous sodium sulfate, and concentrated. The obtained (±) -2-methyl-4a α- (3-methoxyphenyl) -6-aero-1,2,3,4,4a, 5,6,7,8,8a / 3- 2.21 g of decahydroisoquinoline and 3.12 g of (1-)-di- (P-tolyl) _L-tartaric acid were dissolved in methanol and crystallized after concentration. Add methanol to this salt, add (+)-2-methyl_4aa-(3-methoxyphenyl) -6-oxo-1,2,3,4,4a, 5,6 after heating and dissolving, 7,8,8a / 3-Decahydroisoquinoline · (I) -Di- (P-tolualdehyde) -L-tartrate crystal seed, let it stand at room temperature all day and night. The precipitated crystals were collected by filtration to obtain 2.16g of crystals. The crystals of this salt were suspended in 2G sodium hydroxide 1H, and extracted twice with 30 ml of ethyl acetate. The organic layer was washed with a saturated sodium chloride aqueous solution, dried over anhydrous sodium sulfate, and concentrated to obtain 0.89g of (+)-2-methyl-4a〇t- (3-methylphenyl) -6 -Aero-1,2, 3,4, 4a, 5, 6, 7, 8, 8a / 3-decahydroisoquinoline (yield 5 6.8%). This crude crystal was recrystallized (ethyl acetate / η-hexane) to obtain needle-shaped crystals (®. Ρ. 91.0〜 (―)-2-methyl_4aa-(3-methoxyphenyl) -6 -Aero-1,2,3,4,4a, 5,6,7,8,8a / 9 -Decahydroisoquinoline [α] §0 = -67 ° (C = 2. 0. M e Ο Η) IR (KB r) cm '1: 2944, 2908, 2850, 2798, 1709, (please read the precautions on the back before filling in this page) Install & Order _ Line-This paper scale uses the Chinese national standard ( CMS) A 4 specifications (210x297 mm) -174-Α7 Β7 5. Description of the invention () 1605, 1578 NMR (CDC 1 3) 500MHz δ: 1.88-2.00 (3H, m), 2.08 (lH, m), 2.32 (3H, s), 2.31-2.50 (5H, m), 2.60 (lH, m), 2.69 (111. T, J = 11.6Hz), 2.84 (1H, dd, J = ll. 61lz, J = 3.1Hz ), 2.93 (lH, dd, J = i4.〇H2, J = 1.2 Hz), 3,78 (3ll, s), 6.71 (lH, m), 6.97-7.00 (2H, m), 7.21 (lH , m) (+) -2-methyl-4aot-(3-methoxyphenyl) -6-oxo-1,2,3,4, 4a, 5,6,7,8,8a / 3- Decahydroisoquinoline [a] g0 = + 66 ° (C = 2.0, M e Ο II) IR (KB r) cm- ': 2946, 2908, 2844, 2798. 1709, 1605, 1578 NMR (CDC 1 3) 400MHz δ: 1. 88-2. 00 (311, m), 2.07 (lH, m), 2.32 ( 3H, s), 2. 31-2. 50 (511, m), 2. 60 (1II, m), 2.69 (111, t, J = 11.7llZ), 2. 84 (1II, m), 2. 93 (1H, d, J = 14.2 Hz), 3.78 (3H, s), 6.71 (lll, m), 6.97- 7.00 (211, m), 7.21 (111, m) M ass (m / e): 273 (fT) Reference Example 8 Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the precautions on the back before filling out this page) &lt;-)-2- (2,2,2-trichloroethoxycarbonyl ) -4aa-(3-methoxyphenyl) -6-oxo-1,2,3,4, 4a, 5,6,7,8,8a / 3 -decahydroisoquinoline 43 under gas Dissolve 598 mg of proton adsorbent [l, 8-bis &lt; dimethyl amino) naphthalene; 1,8-bis (dimethylamine) sacrifice] in 15 ml of anhydrous digas methane, and drop 0.433 ml of 2,2 under stirring , 2-Trichloroethoxycarbonyl chloride. Secondly, drop it under ice-cooling (_ 卜 2-methyl-4a α-(3-methoxyphenyl) This paper standard is applicable to China National Standards (CNS) Α4 specifications (210X297 mm) ~ -175-Employees of the Central Bureau of Standards of the Ministry of Economic Affairs Printed by the consumer cooperative 66. t · 2 ι a7 B7 k_ —..---V. Description of the invention ()) -6-oxo-1,2,3,4,4 &amp;, 5,6,7,8 , 83 / 3-decahydroisoquinoline 5071 ^ in anhydrous dichloromethane 5ml. Then cooled to room temperature and stirred for 2 hours. The reaction was concentrated and dissolved in 20ml of ethyl acetate, M 10ml of 1N hydrochloric acid , 10ml of water and 10ml of saturated vaporized sodium aqueous solution, then dried with anhydrous sodium sulfate and concentrated to obtain 1.41g of oil. M chromatography tube [silica gel; hexane / ethyl acetate = 1 / 1] Separate and purify this oil to obtain 806g of the sassafras compound. ^ Α] 〇 = -17.9 (C = 1.00> MeOH) IR (liquid membrane method) cm · 1: 2958, 1715, 1607, 1582 NMR (CDC 1 3) 500MHz δ: 1.80 (lH, m), 2.03 (111, m), 2.13 (lH> m), 2.25 (lH, m), 2.31-2.44 (4H, m), 2.85 (1Η, ( η), 2.96 (111, d, J = 14.0Hz), 3.53 (111, m), 3.78 (311, s), 4.03 (111, m), 4.18 (lH, m). 4.71 -4.81 (211, m), 6.75 (111, m), 6.95-6.98 (2H, m), 7.25 (1 II, m)

Mass (m / e): 433 (Μ *) Reference Example 9 (-&gt; -2-cyclopropylcarbonyl-4aa-(3-methylphenyl) -6-oxo-1, 2, 3, 4 , 4a, 5,6,7,8,8a / 3 -decahydroisoquinoline 44 (-)-2- (2,2,2-trifluoroethane carbonyl) -4aa-(3-methoxybenzene Base) -6-oxo-1,2,3,4, 4a, 5,6.7,8,8a / 3 -decahydroisoquinoline 800 «^ dissolved in 20« 11 of acetic acid, add 1.2% zinc powder Stir at room temperature for 3.5 hours. Then use Super Cell to filter the zinc in the reaction mixture, and wash 3 times with K20b1 acetic acid. After concentrating the acetic acid, add a saturated aqueous solution of sodium hydrogen peroxide to make it eminent. Extract with M40ml of chloroform for 3 times The organic layer is washed with saturated vaporized sodium aqueous solution, dried with anhydrous sodium sulfate and concentrated. The paper size is applicable to China National Standard (CNS) Α4 specification (210X297mm) (please read the notes on the back before filling in This page) Ding-176-V. Description of the invention () Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs to obtain 5 24 mg of oil. Secondly, after azeotroping this oil for 2 times with l〇Bl of benzene , Dissolve it in 18ml of anhydrous dichloromethane under argon, add 513b 1 of anhydrous three Ethylamine, 0.267ml of propyl propyl chloride was added dropwise at room temperature, followed by mixing for 4 hours. The dichloromethane was then removed and redissolved in 20π1 ethyl acetate. Take 1N-HC1 and saturated chlorine Wash the sodium hydroxide aqueous solution, dry with anhydrous sodium sulfate and concentrate to obtain 641 ng of oil. Separate and refine this oil by chromatography tube [silica gel; cyclohexane / ethyl acetate = 3/1]. 345 ng of the title compound was obtained (yield 57.4%). Πι. P. = 149 ~ ISO ”(η -hexanol / ethyl acetate recrystallization) [or] = -107 ° (C = 1.0, CHC13) IR (KB r) on- ': 2934, 2872, 1715. 1624, 1599 NMR (CDC 1 3) 400MHz δ: 0.76-0.79 (2H, m), 0.91-1.00 (2H, m), 1.59 (lH, s) , 1. 74- 1. 84 (211, m), 2.03 (1H, m), 2. 16 (1H, d, J = 13. 7llz), 2.25 (lH, m), 2. 38-2.42 (3.5 H, m),? .76 (0.5ll, m), 2. 97 (1H, d, J = 14. 2Hz), 3.07 (0.5H, m), 3.27 (0.5H, m), 3.79 (3H, s), 4.01 (0.5H, m), 4.12 (0.511, m), 4.33 (0.5H, m), 4.59 (0.5H, m), 6.75 (1II, dd, J = 8.3Hz , J = 2.4 llz), 6.95-7.01 (211,01), 7.25 (111, m) Mass (m / e): 327 (M +) Example 36 (+) -2-cyclopropyl Yl-4a a-(3-methoxyphenyl) -1,2, 3, 4, 4a, 5, 11, lla / 3 -octahydro-6H-indeno [2, 3-g) isoquinoline 45 (―)-2-Cyclopropylcarbonyl-4a cx-(3-methylphenyl) -6-oxo-1 (Please read the precautions on the back before writing this page) National Standard (CNS) Grade A 4 specifications (210x297 g) Fifth, invention description (printed by the Ministry of Economic Affairs Central Standards Bureau employee consumer cooperatives A7 B7, 2,3,4,4a, 5,6,7,8,8a / 9-Decahydroisoquinoline 340 mg and phenylhydrazine 0.113 ml were dissolved in 4 ml of ethanol. 0.675 ml of methanesulfonic acid was added to the heating and refluxing, and the mixture was further refluxed for 0.5 hours while sowing. After the reaction mixture was cooled to room temperature, 20 ml of a saturated aqueous sodium hydrogenate solution was added under ice cooling, and the mixture was extracted twice with 30 ml of gas. The organic layers were combined, washed with a saturated vaporized sodium aqueous solution, dried over anhydrous sodium sulfate, and concentrated to obtain 507 mg of an oily substance. This oil was separated and purified by chromatography tube [silica gel; chloroform] * to obtain 354 mg of the title compound (yield 85.0%). IR (KB r) απ '1: 3204, 2902, 1607, 1460, NMR (CDC 1 3) 500MHz ί: 0.75- 0.78 (2H, m), 0.92- 1.00 (2H, m), 1.58 (lH, s) , 1. 75- 1.90 (2H, m), 2.37-2.48 (2li, m), 2.89 (lil, d, J = 15.9Hz), 2.95-3.02 (2H, m), 3.13 (lH.d, J = 15.9Hz), 3.19 (111, m), 3.68 (311, s), 4.08 (0.5H, d, J = 13.4Hz), 4.22 (0.511, d, J = 9.2llz), 4.44 (0.511, d, J = 13.4Hz), 4.69 (0.511, d, J = 9. 2llz), 6.65 (lH, m) 7.00-7. 14 (511, m), 7.22 (lll.m), 7.44 (lH, d, J = 7.3llz), 7. 60 (0. 511, s), 7.67 (0.51 !, s)

Ma ss (m / e): 400 (M *) Example 37 (+ &gt; -2-cyclopropylmethyl-4a ct-(3-methoxyphenyl) -1,2,3,4,4a , 5, ll, lla / 3 -octahydro-611-11 codolo [2,3-g] isoquinoline 46 Lithium aluminum aluminum oxide 100mg suspended in THF 8ml under argon, dropwise under ice cooling ( +) -2_cyclopropylcarbonyl-4a α-(3-methoxyphenyl) -1,2, 3, 4,4a, 5,11,113; 8-octahydro-611-ind112 [2,3 -8] Isoquinoline 345 | 11 THF 17ml solution in anhydrous THF. Then continue to stir at room temperature for 2 hours. In ice-cooled paper size is applicable to China National Standard (CNS) A4 specification (210X297 mm) (please read the back (Notes to fill out this page)

178 A 6 B6 Printed by the Ministry of Economy Central Standards Bureau employee Xiao # Cooperative V. Description of the invention () Under ethyl acetate and saturated methyl sodium tartrate aqueous solution, it was dropped into the reaction mixture alternately and cooled. Use Super Cell to filter the insoluble material and wash 3 times with 20nl ethyl acetate. The mother liquor is concentrated and concentrated to obtain 318 mg of powder. This powder was separated and purified by chromatography tube [silica gel; chloroform / methanol = 19/1] to obtain the title compound 2951 ^ (yield 88.7%). in. p. = 194.2 ~ 194.6¾ (ethyl acetate / ethanol recrystallization) [a] §0 = + 15 1 ° (C = 1.0, CHC 1 3) IR (KB r) on'1: 2932, 2838, 1607, 1580, 1454 NMR (CDC 1 3) 400MHz δ: 0.08-0. 12 (2II, m), 0.48-0.56 (211, m), 0.89 (111, m), 1.99-2.08 (211, m), 2.22-2.33 (2ΙΙ, (η), 2.40 (lll, m), 2.58-2.64 (211, m), 2.88-3.00 (411, ni), 3.07 (111, d, J = 16.lllz), 3.16 (111, d, J = 6.8IIz), 3.67 (3H, s), 6.60 (111 ^), 7.02-7.10 (5H, m), 7.20 (111, m), 7.44 (lil, m ), 7.59 (111, s) Mass (m / e): 386 (M +) Example 38 (+) -2-cyclopropylmethyl-4a a-(3-hydroxyphenyl) -1,2,3 , 4, 4 a, 5, 11, lla / 3-octahydro-6H-B5I Pg and [2,3-g] isoquinoline 47 (+)-2-cyclopropylmethyl- 4aa-(3-methoxyphenyl) -1,2,3,4,4 3,5,11,113 / 3-octahydro-6 ^ »? 4dece [2,31] isoquinoline 285mg and Potassium-t-butoxide 4 9 7rag was dissolved in 7π1 of anhydrous DMF, and 1-propanethiol was added at 0.415 ml. After stirring the mixture at 140 ° C for 3.5 hours, it was cooled to room temperature. It was removed under reduced pressure DMF, add 20ml of saturated sodium hydrogensulfonate aqueous solution to 40ml Chloroform: methanol = 3: 1 mixed solvent extraction (please read the precautions on the back before writing this page) Packing-Line-This paper scale uses Chinese National Standard (CNS) A4 specifications (210x297 public goods) -179 -Printed A 6 B6 by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs. V. Description of invention (3). Combine organic layers, wash with saturated vaporized sodium aqueous solution, dry with anhydrous magnesium sulfate and concentrate to obtain 33.7 mg. Powder. Suspend the powder in 2al of methanol, add methanesulfonic acid to make methanesulfonate, and then separate it by chromatography tube [Sephadex, LH-20; methanol] to obtain the title compound of methanesulfonate 208nig ( (Yield 60.3%). dp = 24 (above TC (methanol recrystallization). [ar] §0 = + 45o (C = 0.19, DMF) IR (KB r) cm '1: 3402, 2718, 1599, 1444 NMR (DMS 0) 500MHz δ: 0.37-0.38 (2H, m), 0.63-〇.67 (2H, m), 1.06 (lH, m), 2.08 (lH, m), 2.3K3H.S), 2.55-2.64 (211, / 11), 2.88-2.94 (2H, m), 2.97-3.07 (3H, m), 3.09 (1H, dJ = ll.〇Hz), 3.33-3.46 (2H, m), 3.52 (1H, d, J = 12.8Hz), 3.74 (lH'd, J = 11.〇h2), 6.53 (lll, dd, J = 7.9H2, J = 1.8Hz), 6.90-6.99 7.04 (1H, t, J = 7. 9 (12), 7. 1 9 (1H, d, J = 7.9Hz), 7.34 (Please read the precautions on the back to fill in this yellow)

lH, d, J = 7.3Hz), 9.25 (1H, s), 9.39 (111, brs), 10.61 (lH, s) Mass (FA B): 373 (M + + 1) Elemental analysis C25H28N2 0 · C Η 3 S 〇3 H © C Η NS 计 箕 値 66.64 6.88 5.98 6.84 Measurement value 66.45 6.96 5.90 6.80 Reference Example 1 0 (+)-2- (2, 2,2-trichloroethoxycarboxy)-4 &amp;; a-(3-methoxyphenyl) -6-oxo-1, 2, 3, 4, 4a, 5, 6, 7, 8, 8a / 3 -decahydroisoquinoline 48 China H Family Standard (CNS) A 4 specifications (210x297 metric) 180 A 6 B 6 Ministry of Economics + Central Standards and A Gongxiao Cooperative Cooperative Printed V. Description of Invention () Protons are attracted under argon gas. 6 01 rag was dissolved in 15 ml of anhydrous digas methane, and 0.4 35 ml of 2,2,2-trichloroethane gas carbonyl chloride was dropped with stirring. Secondly, drop (+)-2-methyl-4aa-(3-methylphenyl) -6-oxo-1,2,3,4,4a, 5,6,7,8,8a under ice cooling Zhao-decahydroisoquinoline 509mg anhydrous digas methane 5ml dissolved. Then return to room temperature and stir for 1.5 hours. The reaction solution was concentrated and then dissolved in 20 ml of ethyl acetate, washed with 5 ml of 1N-salt 'acid, 5 nil water and 10% saturated sodium chloride aqueous solution, dried over anhydrous sodium sulfate and concentrated to obtain 1 . Q 9g of oil. Separate and purify with a chromatography tube [silica gel; cyclohexane / ethyl acetate = 1/1] to obtain the title compound SlOmg (yield 100%). [a] D = +17. 8 (C = 1. 02 &gt; MeOH) IR-(liquid method) cm-1: 2990, Ί713, 1607, 1582 NMR (CDC 1 3) 400MHz 5: 1.80 (lH, m), 2.03 (1H, m), 2.13 (lH, m), 2.25 (in, m), 2.31-2.44 (411,0,), 2.85 (lH.n,), 2.96 (111, d, J = 14.2ilz), 3.53 (111.m), 3.78 (3H, s), 4.02 (1H, m), 4.18 (111 ^), 4.71-4.81 (2H, m) 6.75 (lH, m), 6.95-6.98 ( 2H, m), 7.25 (lH, m) Mass (m / e): 433 (M *)-'-*., Reference example 1 1 (+) -2-Amphetyl Pogo-4a cc-(3 -Methoxybenzene) -6-m generation -1.2.3,4,4a · 5,6,7,8,8a / 3 -Ten window: Xingqueline 4 9 will (+)-2 -(2. 2, 2-three-grained gas enamel station)-4 a Cl-(3-methybenzene station)-6-gas generation -1, 2, 3.4. 4 a, 5, 6, 7 , 8,8 a / 3 -ten M isoforphyrin 800 mg dissolved in 2 Ora 1 acetic acid, added 1.2 g of zinc powder. At the stem temperature 丨 Η accompany 4 hours. Then use Super C e 1 1 to travel through the anti-shine mixture, and further to 2 0 (please read the precautions on the back side * -_ write this page) -i Ήν CNS) A 4 specifications (210x297 gong) -181-A 6 B6 Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of invention () Wash 3 times of acetic acid in ml. After concentrating the acetic acid, saturated aqueous sodium hydrogenate solution was added to make it alkaline, and extracted 3 times with 4Gdi1 gas. The organic layer was washed with a saturated aqueous solution of sodium chloride, dried over anhydrous sodium sulfate and concentrated to obtain 520 ng of oil. Next, after azeotropically dissolving this oil with lGml of benzene, it was dissolved in 18 ml of anhydrous dichloromethane under argon, .0.53 anhydrous anhydrous triethylamine was added, and dropwise at room temperature. 2 6 7 nl of cyclopropane carbonyl chloride, followed by stirring for 4 hours. Subsequently, the methane gas was removed and dissolved in 20 ml of ethyl acetate. It was washed with 1N-HC1 and saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate and concentrated to obtain 427ng oil. This oil was isolated and purified by chromatography tube [silica gel; cyclohexane / ethyl acetate = 3/1] to obtain the title compound 2 92rag (yield 48.6%). m. p. = 1 5 0 ~ 1 5 1 * C (Dry acid worker Qian A recrystallization) 1 &gt;] §. = + 110 ° (C = 1.0, CHC13) IR (KB r) cm- ': 2934, 2872, 1715, 1624, 1599 NMR (CDC 1 3) 400MHz δ: 0.76-0.79 (211, m), 0.91-1.00 (2H, m), 1.59 (111, s), 1.74- 1. 84 (211, m), 2.03 (1H, m), 2.16 (in, d, J = 13.7IIz), 2_25 (lH, m), 2.38-2.42 (3.5H, m), 2.76 (0.5H, m), 2.97 (111, d, J = 14.2llz), 3.07 (0.5l!, M), 3.27 (0.5II, m), 3.79 (311 , s), 4.01 (0.5II, m), 4.12 (0.511, m), 4.33 (0.5ll, m), 4.59 (0.5H, m), 6.75 (111 ^ (1 ^ = 8.3112 ,: = 2.4110, 6. 95-7. 01 (211, m), 7.25 (111, m) Mass (m / e): 327 (M *) Example 3 9 (Please read the notes on the back first (Fill in this page) This paper is printed in Chinese National Standard (CNS) 4 specifications (210x297 g; ¢) 182 B6 Printed by the Ministry of Economic Affairs, Central Standards Bureau, Employee Consumer #Cooperative V. Description of invention () (-)-2-ring Propylcarbonyl-4act-(3-methylphenyl) -l, 2,3,4,4a, 5, ll, lla / 3-octahydro-6H-ind [2,3-g] isoquinoline 50 (+)-2-Cyclopropylcarbonyl-4aa- (3-methoxyphenyl) -6-oxo-1,2,3,4,4a, 5,6,7,8,8a / 3- Decahydroisoquinoline 14 5mg and phenylhydrazine 0.048ml dissolved in 2ml of ethanol , Add 0.288 ml of methanesulfonic acid to the mixture under heating and reflux, and reflux for 0.5 hours while stirring. After cooling the reaction mixture to room temperature, add 15 ml of saturated aqueous sodium bicarbonate solution under ice-cooling to 30 ml of Extract twice with ammonia. Combine the organic layers, wash with saturated sodium chloride aqueous solution, dry over anhydrous sodium sulfate and concentrate to obtain 194ng oil. Separate and refine this oil by chromatography tube [silica gel; chloroform] , To obtain the title compound of 160nig. IR (KBr) cm-1: 3204, 2902, 1607, 1460 NMR (CDC 1 3) 400MHz 5: 0.75-0.78 (211, m), 0.9 2-1.00 (211, m) , 1.58 (111, s), 1.75- 1.90 (211,01), 2.37- 2.48 (2 II.m), 2.88- 3. 02 (311, m), 3. 12-3. 30 (211, m) , 3.68 (3ll, s), 4.08-4.69 (211, m), 6.65 (111, m), 7.00-7.14 (511, m), 7.22 (lH, m), 7.44 (111 ^), 7.63 ( 1II, brs) Mass (m / e): 400 (M +) Example 40 (—)-2-cyclopropylmethyl-4a a-(3-methylphenyl) -1,2,3,4, 4a, 5,11, lla / 3-octahydro-6H-ind 11¾ and [2,3-g] isoquinoline 51 Under argon, 44mg of lithium aluminum hydride was suspended in anhydrous THF 3ral, under ice cooling Drop (a) -2-cyclopropylcarbonyl-4a α-(3-methoxyphenyl) -1,2,3, 4,4a, 5, ll, lla / S-octahydro-6H-indox S and [2,3-g] isoquinoline 15〇Bg (please read the precautions on the back and then fill out this page) The paper size is free to use China Sleepless Family Standard (CNS) A 4 specifications (210x297 g *) 183 Economy Printed by the Ministry of Central Standards Bureau employee consumer cooperative

