CN101309586A

CN101309586A - Thiazoles used as fungicides

Info

Publication number: CN101309586A
Application number: CNA2006800428893A
Authority: CN
Inventors: J·N·格罗伊; O·盖特森; R·邓克尔; O·古思; S·希尔布兰德; K·伊尔克; P·施赖尔; U·沃肯道夫-诺依曼; P·达蒙; A·沃斯特; 波多野広幸
Original assignee: Bayer CropScience AG
Current assignee: Bayer CropScience AG
Priority date: 2005-09-24
Filing date: 2006-09-12
Publication date: 2008-11-19
Also published as: UA91565C2; ZA200802480B

Abstract

Disclosed is the use of compounds of formula (I), wherein R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R<8> as well as X, Y, Z have the meanings indicated in the description, as fungicides. Also disclosed are compounds of formula (Ia), wherein R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R<8>, R<14>, A, X, Y, and Z have the meanings indicated in the description, methods for producing said substances, and the use thereof for controlling undesired microorganisms.

Description

Thiazole compound as bactericide

The present invention relates to thiazole compound and be used to prevent and treat the harmful microbe purposes.

Known some thiazole compound can be used as crop protection agents (seeing WO-A 2003/029249).

Yet, since to modern bactericide aspect ecological with the requirement of economic aspect, for example the formation of relevant activity profile, toxicity, selectivity, rate of application, residue and favourable preparation aspect requires sustainable growth, and owing to may there be for example problem of resistance of other problems, therefore exploitation new, that be better than the bactericide of existing bactericide with regard to some aspect at least all there is demand always.

Find unexpectedly that now thiazole compound of the present invention has reached described purpose at least in some aspects, therefore be suitable for and make bactericide.

In these thiazole compounds some is as pharmaceutical active compounds known (seeing, for example WO-A 2005/012298, WO-A 2005/005438 or WO-A 2004/078682), but their beat all bactericidal activities are still unknown.

The invention provides formula (I) compound (thiazole compound of formula (I)) and agrochemicals active salt thereof purposes as bactericide

Wherein each symbol is as giving a definition:

R ¹To R ⁴Be hydrogen, halogen, cyano group, hydroxyl, nitro, OR independently of one another ¹¹, SR ¹¹, SOR ¹¹, SO ₂R ¹¹, SO ₂N (R ¹¹) ₂, C=OR ¹¹, NR ¹¹COOR ¹², N (R ¹¹) ₂, NR ¹¹COR ¹¹, NR ¹¹COR ¹², NR ¹¹SO ₂R ¹², OCON (R ¹¹) ₂, OC=OR ¹¹, CON (R ¹¹) ₂, COOR ¹¹, (CH ₂) _mOR ¹¹, (CH ₂) _mSR ¹¹, (CH ₂) _mN (R ¹¹) ₂, (CH ₂) _mCOOR ¹², (CH ₂) _mNR ¹¹COOR ¹¹, the unsubstituted or C that replaces ₁-C ₈Alkyl, C ₁-C ₈Haloalkyl, C ₃-C ₈Cycloalkyl; M=1-8 wherein

Perhaps two adjacent radicals R under various situations ¹, R ²Or R ², R ³Or R ³, R ⁸Or R ⁸, R ⁴Constitute five yuan or hexa-member heterocycle unsubstituted or that replace together,

R ⁵Be hydrogen, the unsubstituted or C that replaces ₁-C ₈Alkyl, the unsubstituted or C that replaces ₁-C ₄Alkyl C (=O), C ₁-C ₄Alkyl OC (=O), the unsubstituted or C that replaces ₁-C ₄Alkoxyl (C ₁-C ₄) alkyl, the unsubstituted or C that replaces ₂-C ₆Thiazolinyl, the unsubstituted or C that replaces ₂-C ₆Alkynyl, C ₁-C ₆Alkyl sulphinyl, C ₁-C ₆Alkyl sulphonyl, C ₃-C ₈Cycloalkyl; The C that has 1 to 9 fluorine, chlorine and/or bromine atoms separately ₁-C ₆Haloalkyl, C ₁-C ₄Haloalkyl sulfinyl, C ₁-C ₄Halogenated alkyl sulfonyl, halo-C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl, C ₃-C ₈Halogenated cycloalkyl; Formoxyl, formoxyl-C ₁-C ₃Alkyl, (C ₁-C ₃Alkyl) carbonyl-C ₁-C ₃Alkyl, (C ₁-C ₃Alkoxyl) carbonyl-C ₁-C ₃Alkyl; Halo-(the C that has 1 to 13 fluorine, chlorine and/or bromine atoms separately ₁-C ₃Alkyl) carbonyl-C ₁-C ₃Alkyl, halo-(C ₁-C ₃Alkoxyl) carbonyl-C ₁-C ₃Alkyl; (C ₁-C ₈Alkyl) carbonyl, (C ₁-C ₈Alkoxyl) carbonyl, (C ₁-C ₈Alkylthio group) carbonyl, (C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl) carbonyl, (C ₃-C ₆Alkene oxygen base) carbonyl, (C ₃-C ₆Alkynyloxy group) carbonyl, (C ₃-C ₈Cycloalkyl) carbonyl; (the C that has 1 to 9 fluorine, chlorine and/or bromine atoms separately ₁-C ₆Haloalkyl) carbonyl, (C ₁-C ₆Halogenated alkylthio) carbonyl, (C ₁-C ₆Halogenated alkoxy) carbonyl, (C ₃-C ₆Haloalkene oxygen base) carbonyl, (C ₃-C ₆The halo alkynyloxy group) carbonyl, (halo-C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl) carbonyl, (C ₃-C ₈Halogenated cycloalkyl) carbonyl, perhaps-CH ₂-C ≡ C-R ^1-A,-CH ₂-CH=CH-R ^1-A,-CH=C=CH-R ^1-A,-C (=O) C (=O) R ²,-CONR ³R ⁴,-CH ₂NR ⁵R ⁶, C ₁-C ₄Trialkylsilkl or C ₁-C ₄Dialkyl group one phenyl silicyl,

R ^1-ARepresent hydrogen, C ₁-C ₆Alkyl, C ₁-C ₆Haloalkyl, C ₂-C ₆Thiazolinyl, C ₂-C ₆Alkynyl, C ₃-C ₇Cycloalkyl, (C ₁-C ₄Alkoxyl) carbonyl, (C ₃-C ₆Alkene oxygen base) carbonyl, (C ₃-C ₆Alkynyloxy group) carbonyl or cyano group,