Sul € 〇4 A6 _B6 __ V. Description of the invention () 7ml of anhydrous THF solution, followed by stirring at room temperature for 1 hour. Under ice cooling, ethyl acetate and saturated potassium sodium tartrate aqueous solution were alternately dropped into the reaction mixture, and quenched. Use Super Cell to filter the insoluble matter and wash 3 times with 20 ml of ethyl acetate. Concentrate the mother liquor to obtain 14 lug of powder. This powder was separated and purified by chromatography tube [silica gel; gaseous / methanol = 19/1] to obtain 1321 ^ of the title compound (yield 91.2%). m · P · = 19 5. 0 ~ 1 9 5 · 3 T (Recrystallization of mellow acid melon) [a] § ° = -137 ° (C = 1.0, CHC 1 3) IR (KB r) cm'1 : 2930, 2838, 1607, 1578, 1454 NMR (CDC 1 3) 400HHz i: 0.08-0.12 (2H, m), 0.48-0.56 (2H, m), 0.89 (lH, m), 1.99-2.08 (2H, m), 2.24-2.35 (211, m), 2.40 (lH, m), 2.58-2.66 (2il, m), 2.89-3.00 UH, m), 3.07 (lH, d, J = 15.6Hz), 3. 17 (1II; d, J = 7.8Hz), 3.67 (3H, s) _ 6.60 (lll, m), 7.02-7.10 (511,111), 7.20 (^^), 7.44 (lH, m), 7.59C1H, s )

Mass (m / e): 386 (M +) Example 41 (—)-2-cyclopropylmethyl-4act-(3-hydroxyphenyl) -1,2,3, 4,4a, 5,11, 1 la / 3 -octahydro-6H-D is eye-catching and [2,3-g] isoquinoline 52 will (())-2-cyclopropylmethyl-4aa- (3-methylbenzene) under argon Radical) -1,2,3,4,43,5,11,113 / 5-octahydro-6} 1-indole [2,3-§] isoquinoline 127rag and potassium-t-butoxide 221ng Dissolve in 3ml of anhydrous DMF, add propane thiol Q. 185ml. After the mixture was stirred at 140 ° C for 3 hours, it was cooled to room temperature. Remove the DMF under reduced pressure and add 10ml of saturated hydrogen sulfonate. This paper standard is used in the Chinese National Standard (CNS) A4 specification (210X297 male dragon) (please read the precautions on the back and fill in this page). Pack 6 A6 Printed by Employee Cooperative of Central Bureau of Standards of the Ministry of Economy V. Description of invention () Sodium aqueous solution, extracted 3 times with 20 m 1 of chloroform: methanol = 3: 1 mixed solvent. The organic layers were combined, washed with saturated aqueous sodium chloride solution, dried over anhydrous magnesium sulfate, and concentrated to obtain 150 mg of powder. Suspend the powder in 1ml of methanol, add methanesulfonic acid to make methanesulfonate, and separate and purify it by chromatography tube [Sephadex, LH-20; methanol] to obtain the title compound methanesulfonate 54nig (yield) 35. 1%). 'd. P = 2 4 0 ° C or more (methanol recrystallization) [a] § ° = -480 (C = 0. 21. DMF) IR (KB r) cur 1: 3404, 27 10, 1601, 1444 NMR (DMS 0) 500MHz d: 0.37-0.38 (2H, m), 0.63 -0.66 (2H, m), 1.06 (111, Γη), 2.08 (1H, m), 2.31 (3H, s), 2.55 -2.64 ( 211, m), 2.88- 2.94 (2H, m), 2.97-3.07 (3H, m), 3.12 (1H, d, J = 16.5Hz), 3.33-3.46 (2H, m), 3.51 (1II, d, J = 11.0Hz), 3.73 (1H, d, J = 11.6Hz), 6.53 (1H, d, J = 7.9Hz), 6.90-6.99 (4H, m), 7.03 (lH, t, J = 7.9Hz) , 7.19 (1H, d, J = 7.9Hz), 7.34 (lll, d, J = 7.3Hz), 9.24 (lH, s), 9.38 (1H, brs), 10.61 ClH.s) Mass (FAB ): 373 (M + +1) elemental analysis CzsHzeNz 0-CH3 S03 H-0. 6 Hz 0 CH NS calculation value 65. 14 6.98 5.84 6.69 measurement value 65.22 6.83 5.75 6.67 Use and reference examples 7, 8, 9, 10 And 11, as well as Examples 36, 37, 38, 39, 40, and 41, the same method can be used to obtain the compounds described so far (please read the precautions on the back before filling this page) Happy to use Chinese National Standard (CNS) A 4 specifications (210x297 mm) -185-S01GJ4 A 6 B6 V. Description of invention ( Of the (+) and (-) thereof. Example 4 2 2-methyl-43〇 (-(3-methoxyphenyl) -113 / 3-hydroxy-1,2,3,4,43,5,11, lla / S-octahydro-6H -D5I Bg and [2,3-g] isoquinoline 5 3

(Please read the precautions on the back before filling out this page) Printed by the Ministry of Economic Affairs Central Standards Bureau Employee Consumer Cooperative will be 2-methyl-4aa- (3-methoxyphenyl) -6-oxo-8a / S-hydroxyl -1, 2,3,4,4a, 5,6,7,8,8a / 3 -decahydroisocyanate (I02mg, 0.35πββ1) dissolved in ethanol (3nl), add phenylhydrazine (38.2W1, 0.39 mmol). After heating to 80¾, add alkane sulfonic acid (228 «1, 3.5πηπο1), and react at the aforementioned temperature for 2 hours. After cooling to room temperature, it was poured into saturated aqueous sodium bisulfonate solution (20 ml) and extracted with helium (15 nilx 2). Wash with saturated saline (10ml), dry and concentrate, then purify it with a chromatography tube (7 7 34 8g; gaseous 4 gaseous / ammonia saturated chloroform = 3/1) to obtain the sassafras compound (114 %, With solvent). IR (KBr) cm- ': 3304, 2918, 1G05, 1580, 1464, 1236, 1040, 785, 741, NHR (CDCl 3,500MHz) δ: 2.20-2.30 (2! L, m), 2.33 (3Η, s ), 2.40 (lH, dt, J = 12.8, 4.3H), 2.66 (2Η, s), 2.70-2.75 (lH'm), 2.79 (111, d, J = 15.9Hz), 2.92 (111, d , J = 15. 3Ηζ), 3.22 (1 Η, t, J = Binding · Binding-This paper size is easy to use Chinese National Standard (CNS) A 4 specifications (210x297 g) 186 3υ1 € 〇4 A 6 Β6 Ministry of Economic Affairs Printed by the Beigong Consumer Cooperative of the Central Standards Bureau. Description of invention (15.9Hz), 3.64 (311, s), 6.63 (1H, dt, J = 6.7, 1.8Hz), 7.04-7.10 (5H, m), 7.20 (1 H, dd, J = 6.7, 1.8 Hz), 7.44 (111, d, J = 6.7 Hz), 7.62 (1H, brs) 'Mass (El): 362 (H +) The following is the same, respectively with P -Tolyl hydrazine, in-tolyl trap, o-tolyl hydrazine, 4-gas phenyl hydrazine., 3-chlorophenyl hydrazine, 2-chloro phenyl trap, 4-fluorobenzene · hydrazide, 3-fluoro Phenylhydrazine, 2-fluorophenylhydrazine, 4-bromophenylhydrazine, 3-bromophenylhydrazine, 2-bromophenyl trap, 4-nitrophenylhydrazine, 3-nitrophenylhydrazine, 2- Nitrophenyl trap substituted phenyl trap, phenylmethylhydrazine substituted phenyl trap, available 2-methyl-4 &amp; 〇 [-(3- (Methylphenyl) -9-methyl-11 &amp; / 3-xiangyl-1,2,3,4,43, 5,11,113-octahydro-6} 1-indo [2,3-dan] Isoquinoline, 2-methyl-43 α-(3-methylphenyl) -8-methyl-lla / 9 -hydroxy-1,2,3,4,4a, 5, 11, 11a-octahydro -6H-indino [2,3-g] isoquinoline, 2-methyl-4aa_ (3-methylphenyl) -10-methyl-llayS-hydroxy-1, 2, 3,4,4a , 5, 11, 11a-octahydro-6H-05I benzo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -7-methyl-lla / 3 -Hydroxy-1,2, 3,4, 4 a, 5, 11, 11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methyl Oxyphenyl) -9-chloro-113 / 3-hydroxy-1,2,3,4,431,5,11,11 &amp; -octahydro-611-ind 11 $ and [2,3-g] isoquinoline, 2-methyl-4aa- (3-methylphenyl) -8-chloro-lla / 3 -8-chloro-lla0-methyl-l, 2,3,4,4a, 5, ll, lla-Afi -6H-indolo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methylphenyl) -10-chloro-113 / 3-hydroxy-1,2,3,4,421 , 5,11,11 &amp; -octahydro-611-indolo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -7-chloro-lla / 3 -Hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indho [2, (please read first Read the precautions on the back and then fill out this page) This paper standard uses the Chinese standard (CNS) A 4 specifications (210x297 male dragons) 187 Printed by the staff of the Central Standards Bureau of the Ministry of Economic Affairs A 6 B 6_ V. Description of invention () 3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -9-fluoro-lla / S-hydroxy-1,2,3,4,4a, 5,11, 11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-methyl-4aa-(3-methoxyphenyl) -8-fluoro-lla / 3 -hydroxy-1,2 , .3,4,4 &amp;, 5,11,113-octahydro-61 ^ indolo [2,3-§] isoquinoline, 2-methyl-4 &amp; 〇 (-(3-methoxyphenyl) -10-fluoro-11 &amp; / 9-hydroxy-1,2,3,4,43,5,11,113-octahydro-61 ^ -indolo [2,31] isoquinoline, 2-methyl -4 'aa-(3-methoxybenzyl) -7-fluoro- lla / 3-hydroxy-1,2,3, 4,4a, 5, 11, 11a -octazo-6H_D ^ 丨 1¾ and (2 , 3-g] Iso-salenol, 2-methyl_4aa_ (3_methylphenyl) -9-bromo-lla / 3-hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octa Hydrogen-6H-D? | Tlg [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -8-bromo-11a / 3-hydroxy-1,2, 3, 4, 4a, 5, 11,1 la-octahydro-SH-indibenzo [2,3-g] isosleepoline, 2-methyl-4aa- (3-methoxybenzene ) -10-Mo-113 /?-Hydroxy-1,2,3,4,43,5,11,113-Octahydro-6 ^ Io [2,3-g] isoquinoline, 2-methyl- 4aa- (3-methoxyphenyl) -7-bromo-11a /?-Hydroxy-1,2,3,4,43,5,11,113-octahydro-6} 1-indaza [2, 31] Isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -9-nitro-lla / 3-hydroxy-1,2,3,4,43,5,11,113-octa- 6} 1-1 ^ 丨 Decoupling; _2,3-2] isosialoline, 2-methyl-4aa-(3-methylphenyl) -8-nitro-1 lla / S -hydroxy-1,2 , 3,4, 43,5,11,113-octahydro-61 ind [丨 8- [2,3-dan] isoquinoline, 2-methyl-4aa-(3-methoxyphenyl) -10-nitro Yl-lla &gt; 9-hydroxy-l, 2,3,4,4a, 5, 11,11a-octahydro-6H-ton 丨 2 [2,3-g] isoquinoline, 2-methyl- 4aCx-(3 -methoxyphenyl) -7 -nitro-11 a / 3 -hydroxy-1, 2,3, 4, 4 a, 5,11, 1 1 a -octahydro-6H-ind11¾ [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -lla / 3-hydroxy-1, 2,3, 4, 4a, 5, 11, 11a-octa Hydrogen-6-methyl (please read the precautions on the back before filling in this page) Packing · Thread * This paper scale uses Chinese National Standard (CNS) A4 specifications (210X297mm) 188

SulCJ4 A6 B6 5. Description of the invention (-Indo [2, 3-g] isoquinoline. Example 43. 2-methyl-43〇 (-(3-hydroxyphenyl) -113 / 3-hydroxy- 1,2,3,4,43, 11, 11a-octahydro-6H-indazolo [2, 3-g] isoquinoline 54

(54) (Please read the precautions on the back before filling out this page) Printed by the employee consumer cooperative of the Department of Economics, Biyang, Bureau of Economics, the above-mentioned 2-methyl-4aa- (3-methylphenyl) -llayS-hydroxyl -1,2,3,4,4 &amp;, 5,11,113-octahydro-6 »1-indolo [2,3-ju] isoquinoline dissolved in DMF (anhydrous, 5ml), add propane thiol ( 0.25nl, 2.8mo1), potassium-t-butoxide (220 mg, 2.0mo1), and react at 150 ° C for 3 hours. The solvent was distilled off under reduced pressure, and a saturated aqueous solution of sodium hydrogensulfonate (10 ml) was added, followed by extraction with ethanol / aeroform (3/1, 1 10 μm 1 X 2). Washed with saturated saline, dried and concentrated, purified with a silica gel chromatography tube 0 7 34 1 0 g; nitrogen acetone> ammonia saturated atmosphere 5% methanol / ammonia saturated nitrogen acetone) to obtain the title compound 55.6 mg (45%; 2 stages), dissolve it in methanol, add methanesulfonic acid (10.9 u 1) to make a salt, and separate it. mp: 189 ~ 1923C (methanesulfonate, which turns brown from 172 ° C) IR (KBr) cm &quot; 1: 3408,2926,1584,1454,1323,1236, 1048,897, 741 Binding-binding line. This paper scale uses Chinese National Standard (CNS) A4 specifications (210x297 gong) 189 V. Description of invention ()

Mass (EI): 348 (M +) A 6 B 6 Elemental analysis: C 2 2 Η 2 4 N 2〇2 ch3so3h 112 0 -ibT © C Η Ν S Calculation value 59.72 6.54 6.05 6.93 Measurement value 59.58 6.72 5.96 7.01 Ministry of Economic Affairs The employee consumption cooperative of the Central Standards Bureau printed the following, the same 2-methyl-4aa-(3_methoxyphenyl) -lla / S -hydroxy-1,2,3,4,43,5,11,113- Octahydro-611-indazolo [2,31] isoquinoline was replaced by 2-methyl-4a α-(3-methoxyphenyl) -8-methyl-11 3-zhao-hydroxy-1, 2,3,4,43,5,11,113-octahydro-6? 1-indolo [2,31] isoquinoline, 2-methyl-4ac (-(3-methoxyphenyl)- 10-methyl-11a-hydroxy-1,2,3,4,43,5,11,113-octahydro-6} 1-indolo [2,3-§] isoquinoline, 2-methyl -4aa-(3-methylphenyl) -7-methyl-11a /?-Hydroxy-1, 2,3,4,43,5,11,113-octahydro-6})-indazoline [2,31] isoquinoline, 2-methyl-4 &amp; 〇 (-(3-methoxyphenyl) -9-chloro-113 / 3-hydroxy-1,2,3,4, 43,5, 11,113-octahydro-6-indo [2,3- £] isoquinoline, 2-methyl- "〇 (-(3-methoxyphenyl) -8-gas-11 &amp; / 3-hydroxyl -1,2,3,4,401,5,11, 1U-octahydro [2,3-g] isoquinoline, 2-methyl-4aa- (3-methyl gas Group) -10-chloro-lla / 3-hydroxy-1,2,3,4, 4a, 5,11,11a-octahydro-6H-indoxy [2,3-g] isoxaline, 2- Methyl-4aa- (3-methoxyphenyl) -7-gas-lla / 9-hydroxy-l, 2,3,4,4a, 5, 11, 11a-octa--6H-ton bispyro (2 , 3-g] isoquinoline, 2-methyl-4aa- (3-methylphenyl) -9-fluoro-1 la / Q-hydroxy-1,2,3,4,4a, 5, 1 1 , 1 la-octahydro-6H-indhuo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methylpyridine _)-8-fluoro-lla / S-hydroxy-1 ， 2,3,4,43,5,11,113-octahydro-6 ^ 濤 bi [2,3- £:] different (please read the precautions on the back before reading this page). This paper scale is printed in Chinese National Standard (CNS) A4 specification (210x297 male dragon) -190-A 6 B6 Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economy V. Description of invention () Quinoline, 2-methyl- 4aa-(3-methoxyphenyl) -10-fluoro-lla / 3-hydroxy-1, 2,3,4,43,5,11,113-octahydro-61 indole [2,31] isoquine_ , 2-methyl-43〇1- (3-methylphenyl) -7-fluoro-113 / 9-hydroxy-1,2,3,4, 43,5,11,113-octahydro-6} 1- Vermis 02- [2,3-2] isoquinoline, 2-methyl-4act-(3-methoxyphenyl) -9-bromo-11a / 3 -hydroxy-1,2, 3,4,4 a , 5, 11, 11a-octahydro-6H-indopodo [2,3-g] isoquinoline., 2-methyl-4aa- (3-methoxyphenyl) -8-bromo-lla / 3-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-indolo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methyl Oxyphenyl) -10-bromo-lla / S-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-P? | Benzo [2,3-g] isoquine Porphyrin, 2-methyl-4aa- (3-methylphenyl) -7-bromo-113 / 3-hydroxy-1, 2, 3, 4, 43, 5, 11, 113-octahydro-6}] -Indo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -9-nitro-lla / 3-hydroxy-1,2,3,4, 4a, 5, ll, lla-octahydro-6H-indo- [2,3-g] isobrazide, 2-methyl-4a〇t- (3-methoxyphenyl) -8-nitro- lla / 3 -Methyl-l, 2,3,4,4a, 5, ll, lla-octahydro-6H-ind Pg and [2,3-g] isoquinoline, 2-methyl-4act-( 3-Methoxyphenyl) -10_nitro-lla / 3-hydroxy-1,2, 3,4,43,5,11,118-octaqi-6} 1-gully [2,3 -Dan] isosia | 1 (: Wood, 2-methyl-43 «-(3-methoxyphenyl) -7-nitro-113 / 3-hydroxy-1,2,3,4, 4 &amp;, 5,11,11 &amp; -octahydro-61 ind [! 8 and [2,31] isoquinoline, 2-methyl-4aa-(3-methoxyphenyl) -11a zhao-hydroxy-1,2, 3,4, 4a, 5,11,11a-octahydro-6-methyl-1¾ 丨 Pg- [2,3-g] isoquinoline to give 2-methyl-4aa- (3-hydroxyphenyl) -9-methyl Yl- lla / 3-hydroxy-1,2,3,4,4a, 5,11, 11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -8-methyl-lla / 3-hydroxy-1, 2, 3, 4, 4a, 5, 11, 1 la-octahydro (please read the notes on the back before writing This page) Installation · Line-This paper standard uses the Chinese National Standard (CNS) standard 4 (210x297 mm) -191-Printed by the Central Bureau of Standards of the Ministry of Economy, A6 _B6_ V. Description of invention () -6H -Indo [2,3-g] isoquinoline, 2-methyl-4aa_ (3-methoxyphenyl) -10-methyl-lla &gt; S-hydroxy-1,2,3,4,4a , 5,11,11a-octahexa-6H-indo [2,3-g] isoquinoline, 2-methyl-4acx- (3-methoxyphenyl) -7-methyl-lla / 3 -Hydroxy-1,2, 3,4,4a, 5,11,11a-octahydro-6 H-indodecano [2,3-g] isoquinoline, 2-methyl-4aa- (3- Methoxyphenyl) -9-chloro-11a ha-hydroxy-1,2,3,4,4a, 5, ll, 11a-octahydro-6m Shun [2, '3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -8-chloro-lla / 3-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-worm Iso [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -10-chloro-lla / S-hydroxy-1, 2,3,4,4 &amp;, 5,11,113-octahydro-6} 1-acrido [2,3-§] isoquinoline, 2-methyl-43〇 (-(3-methylphenyl) -7-nitrogen-113 / 3 -Hydroxy-1,2,3,4, 48,5,11,113-octahydro-6} 1-1 ^ 丨 eye and [2,3-forget] isosia, 2-methyl-4 pattern ^-( 3-methoxyphenyl) -9-fluoro-11 &amp; / 3-hydroxy-1,2,3,4,43,5,11, 11a -octa-oxy-and [2,3-g] 2 -methyl- 4aa ~ (3-methoxyphenyl) -δ-fluoro-11a / 3 -hydrocarbyl-1,2, 3,4,4 a, 5, 11,11a-octahydro-6H-worm And [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -10 -gas- -cyclyl-1,2,3,4,4a, 5,11, 11a · &quot; octazo-6H-D ^ | eye and [2,3-g] isosleep, 2-methyl-4ao:-(3-methoxyphenyl) -7-fluoro-lla / 3- Hydroxy-1,2,3,4,4a, 5, .l 1,11a-octahydro-6H-indDg and [2,3-g] isoquinoline, 2-methyl-4aa- (3-methyl Oxyphenyl) _9-bromo-11a /?-Hydroxy-1,2,3,4,43,5,11,113-octahydro-6} 1-indo [2,31] isoquinoline, 2-methyl -4aa-(3-methoxyphenyl) -8-bromo- lla / 9-hydroxy-1,2,3,4, ", 5,11,113- Octahydro-6 ^ indo [2,3-2] isoquinoline, 2-methyl-43 «-(3-methoxyphenyl) -10-bromo-113 / 3-hydroxy-1,2, 3,4,4 &amp; (Please read the precautions on the back before filling in this page) Binding-Threading · This paper scale uses the Chinese National Standard (CNS) A 4 specifications (210x297 mm) A 6 B 6 5. Inventions Description (), 5,11,113-octahydro-6} 1-ind0 bag and [2,31] isoquinoline, 2-methyl-4 act-(3-methylphenyl) -7-bromo-lla / S-hydroxy-1,2,3,4,4a, 5,11, 11a-octahydro-6H-indPg and [2,3-g] isoquinoline, 2-methyl-4aa- (3- Methoxyphenyl) -9-nitro-lla / 3-hydroxy-1,2,3, 4, 4a, 5, 11, 11a-octahydro-6H-indazoline (2,3-g) isoquine Porphyrin, 2-methyl-4aa- (3-methoxyphenyl) -8-nitro-lla / 3-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro_-6H -Indolo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -10-nitro- lla ^ S-hydroxy-1,2,3, 4, 4a, 5,11,11 a-octahydro-6H-indo [2,3-g] isoquinoline, 2-methyl-4aa- (3-methoxyphenyl) -7-nitro-lla / 3 -Hydroxy-1, 2, 3, 4, 4a, 5, 11, 1 la-octahydro-SH-Zhaohuo [2,3-giisoquinoline, 2-methyl-4act- (3- Methylphenyl) -11 a / 3 -hydroxy-1, 2, 3, 4, 4 a, 5,11,1 la-octatri-6-methyl-indolo [2, 3-g] isoquinoline. Example 4 4 2-cyclopropyl glassy-4aa-(3-methoxyphenyl) -lla / 3 -methyl-1,2, 3, 4, 4a, 5, 11, 1 la-octahydro- 6H-Indo [2, 3-g] isoquinoline 55

OH (please read the precautions on the back before filling in this page) Packing · Ordering_Line. Printed by Beigong Consumer Cooperative, Bureau of Standards, Ministry of Economy

Combine 2-cyclopropylmethyl-4a «-(3-methylphenyl) -6-chloro-8a-hydroxy-1,2,3,4,43,5,6,7,8,83 -Decahydroisoquinoline (1021 ^, 0.3 1 paper size, Chinese National Standard (CNS) A4 specifications (210x297 male dragon) are used in the paper -193-^ 〇16〇4 A 6 B6 Printed by the cooperative. 5. Description of the invention () nmol) is dissolved in ethanol (3nl) and phenylhydrazine (34 / zl, 0.34mmol) is added. After heating to 80 ° C, add methanesulfonic acid (202 Wi, 3.1mmol), react at the aforementioned temperature for 3 hours, after cooling to room temperature, pour into saturated aqueous sodium hydrogensulfonate solution (12ml) to Gas imitation extraction (10nlx2). Washed with saturated saline (10π1), dried and concentrated, then purified with a silica gel chromatography tube (9385 10 g; nitroform-2% methanol / chloroform 45% methanol / chloroform) to obtain the standard compound 96 . 6mg (77%). IR (liquid film method) 011- ^: 3302,2914,1605,1580,1456,1236,1040,87 4,741 NMR (CDC1 3, 500Mllz) tO.04-0.10 (211, m), 0.45-0.53 (211, m), 0.72-0. 84 (111, m), 2. 18-2. 26 (211, m), 2. 36 (111, s), 2. 36 (111, dt, J = 12. 4, 4. OHz), 2. 57- 2. 66 (211, m), 2.64 (2li, s), 2.68-2.73 (1 H, m), 2.81 (1H, d, J = 15. 8llz), 2.90 ( 111, d, J = 15. 4llz), 3.20 (1H, t, J = 15.8llz), 3. 65 (3il, s), 6. 62 (111, dt, J = 6.7, 1. 8llz), 7 . 00-7. 07 (5ll, m), 7.21 (lil.dd, J = 6.7, l.BHz), 7.44 (1II, d, J = 6.7 Hz), 7.48 (1! (, Brs) Mass (El ): 402 (M +) The following is the same, the 2-cyclopropylmethyl_4a a-(3-methoxyphenyl) -6 -oxo-8a / G-hydroxy-1,2,3,4, 4a, 5,6,7,8,8a-decahydroisoquinoline were replaced by 2-benzyl-4a α- (3-methoxybenzophenanthrene) -6-oxo-8azhao-hydroxy-1, 2,3,4,4a, 5, 6,7,8,8a-decahydroisoquinoline, 2- (2-phenylethylpyrazine) -4aa-(3-methoxyphenyl) -6 -chloro- 8a / 3-hydroxy-l, 2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -6 -Oxygen (please read the notes on the back before writing this page) The paper scale is free to use the Chinese National Standard (CHS) A 4 specifications (210x297 gong) A 6 B 6 Central Ministry of Economic Affairs, the Ministry of Economic Affairs, the Ministry of Economic Affairs, the three industrial and consumer cooperation du printed five, description of invention () Substitute-to 3-hydroxyl-1, 2,3,4,43,5,6,7,8,83-decahydroisoquino, to give 2-benzyl-4aa-(3-methoxyphenyl) -lla / 3 -hydroxy-l, 2 , 3,4,4a, 5, 11,113-octahydro-611-indolo [2,31] isoquinoline, 2- (2-phenethyl) -43〇 (-(3-methoxyphenyl) -113 / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-6H-indo [2,3-g] isoquinoline, 2-allyl-4acx- (3-Methoxyphenyl) -lla / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-6} 1-mum | US benzo [2, 3-g] iso quinoline. Also, the same, replace the phenylhydrazine with a P-tolyl trap, and use Bu Jing propyl methyl-4aa- (3-methyl gas phenyl)-6-gas generation-8a / 3-hydroxyl-1 , 2, 3,4,4a, 5,6, 7,8,8a -decahydroisosaloride, 2-benzyl-4aa-(3-methoxyphenyl) -6-gaso-8a / 3- Hydroxy-1, 2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -6 -Chloro-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decaquinoquinoline, 2-allyl-4aa- (3-methoxy Phenyl) -6-aero--8a0-hydroxy-l, 2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, then 2-cyclopropylmethyl- 4a a-(3-methoxyphenyl) -9-methyl- lla / 3-hydroxy-1,2,3,4,4a, 5, 11, 11a-octahydro [2,3-g] iso Quinoline, 2-benzyl-4aa- (3-methoxyphenyl) -9-methyl-1 la /?-Hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octahydro- 6H-indolo [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -9-methyl-11a-hydroxy-1,2 , 3, 4, 4 a, 5, 11, 11 a -octahydro-6 Η-indPS [2, 3-g] isoquinoline, 2-allyl-4 a α-(3 -methoxy Benzyl) -9-methyl-11a / 3-hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octa Μ-6 Η-ton US and [2, 3-g] isoquinoline. (Please read the precautions on the back before writing this page). The size of this paper is in accordance with Chinese National Standard (CNS) A 4 specifications (210x297 gong) 195

A 6 _B_6_ printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of the invention () Also, the same, replacing phenylhydrazine with m-tolylhydrazine and using 2-cyclopropylmethyl-4a α- (3-methoxyphenyl) -6-oxo-8a / 3-hydroxy-1,2, 3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-benzyl -4aa-(3-methoxybenzyl) -6-gaso_8a / 3 -hydroxy-1,2, 3, 4, 4a, 5, 6,7, δ, 8a-decahydroisoquine_, 2 -(2-phenethyl) -4aa-(3-methylchlorophenyl) -6-fluoro-8a Lu-hydroxy-1,2,3,4, 4a, 5,6, 7,8,8a- Decahydroisoquinoline, 2-allyl-4 act-(3-methylphenyl) -6-oxo-8a / 3 -hydroxy-1,2,3,4,4a, 5,6,7 , 8,8a-decahydroisoquino_, then 2-cyclopropylmethyl-4a a-(3-methylphenyl) -8-methyl-lla / 3-hydroxy-1,2,3 , 4,4a, 5,11,11 a-octahydro-6H-indodec [2,3-g] isoquinoline, 2-cyclopropylmethyl-4a〇t- (3-methoxybenzene Group) -10-methyl-lla / Q-hydroxyl-l, 2,3,4,4a, 5, ll, lla-octahydro-SH-indole [2,3-g] isoquinoline, 2 -Benzyl-4ac (-(3-methoxyphenyl) -8-methyl- lla / 3 -hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6 H- indica Benzo [2,3-g] isoquinoline, 2-benzyl-4act- (3-methoxybenzene ) -1〇-methyl-la-1 / 3-hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indo [2,3-g] isoquinoline, 2 -(2-phenethyl) -4aa- (3-methylchlorophenyl) -8-methyl- llayQ-hydroxy-1,2,3,4,43,5,11,113-octaki-6} ^ ind Humo 〔2,3-g〕 isoquinoline, 2- (2-phenethyl) _4aa- (3-methoxyphenyl) -10 -methylhydroxy-1,2,3,4,4a, 5 , 11, 11a -octa®- 6H-indo [2, 3-g] isoquinoline, 2-allyl-4 a α-(3 -methylphenyl) -8-methyl- lla / 3-hydroxy-1,2,3,4, 4a, 5,11,11a-octahydro-6HH Zhaozo [2,3-g] isoquinoline, 2-allyl-4act-(3-methylchloro Phenyl) -10 -methyl-1 la / 3 -hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-〇ζ | benzo [2, 3-g] iso quinoline. (Please read the precautions on the back before filling out this page) Pack. Line. The size of this paper is in accordance with the Chinese National Standard (CNS) A 4 specifications (210x297 public goods). 196 Printed by the staff of the Central Standards Bureau of the Ministry of Economic Affairs, A6 _ B6_ V. Description of the invention () In addition, the same, the phenyl trap was replaced with 0-tolyl hydrazine, and 2-cyclopropylmethyl-4aa- (3-methylphenyl) -6-gas was used at the same time Generation-8a / 3-hydroxy-1,2,3,4,43,5,6,7,8,83-decahydroisosleep_, 2-: ¥: radical-43〇 [-(3-methoxy Phenyl) -6-oxo-8a / S-hydroxy-1, 2,3,4,4a, 5,6,7,8,8a-decahydroisosleep, 2- (2-phenylethyl) -4a〇t-(3-methoxyphenyl) -6-oxo-8a / 9-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline , 2-allyl-yl-4 &amp; 〇 (-(3-methoxyphenyl) -6-oxo-83; 3-hydroxy-1,2,3,4,43,5,6,7,8 , 8a-decahydroisoquinoline, respectively, 2-cyclopropylmethyl-4a 〇t- (3-methoxyphenyl) -7-methyl-Ua / 3-hydroxy-1,2,3, 4,4a, 5,11, lla-octahydro-6HHBS (2,3-g) isoquinoline, 2-benzyl-4act- (3-methoxyphenyl) -7-methyl-lla / ϊ -Hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-indazolo [2,3-g] isoquinoline, 2- (2-benzene Ethyl) -4a〇t- (3-methylchlorophenyl) -7-methyl-11a Θ-hydroxy-1,2,3, 4, 4a, 5,11, 11 a-octahydro-6H-ind Pg (〔2,3-g〕 isoquinoline, 2-allyl-4a〇t- (3-methoxyphenyl) -7-methyl-113> 9-hydroxy-1,2,3,4 , 43,5,11,113-octahydro-6} 1- vermino [2, 3-g] isoquinoline, and the same, replace the benzodiazepine with 4-azabenzyl and use 2- Cyclopropylmethyl- 4aa-(3-methoxybenzene even) -6-aero-8a / S-hydroxy-1,2, 3, 4, 4a, 5, 6, 7, 8, 8a-decahydro Isoquinoline, 2-benzyl--4a α-(3-methoxyphenyl) -6-oxo-8 a zhao-hydroxy-1, 2, 3, 4, 4 a, 5, 6, 7, 8, 8 a -decahydroisoquinoline, 2-(2 -phenethyl) -4 a α-(3 -methylphenyl) -6 -oxo-8 a Ling-hydroxy-1, 2, 3 , 4,4a, 5, 6, 7, 8,8a-decahydroisoquinoline, 2-allyl-4 aa-(3-methoxyphenyl) -6 -gaso-8a /?-Hydroxy- 1,2,3,4,4a, 5, 6, 7, 8,8a- fhydroisoquine_, respectively, 2-cyclopropenylmethyl-4a α-(3-methyl (please read the back Please fill out this page again for precautions) Binding · Order _ This paper standard uses Chinese National Standard (CNS) A 4 specifications (2 丨 0x297 public) 197 A 6 B 6 Economy Printed by the Central Bureau of Standards ’Staff Cooperative V. Description of Invention () Oxyphenyl) -9-chloro-lla / 3-hydroxy-1,2,3,4, 4a, 5,11,11a-octahydro-6H -Indigo (2,3-g) isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -9-chloro-11a / 3 -hydroxy-1,2, 3, 4, 4a , 5, 11, 11a-octahydro-6H-ind [1¾ and [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -9- Chloro-113 / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-61 vermiculite 08- [2,3-g] isosialoline, 2-allyl-4-aa -Methoxyphenyl) -9-gas-113 0-hydroxy-1,2,3,4,43,5,11,113-octahydro-61 ^ indoxo [2,3-g] isoquine Porphyrin. Also, in the same way, replace phenylhydrazine with a 3-gas phenyl trap and use 2-cyclopropylmethyl-4ac &lt;-( 3-methoxyphenyl) -6-oxo-8a / 3- Hydroxy-1,2, 3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-benzyl-4aa-(3-methylphenyl) -6-gaso-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquin «, 2- (2-phenethyl) -4a α-(3-methylbenzene Group) -6-oxo-8a / 3 -keto-1,2,3, 4,4a, 5,6, 7, 8,8a -decahydroisopyroline, 2-allyl-4aa- (3-Methoxyphenyl) -6-oxo-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, respectively get 2 -Cyclopropylmethyl-4a a-(3-methoxyphenyl) -8-chloro-11a / 9 -hydroxy-1,2,3, 4, 4a, 5, 11,11a-octahydro-6H- Indolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -1 0 -chloro-11 a / 3 -hydroxy-1, 2, 3 , 4, 4 a, 5, 11, 11 a -octahydro-6H-indazolo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -8- Nitrogen-llayS-Jingshi-1, 2, 3, 4, 4a, 5, 11, 1 la-octahydro-6H-indBg and [2, 3-g] isoquinoline, 2-ryl-4a cr-(3 -methylphenyl) -1 0 -atmosphere-lla / 3 -hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-B (1¾ and [2, 3-g] isoquinoline, 2- (2-phenylethyl) -4aa- (3-methylphenyl) -8-chloro- (please (Read the notes on the back before filling this page)