X is nitrogen or CR ⁸,

Y is nitrogen or CR ⁹,

Z is nitrogen or CR ¹⁰,

R ⁶Be hydrogen, halogen, cyano group, hydroxyl, OR ¹¹, SR ¹¹, COR ¹¹, CO ₂R ¹¹, the unsubstituted or C that replaces ₁-C ₈Alkyl, C ₁-C ₈Haloalkyl, C ₁-C ₄Trialkylsilkl, N (R ¹¹) ₂, NR ¹¹COR ¹¹, NR ¹¹COR ¹², NR ¹¹SO _nR ¹¹, CON (R ¹¹) ₂, C ₃-C ₈Cycloalkyl, aryl, heteroaryl; N=0-2 wherein,

R ⁷Be hydrogen, halogen, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹, the unsubstituted or C that replaces ₁-C ₈Alkyl, the unsubstituted or C that replaces ₃-C ₆Cycloalkyl, C ₁-C ₄Trialkylsilkl, COOR ¹¹, CON (R ¹¹) ₂, COR ¹¹

Perhaps

R ⁷And R ¹⁰Constitute saturated or unsaturated bridge together with following structure:

R wherein ¹³Independently of one another=hydrogen, halogen, the unsubstituted or C that replaces ₁-C ₃Alkyl, the unsubstituted or C that replaces ₁-C ₃Alkoxyl or

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

R ⁸Be hydrogen, halogen, cyano group, hydroxyl, nitro, OR ¹¹, SR ¹¹, SOR ¹¹, SO ₂R ¹¹, SO ₂N (R ¹¹) ₂, C=OR ¹¹, NR ¹¹COOR ¹², N (R ¹¹) ₂, NR ¹¹COR ¹¹, NR ¹¹COR ¹², NR ¹¹SO ₂R ¹², OCON (R ¹¹) ₂, OC=OR ¹¹, CON (R ¹¹) ₂, COOR ¹¹, (CH ₂) _mOR ¹¹, (CH ₂) _mSR ¹¹, (CH ₂) _mN (R ¹¹) ₂, (CH ₂) _mCOOR ¹², (CH ₂) _mNR ¹¹COOR ¹¹, the unsubstituted or C that replaces ₁-C ₈Alkyl, C ₁-C ₈Haloalkyl, C ₃-C ₈Cycloalkyl; M=1-8 wherein,

R ⁹Be hydrogen, halogen, N (R ¹¹) ₂, cyano group, hydroxyl, OR ¹¹, SR ¹¹, COR ¹¹, the unsubstituted or C that replaces ₁-C ₈Alkyl or C unsubstituted or that replace ₃-C ₈Cycloalkyl,

R ¹⁰Be hydrogen, halogen, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹, the unsubstituted or C that replaces ₁-C ₈Alkyl, C ₁-C ₄Trialkylsilkl, COOR ¹¹, CON (R ¹¹) ₂,

R ¹¹Identical or different and be hydrogen, the unsubstituted or C that replaces ₁-C ₈Alkyl, C ₁-C ₈Haloalkyl, C ₁-C ₄Trialkylsilkl, aryl,

Perhaps

If two R ¹¹Group is connected on the nitrogen-atoms, then two R ¹¹Group can form one can contain the most nearly 5 saturated or unsaturated rings that are selected from heteroatomic 3 to 7 yuan unsubstituted or replacement of N, O and S in addition again, and wherein two oxygen atoms are non-conterminous,

Perhaps

If two R ¹¹Group is at group NR ¹¹COR ¹¹In adjacent, two R then ¹¹Group can form one can contain the most nearly 5 saturated or unsaturated rings that are selected from heteroatomic 3 to 7 yuan unsubstituted or replacement of N, O and S in addition again, and wherein two oxygen atoms are non-conterminous,

R ¹²Identical or different and be unsubstituted or the C that replaces ₁-C ₈Alkyl, C ₁-C ₈Haloalkyl, (CH ₂) _pOR ¹¹, C ₁-C ₄Trialkylsilkl; P=1-4 wherein.

Formula (I) compound is very suitable for preventing and treating harmful microorganism.Especially, they have strong bactericidal activity, not only can be used for crop protection but also can be used for material protection.

Formula (I) provides the broad definition of The compounds of this invention.

Preferred such formula (I) compound, wherein one or more in each symbol have one of following given preferred meaning, that is,

Perhaps two adjacent radicals R under various situations ¹, R ²Or R ², R ³Or R ³, R ⁸Or R ⁸, R ⁴Constitute five yuan or a hexa-member heterocycle unsubstituted or that replaced by following substituting group together, wherein substituting group is 1 to 4 halogen atom or 1 to 4 C ₁-C ₃Alkyl group, and described heterocycle each self-containedly reach two oxygen atoms at most,

R ⁵Be hydrogen, methyl, ethyl, propyl group, 1-Methylethyl, butyl, 1-methyl-propyl, 2-methyl-propyl, 1,1-dimethyl ethyl, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂

Acetyl group, C ₂H ₅C (=O), C ₃H ₇C (=O), C ₄H ₉C (=O), CF ₃C (=O), C ₂F ₅C (=O), CH ₃OC (=O), C ₂H ₅OC (=O), C ₃H ₇OC (=O), C ₃H ₇OC (=O), C ₄H ₉OC (=O), CF ₃OC (=O), CCl ₃OC (=O), C ₂F ₅OC (=O), CH ₂OCH ₃C ₂H ₄OCH ₃, CH=CH ₂, CH ₂CH=CH ₂, C ≡ CH, CH ₂C ≡ CH, SOCH ₃, SOC ₂H ₅, SOC ₃H ₇SO ₂CH ₃, SO ₂C ₂H ₅, SO ₂C ₃H ₇, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl; CH ₂OCF ₃C ₂H ₄OCF ₃, C=ONH ₂, SiMe ₃, SiMe ₂TBu, SiMe ₂Ph, (reach hereinafter, Ph is a phenyl herein)