The size of this paper is in accordance with Chinese National Standard (CNS) A4 specifications (210x297 public goods) 198 A 6 B 6 Printed by Beigong Consumer Cooperation of the Central Standards Bureau of the Ministry of Economic Affairs. 5. Description of the invention () lla / S-hydroxy-1, 2,3,4,4a, 5,11,11a-octahydro-6H-indo [2,3-g] isoquino, 2- (2-phenethyl) -4act- (3-methoxy Phenyl) -10-chloro-113 / 3-hydroxy-1,2,3,4,4 &amp;, 5,11,11 &amp; -octahydro-611-ind13rono [2,3-g] isoquine Porphyrin, 2-allyl-4aa- (3-methoxyphenyl) -8-gas-lla; S-hydroxy-1,2,3,4,43,5,11,113-octahydro-6? 1-Indo [2,3-2] isoquinoline, 2-allyl-4aa- (3-methylphenyl) -10-gas-lla / 3-hydroxyl-1,2,3, 4,4a, 5, ll, lla-octahydro-6H-indo [2,3-g] isoquinoline. Also, in the same manner, phenylhydrazine is replaced by 2-chloropropylhydrazine, and 2-cyclopropylmethyl-4ac &lt;-( 3-methylphenyl) -6-amino-Sa / 3-hydroxyl group is used -1,2, 3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-benzyl-4a〇c-(3-methoxyphenyl) -6-oxo- 83-hydroxy-1,2,3,4,4 &, 5,6,7,8,83-decahydroisoquinoline, 2- (2-phenethyl) -4aa-(3-methoxybenzene Radical) -6-gaso-8a / 3 _jingji-1,2,3,4,43,5,6,7,8,83-decahydroisoquine_, 2-xanthene-4 aa- (3-Methoxyphenyl) -6-oxo-8a / 9-hydroxy-1,2,3,4,4a, 5, 6, 7, 8,8a-decahydroisoquinoline, respectively get 2 -Cyclopropyl very methyl-4a α-(3-methoxyphenyl) -7-chloro-11 &amp; / 3-hydroxy-1,2,3,4,4 &amp;, 5,11,11 &amp; -octahydro -6H-Indino [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -7_aza-lla / 3-hydroxypyridine-1, 2,3, 4, 4a, 5, 1 1, lla-octahydro-6H-indigo [2, 3-g;) isoquinoline, 2-(2 -phenethyl) -4 a «-(3 -methyl gas Phenyl) -7 -chloro-1 1 a / 3 -hydroxy-1, 2, 3, 4, 4 a, 5, 1 1, 1 1 a -octahydro-6 Η -tonophthalo [2,3- g] Isoquinoline, 2-allyl-4aa_ (3-methylphenyl) -7-nitrogen-11 &amp; / 8-hydroxy-1, 2,3,4,43,5,11,113-octahydro-6}]-indol [2,3-g] isoquinoline. (Please read the precautions on the back before filling in this page) Packing and threading. The paper size is printed using the Chinese National Standard (CNS) A4 specifications (210x297 g; ¢) 199 Printed by Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs V. Description of the invention () In the same way, the phenylhydrazine is replaced by a 4-fluorophenyl trap, and 2-cyclopropylmethyl-4a α-(3-methoxyphenyl) -6-gas is used Generation-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-benzyl-4a〇t- (3-methoxyphenyl ) -6-oxo-8a / S-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decaisoquinoline '2- (2-phenethyl) -4aa -(3-methoxyphenyl) -6-oxo-8a / 3 -hydroxy-1,2,3,4,4a, 5,6,7,8,8 a-decahydroisoquinoline, 2- Allyl-4 'act-(3-methoxyphenyl) -6-oxo- &amp; a / 3-hydroxy-l, 2,3,4,4a, 5,6,7, 8,8a- Decahydroisoquinoline, then 2-cyclopropylmethyl-4a a-(3-methylphenyl) -9-fluoro-lla / 3-hydroxy-1, 2,3,4,4a, 5 , Ll, lla-octahydro-6H-duplexo [2,3-g] isoquinoline, 2-benzyl-4a〇t- (3-methoxyphenyl) -9-fluoro-11a / 3- Hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-P5I benzo [2,3-g] isoquinoline, 2- (2-benzene Radical) -4aa- (3-methoxyphenyl) -9-fluoro-113 / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-6buind〇8 and [ 2,3-g] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -9-fluoro-lla ^ S-hydroxy-1,2,3,4,4a, 5,11 , 11a-octahydro-6H-indolo [2,3-g] isoquinoline. Also, the same, replace the phenyl trap with 3-fluorophenylhydrazine, and use 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -6_oxo_8a / 9-hydroxyl -1,2, 3, 4, 4 a, 5, 6, 7, 8,8a-decahydroisoquinoline, 2-benzyl-4 a α-(3 -methoxyphenyl) -6-oxo -8ayS-hydroxyl-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2- (2-phenylethylidene) -43 «-(3-methyl gas Phenyl) -6-fluoro-8a / 9-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decazaisoquinoline, 2-allyl-4aa- (3 -methylphenyl) -6 -aero- 8a / 5 -jing-l, 2,3,4,4a, 5,6, 7, 8, 8 a -decaisoquinoline, respectively Get 2-cyclopropylmethyl-4 aa-((Please read the precautions on the back before filling in this page) Dingben paper size is used in China National Standard (CNS) A 4 specifications (210X297 Gongxuan) 200 Central Ministry of Economic Affairs Printed by the Bureau of Economics and Management Beigong Consumer Cooperative A6 B6 _ 5. Description of the invention ()-3-methoxyphenyl) -8-fluoro-11a / 3 -hydroxy-1, 2, 3, 4, 4a, 5, 11 , 11a-octahydro-6H-indazolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4act- (3-methoxyphenyl) -10-fluoro-lla / S-hydroxyl -1, 2., 3, 4, 4a, 5, 11, 11a-octahydro-6H-indzhao [2, -3 -g] isoquinoline, 2-benzyl-4act- (3-methylphenyl) -8-fluoro-lla / 3-hydroxy-1, 2,3,4,4a, 5, 11,11a-octa Hydrogen-6H-P51 benzo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -10-fluoro-lla / 9-hydroxy_l, 2,3, 4,4a, 5, 11, 11a-octahydro-6H-D5I pentac [2,3-g] isoquinoline, 2- (2-phenethyl) -4ac (-(3-methylphenyl) -8-fluoro-lla / 3-hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-H5I and [2, 3-g] isoquinoline, 2- (2- Phenethyl) -4act- (3-methoxyphenyl) -1〇-fluoro-lla / S-hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-ind Bg Benzo [2, 3-g] isodocin, 2-allyl-4aa- (3-methoxyphenyl) -8-fluoro-lla / 3-hydroxy-1, 2, 3, 4, 43, 5 , 11,11 &amp; -octahydro-6 {{-indolo [2,3-2] isoquinoline, 2-allyl-4a α-(3-methoxyphenyl) -10-fluoro-lla / S -Hydroxy-1,2,3,4,43,5,11,11 &amp; -octahydro-6} 1-1)? 丨 Indo [2,3-2] isoquine_. In the same way, the phenylhydrazine is replaced with a 2-fluorophenyl trap, and 2-cyclopropylmethyl-4a α- (3-methoxyphenyl) -6-chloro-8a / 3-hydroxyl is used -1,2, 3,4,4a, 5,6,7,8,8a-decaisoquine, 2-benzyl-4aa-(3-methoxyphenyl) -6-gaso-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline 2- (2-phenethyl) -4aa-(3-methoxyphenyl)- 6-oxo-8a / S-hydroxy-1, 2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-allyl-4 act-(3-methyl Gas stupid group) -6-oxo-8a / 3-hydroxy-1,2, 3,4,4a, 5, 6, 7, 8,8a-decahydroisoquinoline, respectively get 2-cyclopropyl Methyl-4a ct-(3-A (Please read the precautions on the back before filling in this page) Packing · This paper standard is universal Chinese Standard (CNS) A 4 specifications (210x297 male dragon) 201 Central Bureau of Standards of the Ministry of Economic Affairs Printed by Beigong Consumer Cooperative A6 B 6_V. Description of the invention ()-. Gas phenyl) -7-fluoro- lla; S-hydroxy-1, 2, 3, 4, 4 a, 5, 11, 11 a -Octahydro-SH-indBdeco [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -7-fluoro-lla / S-hydroxy-1, 2 , 3,4,4a, 5, 11, 11a-octahydro-6H-indolo [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxybenzeneGroup) -7-fluoro-ila / S-hydroxy-l, 2,3,4,4a, 5, 11, 11a-octahydro-6H-0? | Dg and [2,3-g] isoquinoline, 2-allyl-4aa- (3-methylphenyl) -7-fluoro-11a /?-Hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6HH _ and [ 2, 3-g] isoquinoline. In the same way, the phenyl trap is substituted with 4-bromophenylhydrazine, and 2-cyclopropylmethyl-4aa- (3-methylphenyl) -6-oxo-8a / 3-hydroxy- 1,2, 3,4,4a, 5,6,7,8,8a -decahydroisosleep, 2-benzyl-4acx-(3-methoxyphenyl) -6-oxo-8a / 3 -Hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl)- 6-oxo-8a / 3 -hydroxy-1,2,3,4,4a, 5,6,7, 8,8a-decahydroisoquinoline, 2-allyl-4aa-(3-methyl gas Phenyl) -6-aero-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, respectively, 2-cyclopropyl methyl Yl-4a cx-(3-methoxyphenyl) -9-bromo-lla / 3 -hydroxy-1,2,3, 4, 4a, 5, 11, 11 a-octahydro-6H-indazolo [ 2,3-g] isoquinoline, 2-sulfanyl-4aa- (3-methoxyphenyl) -7-bromo-1130-hydroxy-1,2,3,4,43,5,11,11 &amp; -Octahydro-611-indigo [2,3-g] isoquinoline, 2- (2-phenethyl)-4aa- (3-methoxyphenyl) -9-bromo-11a / 3- Hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-allyl-4aa- (3-methoxy Benzene) -9-bromo-113 / 5-hydroxy-1,2,3,4,43,5,11,113-octahydro-6 ^ ind 11 $ and [2,3-g] isoquinoline. (Please read the precautions on the back before filling out this page) Pack. This paper is used in Chinese National Standard (CNS) A4 specifications (210x297 male dragon) 202 Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs 3ύ1 ^ 4 Α6 _Β6 ___ Fifth, the description of the invention ()-. And, the same, replace the phenyl hydrazine with 3-bromophenyl hydrazine, and use 2-cyclopropylmethyl-4aa- (3-methylphenyl) -6 -Aero-8a / 3 -Hydroxy-1, 2, 3, 4, 4a, 5, 6, 7,8, Ba-decahydroisoxaline, 2-benzyl-4aa-(3-methoxyphenyl ) -6-oxo-8a therapy-hydroxy-1,2, 3,4, 4a, 5, 6, 7,8,8a-decahydroisoquinoline, 2- (2-phenethyl) -4 aa -(3-methoxyphenyl) -6-fluoro-8a yS -hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-allyl Yl-4aa-(3-methylphenyl) -6-fluoro-8a / 9-hydroxy-l, 2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, Then respectively 2- 2-propylpropyl-4a a- (3-methoxyphenyl) -8-bromo-lla / 3-hydroxy-1,2, 3,4,4 a, 5, 11, 11a- Octahydro-6H-indo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4act- (3-methoxyphenyl) -10-bromo-113 / 5-hydroxy-1, 2,3,4,43,5,11,113-octahydro-6H-P? 丨 flS and [2,3-g] isoquinine, 2 -Benzyl- 4aa- (3-methoxyphenyl) -8-mo-lla / 3_hydroxy_l, 2,3,4,4a, 5, ll, lla ^, M-6H-n5l bite [ 2,3-g] Iso-salenol, 2-benzyl-4aa- (3-methoxyphenyl) -10-bromo-11 &amp; / 3-hydroxy-1,2,3,4,4 &amp;, 5, 11,113-octahydro-611-indazolo [2,3-g] isoquinoline, 2- (2-phenethyl) -4act- (3-methylphenyl) -8-bromo-113 / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-6 {1-ind [1 $ benzo [2,3-g] isoquinoline, 2- (2-phenylethyl Group) -4aa- (3-methoxyphenyl) -10-bromo-113-hydroxy-1,2,3,4,43,5,11,113-octahydro-611-indole 8 [2 , 3-g] isoquinoline, 2-allyl-4a〇t- (3-methoxyphenyl) -8-bromo-11a-hydroxy-1,2,3,4,43,5,11 , 113-octahydro-6 ^ 1- vermolo [2,31] isolu_, 2 -allylpropyl_4a〇t-(3 -methoxyphenyl) -10 -mo-llayS -jing- 1,2,3,4,43,5,11,113-octahydro-6 ^ ind11 | Peo [2,31] isoquine_: Ο (Please read the precautions on the back before filling out this page) ,?! * Line-This paper scale is used in China National Standard (CNS) A4 specifications (210x297 public goods) -203-A6 B6 _ Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Ming ()-_ Again, the phenyl trap is replaced with 2-bromophenylhydrazine, and 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -6-gaso-8a is used / 3-hydroxy-1,2, 3,4, 4a, 5,6,7,8,8a-decaisoquinoline, 2-benzyl-4aa-(3-methylphenyl) -6-oxygen Generation-8a / »-Hydroxy-1,2, 3,4, 4a, 5, 6, 7,8,8a-decahydroisoquinoline, 2- (2-phenethyl) -4aa-(3-methyl Gas phenyl) -6-keto-8a Lu-hydroxy-1,2,3,4,4a, 5, 6,7,8,8a-decahydroisoquinoline, 2-allyl-4 aa- (3-Methylphenyl) -6-oxo-8a / S-hydroxy-l, 2,3,4,4a, 5,6 ,? , 8,8a-decahydroisoquinoline, then 2-cyclopropylmethyl-4a a-(3-methylphenyl) -7-lla / 9 -hydroxy-1,2,3,4, 4a, 5, 11,11a-octahydro-6H-indD5 [2,3-g] isoquinoline, 2-benzyl-4acx- (3-methoxybenzyl) -7-bromo-11 &amp; / ? -Hydroxy-1,2,3,4,4, 5,11,113-octahydro-6} 1-indo [2,3-g] isoquinoline, 2- (2-phenethyl)- 4aa- (3-methoxyphenyl) -7-bromo-11 &amp;; 8-hydroxy-1,2,3,4,43,5,11,11 &amp; -octahydro-611-indole (2 , 3-g] isoquino_, 2-allyl-4act- (3-methoxyphenyl) -7-bromo-lla / 3-hydroxy-1,2,3,4,4 3,5,11,113 -Octahydro-611-indo [2,3- £] isoquinoline. Also, in the same manner, phenylhydrazine is substituted with 4-nitrophenylhydrazine, and 2-cyclopropylmethyl-4aa- (3-methylphenyl) -6-oxo-8a &gt; 8- Hydroxy-1, 2, 3, 4, 4a, 5, 6, 7, 8, 8a-decahydroisoquinoline, 2-benzyl-4aa-(3-methylphenyl) -6-amino-8a / 3 -hydroxy-l, 2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2- (2-benzylethyl) -4aa- (3-methoxyphenyl ) -6-oxo-8 a / 3 -hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-allyl-4aa-(3 -Methoxyphenyl) -6-oxo-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, then get 2-ring Propyl Methyl-4 a ot-(3 (please read the precautions on the back before filling in this page) Binding-The paper size General Chinese National Standard (CNS) A 4 specifications (210X297) ¢-204-Ministry of Economic Affairs Printed by the Central Standards Bureau Beigong Consumer Cooperative A6 B6_ V. Description of the invention ()--methyl gas phenyl) -9-nitro-113 Zhao-Jingji -1,2,3,4,43,5,11, 11 &amp; -octahydro-611-indolo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -9-nitro-lla / 3-hydroxy-1 , 2,3, 4,4a, 5,11,11a-octahydro-6H-〇5i clonop [2,3-g] isoquinoline, 2- (2-phenethyl -4aa- (3-methoxyphenyl) -9-nitro-1U / S-hydroxy-1,2,3,4,4a, 5, 11,11a-octahydro-SH-indolo [2, 3-g] isoquinoline, 2-allyl-4aa- (3-methoxybenzyl) -9-nitro-lla / 3-xiangyl-1,2,3,4,4a, 5,11 , 11a-octahydro-6H-D5I Pg and [2, 3-g] isoquinoline. Also, in the same way, replace the phenyl trap with a 3-nitrophenyl trap and use 2-cyclopropylmethyl-4a α- (3-methoxyphenyl) -6-gaso-8a / S -Hydroxy-1, 2,3,4,4 technology, 5,6,7,8,8 &amp; -decahydroisoquinoline, 2-benzyl-43 € (-(3-methoxyphenyl) -6 -Aero- 8a / 3 -Hydroxy-1,2, 3, 4, 4a, 5,6, 7,8,8a-Decahydroisoquine W, 2- (2-phenethyl) -4act-(3 -Methoxyphenyl) -6-aero-8a / 3 -hydroxy-1,2,3,4,4a, 5, 6, 7,8,8a-decazaisoquinoline, 2-allyl- 43 «-(3-methylphenyl) -6-oxo-83 &gt; 3-hydroxy-1,2,3,4,43,5,6,7,8,8a-decahydroisoquinoline, then Respectively, 2-cyclopropylmethyl-4a ct-(3-methylphenyl) -8-nitro- lla / 3 -keto-1,2,3,4,4a, 5,11,11a- Octahydro-SH-indox [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -10-nitro-lla / 3-hydroxy-l , 2,3,4,4a, 5, ll, lla-octahydro-6H-indigo (2,3-g) isoquinoline, 2-benzyl-4ac (-(3-methoxyphenyl) -8-nitro-lla / 3-sangyl-1,2,3,4,4a, 5,11,11a-octahydro-6H-indPg (〔2,3-g〕 isoquine_, 2- Zanyl-4act- (3-methoxyphenyl) -10 -nitro- lla / S -keto-1,2,3,4, 4a, 5, 11,11a-octahydro-6H-indPS 〔2,3-g〕 Isoquinoline, 2- (2-phenethyl) -4aa- (3-A (please read the precautions on the back before filling out this page) Binding · Ordering-This paper is used for the standard of 0 countries (CNS) A4 specifications (210x297 mm) 205 Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs Λ6_B £ _ V. Description of invention ()-. 'Oxyphenyl) -8-nitro-11a -hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indBg and [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl ) -10-nitro-11a / 3 -hydroxy-1,2,3, 4,4a, 5, 11, 11a-octahydro [2,3-g] isoquinoline, 2-allyl-4aa -(3-Methylphenyl) -8-nitro-11a / 3 -hydroxy-1,2, 3,4,4a, 5, 11, 11a-octahydro-6H-indolo [2,3- g] Isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -10-nitro-lla / 3-hydroxy-1,2, 3, 4, 4a, 5, 11, 11a- Octahydro-6H-indolino-5 [2,3-g] isoquinoline. In the same way, the phenyl trap is replaced with a 2-nitropropyl trap, and 2-cyclopropylmethyl-4aa-(3-methoxyphenyl) -6-oxo-8a / 3-hydroxyl is used -1, 2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-benzyl-4aa-(3-methylchlorophenyl) -6-oxo-8a / 3 -Hydroxy-1,2,3, 4, 4 a, 5,6, 7,8,8a-decahydroisoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl ) -6-oxo-8 a / 3 -hydroxy-1,2,3, 4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-allyl-4act-(3 -Methoxyphenyl) -6-aero-8a / 3 -hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, then 2-ring Propylmethyl-4acr-(3-methylphenyl) -7-nitro- lla / 3-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-indBg Benzo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -7-nitro-11a / 3-hydroxy-1,2, 3, 4, 4a, 5 , 11,11a-octahydro-6H-indolo [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methylphenyl) -7-nitro- lla / 3 -Hydroxy-1,2, 3, 4,4a, 5, 11, 11a-octahydro-6H-indBS [2,3-g] isoquinoline, 2-allyl-4act- ( 3-methoxyphenyl) -7-nitro-11a / 3-hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indDg [2, 3 -g] isoquinoline. (Please read the precautions on the back before filling out this page) This paper standard is universal Chinese National Standard (CNS) A4 specifications (210x297 metric) Λ 6 Β6 Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of invention () -. Also, the same, replace the phenylhydrazine with a benzyl trap, and use 2-cyclopropylmethyl-4a〇t-(3-methoxyphenyl) -6-oxo-8a / 3 -Hydroxy-1,2,3, 4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-benzyl-4aa-(3-methoxyphenyl) -6-gaso- 8a / 3 -hydroxy-1,2, 3,4, 4a, 5,6,7,8,8a-decahydroisoquinoline, 2- (2-phenethyl) -43〇1- (3-methyl Oxyphenyl) -6-oxo-83 / 9-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline, 2-allyl-4 acr -(3-methoxyphenyl) -6-oxo-8a / 3 -hydroxy-1,2,3,4, 4a, 5, 6,7, 8,8a-decahydroisoquinoline, respectively 2-cyclopropylmethyl-4act-(3-methoxyphenyl) -llayS -hydroxy-1,2,3, 4, 4a, 5, 11, 11a-octatri-6-methyl-indolo [2,3-g] isoquinoline, 2-sulfanyl-4acc- (3-methoxyphenyl) -11a &gt; 9-hydroxy-1,2, 3, 4, 4a, 5, 11, 11a- Octahydro-6-methyl-indeno [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -11 a / 3 -hydroxy-1,2,3, 4, 4a, 5, 11, 11a-octahydro-6-methyl-indo-p- [2, 3-g] isoquinoline, 2-allyl -4aa- (3-methoxyphenyl) -lla / 3-hydroxy-1,2,3,4,43,5,11,118-octahydro-6-methyl-indolo [2,3 -Ming] isoquinoline. Example 45 2-cyclopropylmethyl-4aa-(3-hydroxyphenyl) -llayS -hydroxy-1,2,3, 4, 4a, 5,11, 11a-octahydro-6H-ind Ug and [ 2, 3-g] isoquinoline 56

0H

The size of this paper is based on the Chinese National Standard (CNS) A4 specification (210x297 g *) 207 (please read the precautions on the back before filling the nest page).

V. Description of the invention () The 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -lla / 3-hydroxy-1, 2,3,4,43,5,11,113-octahydrogen -611-Isoquino [2,31] isoquinoline (70 g, 0.17bido1) was dissolved in DMF (anhydrous, 2ml), and propane thiol (0.12ml, 1.3mmol), potassium-t-butane vapor was added (98mg, 0.87 off 〇1), react at 150 ° C for 3 hours. Because there are still unreacted substances, propanol mercaptan (0.06ml, 0.7inmol), gent-t-butoxide (49ng, 0.44 ππ〇1) was added for 2 hours, and then propane mercaptan (0.12ml) was added , 1.3 mmol), potassium-t-butoxide (98ag, 0.87βππο1) for 2 hours. The solvent was distilled off under reduced pressure, saturated aqueous sodium bicarbonate solution (8m 1) was added, and extracted with ethanol / chloroform (3/1, 8bi1x 3). After washing with saturated saline, drying and concentrating, it was purified with a silica gel chromatography tube (938.585g; chloroform 4 ammonia saturated chloroform 5% methanol / ammonia saturated chloroform) to obtain the title compound 39. 7 mg (5 9 %). Dissolve it in chloroform (2ml) and methanol (0.2ml), add methanesulfonic acid to make a salt, and separate it. mp: 153 ~ 157 ° C (methanesulfonate)

Mass (BI): 388 (M +) (please read the precautions on the back before filling in this page) Binding-Order _ Printed Elements Analysis of Beigong Consumer Cooperative, Central Standards Bureau, Ministry of Economic Affairs * CzsHzeNzOzCH 3 S 0 3 Η 1.5ΗZ0 tLT DC Η Ν S calculation value 61.04 6.90 5.47 6.27 measurement value 60.95 6.73 5.34 6.31 The following is the same, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -113 / 9-hydroxy-1,2, 3,4,4 3,5,11,113-octahydro-61 indole [2, this paper scale is used in China National Standards (CHS) A 4 specifications (210x297 male dragons) 208 A 6 B6 Central Bureau of Standards, Ministry of Economic Affairs Printed by Employee Consumer Cooperative V. Description of the invention ()-3-g] Isoquinoline replaced by 2-benzyl-4aa-(3-methoxyphenyl) -lla / 3 -hydroxy-1,2,3, 4,43,5,11,113-octahydro-611-indolo [2,3-8] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -lla / 9-hydroxy-1,2, 3,4,43,5,11,118-octahydro-611-indigo [2,31] isoquinoline, 2-allyl-43 «-(3-methoxybenzene Group) -113 / 5-hydroxy-1,2,3,4,43,5, 11,113-octahydro-611-indole [2,31] isoquinoline, 2-cyclopropylmethyl-43. (-(3-methoxyphenyl) -9-methyl-113 / 9-hydroxy-1,2,3,4,43,5, ll , Lla-octahydro [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -9-methyl-lla ^ S-hydroxy-1,2,3, 4, 4a, 5,11,11a -octahydro-6H-indazolo [2,3-g] isosialoline, 2- (2-phenethyl) -4ac (-(3-methoxyphenyl) -9-methyl- lla / 3-hydroxy-1,2,3,4,4a, 5,11,11a -octahydro-6H-D? 丨 0? And [2,3-g] isoquino, 2 -Isopropyl- 4aa- (3-methoxyphenyl) -9-methyl- lla / 3-hydroxy-1,2,3,4,4a, 5,11,11a-octahelium-6H-D5 Iso [2,3-g] isoquinine, 2-cyclopropylmethyl-4a〇c- (3-methoxyphenyl) -8-methyl-lla / S-hydroxy-1,2,3 , 4,4a, 5,11,11a-octahydro-6H-〇5 | BS and [2,3-g] isolu, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -10-Methyl-lla / 3-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-D? | PS and (2,3-g) isoquine_, 2 -笮 基 -4aa- (3-methylphenyl) -8-methyl-lla / S-hydroxy-1,2, 3,4,4a, 5,11,11a-octahydro-6H-indeno 〔 2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -10-methyl-113 / 8-hydroxy-1,2,3,4,4, 5, 11,11 Kai-octahydro-6H-D? 丨 Dolo [2,3-g] isoquino_, 2- (2-phenethyl) -4act- (3-methylphenyl) -8-methyl Yl-lla; S-hydroxy-1,2, 3, 4, 4a, 5, 11, 11 a-octahydro-6H- «丨 [[3,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-A (Please read the notes on the back before (Fill in this page) Binding-Order _ This paper standard uses the Chinese National Standard (CNS) A 4 specifications (210x297 male dragon) -209-3ΰ16〇4 A 6 Β6 V. Description of invention () Employee Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs Printed gas phenyl) -10-methyl-lla; S-hydroxy-1,2, 3, 4, 4 a, 5, 11, 11a-octahydro-6H-indapi [2,3-g] Isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -8-methyl-lla / 3-hydroxy-1,2, 3,4,4a, 5, 11,11a-octahydro -6H-0? Iso [2,3-g] isoquinoline, 2-allyl-4act- (3-methoxyphenyl) -10-methyl-lla / S-hydroxy-1,2 , 3,4,4a, 5, 11, 11a-octahydro-6H-indos [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -7-methyl-11a / 3 -hydroxy-1,2,3,4,4a, 5, 11,11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-benzyl Yl-4aa- (3-methoxyphenyl) -7-methyl-113 / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-611-indhum [2 , 3-g] isoquinoline, 2- (2-phenethyl) -4act- (3-methoxyphenyl) -7-methyl-113 / 3-hydroxy-1,2,3, 4, ", 5,11,113-octahydro-611-indolo [2,3-g] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -7-methyl-11a / 3 -hydroxy-1,2,3, 4, 4a, 5, 11, 11a-octahydro-6H-indeno [2,3-g] isoquino, 2-cyclopropylmethyl-4act- ( 3-methyl gas phenyl) -9-nitrogen-118 / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-^^ &quot; decene [2,3-g] Isoquinoline, 2-benzyl-4act- (3-methylphenyl)-^^ la / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-6} 1 -Indo [2,31] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -9-chloro-lla / 3-hydroxy-1,2,3, 4,43,5,11,113-octahydro-6} 1-_bezo [2,31] isoquinoline, 2-allyl-43〇 (-(3-methoxyphenyl)-^ ^ &amp; / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-6 ^^ knockout [2,3-2] isoquinoline, 2-cyclopropylmethyl-4a «-(3-Methylphenyl) -8-nitrogen-Ua / 3-hydroxy-1,2,3,4,43,5,11,113-octa-611-ind" 5 and [2,31] iso Quinoline, 2-cyclopropylmethyl-43〇 (-(3-methoxyphenyl) -10-chloro-113 / 3-hydroxy-1,2,3,4, the paper standard is the general Chinese national standard ( CNS) A4 specifications (210x297 public goods) -210-(Please read the precautions on the back before filling This page) Ding Xiang ^ 〇lC54 A6 B6 V. Description of invention (printed by the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 4a, 5, ll, lla-octahydro-6H-P? | IIS and (2,3-g 〕 Isoquinoline, 2-benzyl-4 &amp; «-(3-methoxyphenyl) -8-chloro-113 / 3-hydroxy-1,2,3,4,4, 5,11, 11a- Octahydro-6H-indo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methylphenyl) -10-gas-lla / 3-hydroxy-1,2,3 , 4,4a, 5,11,11a-octahydro-6H-0? -Indo [2,3-g] isoquinoline, 2- (2-phenethyl) -4acc- (3-methoxybenzene Group) -8-gas- lla / 9-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-indolo [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methylphenyl) -10-chloro-lla / 3-hydroxyl-l, 2,3,4,4a, 5, ll, lla-octahydro-6H- Indolo [2,3-g] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -8-chloro-113-hydroxy-1,2,3,4,43, 5,11,113-octahydro-6? 1-indo [2,3-g] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -10-ambient-11a / 3- Hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3- Methoxyphenyl) -7-chloro-113-hydroxy-1,2,3,4,4 3,5,11,113-octahydro-6? 1-indene Hey [2,3-g] isoquinoline, 2- ¥ yl-43 «-(3-methoxyphenyl) -7-nitro-lla / 3-hydroxy-1,2, 3,4,4a, 5, 11,11a-octahydro-6H-indazolo [2, 3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -7-chloro- 11 2 ^ -hydroxy-1,2,3,4,43,5,11,113-octahydro-6} 1-indolo [2,31] isoquinoline, 2-allyl-4aa- ( 3-methylchlorophenyl) -7-chloro-lla / 3-hydroxy-1,2,3,4,4 &amp;, 5,11,113-octahydro-611-indodecano [2,31] isoquinoline , 2-Cyclopropylmethyl-4act- (3-methoxyphenyl) -9-fluoro-lla / S-hydroxy-1,2,3,4,43,5,11,113-octahydro-6 ^ 丨 Bien [2,31] isoquinoline, 2-benzyl-4 &amp; 〇 (-(3-methoxyphenyl) -9-fluoro-113 / 3-hydroxy-1,2,3,4, 43,5,11,113-octahydro-6} 1-1!? 4? And [2,31] isoquinoline, 2- (2- (please read the precautions on the back before writing this page) . This paper scale is universal Chinese National Standard (CNS) A4 specifications (210x297 male dragon) -211-211 Λ 6 B6 S〇lC〇4 V. Description of invention ()-Phenethyl) -43〇 (-(3- Methylphenyl) -9-fluoro-11 &amp; 々-hydroxy-1,2,3,4, 4a, 5,11,11a-octahydro-6H-indazolo [2,3-g] isoquinoline , 2-allyl-4aa-(3-methoxy Group) -9-fluoro-lla0-keto-l, 2,3,4,4a, 5, 11,113-octahydro-6} 1-115 丨 115 [2,31] isoquinoline, 2-cyclopropyl Methyl-4a ct-(3-methylphenyl) -8-fluoro-lla / Q -hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-B? 丨Isoquino [2,3-g] isoquinoline, 2-cyclopropylmethyl-4 act-(3-methoxyphenyl) -10-fluoro-lla / 3 -hydroxy-1,2,3, 4 , 4a, 5, 11, 11a-octahydro-6H-indBg and [2,3-g] isoquinoline, 2-benzyl-4acx- (3-methylphenyl) -8-fluoro-11a / 3 -Hydroxy-1,2, 3,4,4a, 5, 11,11a-octahydro-6H-indPg- [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methyl Gas phenyl) -10-fluoro-113 / 5-hydroxy-1,2,3,4,43,5,11,113-octahydro-6} 1-indazolo [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -8-fluoro-1 la; S-hydroxy-1,2,3, 4, 4a, 5, 11, 11a-octahydro -6H-Dumb [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -1 0-fluoro-11a / 3 -hydroxy-1 , 2, 3, 4, 4 a, 5,11, 11a-octahydro-6H-indazolo C2,3-g] iso 1¾-liner, 2-propane_4aa- (3-methoxyphenyl) -8 -fluoro-113 / 9-hydroxy-1,2,3,4,4 3,5,11,113-octahydro-611- verendolo [2, 3- | [] isoquinoline, 2- Allyl-4act- (3-methylphenyl) -10-fluoro-11 ugly / 3-hydroxy-1,2,3,4,43,5,11,11hexane-octahydro-51 ^ -ind Mizo [2,3-2] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -7-fluoro-11 3 / 9-hydroxy-1,2,3,4 , 43,5,11,113-octahydro-6}}-indodecano [2,3-ming] isoquinoline, 2-sulfonyl-4act- (3-methoxyphenyl) -7-fluoro -lla / 3-hydroxy-1,2,3,4, ", 5,11,113-octahydro-6} 1-indo [2,31] isoquinoline, 2- (2-phenethyl ) -4aa- (3-methoxyphenyl) -7-fluoro-lla / 3-hydroxy-1 This paper scale is used in the 0 national standard (CNS) A 4 specifications (210X297 male dragon) (please read the back Matters needing attention and then fill out this page) Outfit-Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 212 5. Description of Invention (A 6 B6 Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy, 2, 3, 4, 43, 5, 11,113-octahydro-6 {1-indazolo [2,3-8] isoquinoline, 2-allyl-43〇 (-(3-methoxyphenyl) -7-fluoro-11 &amp;; 6 -Hydroxy-1,2,3,4,43,5,11,113-octahydro-6 ^ 1-115 丨 [12 [〔2,3-§] isoquino_, 2-cyclopropylmethyl-43〇 (-(3-methoxyphenyl) -9-bromo-113 / 3-hydroxy-1,2,3,4, 48,5,11,113-octahydro-6} 1-1 ^ 丨 Complex [2,3-8] Iso-lu, 2-: ¥: yl-4hex- (3-methoxyphenyl) -9-bromo-113 / 3-hydroxy-1, 2,3,4,43,5,11, 11a-octahydro-6H-indeno [2,3-g] isoquinoline, 2- (2-phenethyl) -4a cc- (3-methylchloro Phenyl) -9-bromo-lla / S-hydroxy-l, 2,3,4,4a, 5, ll, 11a -octahydro-rungo [2,3-g] isosalogenyl, 2-pyridinyl -4aa_ (3-methylphenyl) -9-bromo-lla / 3-hydroxy-1, 2,3,4,4a, 5, ll, lla-octahydro-6H-P¾ |! IS 和 〔2 , 3-g] isoquinol, 2-cyclopropylmethyl-4ao (-(3-methoxyphenyl) -8-bromo-lla / S-hydroxy-1,2,3,4, 4a, 5 , 11,11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -10-bromo-11a point- Hydroxy-1,2, 3,4,4a, 5,11,11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxybenzene Group) -8-bromo-113 / 9-hydroxy-1,2,3,4,43,5,11,113-octahydro-6} 1-indolo [2,3-g] isoquinoline, 2- Benzyl-4aa- (3-methoxyphenyl) -10-bromo-11a /?-Hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-inds PS (2 , 3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -8-bromo-11a / 3 -hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indica ^ 〔 2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) white 113zhao-hydroxy-1,2,3,4,43,5,11, 113-octahydro-6} 1-ind [^ 和

[2,3-g] isoquinoline, 2-allyl-4aa- (3-methoxyphenyl) -8-bromo-lla / Θ-hydroxy-1, 2,3,4,4a, 5, ll, lla-Octahydro-6H-indignand (2,3 paper size, please use Chinese National Standard (CNS) A4 specifications (210X297mm) 213 (please read the precautions on the back and fill in this page) · Order_ Line ·

A 6 _136_ V. Description of invention ()-Printed by Beigong Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs -g] Isoquinoline, 2-allyl-4aa- (3-methylphenyl) -10-bromo-lla / 3 -Xiang-1,2,3,4,43,5,11,113-octahydro-6} 1-115 | Bino [2,3-dan] isoquinoline, 2-cyclopropylmethyl Yl-4acx-(3-methoxyphenyl) -7-bromo-113 / 3-hydroxy-1,2,3,4,48,5,11,113-octahydro-611-indole2 [2,3 -Miso] isoquinoline, 2-benzyl-4aa- (3-methoxyphenyl) -7-bromo-llayS-hydroxy-1,2,3,4,43,5,11,113-octahydro- 6 Bu indodecene [2,3-jun] isoquinoline, 2- (2-phenethyl) -43 «-(3-methoxyphenyl) -7-bromo-113 / 9-hydroxy-1 , 2,3, 4,4a, 5, ll, lla-octahydro-6H-ind11¾ and (2,3-g) isoquinoline, 2-allyl-43〇 (-(3-methylbenzene Group) -7-bromo-113 / 3-hydroxy-1,2,3,4,43, 5,11,11a-octahydro-6H-indolo [2,3-g] isoquinoline, 2- Cyclopropylmethyl-43 «-(3-methylphenyl) -9-nitro-113 / 5-hydroxy-1, 2,3,4,43, 5,11,113-octaargon-6} 1- Indaza [2,3-2] isoquinoline, 2-benzyl-4 aa-(3-methoxyphenyl) -9-nitro- lla / 3-hydroxy-1,2,3,4, 4a, 5,11,11a-octahydro-6H-indo [2,3-g] isoquinoline, 2- (2-phenethyl -4 act-(3-methylphenyl) -9-nitro-lla / 3 -hydroxy-1,2,3,4,4a, 5,11, 113-octahydro-6 ^ indazol [2 , 31] Isoquinoline, 2-allyl-43 «-(3-methoxyphenyl) -9-nitro-lla / 3-hydroxy-1,2,3,4,4a, 5,11, 11a -octahydro-6H-indo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4act- (3-methylphenyl) -8-nitro-lla / 3-hydroxyl -1,2,3,4,4a, 5,11,11a 'octa [2,3-g] isoquino, 2-cyclopropylmethyl-4a〇t_ (3-methoxyphenyl)- 10-Nitro-lla / S-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-D? 丨 Diazo [2,3-g] isoquinoline, 2- Benzyl-4aa- (3-methoxyphenyl) -8-nitro-lla / 3-hydroxy-1,2,3,4, 4a, 5, 11,11a-octahydro-6H-indazolo [ 2,3-g] isoquinoline, 2-benzyl-4aa- (3-methoxy 214 (please read the precautions on the back before filling out this page) This paper scale is universal China National Standard (CNS) A 4 specifications ( 210X297 (public goods) A6 B6_ printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 5. Description of invention ()-phenyl) -10 -nitro- lla / 3 -jingji-1,2, 3,4,4a, 5 , 11,11a -Octah-6H-indPS- [2,3-g] isoquinoline, 2- (2-phenethyl) -4act- (3-methoxyphenyl) -8- -Lla / 3-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-ind Pg and [2,3-g] isoquinoline, 2- (2-phenylethyl Group) -4aa- (3-methoxyphenyl) -10-nitro-lla / 3-keto-1,2,3,4,4a, 5,11,11a-octahydro-6H-ind Ug and [2,3-g] isoquino-, 2-allyl-4aa- (3-methoxyphenyl) -8-nitro-lla / 3-keto-1,2,3,4,4a, 5,11,11a -octahydro-6H-D? 丨 DS- [2,3-g] isosialoline, 2-allyl-4aa- (3-methoxyphenyl) -10 -nitro-lla ; S-benzyl-1,2, 3,4,4a, 5,11, 11a -octahydro-6H-D? | B5 benzo [2,3-g] isoquino, 2-cyclopropylmethyl -4aa- (3-methoxyphenyl) -7-nitro-lla / S-xiang-1,2,3,4,4a, 5,11,11a-octahydro-6H-indolo [2 , 3-g] isoquinoline, 2-benzyl-4aa- (3-methoxybenzyl) -7-nitro-lla / 3-hydroxy-1,2,3,4,43,5,11, 113-octahydro-611-11? | Πdecano [2,3-g] isoquinoline, 2- (2-phenethyl) -4acc- (3-methoxyphenyl) -7-nitro- 11a point-Keto-1,2,3,4,43,5,11,113-octahydro-6} 1-indPS [2,3-g] isoquinoline, 2-allyl-4act -(3-methoxyphenyl) -7-nitro-11 &amp; / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-611-indazolo [2,3-g 〕 Isoquinoline, 2-ring Propylmethyl-4aa- (3-methoxyphenyl) -11 3 cold-hydroxy-1,2,3,4,43,5,11,113-octahydro-6-methyl-indole [18 and [2,3-g] isoquinoline, 2-sulfanyl-4aa- (3-methoxyphenyl) -lla / S-hydroxy-1,2,3,4,4 a, 5,11,11 a Zhao-octahydro-6-methyl-ind 11¾- [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-methoxyphenyl) -iia / s-hydroxyl -1, 2, 3, 4, 4a, 5, 11, 11a / 3-octahydro-6-methyl-indolo [2,3-g] isoquinoline, 2-allyl-4aa- ( 3-Methoxyphenyl) -lia / 3-hydroxy-1,2, the size of this paper uses the Chinese National Standard (CNS) A4 specifications (210x297 g; ¢)-215-(Please read the precautions on the back first (Fill in this page) Installed, tT_ A 6 B 6 Printed by the Consumer Consumption Cooperative of the Bureau of Standards, Ministry of Economic Affairs V. Invention Instructions ()-3, 4, 4a, 5, 11, 11a / 9-octahydro-6-A -Indo [2,3-g] isoquinoline, then 2-benzyl-4a «-(3-hydroxyphenyl) -lla / 3-hydroxy-1, 2, 3,4,4a , 5, 11,11a-octahydro-6Η-Ρζ | Ρ 荣 和 [2,3-g] isoquinoline, 2- (2-phenethyl) -43〇 (-(3-hydroxyphenyl)- 113; 3-hydroxy-1,2,3,4,4 &amp;, 5, 11,113-octahydro-61 ^ beer 丨 11 | And [2,3-§] isoquinine, 2-allyl-4 &amp; 〇 (-(3-hydroxyphenyl) -11 &amp; / 3-hydroxy-1,2,3,4,43,5 , 11,113-octahydro-6H-indazolo [2,3-g] isoquinoline, 2-cyclophenylpropylmethyl-4acx- (3-hydroxyphenyl) -9-chloro-lla / 9-hydroxyl -1,2,3, 4,4a, 5,11,11a-octahydro-6 H-indazolo [2,3-g] isoquinoline, 2-benzyl-4aa-(3-hydroxyphenyl ) -9-methyl-11 a / 3 -hydroxy-1, 2, 3, 4, 4 a, 5, 11, 11 a -octahydro-6 Η -ind0¾ and [2,3-g] isoquine Porphyrin, 2- (2-phenethyl) -4aa- (3-hydroxyphenyl) -9-methyl-11a / 3-hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octa Hydrogen-6H-indazolo [2,3-g] isocinoline, 2-allyl-4aa- (3-hydroxyphenyl) -9-methyl-113 /?-Hydroxy-1,2,3 , 4,43,5,11,113-octahydro-6! 1-vertebral iso [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-pyridyl) -8- Methyl-11 3 / 9-hydroxy-1,2,3,4,43,5,11,113-octahydro-61 ^ -tonne [2,31] isoquinoline, 2-cyclopropylmethyl- 4aa- (3-hydroxyphenyl) -10-methyl-11a ha-hydroxy-1,2,3,4,43,5,11,11 &amp; -octahydro ^ -ind [1duo [2,31 〕 Isoquinoline, 2-phenyl-4aa- (3-hydroxyphenyl) -8-methyl-lla / 3-hydroxy-1,2,3, 4,43,5,11,113-octahydro-6 ^ 1-indolo [2,31] isoquinoline K / iii m Ψ Η E3 other strontium (0 ^) ¥ 4 specifications (210x297 g; « ) _ 91 f. (Please read the precautions on the back before writing this page) Packing. Threading. A6 _______ B6_ printed by the Cooperative Society of the Central Standards Bureau of the Ministry of Economy V. Invention description () 1. 2-benzyl-4a «-(3-hydroxyphenyl) -10-methyl-lla; Q-hydroxy-1,2, 3,4,43,5,11,11 &amp; -octahydro-6 [1 -Indophthalo [2,31] isoquinoline, 2- (2-phenethyl) -43 «-(3-hydroxyphenyl) -8-methyl-113 /?-Hydroxy-1,2,3 , 4,4a, 5,11,11a-octahydro-6H-indo [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-hydroxyphenyl)- 10-methyl-lla / 3-hydroxy-1,2,3, 4,4 &amp;, 5,11,113-octahydro-6 ^ 1-indazolo [2,31] isoquinoline, 2-allyl -4aa- (3-hydroxyphenyl) -8-methyl-lla / S-hydroxy-1, 2,3,4,4a, 5,11,113-octahydro-6 ^ 丨 conjugated [2,3-ju 〕 Isoquinoline, 2-allyl-4 acx-(3-hydroxyphenyl) -10-methyl- lla / 3 -hydroxy-1, 2,3,4, .4a, 5, ll, 11a- Octahydro-6H-indolo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4a a-(3-hydroxyphenyl) -7-methyl-1 lla / S-hydroxy-1 , 2,3,4,4a, 5,11 , 11 a-octahydro-6H-indogeno [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -7-methyl-lla / 3-hydroxy- 1,2,3, 4,4a, 5, 11,11a-octahydro-6 Η-indos [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3 -Hydroxyphenyl) —7-methyl-113 ^ 3-Renyl-1,2,3,4,4 &amp;, 5,11,1151-octahydro-61 two 丨 8 8 [2,3-g ] Isosleep 1) (wood, 2-propenyl-4aa- (3-xiangphenyl) -7-methyl-11a-hydroxy-1,2,3,4,4 a, 5, 11, 11 a-Octahydro-6H-indigo [2,3-g] isosleep, 2-cyclopropylmethyl-4aa- (3-pyridyl) -9-chloro-11hex / 3-hydroxy- 1,2,3,4,43,5,11,11 &amp; -octahydro-6 ^ 丨 iso [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -9-gas-lla / 3-hydroxy-1,2,3,4,4 &amp;, 5.11,113-octahydro-6} 1-indo [2,3-dan] isohumata Ψ due to K 觇Grid (210x297 public goods) -216-1-(please read the precautions on the back before filling out this page) 装-,, τ_ 线 '

oiii G A6 B6 5. Description of the invention (Porphyrin, 2- (2-phenethyl) -4aa- (3-hydroxyphenyl) -9-nitrogen-llap-hydroxy-1, 2,3,4,4 &amp;, 5,11,113-octahydro-61 ^ indo [2,31] isoquinoline, 2-allyl-4acx- (3-hydroxyphenyl) -9-chloro-lla ^ S-hydroxy-1 , 2, 3,4, 43,5,11,118-octahydro-6} 1-indole 5 [2,3-ming] isoquinoline, 2-cyclopropylmethyl-43 ^-(3 -Hydroxyphenyl) -8-chloro-113 / 9-hydroxy-1,2,3,4,43, 5,11,113-octahydro-6 {^ 的 丨 11decobe 〔2,3- 茶〕 Isialia 11 ^, 2-cyclopropylmethyl-4a α-(3-hydroxyphenyl) -10-gas-lla / 3-hydroxy-1,2,3, 4,4a, 5, 11,113-octahydro -611-Indo [2,31] isoquinoline, 2-benzyl-43〇 (-(3-hydroxyphenyl) -8-ambient-11a / 3-hydroxy-1, 2,3, 4, 4a, 5, 11, 11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -10-chloro-lla / S- Hydroxyl-1,2,3,4,43,5,11,113-octahydro-6 {]-P cited {^ and [printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economy [2,3-g] isoquin Porphyrin, 2- (2-phenethyl) -4aa- (3-hydroxyphenyl azhao-hydroxy-1, 2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indo- [ 2,3-g] isoquinoline, 2- (2-phenethyl) -4 3 «-(3-Hydroxyphenyl) -10-Aromatic-11a / 3 -Hydroxy-1,2,3, 4, 4a, 5, 11, 11a-octahydro-6H-indazol [2,3- g) Different pupils, 2-pyridinyl-4aa_ (3-xiangphenyl) -8-qi-11 3 /?-hydroxy-1, 2,3,4,43,5,11,113-octahydro -6 ^ | 1 ^ [2,31] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -10-ambient-lla / 3-hydroxy-1,2,3,4, 4a, 5,11,11a-octahydro-6H-indus iso [2,3-g] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -7-nitro-lla / 9 -Hydroxy-1,2,3,4,4 &amp;, 5,11,11 &amp; -octahydro-611-lumbo [2,31] isoquinoline, 2-benzyl-43 «-(3 -Hydroxyphenyl) -7-chloro-1130-hydroxy-1,2,3,4,4 &amp;, 5,11,113-octahydro-6} 1-indo [2,31] isoquinoline, 2- (2-phenethyl) -43〇 &lt;-( 3-hydroxyphenyl) -7-chloro-113 / 9-hydroxy-1,2,3,4,4 &amp;, 5, (please read first (Notes on the back then fill this page)