X is nitrogen or CR ⁸,

Y is nitrogen or CR ⁹,

Z is nitrogen or CR ¹⁰,

Wherein or Y and Z be nitrogen,

Perhaps Y is that nitrogen and Z are CR ¹⁰,

Perhaps Y is CR ⁹And Z is a nitrogen,

R ⁶Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, OR ¹¹, O-Me, O-Et, O-Pr, O-iPr, O-Bu, O-secBu, O-isoBu, O-tBu, OCH (CH ₃) CH ₂OH, OCH (CH ₃) CH ₂OCH ₃, OCH (C ₂H ₅) CH ₂OH, OCH (C ₂H ₅) CH ₂OCH ₃, O (CH ₂) ₂OCH ₃, O (CH ₂) ₂OH, O (CH ₂) ₃OCH ₃, O (CH ₂) ₃OH, OCF ₃, SR ¹¹, S-Me, S-Et, S-Pr, S-iPr, S-Bu, S-secBu, S-isoBu, S-tBu, SCF ₃, SOR ¹¹, SO-Me, SO-Et, SO-Pr, SO-iPr, SO-Bu, SO-secBu, SO-isoBu, SO-tBu, SO ₂R ¹¹, SO ₂-Me, SO ₂-Et, SO ₂-Pr, SO ₂-iPr, SO ₂-Bu, SO ₂-secBu, SO ₂-isoBu, SO ₂-tBu, COR ¹¹, COMe, COEt, COPr, COiPr, COBu, COsecBu, COisoBu, COtBu, COCF ₃, CO ₂R ¹¹, CO ₂Me, CO ₂Et, CO ₂Pr, CO ₂IPr, CO ₂Bu, CO ₂SecBu, CO ₂IsoBu, CO ₂TBu, CO ₂CH (CH ₃) CH ₂OH, CO ₂CH (CH ₃) CH ₂OCH ₃, CO ₂CH (C ₂H ₅) CH ₂OH, CO ₂CH (C ₂H ₅) CH ₂OCH ₃, CO ₂(CH ₂) ₂OCH ₃, CO ₂(CH ₂) ₂OH, CO ₂(CH ₂) ₃OCH ₃, CO ₂(CH ₂) ₃OH, NR ¹¹CO ₂R ¹¹, NR ¹¹CO ₂Me, NR ¹¹CO ₂Et, NR ¹¹CO ₂Pr, NR ¹¹CO ₂IPr, NR ¹¹CO ₂Bu, NR ¹¹CO ₂SecBu, NR ¹¹CO ₂IsoBu, NR ¹¹CO ₂TBu, NR ¹¹COR ¹¹, NR ¹¹COMe, NR ¹¹COEt, NR ¹¹COPr, NR ¹¹COiPr, NR ¹¹COBu, NR ¹¹COsecBu, NR ¹¹COisoBu, NR ¹¹COtBu, methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CH ₂OCH ₃, (CH ₂) ₂OCH ₃, CH (CH ₃) CH ₂OCH ₃, (CH ₂) ₂OH, CH (CH ₃) CH ₂OH, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂

R ⁷Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂, COR ¹¹,

Perhaps

R wherein ¹³Independently of one another=hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, propyl group, 1-Methylethyl, CF ₂H, CF ₃, C ₂F ₅, OCH ₃, OC ₂H ₅, OCF ₃, OC ₂F ₅Perhaps

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

R ⁹Be hydrogen, fluorine, chlorine, bromine, iodine, N (R ¹¹) ₂, NMe ₂, NEt ₂, NHMe, NH ₂, NH tBu, NHEt, NHPr, NHiPr, NHBu, NHsecBu, NHisoBu, 4-methyl piperazine-1-base, piperazine-1-base, morpholine-1-base, cyano group, hydroxyl, OR ¹¹, O-Me, O-Et, O-Pr, O-iPr, O-Bu, O-secBu, O-isoBu, O-tBu, O-(CH ₂) ₂OH, O-(CH ₂) ₂OCH ₃, O-(CH ₂) ₃OH, O-(CH ₂) ₃OCH ₃, OCF ₃, SR ¹¹, SH, S-Me, S-Et, S-Pr, S-iPr, S-Bu, S-secBu, S-isoBu, S-tBu, SCF ₃, COR ¹¹, COMe, COEt, COPr, COiPr, COBu, COsecBu, COisoBu, COtBu, COCF ₃Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂,

R ¹¹Identical or different and be hydrogen, methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl, 1-ethyl-2-methyl-propyl, CH ₂CH ₂OMe, CH (CH ₃) CH ₂OMe, CH ₂CH (CH ₃) OMe, CH ₂CH ₂OEt, CH (CH ₃) CH ₂OEt, CH ₂CH (CH ₃) OEt, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, phenyl

Perhaps

R ¹²Be methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, CH ₂OR ¹¹, (CH ₂) ₂OR ¹¹, (CH ₂) ₃OR ¹¹, (CH ₂) ₄OR ¹¹, SiMe ₃

Preferred especially such formula (I) compound, wherein one or more in each symbol have one of following implication:

Perhaps two adjacent radicals R under various situations ¹, R ²Or R ², R ³Or R ³, R ⁸Or R ⁸, R ⁴Constitute 2 together, 3-dihydro-1,4-dioxine, 2,2,3,3-tetrafluoro-2,3-dihydro-1,4-dioxine, 1,3-dioxole or 2,2-two fluoro-1,3-dioxole ring,

R ⁵Be hydrogen, methyl, ethyl, propyl group, 1-Methylethyl, butyl, 1-methyl-propyl, 2-methyl-propyl, 1,1-dimethyl ethyl, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂Acetyl group, C ₂H ₅C (=O), C ₃H ₇C (=O), C ₄H ₉C (=O), CF ₃C (=O), C ₂F ₅C (=O), CH ₂OCH ₃C ₂H ₄OCH ₃, CH=CH ₂, CH ₂CH=CH ₂, C ≡ CH, CH ₂C ≡ CH, SOCH ₃, SOC ₂H ₅, SOC ₃H ₇SO ₂CH ₃, SO ₂C ₂H ₅, SO ₂C ₃H ₇, cyclopropyl, CH ₂OCF ₃C ₂H ₄OCF ₃, C=ONH ₂, SiMe ₃, SiMe ₂TBu, SiMe ₂Ph

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

Perhaps

R wherein ¹³Independently of one another=hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, propyl group, 1-Methylethyl, CF ₂H, CF ₃, C ₂F ₅, OCH ₃OC ₂H ₅, OCF ₃, OC ₂F ₅Or

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, OCF ₃, OCF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂,

R ¹¹Identical or different and be hydrogen, methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl, 1-ethyl-2-methyl-propyl, CH ₂CH ₂OMe, CH (CH ₃) CH ₂OMe, CH ₂CH (CH ₃) OMe, CH ₂CH ₂OEt, CH (CH ₃) CH ₂OEt, CH ₂CH (CH ₃) OEt, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, phenyl

Perhaps

If two R ¹¹Group is connected on the nitrogen-atoms, and then these groups can be represented piperidines-1-base, piperazine-1-base, 4-methyl piperazine-1-base or morpholine-1-base together,

Perhaps

Preferred extremely especially such formula (I) compound, wherein one or more in each symbol have one of following implication:

CF ₃，CF ₂H，CCl ₃，C ₂F ₅，C ₃F ₇，CF(CF ₃) ₂

R ⁵Be hydrogen, acetyl group, trifluoroacetyl group,

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

R ⁷Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, NMe ₂, NEt ₂, NHMe, NH ₂, NHtBu, NHEt, NHPr, NHiPr, NHBu, NHiBu, NHsecBu, piperazine-1-base, 4-methyl piperazine-1-base, morpholine-1-base, nitro, OR ¹¹, O-Me, O-Et, O-Pr, O-iPr, O-Bu, O-secBu, O-isoBu, O-tBu, OCH (CH ₃) CH ₂OH, OCH (CH ₃) CH ₂OCH ₃, OCH (C ₂H ₅) CH ₂OH, OCH (C ₂H ₅) CH ₂OCH ₃, O (CH ₂) ₂OCH ₃, O (CH ₂) ₂OH, O (CH ₂) ₃OCH ₃, O (CH ₂) ₃OH, OCF ₃, SR ¹¹, S-Me, S-Et, S-Pr, S-iPr, S-Bu, S-secBu, S-isoBu, S-tBu, SCF ₃Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CO ₂Me, CO ₂Et, CO ₂Pr, CO ₂IPr, CO ₂Bu, CO ₂SecBu, CO ₂IsoBu, CO ₂TBu, CON (R ¹¹) ₂, CONH ₂, CONHMe, CONMe ₂, CONHEt, CONEt ₂, CO-morpholine, CO-piperidines, CO-piperazine, CO-(4-methyl piperazine), CONHCH (CH ₃) CH ₂OH, CONHCH (CH ₃) CH ₂OCH ₃, CONHCH (C ₂H ₅) CH ₂OH, CONHCH (C ₂H ₅) CH ₂OCH ₃, CONH (CH ₂) ₂OCH ₃, CONH (CH ₂) ₂OH, CONH (CH ₂) ₃OCH ₃, CONH (CH ₂) ₃OH, COR ¹¹, COMe, COEt, COPr, COiPr, COBu, COsecBu, COisoBu, COtBu, COF ₃,

Perhaps

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, NMe ₂, NEt ₂, NHMe, NH ₂, NHtBu,, NHEt, NHPr, NHiPr, NHBu, NHsecBu, NHisoBu, 4-methyl piperazine-1-base, piperazine-1-base, morpholine-1-base, nitro, OR ¹¹, O-Me, O-Et, O-Pr, O-iPr, O-Bu, O-secBu, O-isoBu, O-tBu, OCH (CH ₃) CH ₂OH, OCH (CH ₃) CH ₂OCH ₃, OCH (C ₂H ₅) CH ₂OH, OCH (C ₂H ₅) CH ₂OCH ₃, O (CH ₂) ₂OCH ₃, O (CH ₂) ₂OH, O (CH ₂) ₃OCH ₃, O (CH ₂) ₃OH, OCF ₃, SR ¹¹, S-Me, S-Et, S-Pr, S-iPr, S-Bu, S-secBu, S-isoBu, S-tBu, SCF ₃Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CO ₂Me, CO ₂Et, CO ₂Pr, CO ₂IPr, CO ₂Bu, CO ₂SecBu, CO ₂IsoBu, CO ₂TBu, CON (R ¹¹) ₂CONH ₂, CONHMe, CONMe ₂, CONHEt, CONEt ₂, CO-morpholine, CO-piperidines, CO-piperazine, CO-(4-methyl piperazine), CONHCH (CH ₃) CH ₂OH, CONHCH (CH ₃) CH ₂OCH ₃, CONHCH (C ₂H ₅) CH ₂OH, CONHCH (C ₂H ₅) CH ₂OCH ₃, CONH (CH ₂) ₂OCH ₃, CONH (CH ₂) ₂OH, CONH (CH ₂) ₃OCH ₃, CONH (CH ₂) ₃OH,

Perhaps

In addition, preferred extremely especially such formula (I) compound, wherein one or more in each symbol have one of following implication:

R ¹To R ⁴Be hydrogen, fluorine, chlorine, cyano group, hydroxyl, nitro, OMe, CF independently of one another ₃, COCH ₃, COOCH ₃, COOH, N (Me) ₂, NHCOCH ₃, NHCOCF ₃, NHSO ₂CH ₃, NHCOOCH ₃, NHCOO (CH ₂CH ₂) OCH ₃, 4-N-methyl piperazine-1-base, CH ₂NH ₂, CH ₂NHCOOCH ₃, CH ₂NHCOOtBu, methyl,

Perhaps two adjacent radicals R under various situations ¹, R ²Or R ², R ³Or R ³, R ⁸Or R ⁸, R ⁴Constitute 2 together, 3-dihydro-1,4-dioxine ring or 1,3-dioxole ring,

R ⁵Be hydrogen, COCH ₃,

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

R ⁶Be hydrogen, S-Me, NHCOMe, NHCOCF ₃, NMe ₂, NHMe, NH ₂, NHtBu, NHCH (CH ₃) CH ₂OH, NHCH (CH ₃) CH ₂OCH ₃, CONMe ₂, cyclopropyl, cyclohexyl, phenyl, N-1,3-oxazolidine-2-ketone, N-4-methyl isophthalic acid, 3-oxazolidine-2-ketone, NHCH ₂Oxolane-2-base,

R ⁷Be hydrogen, methyl, 1-methyl-propyl, CF ₃, CF ₂H, cyclopropyl,

Perhaps

R wherein ¹³=hydrogen,

R ⁸Be hydrogen, fluorine, chlorine, cyano group, hydroxyl, nitro, OMe, CF ₃, COCH ₃, COOCH ₃, COOH, N (Me) ₂, NHCOCH ₃, NHCOCF ₃, NHSO ₂CH ₃, NHCOOCH ₃, NHCOO (CH ₂CH ₂) OCH ₃, 4-N-methyl piperazine-1-base, CH ₂NH ₂, CH ₂NHCOOCH ₃, CH ₂NHCOOtBu, methyl,

R ¹⁰Be hydrogen

Perhaps

R wherein ¹³=hydrogen.