This paper scale uses the Chinese National Standard (CNS) A4 specifications (210x297 male dragons) 217 Printed by the Ministry of Economic Affairs Central Standards Bureau Employee Consumer Cooperative A 6 B6_ V. Description of invention ()-11.113- octahydro-611-ind [^ And [2,3-Ju] isoquinoline, 2-allyl-4 act-(3-hydroxyphenyl) -7-nitro-lla / 3-hydroxy-1,2,3, 4,4a, 5 , 11,11a -Octahydro- Iso [2,3-g] isosialin, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -9-fluoro-11a /?-Hydroxy- 1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indolo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl)- 9-fluoro-11a / 3 -hydroxy-1,2, 3, 4, 4a, 5, 11, 11a-octahydro-6H-indho [2,3-g] isoquinoline, 2- (2- Phenethyl) -4aa- (3-hydroxyphenyl) -9-fluoro-11 &amp; / 5-hydroxy-1,2,3,4,4 Kai, 5,11,113-octahydro-6} 1-indeye And [2,3-g] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -9-fluoro-lla / 3-hydroxy-1,2,3,4,43,5, 11,113-octahydro-6} 1-indolo [2,31] isoquinoline, 2-cyclopropylmethyl-4a〇c-(3-hydroxyphenyl) -8-fluoro-11a / 3 -Hydroxy-1,2,3,4,43,5,11,113-octahydro-61 ^ -indoxo [2,3- 豸] isoquinoline, 2-cyclopropylmethyl-4aa-(3- Hydroxybenzene ) -10-Fluoro-lla / S-hydroxy-1.2.3.4.46.5.11.113-octahydro-6} 1-115 丨 02 [2,3-end] isoquinoline, 2-benzyl-43 «- (3-Hydroxyphenyl) -8-fluoro-113 / 3-hydroxy-1,2,3,4,4%, 5,11,11 &amp; -octahydro-61 {-ind 5 (〔2,3 -犟] isoquinoline, 2-benzyl-43〇 (-(3-hydroxyphenyl) -10-fluoro-113 /?-Hydroxy-1,2,3,4,43,5,11,11a- Octahydro-6H-indodecano [2,3-g] isoquinoline, 2- (2-phenethyl) -4 aa-(3-hydroxyphenyl) -8-fluoro-lla / 3 -hydroxyl -l, 2,3,4,4a, 5, ll, lla -octahydro-6H-indeno [2,3-g] isoquino, 2- (2-phenethyl) -4aa- (3 -Hydroxyphenyl) -10-fluoro- lla / 3 -hydroxy-1, 2, 3,4,4a, 5, 11,11a-octaqi-6H -1¾ 丨 bite [2,3-g] isosia Leaching, 2-allylpropyl-4aa- (3-xiangphenyl) -8-fluoro-lla / S-hydroxy-1,2,3,4,4 &amp;, 5,11,113-octahydro-611-ind B2 And [2,3-g] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -10- This paper scale is used in the national standard (CNS) A 4 specifications (210X297 public ¢) 218 (Please read the precautions on the back before filling in this page) • 1T, printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs A 6 ____B6_ V. Description of invention () _ Fluorine-113 / 8-hydroxyl -1,2,3,4,43,5,11,113-octahydro-6 (1-indigo [2,3 -g] isoquino, 2-cyclopropylmethyl-4 a α- (3-Phenyl) -7-Fluoro-11Cho / 8-Hydroxy-1,2,3,4,43,5,11,113-Octahydro-611-Indo [2,3_g] iso Quinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -7-fluoro-lla / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-6} 1 -Indo [2,3-1] isoquinoline, 2- (2-phenethyl) -43〇 (-(3-hydroxyphenyl) -7-fluoro-113; 3-hydroxy-1,2 , 3,4,43,5,11,113-octahydro-611-indazolo [2,3-ming] isoquinoline, 2-allyl-4 &amp; 〇 (-(3-hydroxyphenyl) -7-fluoro-113 / 9-hydroxy-1,2,3,4,43, 5,11,113-octahydro-61 ^ -indoxo [2,3-2] isoquinoline, 2-cyclopropyl Methyl-43〇 (-(3-hydroxyphenyl) -9-bromo-113 / 9-hydroxy-1,2,3,4,43,5,11, 11a-octahydro-SH-inverted [ 2,3-g] isoquinoline, 2-benzyl-4aot- (3-hydroxyphenyl) -9-bromo-lla / S-hydroxy-1, 2,3,4,4a, 5, 11, 11a -Octahydro-6H-indazolo [2,3-g] isoquinoline, 2- (2-phenethyl) -4ac (-(3-hydroxyphenyl) -9-bromo-lla / 3-hydroxyl -1,2,3,4,4a, 5,11, 11 a-octahydro-6 H-indo [2,3-g] isoquinoline, 2-allyl-4act- (3-hydroxyl Phenyl) -9-bromo-113 /?-Hydroxy- 1,2,3,4,43,5,11,113-octahydro-6} 1-indazolo [2,3-g] isoquino,, 2-cyclopropylmethyl-4act- (3- Hydroxyphenyl) -8-bromo_ 113 / 3-hydroxy-1,2,3,4,4 and 5,11,113-octahydro-611-indazolo [2,3-g] isoquinoline, 2 -Cyclopropylmethyl-4acr- (3-hydroxyphenyl) -1〇-bromo-11 3 / 3-hydroxy-1,2,3,4,43,5,11,113-octahydro-6bu Indole (2,31) isoquinoline, 2-benzyl-4act- (3-hydroxyphenyl) -8-bromo-llayS-hydroxy-1, 2,3,4,43,5,11, 11 &amp; -octahydro-6} 1-indo [2,31] isoquino, 2-benzyl-4aa-(3-hydroxyphenyl) -10-bromo-lla / S-hydroxy-1,2 , 3,4, 4a, 5, ll, lla-octahydro-6H-indeno [2,3-g] isoquine_, 2- (2-styrene paper standard Chinese National Standard (CNS) A4 specifications (210X297 public) 219 (please read the precautions on the back before filling out this page) Outfit-Λ 6 Β6 V. Description of invention ()-Printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs (please read the back of the first Matters needing attention and then fill out this page) radical) -43 «-(3-hydroxyphenyl) -8-bromo-113 &gt; 9-hydroxy-1,2,3,4,43,5,11,113- 八 氲 -6} ^ Indica, (11 ^ 2,31) isoquinoline, 2- (2-phenethyl) -4aa- (3-hydroxyphenyl) -l ^^ la / 3-hydroxy-l, 2,3,4,4a, 5, ll, 11a-octahydro-6H-indoxo [2,3-g] isoquinoline, 2-allyl-4a 〇t- (3-hydroxyphenyl) -8-bromo-11a point-hydroxy-1,2,3,4,4a, 5,11,11a-octahydro-6H-indoxo-2 [3- g] Isoquinoline, 2-allyl-4acx- (3-hydroxyphenyl) -10-bromo-lla / 3-hydroxy-1,2,3,4,4a, 5, 11,11a-octahydrogen -6H-Ind P-bag [2,3-g] isoquinoline, 2-cyclopropylmethyl-4act- (3-hydroxyphenyl) -7-bromo- lla / S-hydroxy-1,2, 3,4,43,5,11,113-octahydro-6? 1-lumbo-deca [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -7-bromo -113 /?-Hydroxy-1,2,3,4,43,5,11,113-octahydro-6? 1-indyl ^ [2,3-g] isoquinoline, 2- (2- Phenethyl) -4aa- (3-hydroxyphenyl) -7-bromo-11 3 /?-Hydroxy-1,2,3,4,43,5,11,11 &amp; -octahydro-61 indoxo [2,3-3] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -7-bromo-lla / 3-hydroxy-1,2,3,4,43,5,11 , 113-octahydro-611-indino [2,31] isoquinoline, 2-cyclopropylmethyl-4aa- (3-hydroxyphenyl) -9-nitro-lla; S-hydroxy-1 , 2,3,4,43,5,11,113-octahydro-61 vermiculo [2,3-ming] isoquinoline, 2-benzyl-43 € (-(3-hydroxyphenyl)- 9-nitro-11 3 / 3-Hydroxy-1,2,3,4,4hexane, 5,11,11 &amp; -octahydro-6} 1-reading [2,3- 豸] isoquinoline, 2- (2- Phenethyl) -43〇 &lt;-( 3-hydroxyphenyl) -9-nitro-113 &gt; 9-hydroxy-1,2,3,4,4 &amp;, 5,11,113-octahydro-6 ^ Indo [2,31] isoquinoline, 2-allyl-4 and "-(3-hydroxyphenyl) -9-nitro-113 / 3-hydroxy-1,2,3,4, 43,5,11, 11a-octahydro-6H-indo [2,3-g] isoquinoline, 2-cyclopropylmethyl-4 act-(3-hydroxyphenyl) -8-nitro -lla / 3 -Hydroxy-1,2,3, 4,4a, 5,11, the paper size is free to use China National Standards (CNS) A 4 specifications (210x297 mm) -220-Employee consumption of the Central Standards Bureau of the Ministry of Economic Affairs Printed by the cooperative A 6 B6 V. Description of the invention ()-11a-octahydro-6H-D? Shun Peng [2,3-g] isoquinoline, 2-jingpropylmethyl-4 act-(3- Hydroxyphenyl) -10-nitro-lla / 3-hydroxy-1,2,3,4,4a, 5, 11,11a-octahydro-6H-indolo [2,3-g] isoquinoline , 2-benzyl-4aa- (3-hydroxyphenyl) -8-nitro-1U / 3-hydroxy-1, 2,3,4,4a, 5, 11, 11a-octahydro-6H-indind Benzo [2,3-g] isoquinoline, 2-benzyl-4aa- (3-hydroxyphenyl) -10-nitro-11a / 9-hydroxy-1,2, 3, 4,4a, 5, 11, 11a-octahydro-US (〔2,3-g〕 iso Porphyrin, 2- (2-phenethyl) -4act- (3-hydroxyphenyl) -8-nitro-lla / 9-hydroxy-l, 2,3,4,4a, 5, ll, 11a-octa Hydrogen-6I ^ g- [2,3-g] isoquinoline, 2- (2-phenethyl) -4act-lla / 3-hydroxy-1,2,3,4,43,5,11, 11 &amp; -octahydro-611-indophthalo-3-g] isoquinoline, 2-allyl-4aa- (3-hydroxyphenyl) -8-nitro-lla / 3-hydroxy-1,2, 3,4,43,5,11,113-octahydro-6} 1-ind [1 £ (2,3-dan) isoquinoline, 2-allyl-4aa-(3-hydroxyphenyl) -10-nitro-lla / 3 -hydroxy-1,2,3,4,43,5,11,113-octahydro-6 ^ indolo [2,3- £] isoquinoline, 2-cyclopropyl Methyl-4aa- (3-hydroxyphenyl) -7-nitro-lla / S-hydroxy-1,2,3,4,43,5,11,11 &amp; -octahydro-6} 1-ind 1 ^ (〔2,3- |] isoquinoline, 2-benzyl-4 &amp; 〇 (-(3-hydroxyphenyl) -7-nitro-11 &amp; / 3-hydroxy-1,2,3,4 , 43,5,11,113-octahydro-6} 1-indino [2,31] isoquinoline, 2- (2-phenethyl)-"〇 (-(3-hydroxyphenyl) -7- Nitro-11 &amp; / 3-hydroxy-1,2,3,4, 4a, 5, ll, lla-octahydro-6H-ind Πβ (2,3-g) isoquinoline, 2-allyl -43〇 (-(3-hydroxyphenyl) -7-nitro-113 / 3-hydroxy-1,2,3,4,43,5, ll, lla-octahydro-6H-indole pouch [ 2,3-g] isoquinoline, 2-ring Propylmethyl-4aa-(3-hydroxyphenyl) -lla / 3-hydroxy-1,2,3,4,4a, 5, ll, lla-A hydrogen-6-methyl-indo [2 , 3-g] isoquinoline, 2-benzyl-4a α-(3-hydroxyben paper standard Chinese National Standard (CNS) A4 specifications (210x297 male dragon) -221-(please read the notes on the back Please fill in this page for details) Binding-Order 'Year: Month A7 B7 V. Description of Invention (phenyl) -1 la / 3 -hydroxy-1,2, 3,4, 4a, 5, 11, 11a / 3- Octahydro-6-methyl-〇? 1 benzo [2,3-g] isoquinoline, 2- (2-phenethyl) -4aa- (3-hydroxyphenyl) -113 / 9-hydroxy- 1,2,3,4,43,5,11,11 Jue; 9-octahydro-6-methyl-indolo [2,3-g] isoquinoline, 2-allyl-4aot- ( 3-hydroxyphenyl) -11 a / 3 -hydroxy-1,2,3,4,4a, 5, 11, 11a / 3 -octa-6-methyl-0¾ 跺 bi [2,3-g] Isoquinoline. Reference Example 12 2- (2,2,2-trichloroethoxycarbonyl) -4a- (3-methoxyphenyl) -6-acetoxy-2,3,4,4a, 5,6,7 , 8-octahydroisoquinoline 57 〇cud sense.

(57) och3 I -------------- ίτ ------ f _ ^ for (please read the precautions on the back before filling out this page) Bei Gong, Central Bureau of Standards, Ministry of Economic Affairs The consumer cooperation du printed under the argon ochre hood will 2-methyl-4a- (3-methoxyphenyl) -6-acetoxy-2,3,4,4a, 5.6,7,8-octa Hydroisoquinoline (19.5g) was dissolved in 1,2-dichloroethane (100ml), and a proton adsorbent (6.6g) was added. Under 2, it was added 2,2,2-trifluoroethylchloroform S purpose (12.8ml), the resulting suspension was warmed to room temperature and stirred for 15 hours. After the solvent was distilled off under reduced pressure, ether (400ml) was added, washed with 1N benzoic acid (150ml X 2), saturated brine (100ml) After drying, it was purified with a silica gel chromatography tube (cyclohexane / ethyl acetate = 10: 14 5 ·· 1) to obtain 21.2 g (72%) of the Sassafras compound (6-position acetyloxy mixture). Partially separated 6-position acetoxy isomer map. This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm). 222 Printed by the Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs A 6 _____B6__ V. Invention Description ()-. Highly polar component (6 α acetoxyl) IR (liquid membrane method) ^-^: 302 4,1717,1415,1255,1216,758 NMR (CDC) 3,400Milz) 31 (3li, d, J = 4.8Hz), 1.57- 1.65 (211, m), 1.75- 1.86 (2H, m), 1 ..98- 2. 06 (1II, m), 2.14-2.23 (111,111) 2.63-2.74 (111, m), 2.77-2.88 (1H, m), 3. 08 (1H, d, J = 15. Lliz ), 3. 80 (311, s), 3.82-3.89 (1II, m), 4.67- 4.85 (211, m), 4, 98 (111, s), 6.70 (1 H, dd, J = 6.3, 2 . OIlz), 6. 80 (1 !!, dd, J = 2.5, 1.91 (z), 6.85 (111, d, J-7.8IIz), 7.01 (111, d, J = 7.8liz), 7.22 (111 , t, J = 7.8112) Mass (El): 475 (M *) High decomposition energy mass spectrum: c2, hZ4o5 ncI32 Calculated value 475.0720 Measured value 475.07 16. Low-polarity component (6 ethoxylate), IR (liquid film method) 0 ^^ 2954,1725,1410,1251,1141,1046,754 NMR (CDCJ 3,400HHz) ί: 1.39-1.53 (2i !, m) , 1.83-2.09 (3Η, m), 2.02 (311, s), 2.25-2.30 (211, m), 2.83-3.07 (211 ^), 3.82 (3H, s), 3.85-3.95 (lH , m), 4. 54-4.61 (111, n〇, 4.70- 4.88 (2H, m), 6.77 (IH.dd, J = 7.8,2.4Hz), 6. 91-6.95 (211, m) , 6.98 (111, d, J = 9.3Hz), 7.27 (1H, t, J = 7.8Hz) Mass (El): 475 (M +) High decomposition energy mass spectrum: C 2i II 2 4 0 s NC 13 Calculated value 475.0720 and measured value 475.0718. Example 46 2- (2,2, 2-trichloroethoxycarbonyl) -4a / S-(3-methylphenyl) -6-ethyl (please read the notes on the back first (Fill in this page again) 装 · This paper scale is universal Chinese National Standard (CNS) A 4 specifications (210x297 public splashes) 223

SulC Λ 6 B6 5. Description of the invention ()-. Acetyl-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline 58 η

(58) (Please read the precautions on the back before filling this page) Printed under the envelope of argon by the Consumer Labor Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. 2- (2,2,2-Trichloroethoxycarbonyl)- 4a- (3-methoxyphenyl) -6-acetoxy-1,2,3,4,4a, 5,6,7,8, -octahydroisoquinoline (16.5 g) dissolved in di Gas methane (200ml), cooled to 0 ° C. Add π-nitrobenzoic acid U, 6g) and react for 1.5 hours. The solvent was distilled off, and the obtained solid was used for the next reaction. Dissolve the above crude product in acetic acid (150ml) and add a little boron hydride when cooling to 0 ° C. Warm to room temperature and react for 15 minutes. Acetic acid was removed under reduced pressure, saturated aqueous sodium hydrogensulfonate solution (300 ral) was added, and extracted with ethyl acetate (200 ml X 3). After drying with sodium sulfate, the solvent was distilled off and purified with a silica gel chromatography tube (gas imitation) to obtain 10.8 g (63¾) of the title compound (6-position acetyloxy mixture). Determine the spectrum of partially separated low-polarity components. IR (liquid film method) 011- ^: 3462,2958,1715,1605,1582,1437,1249, 1033,758 NMR (CDC13,90MHz) &lt; 5: 1.55-1.65 (2H, m), 1. 65-1.85 (2H, m), 1.92 (311, s), 1.97-2.18 (2H, m), 2.20-2.57 (311, m), 3.50 (1H, t, J = 7.8Hz), 3.79 (3H, s), 3.80-3 .95 (211, m), 4.78 (2H, d, J = 6.5 llz), this paper standard is used in the middle of sleep a family standard (CNS) A 4 specifications (210x297 cm) -224-V. Description of the invention (A 6 B6 5.10-5.30 (1 丨 丨, m), 6.68- 6.84 (2li, m), 6.92-7_25 (2Η, π〇 Mass (1Π): 493 (Μ + ). Example 4 7 2 -Methyl-4aa-(3-methylchlorophenyl) _6,8a / S-dibenzyl-1,2,3,4,4a, 5,6,7,8,8a -Decahydroisoquinoline 59 ch3.n

(59) (Please read the precautions on the back before filling in this page) Installed · Printed by the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs under the argon atmosphere to cover 2- (2,2,2-trichloroethoxycarbonyl) -4a a-(3-methylphenyl) -6-acetoxy-8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8, 8a-decahydroisoquine咻 (1.5g) was dissolved in anhydrous THF (20ml), lithium aluminum hydride (0.35g) was added. After reacting at room temperature for 30 minutes, it was cooled to 0 ° C. Saturated aqueous solution of Rochelle salt (potassium sodium tartrate) was slowly dropped. Once it became a solid, chloroform (20ra 1) was added and stirred well, then filtered through Ce 1 i t e (diatomaceous earth for filtration). Wash thoroughly with nitrogen simulant, collect the liquid, concentrate it under reduced pressure, and then purify it with a silica gel chromatography tube (gas simulative 4 ammonia saturated gas Θ 5% methanol / gas saturated nitrogen simulant) to obtain the title compound Q. 63g (71%, 6-hydroxyl mixture). IR (KBr) απ '1:34 1 2, 1 599, 1 493,1 236.107 1,893,795,723,540 Mass (El): 291 0 "). Order · Line · This paper scale uses the Chinese a standard (CNS) A4 specifications (210x297 public ¢) 225 3ulCo4 A 6 B6 5. Description of the invention ()-Example 48 2-methyl-4aa-(3-methoxyphenyl) -6-oxo-8a / Q-hydroxy-1,2 , 3,4,4a, 5, 6, 7,8,8a -decahydroisocyanate 60

(Please read the precautions on the back before filling out this page) Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs under the argon atmosphere to dissolve the oxalate (0.19ml) in anhydrous digas methane (12ml) and cool to -55 ° C. After dissolving DMSO in methane (1.5 ml), it was slowly dropped into it, and it was stored and stirred at the aforementioned temperature for 2 minutes. Then 2-methyl-4 aa-(3-methoxyphenyl) -6,8a / 3 -dihydroxy-1,2,3,4,4a, 5,6,7,8, 8a- + hydrogen Isoquinoline (0.5g) was dissolved in diazomethane (2inl) and dropped into it, and the washing solution (dichloromethane, 2ml) was added. After stirring at -55 ° C for 30 minutes, triethylamine (1.2Π1) was added and the temperature was raised to room temperature. Distilled water (20nl) was added for liquid separation, and the aqueous layer was further extracted with dichloromethane (12B1X2). The collected organic layer was washed with saturated brine (10 ml), dried and concentrated, and then purified with a silica gel chromatography tube ((chloroform 42% methanol / chloroform 45% methanol / airform) to obtain the title compound. .45g (91%). Recrystallized from n_hexane / ethyl acetate to obtain pure product 0.38g (77%, ΠΡ96 ~ 97 ° C). IR (KBr) cm * 1: 3400,294 ^, 1711,1G05,1578,1452, 1257, 1 1 14, 1038.895,774,708 'Binding-Binding-Line &lt; This paper scale uses the Chinese National Standard (CNS) f 4 specifications (210X297 mm) 226 A 6 B6 Description of the invention ()-NMR (CDC13, / 100MH2): 1.85-1.93 (211, m), 2.15-2.32 (311,01), 2.33 (311, s), 2.55 (2H, t, J = 11.01lz), 2.62-2.66 (111 ^), 2.77 (HI, d, J = ll.〇IIz), 2.79-2.86 (211, m), 3.13 (1II, d, J = 14.6liz). 3.78 (311, s), 6.72 (111, dd, J = 7. 4, 3. Ollz), 6.96-6.97 (211, M), 7.21 (111, L, J = 8. 5llz) Mass (El): 289 (M +) 0 Example 4 9 4aa-(3-methoxyphenyl) -6-acetoxy-8a /?-Hydroxy-1,2,3, 4,4a, 5,6,7,8,8a -decahydroisoquine Porphyrin 61

OH

(Please read the precautions on the back before filling out this page) Pack. Order '-Line · Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs under the argon atmosphere ) -4aa-(3-methylphenyl) -6-acetaldehydeoxy-8a yS-hydroxy-1,2,3,4,4a, 5,6,7,8, 8a-decahydroisoquinoline (2. Q4g) was dissolved in acetic acid (5Qml), and zinc powder (2.7 Og) was added. After stirring the suspension at room temperature for 4 hours, it was filtered through Ce lit e to remove insoluble materials derived from zinc. Wash thoroughly with acetic acid, combine the liquid, and distill off the acetic acid under reduced pressure. Add saturated aqueous sodium hydrogenate solution (50π1), extract with chloroform (50ΙΠ1Χ3), and then purify with a silica gel chromatography tube (aminoform-5% methanol / saturated chloroform of ammonia) to obtain Q.95 g Ο 2%) of the title compound (6-bit B-IS oxygen mixture). This paper standard uses the Chinese Standard (CNS) A4 specifications (210X297) 227 3〇1C〇4 A 6 B6 V. Description of the invention (IR (liquid makeup method) 01 ^: 3360, 2936, 1712, 1607 , 1582,1455,1248,1 053,888,713 Mass (El): 31901+). Example 50 2-cyclopropylcarbonyl-4a α-(3-methylphenyl) -6-acetoxy-8a cold-hydroxy-1,2,3,4,4a, 5,6,7, 8,8a-decahydroisoquinoline 62 η

(62) (Please read the precautions on the back before filling out this page) Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs under the argon atmosphere. 8 3 Lu-hydroxy-1,2,3,4,43,5,6,7,8,83-decahydroisoquinoline (0.68 tea) was dissolved in anhydrous 1,2-difluoroethane (15ml), Proton adsorbent (0.46g) and cyclopropane carbonyl chloride (0.29ml) were added. The solvent was distilled off under reduced pressure, ether (20 ml) was added, and washed with 1N hydrochloric acid (20 ml) and saturated saline (1 Gml). The oily title compound obtained after drying and concentration was directly used in the next reaction (crude yield 91%). IR (liquid film method) (^-^ 3430,2944,1702,1605,1582,1453,1240,10 29,750Hass (EI): 387 (ίΓ). Similarly, if the cyclopropane carbonyl chloride is replaced by benzoyl Chlorine, phenylacetamide, and this paper are used in China National Standard (CNS) A4 specifications (210x297 male dragons). 228-A6 _____B6_ printed by the Employees ’Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. 5. Description of invention ()-Acrylonitrile ， 刖 respectively get 2-phenyl acetyl-4a ct-(3-methylphenyl) -6-acetoxy-8a / 3 -hydroxy-1,2,3, 4, 4a, 5,6,7 , 8,8a-decahydroisoquinoline, 2-phenylethylacetoyl-4aa- (3-methoxyphenyl) -6-acetoyl-8a / 3-hydroxy-1,2,3,4, 4a, 5, S, 7,8,8a-decahydroisoquinoline, 2-propenal-4act- (3-methoxyphenyl) -6-acetaldehydeamino-8a / 3-hydroxy-1 , 2,3,4,4a, 5, 6, 7,8,8a-decahydroisoquinoline. Example 5 1 2-cyclopropylmethyl-4aa- (3-methoxyphenyl) -6, 8a / S-dihydroxy-1, 2,3,4,4a, 5,6,7,8,8a-decaisoquinoline 630H_ (please read the precautions on the back before filling this page)

The 2-cyclopropyl-branyl-4a α- (3-methoxyphenyl) -6-acetoxy-83-hydroxy-1,2,3 obtained in Example 50 was taken under N. , 4,43,5,6,7,8,8a-decahydroisoquinoline was dissolved in anhydrous THF (20 ml), and lithium aluminum hydride (0.24 g) was added at 0 ° C. After reacting at 01 for 2 hours and at room temperature for 1 hour, an aqueous solution (5 ml) of Rochelle salt (sodium potassium tartrate) was slowly added. Add aeroform (50®1), filter through Celite, and wash with chloroform. The oily title compound obtained by concentration was directly fed into the next reaction (crude yield 85%). IR (Liquid Film Method) 011- ^ 3 / 125,2940,1607,1 582,144 / 1,1292,1091,88 0,753 Mass (El): 331 (M *). The size of this paper uses the Chinese National Standard (CNS) A4 specifications (210X297 mm). 229 V. Description of the invention () A 6 B6 The same, the 2-cyclopropylcarboxy-4aa- (3-methoxybenzene Group) -6-acetoxy-8a-hydroxy-l, 2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline substituted by 2-phenylacyl- 4aa -(3-methoxyphenyl) -6-acetoxy-8a / 3-hydroxy-1,2,3,4,4 &amp;, 5,6,7,8,83-decahydroisoquinine, 2-phenylethyl_yl_ "〇 [-(3-methoxyphenyl) -6-acetoxy-83 &gt; 3-hydroxy-1,2,3,4,43,5,6,7,8 , 83-decahydroisoquinoline., 2-propenyl-4310 (-(3-methylphenyl) -6-ethynyl-8a / 3-hydroxy-1,2,3, 4,4a , 5,6,7,8,8a-decahydroisoquinoline, then 2-benzyl-4acx-(3-methylphenyl) -6,8a / 3 -dihydroxy-1,2, 3,4, 4a, 5, 6, 7, 8, 8a -Deca-isoisocyanate, 2-phenethyl-43 £ ^-(3-methoxyphenyl) -6,83 / 3-dihydroxy- 1,2,3,4,43,5,6,7, 8,83-decahydroisoquinoline, 2-allyl-48〇 (-(3-methoxyphenyl) -6,83 / 3 -Dihydroxy-1, 2,3,4,4a, 5, 6, 7,8,8a-decahydroisoquinoline. Ben Example 5 2 2-cyclopropylmethyl-4a α- (3-methyl Oxyphenyl) -6-gaso-8a-hydroxy-l, 2,3,4i, 4a, 5,6,7,8,8a -Decahydrogenate 64 (please read the precautions on the back before filling in this page) Binding-Order-Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

Under the argon atmosphere, dissolve the grassy gas (0.15π1) in anhydrous two-gas A paper standard Universal Chinese National Standard (CNS) A 4 specifications (210X297 mm) 230 • ί Α6 136 V. Description of the invention (Ministry of Economic Affairs Printed alkane (10ml) by the Consumer Cooperative of the Central Bureau of Standards and cooled to -55¾. After dissolving DMS0 (0.24nl) in anhydrous dichloromethane (lnl), it was slowly dropped and reacted at -55 ° C for 2 minutes. 2-cyclopropylmethyl-4act- (3-methoxyphenyl) -6,8a> 9-dihydroxy-1, 2, 3, 4, 4a, 5, 6, 7, 8, obtained in Example 51 8a-Decahydroisoquinoline was dissolved in anhydrous dichloromethane (2ml) and added to it, and the washing solution (2ml) was added at the same time. After reacting at -55 ° C for 30 minutes, triethylamine (1.09ml) was added and the temperature was raised to Room temperature. After adding distilled water (15ml) to separate the liquid, the aqueous layer was further extracted with dichloromethane (10π1). The organic layer was washed with saturated brine (lGml), dried, concentrated and chromatographed on silica gel Tube (chloroform-2% methanol / chloroform) was purified to obtain the title compound 〇.48g (68% in 3 stages). IR (liquid film method) 011- ^ 3404, 2940, 171 1,1605, 1582, 1493, 1429, 12 41,1038,897,756NMR CCDCl 3, 400MII7.) Δ: 0.11 (2H, d, J = 5.9Ilz), 0.50-0.55 (2H, m), 0.81-0.89 (111, m), 1.86- 1.90 (211, m) , 2.25-2.28 (211, m), 2.32- 2.37 (3il, m), 2.39-2.46 (111, m) .2.53 (111, d, J = 14.3Hz), 2.75-2.87 (4H, m), 3 . 14 (111, d, J = 14.3llz), 3.77 (311, s), 6.70-6. 72 (lH, m), 6. 97- 6. 98 (211, m), 7.20 (111, t, J = 8.811 Mass (EI): 329 (il +) High decomposition energy mass spectrometry: C2lH27〇3 N 渕 値 329.1991 measured value 329.1955. Similarly, the 2-cyclopropylmethyl-4aa-(3-methoxyphenyl ) -6,8 a / 9 -dihydroxy-1,2,3,4,4a, 5, 6,7, 8,8a-decahydroisoquinoline substituted with 2-benzyl-43〇 (-( 3-Methoxyphenyl) -6,83; 9-bis-benzyl-1,2,3,4,4 &amp;, (please read the precautions on the back before filling out this page) National Standard (CNS) A 4 specifications (210x297 g; ¢) 231 3uie〇4 A 6 B6 Printed by the Consumer Standardization Bureau of the Ministry of Economic Affairs of the Central Standard Bureau V. Invention Instructions ()-5, 6, 7, 8, 8a-decahydro Isoquinoline, 2-phenethyl-4aa-(3-methylphenyl) -6,8a Lu-dihydroxy-1,2, 3, 4, 4 a, 5, 6,7,8,8a- Decahydroisoquinoline 2-allyl-4aa-(3-methylphenyl) -6,8a / 3-dihydroxy-1,2,3,4, 4a, 5,6,7,8,8a-decahydroisoquine Phenanthroline, then 2-benzyl-4a a-(3-methoxyphenyl) -6-oxo-8a / S-hydroxy-1, 2, 3,4, 4a, 5, 6, 7,8 , 8a-decahydroisoquinoline. 2-phenethyl-4a a-(3-methoxyphenyl) -6-oxo-8a / 3 -hydroxy-1,2,3,4,43,5,6,7,8,83-dec Isoquinol, 2-isopropyl-43〇 [-(3-methylphenyl) -6-oxo-to / 3-hydroxy-1,2,3,4,43,5,6,7 , 8, 8a-decahydrogenous sleep. Reference Example 1 3 2- (2,2,2-trichloroethoxycarboxy) -4a «-(3-methylphenyl) -2,3,4,4a, 5,6, 7,8-decahydro Isialia 65〇ci3c octa (65) och3 under argon atmosphere, 2-methyl-4act-(3-methylphenyl) -2,3,4, 4a, 5, 6,7,8- Octahydroisoquinoline (1.4 U) was dissolved in 1,2-diazoethane (15 ml), and proton adsorbent (0.59 g) was added to it. 2,2,2-Trichloroethyl chloroformate (1.13 ml) was added dropwise at 0 ° C, and the resulting suspension was warmed to room temperature and stirred for 24 hours. After the solvent was distilled off under reduced pressure, ether (15ral) was added, and washed with 1N hydrochloric acid (10ml, 6ml × 2) and saturated brine (10ml). After drying

The size of this paper is based on China Sleepy Standard (CNS) A4 (210X297 male dragon) (please read the precautions on the back before filling out this page). Binding-Order _ B6 5. Description of the invention (using silica gel chromatography tube ( Cyclohexane / ethyl ester acid compound 2. 30g (100%) .: 1) Refined and obtained the title IR (liquid desorption method) ⑽-1 .. 2936, 1763 , 17 17, 1667, 1607,1582, 1412, 11 25,1054,820,706 NMR (CI) C 1 3, 4 00HHz) (&gt;: I. L 5-1. 25 (III, m), 1. 2G -1.27 (1II, m), 1.40- 1.49 (111, m), 1.52 -1.60 (lH, m), 1.66-1.72 (1Η, m), 1.80 -1.93 (2H, m), 2.15-2.21 ( 2H, m), 2.56C1H, d, J = 13.4Hz), 2.90 -3.01 (lH, m), 3.80 (31l, s), 3.83-3.90 (lH, m), 4.79-4.88 (2H) rn)) 6.75 (lH, dd> J = 7.9,2.5Hz), 6.87 (1 H, s), 6.92 (2H, d, J = 8.5Hz), 7.26 (111, t, J = 7.9Hz) Mass (El): 417 (M +). Similarly, replace 2-methyl-4a a-(3-methoxyphenyl) -2,3,4, 4a, 5, 6,7,8, -octahydroisoquinoline with 2-methyl -4aa- (3-methoxyphenyl) -2, 3,4,43,5,6,7,8-octahydro-2,2-dimethyl-1,3-dioxolane [4,5 -And] isoquinoline, to give 2- (2,2,2-trichloroethoxycarbonyl) -4aa-(3-methoxyphenyl) -2,3,4,4 and 5,6,7, 8-octahydro-2,2-dimethyl-1,3-dioxamol [4,5-g] isoquinoline. Example 5 3 2- (2,2,2-trichloroethoxycarbonyl) -43 «-(3-methoxyphenyl) -83 / 3-hydroxy-1,2,3,4,4a, 5, 6,7,8,8a-decahydroisoquinoline 66

(66) (Please read the precautions on the back before filling this page) This paper uses the Chinese National Standard (CNS) A4 specifications (210 father 297 male) oQU〇4 Λ6 _ B6 V. Description of invention ()- Printed by the Employee Consumer Cooperative of the Central Bureau of Standards under the Ministry of Economic Affairs ; 5,6,7,8-octahydroisoquinoline (0.94g) was dissolved in difluoromethane (20ml) and cooled to 0 ° C. Π-Amino perbenzoic acid (0.55 g) was added and reacted for 15 reactions. The solvent was distilled off, and the obtained solid matter was directly supplied to the next reaction. The above crude product was dissolved in acetic acid (20nl) and cooled to it, and a little sodium borohydride was added. Warm to room temperature and react for 5 minutes. The acetic acid was distilled off under reduced pressure, a saturated aqueous solution of sodium bicarbonate (20ml) was added, extracted with ethyl acetate (20ml X2), and the collected organic layer was washed with saturated brine (15ml). After drying over sodium sulfate, the solvent was distilled off and purified with a silica gel chromatography tube (chloroform) to obtain 0.73 g (74%) of the title compound. iR (liquid desorption method) αη-ι: 3460, 2934, 1705, 1607, 1582, ΜΊ 4, 1245, 1127, 994, 882, 758 NMR (CDC1 a, 4 00MHz) ί: 0.90-1.01 (1II, m), 1.33- 1. 40 (1II, m), 1.52- 1.60 (211, m), 1.67-1.76 (211, m), 1. 80 -1. 90 (1 il, m), 2.05-2. 12 (lH , m), 2.20-2.40 (211, m), 2.48-2.63 (III, m), 3.81 (311, m), 3.86-4.00 (311, m), 4.73 (211, s), 6. 73 (1II , dd, J = 8.6, 2.5IU), 7.03 (1 II, s), 7.06 (111, d, J = 7.9IIz), 7.24 (1 II, t, J = 7.9n2) Mass (El>: 435 ( M ”. Similarly, the 2- (2,2,2-trichloroethoxycarbonyl) -4a- (3-methoxyphenyl) -2, 3, 4, 4a, 5, 6, 7, 8- Substitute octahydroisoquinoline with 2-(2,2,2-tri (Please read the precautions on the back before filling out this page) This paper standard is common in S National Standard (CNS) 4 specifications (210x297 public splash) A 6 B6 5. Description of the invention ()-Gas ethoxycarbonyl) -4 a- (3-methoxyphenyl) -2,3, 4, 4 a, 5,6, 7,8-octahydro-2, 2-Dimethyl-1,3-dioxolo [4,5-g] isoquinoline to give 2- (2,2,2-trifluoroethoxycarbonyl) -43 «-(3-methoxybenzene Radical) -8 &amp; / 6-hydroxy-1,2,3,4, 4 &amp;, 5,6,7, &amp; 3-decahydro-2,2-dimethyl -1,3-dioxamol [4,5-Ju] isoquinoline. Example 54, 4 &amp; «-(3-methylphenyl) -8 &amp; / 5-hydroxy-1,2,3,4 , 43,5,6,7, 8,8a-decahydroisorefrin 67

(67) (Please read the precautions on the back before filling in this page) Pack. 〇CH, Line-Printed by the Beigong Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs will be 2- (2,2,2-trichloroethoxycarbonyl) -43 «-(3-methylchlorophenyl) -8 a / S-hydroxy-1,2,3,4,43,5,6,7,8,83-decahydroisoquinoline (33〇1 ^ ) Dissolved in 90% acetic acid aqueous solution (12ml), added zinc (0.37g) at room temperature for 3 hours, 50 ° C for 15 minutes. The acetic acid was distilled off under reduced pressure, saturated aqueous sodium hydrogenate solution (15ml) and gaseous imitation (15ml) were added, and the mixture was filtered through Celite dioxomane. The filtrate was separated and further extracted with chloroform (10D11X2). The concentrated organic layer was washed with saturated saline (15ml), then dried and concentrated. It was purified with a silica gel chromatography tube (chloroform 45% methanol / gas stream) to obtain the title compound 164mg (83%). This paper scale is printed in China National Standards (CNS) Grade 4 (210X297 Gonglong) A6 __B6__ ^ Invention Description () _ IR (Liquid Film Method) 011- ^ 3358,2938 1607,1582,1452,1249,1054,88 6,712 NMR (CDC 1 3,400MIIz) 6: 0.87-0.98 (111, m), 1.31-1.37 (lll, m), 1.48-1.55 (2H, m), 1.63- 1.71 (211, m), 1.80- 1.92 (1H, m), 2.10 -2.19 (211, m), 2.27 (111, dt, J = 13.4,5.5tlz), 2.35 (1H, dt, J = 12.8,1.8 l! z), 2.54 (lll, d, J = 11.0llz), 2.64 (lH, d, J = 11.6llz), 3.59 (lll, d, J = 11. Oil z), 3.81 (311, s), 6.69 (1II, dd, J = 7.9, 2.4II z) 7. 06-7.09 (211, m), 7.21 (111, t, J = 7.9llz) Mass (El): 261 (M +). Similarly, the 2- (2,2,2-trichloroethoxycarbonyl) -43 «-(3-methoxyphenyl) -8a / S-hydroxy-1,2,3,4,43,5, 6,7,8,83-decahydroisoquinoline replaced by 2- (2,2,2-triazaethoxycarbonyl) -4aa-(3-methylphenyl) -8a / 3-hydroxy-1 , 2, 3,4,4a, 5,6,7,8, 8a-decahydro-2,2-dimethyl-1,3-dioxamol [4,5-g] isoquinoline, giving 4aa -(3-methoxyphenyl) -8a / 3-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydro-2,2-dimethyl-1,3 -Dioxo [4,5-g] isoquinoline. Example 55 2-cyclopropylcarbonyl-4aa-(3-methoxyphenyl) -8a / 8-hydroxy-1,2,3, 4,43,5,6,7,8,88-decahydroiso Quinoline 68 (Please read the precautions on the back before writing this page) Install & Order _