R ¹To R ⁴Be hydrogen, fluorine, chlorine, iodine, cyano group, hydroxyl, nitro, OMe, OCH independently of one another ₂TBu, OCOCH ₃, SO ₂NH ₂, SO ₂N (CH ₃) ₂, COCH ₃, COCH ₂CH ₂CH ₃, COOCH ₂CH ₂OCH ₃, COOCH ₂CH ₂CH ₂OCH ₃, CONHCH ₂CH ₂OCH ₃, NH ₂, N (Me) ₂, NHCOCH ₃, NHSO ₂CH ₃, NHCOOCH ₃, NHCOOCH ₂CH ₃, NHCOOtBu, NHCOOCH ₂CH ₂OCH ₃, 4-N-acetyl group piperazine-1-base, N-pyrrolidin-2-one-1-base, CH ₂NHCOOCH ₃, CH ₂NHCOOtBu, methyl, CF ₃

Perhaps two adjacent radicals R under various situations ¹, R ²Or R ², R ³Or R ³, R ⁸Or R ⁸, R ⁴Constitute 2,3 dihydro furan-2-ketone ring, 2 together, 3-dihydro-1,4-dioxine ring, 2,2,3,3-tetrafluoro-2,3-dihydro-1,4-dioxine ring, 1,3-dioxole ring or 2,2-two fluoro-1,3-dioxole ring,

R ⁵Be hydrogen, COCH ₃, COCF ₃, COOCH ₃

X is nitrogen or CR ⁸,

R ⁸Be hydrogen, O-Me,

Y is a nitrogen,

Z is CR ¹⁰,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, cyano group, CF ₃

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

R ⁶Be methyl, ethyl, isopropyl, cyclopropyl, phenyl, 4-chlorphenyl, 3-pyridine radicals, CH ₂OCH ₃, O (CH ₂) ₂OCH ₃, S-Me, NH ₂, NHMe, NMe ₂, NH tBu, NHBu, NHiBu, N-morpholinyl, NH (CH ₂) ₂OH, NH (CH ₂) ₂OCH ₃, NH (CH ₂) ₃OCH ₃, NHCH (CH ₃) CH ₂OCH ₃, NCH ₃(CH ₂) ₂OCH ₃, NCH ₃(CH ₂) ₃OCH ₃, NHCH ₂Oxolane-2-base, N-1,3-oxazolidine-2-ketone,

R ⁷Be hydrogen, methyl, CF ₃, CF ₂H,

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge.

R ¹To R ⁴Be hydrogen, fluorine, chlorine, iodine, cyano group, hydroxyl, nitro, OMe, OCH independently of one another ₂TBu, OCOCH ₃, SO ₂NH ₂, SO ₂N (CH ₃) ₂, COCH ₃, COCH ₂CH ₂CH ₃, COOCH ₂CH ₂OCH ₃, COOCH ₂CH ₂CH ₂OCH ₃, CONHCH ₂CH ₂OCH ₃, NH ₂, N (Me) ₂, NHCOCH ₃, NHSO ₂CH ₃, NHCOOCH ₃, NHCOOCH ₂CH ₃, NHCOOtBu, NHCOOCH ₂CH ₂OCH ₃, CH ₂NHCOOCH ₃, CH ₂NHCOOtBu, methyl, CF ₃

Perhaps two adjacent radicals R under various situations ¹, R ²Or R ², R ³Or R ³, R ⁸Or R ⁸, R ⁴Constitute 2 together, 3-dihydro-1,4-dioxine ring, 2,2,3,3-tetrafluoro-2,3-dihydro-1,4-dioxine ring, 1,3-dioxole ring or 2,2-two fluoro-1,3-dioxole ring,

R ⁵Be hydrogen, COCH ₃, COCF ₃, COOCH ₃

X is nitrogen or CR ⁸,

R ⁸Be hydrogen, O-Me,

Y is a nitrogen,

Z is CR ¹⁰,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, cyano group, CF ₃,

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂-or CH ₂CH ₂Bridge,

R ⁶Be methyl, ethyl, isopropyl, cyclopropyl, phenyl, 3-pyridine radicals, CH ₂OCH ₃, O (CH ₂) ₂OCH ₃, S-Me, NH ₂, NHMe, NMe ₂, NH tBu, NHBu, NH iBu, N-morpholinyl, NH (CH ₂) ₂OH, NH (CH ₂) ₂OCH ₃, NH (CH ₂) ₃OCH ₃, NHCH (CH ₃) CH ₂OCH ₃, NCH ₃(CH ₂) ₂OCH ₃, NCH ₃(CH ₂) ₃OCH ₃, NHCH ₂Oxolane-2-base, N-1,3-oxazolidine-2-ketone,

R ⁷Be hydrogen, methyl, CF ₃, CF ₂H,

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge.

The definition of above-mentioned each group is combination with one another as required.In addition, single definition can be inapplicable.

In addition, formula (I) compound also can comprise formula (Ia) compound.Formula (Ia) compound and agrochemicals active salt thereof are still unknown, therefore also become the part of theme of the present invention

Wherein each symbol is as giving a definition:

R ⁵Be hydrogen, the unsubstituted or C that replaces ₁-C ₈Alkyl, the unsubstituted or C that replaces ₁-C ₄Alkyl C (=O), C ₁-C ₄Alkyl OC (=O), the unsubstituted or C that replaces ₁-C ₄Alkoxyl (C ₁-C ₄) alkyl, the unsubstituted or C that replaces ₂-C ₆Thiazolinyl, the unsubstituted or C that replaces ₂-C ₆Alkynyl, C ₁-C ₆Alkyl sulphinyl, C ₁-C ₆Alkyl sulphonyl, C ₃-C ₈Cycloalkyl; The C that has 1 to 9 fluorine, chlorine and/or bromine atoms separately ₁-C ₆Haloalkyl, C ₁-C ₄Haloalkyl sulfinyl, C ₁-C ₄Halogenated alkyl sulfonyl, halo-C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl, C ₃-C ₈Halogenated cycloalkyl; Formoxyl, formoxyl-C ₁-C ₃Alkyl, (C ₁-C ₃Alkyl) carbonyl-C ₁-C ₃Alkyl, (C ₁-C ₃Alkoxyl) carbonyl-C ₁-C ₃Alkyl; Halo-(the C that has 1 to 13 fluorine, chlorine and/or bromine atoms separately ₁-C ₃Alkyl) carbonyl-C ₁-C ₃-alkyl, halo-(C ₁-C ₃Alkoxyl) carbonyl-C ₁-C ₃Alkyl; (C ₁-C ₈Alkyl) carbonyl, (C ₁-C ₈Alkoxyl) carbonyl, (C ₁-C ₈Alkylthio group) carbonyl, (C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl) carbonyl, (C ₃-C ₆Alkene oxygen base) carbonyl, (C ₃-C ₆Alkynyloxy group) carbonyl, (C ₃-C ₈Cycloalkyl) carbonyl; (the C that has 1 to 9 fluorine, chlorine and/or bromine atoms separately ₁-C ₆Haloalkyl) carbonyl, (C ₁-C ₆Halogenated alkylthio) carbonyl, (C ₁-C ₆Halogenated alkoxy) carbonyl, (C ₃-C ₆Haloalkene oxygen base) carbonyl, (C ₃-C ₆The halo alkynyloxy group) carbonyl, (halo-C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl) carbonyl, (C ₃-C ₈Halogenated cycloalkyl) carbonyl, perhaps-CH ₂-C ≡ C-R ^1-A,-CH ₂-CH=CH-R ^1-A,-CH=C=CH-R ^1-A,-C (=O) C (=O) R ²,-CONR ³R ⁴,-CH ₂NR ⁵R ⁶, C ₁-C ₄Trialkylsilkl or C ₁-C ₄Dialkyl group one phenyl silicyl,

CH ₂CH (CH ₃) OMe, CH ₂CH ₂OEt, CH (CH ₃) CH ₂OEt, CH ₂CH (CH ₃) OEt, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂, phenyl

Perhaps

If two R ¹¹Group is connected on the nitrogen-atoms, then two R ¹¹Group can form one can contain the most nearly 5 saturated or undersaturated rings that are selected from heteroatomic 3 to 7 yuan unsubstituted or replacement of N, O and S in addition again, and wherein two oxygen atoms are non-conterminous,

Perhaps

If two R ¹¹Group is at group NR ¹¹COR ¹¹In adjacent, two R then ¹¹Group can form one can contain the most nearly 5 saturated or undersaturated rings that are selected from heteroatomic 3 to 7 yuan unsubstituted or replacement of N, O and S in addition again, and wherein two oxygen atoms are non-conterminous,

R ¹²Be methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, CH ₂OR ¹¹, (CH ₂) ₂OR ¹¹, (CH ₂) ₃OR ¹¹, (CH ₂) ₄OR ¹¹, SiMe ₃,

R ¹⁴Be hydrogen independently of one another, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, or cyclopropyl, cyclohexyl, cyclopenta, SiMe ₃,

A is OR ¹⁵, SR ¹⁵, N (R ¹⁵) ₂Or C (R ¹⁶) ₃,

R ¹⁵Be COR independently of one another ¹⁷, COCH ₃, COCF ₃, ethyl, propyl group, 1-Methylethyl, alkyl, C ₁-C ₄Trialkylsilkl, aryl,

Perhaps

R ¹²Identical or different and be unsubstituted or the C that replaces ₁-C ₈Alkyl, C ₁-C ₈Haloalkyl, (CH ₂) _tOR ¹¹, C ₁-C ₄Trialkylsilkl; T=1-4 wherein,

R ¹⁴Be hydrogen, halogen, cyano group, hydroxyl, OR independently of one another ¹¹, SR ¹¹, COR ¹¹, the unsubstituted or C that replaces ₁-C ₈Alkyl, C ₁-C ₈Haloalkyl, C ₁-C ₄Trialkylsilkl or C unsubstituted or that replace ₃-C ₈Cycloalkyl,

A is OR ¹⁵, SR ¹⁵, N (R ¹⁵) ₂Or C (R ¹⁶) ₃

R ¹⁵Be COR independently of one another ¹⁷, the unsubstituted or C that replaces ₂-C ₈Alkyl, C ₁-C ₈Haloalkyl, the unsubstituted or C that replaces ₃-C ₈Cycloalkyl, (CH ₂) _uOR ¹¹U=1-4 wherein,

R ¹⁶Be hydrogen, halogen, cyano group, hydroxyl, OR independently of one another ¹¹, SR ¹¹, COR ¹¹, N (R ¹¹) ₂, the unsubstituted or C that replaces ₁-C ₈Alkyl or C unsubstituted or that replace ₃-C ₈Cycloalkyl;

Perhaps

Two R under various situations ¹⁶Group is represented doubly linked oxygen or doubly linked sulphur,

Perhaps

Two radicals R under various situations ¹⁴, R ¹⁴Or R ¹⁵, R ¹⁵Or R ¹⁶, R ¹⁶Or R ¹⁴, R ¹⁶Constitute saturated or undersaturated 3 to 7 yuan of carbocyclic rings or the optional 4-pyridine radicals that replaces together,

R ¹⁷Be C unsubstituted or that replace ₁-C ₃Alkyl or C ₁-C ₃Haloalkyl.

Formula (Ia) compound is very suitable for preventing and treating harmful microorganism.Especially, they have strong bactericidal activity, not only can be used for crop protection but also can be used for material protection.

Formula (Ia) provides the broad definition of The compounds of this invention.

Preferred such formula (Ia) compound, wherein one or more in each symbol have one of following given preferred meaning, that is,

R ⁵Be hydrogen, methyl, ethyl, propyl group, 1-Methylethyl, butyl, 1-methyl-propyl, 2-methyl-propyl, 1,1-dimethyl ethyl, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂,

Acetyl group, C ₂H ₅C (=O), C ₃H ₇C (=O), C ₄H ₉C (=O), CF ₃C (=O), C ₂F ₅C (=O), CH ₃OC (=O), C ₂H ₅OC (=O), C ₃H ₇OC (=O), C ₃H ₇OC (=O), C ₄H ₉OC (=O), CF ₃OC (=O), CCl ₃OC (=O), C ₂F ₅OC (=O), CH ₂OCH ₃C ₂H ₄OCH ₃, CH=CH ₂, CH ₂CH=CH ₂, C ≡ CH, CH ₂C ≡ CH, SOCH ₃, SOC ₂H ₅, SOC ₃H ₇SO ₂CH ₃, SO ₂C ₂H ₅, SO ₂C ₃H ₇, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl; CH ₂OCF ₃C ₂H ₄OCF ₃, C=ONH ₂, SiMe ₃, SiMe ₂TBu, SiMe ₂Ph,

X is nitrogen or CR ⁸,

Y is nitrogen or CR ⁹,

Z is nitrogen or CR ¹⁰,

Wherein or Y and Z be nitrogen,

Perhaps Y is that nitrogen and Z are CR ¹⁰,

Perhaps Y is CR ⁹And Z is a nitrogen,

R ⁷Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, phenyl, to the Cl-phenyl, to the F-phenyl, to the Br-phenyl, to I-phenyl, p-methoxyphenyl, to Trifluoromethoxyphen-l, 2-pyridine radicals, 3-pyridine radicals, 4-pyridine radicals, 2-thienyl, 3-thienyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂, COR ¹¹,