0H

(68) The standard of this paper is the Chinese Standard B (CNS) Grade 4 (210x297); ":" 236 V. Description of the invention (η Printed by 4P-(3- Methylphenyl) -8a / 3-hydroxy-1,2,3,4,4a, 5,6,7-, 8,8a-decahydroisoquinoline (16 4ng) dissolved in anhydrous 1,2-bis Ethylene ethane (5b1), add proton adsorbent (134ng). Further add cyclopropylcarbonyl chloride (0.14 nl) to react at room temperature for 3G minutes. Distill off the solvent, add ether (15ml), add 1N hydrochloric acid (10inlX2) 1. Wash with saturated brine (lOral). After drying, distill off the solvent and azeotrope the resulting crude product with chloroform-toluene for the next reaction (crude yield 0.20g, 97%). IR (liquid film Method) cm_ ': 3426, 2940, 1700, 1605, 1456, 1245, 1031, 886, 756. Mass (EI): 329 (M +). The same, the 43 «-(3-methoxyphenyl) -83/5 -Hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline substituted with-4aa- (3-methoxyphenyl) -8a / 3-hydroxy-1 , 2,3,4,4a, 5,6,7,8,8a-decahydro-2,2-dimethyl-1,3-dioxamol [4,51] isoquinoline, to give 2-ring Propylcarbonyl-4 &amp; 〇 [-(3-methoxyphenyl) -8a / 3-hydroxy-1,2,3, 4, 4a, 5,6,7, 8,8 a-decahydro-2,2-dimethyl-1,3-dioxa S [4,5-g] isoquinoline. Example 5 6 2- Cyclopropylmethyl-43 «-(3-methoxyphenyl) -83々-hydroxy-1,2,3,4,4a, 5,6,7,8,8a-decahydroisoquinoline 69

〇CH3. This paper scale uses the Chinese National Standard (CNS) A4 specifications (210x297 public) (please read the precautions on the back before filling this page) (69)

A7 B7 Printed by the Beigong Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs. 2-Chenpropylcarbonyl-4a a-(3-methoxyphenyl) -83> 8-hydroxy-1,2,3,4 obtained in Example 55 , 43,5,6,7,8,83-Crude crude decahydroisoquinoline (0.19g) was dissolved in anhydrous THF (5ml). After cooling to 01, lithium aluminum hydride was added and reacted at 0TC for 15 minutes at room temperature React for 1 hour. Slowly drop a saturated aqueous solution of Roche lie salt (sodium potassium tartrate) (0.5 ml) to make it nationalized, suspend in chloroform, and filter it through Celite. Distill off the solvent, M silica gel chromatography tube (chloroform 4 ammonia saturation and chloroform &gt; Purification to obtain Sassafras title compound 0.14g (77%). IR (liquid desorption method) 011- ^ 3 / 126,2938,1607,1582,1 / 156,1290.1093. 1052,1031,884,756 NHIMCDC1 n, 400MHz) δ ： 0. 0 2-0. 0 8 (2II, m), 〇. 4 2-ϋ. 51 (2! L. M), 0.75- 0.83 (lll) ni) l0.83-0.9G (lll, fn ) &gt; 1.30-1.38 (lll, m) &gt; 1. ^ 18-1.58 (2 II, m), 1.58-1.92 (5 II, m) .2.10-2.32 (4II, m), 2.60-2.08 (211 , m), 2.97 (lll, dJ = 10.8llz), 3.81 (3ll, s), 6.69 (lll, dd, J = 8.3II z, 1.911 z), 7.0 4-7.08 (211. m), 7.20 ( 111, t, J = 8.3llz) Mass (IH): 315 (M '). The same, the 2-oxopropylcarbonyl_4aa- (3-methoxyphenyl) -8 &amp; / 3-hydroxy-l, 2,3,4,4a, 5,6,7,8,8a-dec Hydroisoquinoline is replaced by 2-oxopropylcarbonyl-4aa-(3-methoxyphenyl) -8a / 3 -hydroxy-1,2,3,4,4a, 5,6, 7,8,8a -Decahydro-2,2-dimethyl-1,3-diB oxalene [4,5-g] isoquinoline to give 2-cyclopropylmethyl-4act-(3-methoxyphenyl) -8a / 9 -Hydroxy-1,2,3, 4, 4a, 5,6,7,8,8a-Decahydro-2,2-dimethyl-1,3-dioxolane [4, 5- g) This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) (please read the $ item on the back before filling in this page),-= * 238 8β, 2 ^ ύΐί〇4 Μ Β7 Central Ministry of Economic Affairs Printed by the Bureau of Standards and Staff ’s Consumer Cooperative V. Description of the invention (isoquinoline. Example 57 The pharmacological effects of the compounds of the examples are as follows. Combined with the experimental system, Kemeicheng prot / tube (protein / tube · ie each test tube The protein amount of the guinea pig brain is 0.7ug protein mass, diluted with tris buffer solution, and added to the reaction solution. It is used in combination with «, 3H-DAG0U) ([D-Alaa, N- Me-Phe4, Gly-ole] -enkephalin), DPDPE (d) ([D-Pena, D-Pe ne] enkephalin; Pen is Penicillamine · Yu Huisu; enkephalin is enkephalin), EKCU) (Ethylfcetocy-plazocine, ethyl ketone cilazoxine), Naloxone (w) (allyl hydroxymorphine heir, I.e. a morphine antagonist), DADLE (S) ([D-Pene β] -enkephalin), Naloxone (k) ° In addition, the agonist and antagonist activity of the compound of the present invention is the ileum of the guinea pig (ilun) ( GPI), rat wheel seminiferous tubule (MVD), and implemented according to the method of Takenori et al. (Takemori, AE et al. Eur. J. Pharmacol 1982, 85, 163). Table _1 shows the pharmacological activities of the main compounds. These compounds are highly selective antagonists to the delta-receptor of Opioid. Especially 2-cyclopropylmethyl-4aa- (3-metoxyphenyl) -1,2,3, 4,4a, 5,11, lla / 3-octahydro-611-11¾¾ [2,3 -g] The selectivity of isoquinoline is twice that of the currently most selective Naltrindole (NTI) for δ-receptors (《/ δ; 100 = NTI, 205 = (Ki value of the compound = 3.50). It also has no effect on the suppression of the male regain of the guinea pig's back waist. The Kei is 4.8 for DPDPE (a kind of delta-sperm tube delta-receptive and highly selective victory), which can be selectively hindered by DPDPE The resulting shrinkage inhibition. This fact shows that the compound represented by compound 12_ can be said to be a kind of antagonist with high selectivity for tolerance. This paper scale is applicable to the Chinese National Standard (CNS) Λ4 Specifications (210X 297 mm) 239 -------- f. Packing ------ ordered --------- ^ ^ (please read the precautions on the back before filling this page) 3G2C54

66 AB V. Description of invention () ls ° 2.: 7 {: 300--30} (1 .---: 5) {S-T3S5) 1-00 (13so-luoo) Bei Gong, Central Bureau of Standards, Ministry of Economic Affairs Printed by consumer cooperatives j 0 · 00 F · &lt; 1. 72) -.77 (0. 61-0) • s —Ό &lt; Λ 〇Ο Ο —s · 〆. Ο 1 ο ο ο ο 1 i 1 1 1 1 1 1 ο «ο Ο CM 1 — C.1 Ο —4 Ο 〇 · ο ο ο ο» ο * ► · ι · ο IV »Η 1 ο *» * 1 :: G j 1- (3S0 -19S) one (-.7209) -0 (Η- '· ° · η) 357GO (33000 --- 02 Oi {·' ·· '0. N) 0-0 (---- 50 two · i -13 (： i 135 l〇4 · &gt; t- »〇ο ο · 〆- • ο * 〆Ο • 1 1 1 • t 1 1 1 1 1 1 U3 ο ο eight 1 t-» —Ο ο rs * ο ο ι · »— —Λ rj &lt; 〇m— ι · • —:

:: &quot;CD; -0 1 · &quot; · = -110--0)-=. = ----) -so &lt;1.4K; 23i (500-25700) P50 (ο. ° ·· '! .ο?) j (0 ei-i · 33) • i '° This paper scale is used in China National Standard (CNS) A 4 specifications (210x297 mm) lo' κ- • ': so &amp; * 3-0 &lt;-: co ••• no • '27 • '27 sso &lt; ilOO (T--ii) •-'ο j i2 ° —ir °-!: 20c) Iu-uso}: r-'00 &lt; MSC0 &lt; ••-•• -s &lt; -.- 1-3-: ioi (mo--s) '25 &lt; {1. Sl &lt; i 2SOOG j (20000i) ° .s: s · SI. 07) j 0 .-S {0 · &lt; li.03) 1. 23 il.oi-! .-— • u * • · 〇Ο 〇Ο 〇 »η Hi ο ο h ΓΓ 〇! &Gt; I ^ ο ο ο ο . &lt; u σ 'υ ·-1 〇 · &lt; &gt; «Ο D Ο • c · / · &lt; σ *»: r »〇 ·,. 〇, T: \ o,,, o. N \ V; m &lt; = &gt; ο-&gt; 士 二 f J »〇V * &amp; I 23] S aS 德 —J 1.» Cm. 1 〇 &gt; 八 〇W ο »· — 1 · 〇tm Ο-~ Λ Ο * 1 \ ΛΛ · — · 4 / 'Ο A t · &gt; Ο W Ο *-»ίτ LI V * ο» ο &lt; _ &gt; ο * -ι &lt; y »Λ. Ο Ο »CD A. Ο Ο Ο ον Ο ΙΙ β ο · — ο ο ο η» t * * λ · »9 * S ο ο * TJ Λ. Ο ι ·· — &gt; 〇 • ot — »ur &gt; Ο 1 (Γ · vs t« * = &gt; ο 1 03 ν Please read the precautions on the back before filling this page) 240 V. Description of invention () 5 6

66AB Printed by Employee Consumer Cooperative of Central Bureau of Standards, Ministry of Economic Affairs

! (MC:;: S〇, 1. Π (1. 15-2. U) ι US0 1 (96 &lt;-! 970) OI: I :, l〇f: 1- 1 :: 1C 200 »(20η . \ 〇1 &lt;. · j Μ7Ι0 i (5〇n.Vi22. Ί 1 !!. 3 •. J (20n.y) ;. ¢: | (SOnX) U. S 1 (20n.yje. 22 j (S0nM) 3i.1 i. 33 (20n.V) i. U (i0n.M) 30. ir ·: .21 丨 ZO ·? ί 1 ii? 0! lS? j 丨 {ii? -Z £ S〇} j ·. 9C | 2.00 j! C50 j l. 2 \ J 93 »j 1 $ S US | S.Si 丨 〇i20MS00 &gt;! U.S2-ii.i) j (110-1100) i- Q -.33 i. 5! 3.2; 1 Κ30 ί. Μ 1 (: 5ϊ-53300) 5. 30 ι (21100;! 1 2C | iS: 0! (Ί〇30-Π5ΰϊ 1; .SS 127000; i . &lt; 1 ι: H0 1.12, ⑴ 9-1 600) η j U2 ι ίζο +0. il j (359-19 ^ 0) j! 2ί (97. 0-173) 0. 3? (C. ： 0-0.: 1) 6. (3.32-2 !. SJ: .Si (Γ. 07-i. 3 :) 1 · 4〇2230 j 501 (7JS-23200) j 3 "j 3U0 (2S2-517 ) | 3; 2 (UO-1UO) | ⑴0; j (S35-9170) | no (15 卜! Oso) 9090 &lt; II &lt; »· &gt; Γ · O« ✓ * o Π3 ι 0.5 / ι 11700 I 1 ¢ 2070-16900) * 1 ι X 八 ο 0. 03: 0.33 1 άϋΟΟ 1 L 06 i i. 2?! | (2 6500-15 5000) 1 (0. 67-1. 77) j (0. £ 5-Z. Π) o 0. 09 ο SH \} ί. 30 (⑴0-302 1) 1 (0.5S-: 7 :)} $ &lt; 00 (13500-20000) I 1C500 1 (t200- \ 2S00) 1 moo ίίϊΙΟΟ- ^ όΟΟ) io &lt; 0 (S0S0- &amp; SS0) 1,06 (0. 53- !. 29) |:. \: (1.00-i. 20 i. IS (0.10-1. 3¾) 0. S3 0 .9 & (0. ίZO-l. 20) (C. nL. 25) 〇 &gt; 1: 30 (I. 95-5. U) 1.03 (0. 85-i. 2δ) 1: .35! (1. -7- :. 57) O 1 · «-&gt; * r» • o * 1 · »2. 06 (1.: 5-3. 23) 1.? 0 i β. 06 1 i — ——! 9. 0 i?. 72 ί |! — Lfi. S 1 ϊ. 72 compound | i: &lt; σ 3 • C 〇 • r Cf 〇ΓΟ 1 ·: 〇V »-ο Μ-3 〇. XiiS (nM) · The five-in-one experiment with the name of Yung Yung: \ Q, ·, \ 〇, Λ \ r ~ t li 5? C * Ο &quot; Τ3-a 'o: 〇3 〇1 XJ3 • ZΛ 绁 丨 一苎 Ss3.7r3ibn ^ s ^ opioidsiH? (Please read the precautions on the back before filling in this page) Installation · Thread · This paper scale uses the Chinese National Standard (CNS) A 4 specifications (210x297 male dragon) 241 86. 86. Printed Α7 Β7 by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs V. Description of the invention (That is, the immunosuppressive effect of the compound. For the stimulation of Con-A (Confianava 丨 in Α.71 豆 球 蛋 肖):> Regulation T fine suizuo pomelo for making (experimental method) Spleen and spleen were plucked from rats in a sterile way and made by mesh Army cell float. The floating liquid was prepared into 5X10e / Bl, and 100 il was dispensed in each well of a 96-well well plate. Add ConA (1 «g / Bl) 50ju 1 / well of nitogen to the well plate with spleen cells and each concentration of compound (0.1, 0.5, 0.75, 1.0, 2.5, 5.0, 7.5, 10 , 12.5, 15, 17.5, 20U g / ml) 50iu 1 / well, cultured in a 37t: COa incubator for 48 hours. Add [3H] thymidine (2 Ci / 10 w 1 / well) (thymidine is thymidine) 8 hours before the end of training. Eight hours after the addition, the cells were collected on the filter paper with a Cell harvester (cell filtration device). * Toluene scintillation fission substance was added. The M scintillation fission counter was used to measure the radioactivity of enveloped cells [3H] thymidine. The T cell proliferation inhibition rate was calculated by the following formula. Inhibition rate = (radioactivity when no compound is added-radioactivity when compound is added) / (radioactivity when no compound is added-radioactivity when ConA is not added) Μ compound and comparative rate show the inhibition rate of T cell proliferation of NTI . This paper wave scale is applicable to the Chinese National Standard (CNS) Λ4 specifications (210 X 297 mm) ^^^ 1 — ^ ϋ n mV I— fn ^^^^ 1 I * m · I mf ml ^ -m tlf wfc —- ^ i (Please read the notes on the back before filling this page) 242

V. Description of the invention () Table 1 2 Compound concentration (&quot; g / Μ) T cell proliferation inhibition rate% (η = 3) 19 Ν Τ I 0. 1 6 0 0. 5 0 0 0. 7 5 18 0 1 . 0 2. 5 1 0 3 3 0 5. 0 7. 5 9 4 15 1 0 0 3 5 1 0. 0 1 0 0 6 2 1 2. 5 1 0 0 8 5 15.0 1 0 0 9 8 17.5 10 0 10 0 2 0. 0 10 0 10 0 Please read the precautions on the back and fill in the book 100). Installed. The results show that the ICSD value of compound m is 3 / ig / ml, which is the same as NT I ICD Compared with the value of 8.6 ug / ml, it obviously has a strong immunosuppressive effect. In addition, as shown in Table-3, other dumb derivatives have the same or higher T cell proliferation inhibitory activity as the compound JLQ. .Line. Printed by the Employees ’Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs. This paper scale is applicable to the Chinese National Standard (CNS) A4 specifications (210x297 mm) -243-A 6 B6 5. Description of invention () Table 1 3 Indigo skeleton compounds Inhibition of T cell proliferation Printed by the Employees Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

Compound_ 1 C κ · (β ίί / in I) 1 9 2. 7 2 5 3. Ϋ 2 9 0. 9 3 1 2. 6 3 7 1. 9 A 0 2. G 4 7 3. 8 5 2 3. 5 5 6 1 '1. U (please read the precautions on the back before filling in this page). Packing-line. The size of this paper is based on China Standards (CNS) Grade 4 (210x297 Gongcheng) -244- S01C04 V. Description of the invention ()-The above pseudo-exemplified embodiments specifically illustrate the present invention, but the present invention is of course not limited to these. According to the present invention, a highly selective S-opioid receptor antagonist can be supplied very easily and inexpensively, which not only contributes to the research of QPiQid, but also can be used as an immunosuppressant. (Please read the precautions on the back before filling out this page) Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs. This paper uses the Chinese National Standard (CNS) A4 specifications (210X297 male dragon) 245

Claims (1)

Application for patent scope A8 'C8 No. 80 104 699 Application for amendment of patent scope Amendment date: February 1986 1. An lumendole derivative or a pharmacologically acceptable salt thereof, the lumendole derivative may be thin General formula (1) R 3 ⑴ [wherein, L is an alkyl group having a carbon number of 1 to 5, an alkyl group having a carbon number of 4 to 7, an allyl group, a three-gas ethoxycarbonyl group, a benzyloxycarbonyl group, and a carbon number of 4 ~ Cycloalkylcarbonyl group of 7; Ra is hydrogen, alkyl group having 1 to 3 carbon atoms, benzyl group; R3 is radium, fluorine, radium, o, or alkyl group having 1 to 5 carbon atoms; iU is Suan, carbon number is 1 to 1 5 alkyl or benzyl; Re is krypton or hydroxy; and, the general formula (1) includes (+) body, (a) stern, (±) «]. 2 · —kind of general formula (101) ^^^ 1 nn Sul — ^ n tuv mB * ^ — ^ 1 mi in— 41 · ~ 洚 *-(please read the precautions on the back before filling this page) Ministry of Economic Affairs R OH R ι 〇ζ · RI 0 3 Bu R…. (101) 0 S [Where * R i. i is RiotOCO (here R1. 7 means 2,2,2-difluoroethyl, benzyl) or R ^ eCO (where Rue represents a carbon number of 1 ~ 5 alkane. The paper standard is applicable to the Chinese National Standard (CNS ) A4 specification (210X 297 mm) 246 301 ^^ 4 A8 B8 C8 D8 VI. Patent application base, broken ring 3 ~ 6 ring yoke,]; Rina, Rin3 are gas, hydrogen or, and R1De It can form an oxo group; it is argon, hydroxyl or alkaneoxy group having 1 to 5 carbon atoms; RiD6 is hydrogen or an alkoxy group having 1 to 5 carbon atoms; and, the general formula (101) includes (+) », ( A) Isoquinoline derivatives represented by body, (±) «] and their pharmacologically acceptable manufacturing methods, characterized in that the method is based on the general formula (103) (103) ar [where: Rina, Rioa, Hi. *, Ride, Rioe, Hi. , The definition is the same as before;] The enamine carbamic acid of the enamine shown is oxidized to form the general formula (l〇la) -------- "Installed-(Please read the precautions on the back before filling in This page) Printed by Beigong Consumer Cooperative, Central Bureau of Standards, Ministry of Economic Affairs R I 0 3 (101a) [where: Rina, Rina, Ri. *, Rine, Rios, Riot are defined as above; and • The general formula (lola) includes the steps of (+) body, (一) «, (±) tong]. 3. A kind of adult product used for immunosuppressants. It is the standard of the M Shen Shenli template. The paper standard is applicable to the Chinese National Standard (CNS) Α4 specification (210Χ297 mm). 247 Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs. -· Λ A 8 D8 々, the patent application scope of the vermillion derivative or its pharmacologically acceptable M is the active ingredient. This paper scale is applicable to the Chinese National Standard (CNS) A4 specification (210X297mm) -------- J: 袈 ------. 訂 77 ----- li (please read the notes on the back first (Fill in this page again) 248