Perhaps

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

R ⁹Be hydrogen, fluorine, chlorine, bromine, iodine, N (R ¹¹) ₂, NMe ₂, NEt ₂, NHMe, NH ₂, NHtBu, NHEt, NHPr, NHiPr, NHBu, NHsecBu, NHisoBu, 4-methyl piperazine-1-base, piperazine-1-base, morpholine-1-base, cyano group, hydroxyl, OR ¹¹, O-Me, O-Et, O-Pr, O-iPr, O-Bu, O-secBu, O-isoBu, O-tBu, O-(CH ₂) ₂OH, O-(CH ₂) ₂OCH ₃, O-(CH ₂) ₃OH, O-(CH ₂) ₃OCH ₃, OCF ₃, SR ¹¹, SH, S-Me, S-Et, S-Pr, S-iPr, S-Bu, S-secBu, S-isoBu, S-tBu, SCF ₃, COR ¹¹, COMe, COEt, COPr, COiPr, COBu, COsecBu, COisoBu, COtBu, COCF ₃Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl,

R ¹¹Identical or different and be hydrogen, methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl, 1-ethyl-2-methyl-propyl, CH ₂CH ₂OMe, CH (CH ₃) CH ₂OMe, CH ₂CH (CH ₃) OMe, CH ₂CH ₂OEt, CH (CH ₃) CH ₂OEt, CH ₂CH (CH ₃) OEt, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂, phenyl

Perhaps

A is OR ¹⁵, SR ¹⁵, N (R ¹⁵) ₂Or C (R ¹⁶) ₃

R ¹⁵Be COR independently of one another ¹⁷, COCH ₃, COCF ₃Ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl, 1-ethyl-2-methyl-propyl, CH ₂CH ₂OMe, CH (CH ₃) CH ₂OMe, CH ₂CH (CH ₃) OMe, CH ₂CH ₂OEt, CH (CH ₃) CH ₂OEt, CH ₂CH (CH ₃) OEt, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclohexyl, CH ₂OR ¹¹, (CH ₂) ₂OR ¹¹, (CH ₂) ₃OR ¹¹, (CH ₂) ₄OR ¹¹,

R ¹⁶Be hydrogen, halogen, cyano group, hydroxyl, OR independently of one another ¹¹, SR ¹¹, COR ¹¹, N (R ¹¹) ₂Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, CH ₂OR ¹¹, (CH ₂) ₂OR ¹¹, (CH ₂) ₃OR ¹¹, (CH ₂) ₄OR ¹¹, SiMe ₃

Perhaps

Two radicals R under various situations ¹⁴, R ¹⁴Or R ¹⁵, R ¹⁵Or R ¹⁶, R ¹⁶Or R ¹⁴, R ¹⁵Or R ¹⁴, R ¹⁶Constitute cyclopenta, cyclohexyl, cyclopentenyl, cyclohexenyl group, cyclopentadienyl group, cyclohexadienyl, 4-pyridine radicals together,

R ¹⁷Be methyl, ethyl, propyl group, 1-Methylethyl, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂

Preferred especially such formula (Ia) compound, wherein one or more in each symbol have one of following implication:

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

Perhaps

R ⁷And R ¹⁰Constitute a saturated or unsaturated bridge together with following structure:

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

Perhaps

A is OR ¹⁵, N (R ¹⁵) ₂Or C (R ¹⁶) ₃,

R ¹⁵Be COR independently of one another ¹⁷, COCH ₃, COCF ₃Ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl, 1-ethyl-2-methyl-propyl, CH ₂CH ₂OMe, CH (CH ₃) CH ₂OMe, CH ₂CH (CH ₃) OMe, CH ₂CH ₂OEt, CH (CH ₃) CH ₂OEt, CH ₂CH (CH ₃) OEt, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclohexyl, CH ₂OR ¹¹, (CH ₂) ₂OR ¹¹, (CH ₂) ₃OR ¹¹, (CH ₂) ₄OR ¹¹,

R ¹⁶Be hydrogen, halogen, cyano group, hydroxyl, OR independently of one another ¹¹, SR ¹¹, COR ¹¹, N (R ¹¹) ₂Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, CH ₂OR ¹¹, (CH ₂) ₂OR ¹¹, (CH ₂) ₃OR ¹¹, (CH ₂) ₄OR ¹², SiMe ₃

Perhaps

Preferred extremely especially such formula (Ia) compound, wherein one or more in each symbol have one of following implication:

R ⁵Be hydrogen, acetyl group, trifluoroacetyl group,

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

R ⁷Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, phenyl, to the Cl-phenyl, to the F-phenyl, to the Br-phenyl, to I-phenyl, p-methoxyphenyl, to Trifluoromethoxyphen-l, 2-pyridine radicals, 3-pyridine radicals, 4-pyridine radicals, 2-thienyl, 3-thienyl, SiMe ₃, COOR ¹¹, CO ₂Me, CO ₂Et, CO ₂Pr, CO ₂IPr, CO ₂Bu, CO ₂SecBu, CO ₂IsoBu, CO ₂TBu, CO ₂(CH ₂) ₂OH, CO ₂(CH ₂) ₂OCH ₃, CO ₂(CH ₂) ₃OH, CO ₂(CH ₂) ₃OCH ₃, CON (R ¹¹) ₂, CONHEt, CONEt ₂, CONHMe, CONMe ₂, CONHPr, CONPr ₂, CONHBu, CONHsecBu, CONHisoBu, CONHtBu, CONHCH (CH ₃) CH ₂OH, CONHCH (CH ₃) CH ₂OCH ₃, CONHCH (C ₂H ₅) CH ₂OH, CONHCH (C ₂H ₅) CH ₂OCH ₃, CONH (CH ₂) ₂OCH ₃, CONH (CH ₂) ₂OH, CONH (CH ₂) ₃OCH ₃, CONH (CH ₂) ₃OH, CONR ¹¹CH (CH ₃) CH ₂OH, COR ¹¹COMe, COEt, COPr, COiPr, COBu, COsecBu, CO-isoBu, COtBu, COCF ₃

Perhaps

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, NMe ₂, NEt ₂, NHMe, NH ₂, NHtBu,, NHEt, NHPr, NHiPr, NHBu, NHsecBu, NHisoBu, 4-methyl piperazine-1-base, piperazine-1-base, morpholine-1-base, nitro, OR ¹¹, O-Me, O-Et, O-Pr, O-iPr, O-Bu, O-secBu, O-isoBu, O-tBu, OCH (CH ₃) CH ₂OH, OCH (CH ₃) CH ₂OCH ₃, OCH (C ₂H ₅) CH ₂OH, OCH (C ₂H ₅) CH ₂OCH ₃, O (CH ₂) ₂OCH ₃, O (CH ₂) ₂OH, O (CH ₂) ₃OCH ₃, O (CH ₂) ₃OH, OCF ₃, SR ¹¹, S-Me, S-Et, S-Pr, S-iPr, S-Bu, S-secBu, S-isoBu, S-tBu, SCF ₃Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CO ₂Me, CO ₂Et, CO ₂Pr, CO ₂IPr, CO ₂Bu, CO ₂SecBu, CO ₂IsoBu, CO ₂TBu, CON (R ¹¹) ₂, CONH ₂, CONHMe, CONMe ₂, CONHEt, CONEt ₂, CO-morpholine, CO-piperidines, CO-piperazine, CO-(4-methyl piperazine), CONHCH (CH ₃) CH ₂OH, CONHCH (CH ₃) CH ₂OCH ₃, CONHCH (C ₂H ₅) CH ₂OH, CONHCH (C ₂H ₅) CH ₂OCH ₃, CONH (CH ₂) ₂OCH ₃, CONH (CH ₂) ₂OH, CONH (CH ₂) ₃OCH ₃, CONH (CH ₂) ₃OH,

R ¹¹Identical or different and be hydrogen, methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl, 1-ethyl-2-methyl-propyl, CH ₂CH ₂OMe, CH (CH ₃) CH ₂OMe, CH ₂CH (CH ₃) OMe, CH ₂CH ₂OEt, CH (CH ₃) CH ₂OEt, CH ₂CH (CH ₃) OEt, CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂, phenyl

Perhaps

R ¹²Be methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, CH ₂OR ¹¹, (CH ₂) ₂OR ¹¹, (CH ₂) ₃OR ¹¹, (CH ₂) ₄OR ¹¹SiMe ₃,

A is OR ¹⁵, N (R ¹⁵) ₂Or C (R ¹⁶) ₃,

Perhaps

In addition, preferred extremely especially such formula (Ia) compound, wherein one or more in each symbol have one of following implication:

R ⁵Be hydrogen, COCH ₃,

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

R ⁷Be hydrogen, methyl, 1-methyl-propyl, CF ₃, CF ₂H, cyclopropyl,

Perhaps

R wherein ¹³=hydrogen,

R ¹⁰Be hydrogen,

Perhaps

R wherein ¹³=hydrogen

R ¹¹Identical or different and be hydrogen, methyl, ethyl, CH (CH ₃) CH ₂OMe, CH ₂CH (CH ₃) OMe, CH ₂CH ₂OEt, CH (CH ₃) CH ₂OEt, CH ₂CH (CH ₃) OEt, cyclopropyl, cyclohexyl,

Perhaps

If two R ¹¹Group is connected on the nitrogen-atoms, and then these groups can be represented 4-methyl piperazine-1-base together,

R ¹²Be methyl, ethyl, propyl group, 1-Methylethyl, CF ₃, cyclopropyl, cyclohexyl,

R ¹⁴Be hydrogen, methyl, cyclopropyl independently of one another,

A is OR ¹⁵Or C (R ¹⁶) ₃,

R ¹⁵Be ethyl,

R ¹⁶Be hydrogen,

R ⁵Be hydrogen, COCH ₃, COCF ₃, COOCH ₃,

X is nitrogen or CR ⁸,

R ⁸Be hydrogen, O-Me,

Y is a nitrogen,

Z is CR ¹⁰,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, cyano group, CF ₃

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

R ⁷Be hydrogen, methyl, CF ₃, CF ₂H,

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

Perhaps

R ¹⁴Be hydrogen, methyl, cyclopropyl independently of one another,

A is OR ¹⁵Or C (R ¹⁶) ₃,

R ¹⁵Be ethyl,

R ¹⁶Be hydrogen,

R ⁵Be hydrogen, COCH ₃, COCF ₃, COOCH ₃,

X is nitrogen or CR ⁸,

R ⁸Be hydrogen, O-Me,

Y is a nitrogen,

Z is CR ¹⁰,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, cyano group, CF ₃

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

R ⁶Be ethyl, isopropyl, CH ₂OCH ₃, cyclopropyl, 3-pyridine radicals,

R ⁷Be hydrogen, methyl, CF ₃, CF ₂H,

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

Perhaps

R ¹⁴Be hydrogen, methyl, cyclopropyl independently of one another,

A is OR ¹⁵Or C (R ¹⁶) ₃,

R ¹⁵Be ethyl,

R ¹⁶Be hydrogen,

R ¹To R ⁴Be hydrogen, fluorine, chlorine, cyano group, hydroxyl, nitro, OMe, CF independently of one another ₃, COCH ₃, COOCH ₃, COOH, N (Me) ₂, NHCOCH ₃, NHSO ₂CH ₃, NHCOOCH ₃, NHCOO (CH ₂CH ₂) OCH ₃, 4-N-methyl-piperazine-1-base, CH ₂NH ₂, CH ₂NHCOOCH ₃, CH ₂NHCOOtBu,

R ⁵Be hydrogen,

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

R ⁷Be hydrogen, methyl, 1-methyl-propyl, CF ₃, cyclopropyl,

Perhaps

R wherein ¹³=hydrogen,

R ⁸Be hydrogen, fluorine, chlorine, cyano group, hydroxyl, nitro, OMe, CF ₃, COCH ₃, COOCH ₃, COOH, N (Me) ₂, NHCOCH ₃, NHSO ₂CH ₃, NHCOOCH ₃, NHCOO (CH ₂CH ₂) OCH ₃, 4-N-methyl piperazine-1-base, CH ₂NH ₂, CH ₂NHCOOCH ₃, CH ₂NHCOOtBu,

R ¹⁰Be hydrogen

Perhaps

R wherein ¹³=hydrogen,

Perhaps

R ¹⁴Be hydrogen, methyl independently of one another,

A is OR ¹⁵Or C (R ¹⁶) ₃,

R ¹⁵Be ethyl,

R ¹⁶Be hydrogen,

In the definition of each given symbol, used collective term (collectiveterm) is the following substituting group of representative usually in following formula:

Halogen: fluorine, chlorine, bromine and iodine;

Alkyl: have the saturated straight or branched alkyl of 1 to 4,6 or 8 carbon atom, for example C ₁-C ₆Alkyl, as methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl;

Haloalkyl: have the straight or branched alkyl group (as mentioned above) of 1 to 8 carbon atom, wherein some or all hydrogen atom can be replaced by aforesaid halogen atom in these groups, for example C ₁-C ₃Haloalkyl, as chloromethyl, bromomethyl, dichloromethyl, trichloromethyl, methyl fluoride, difluoromethyl, trifluoromethyl, chlorine methyl fluoride, dichloro one methyl fluoride, a chlorodifluoramethyl-, 1-chloroethyl, 1-bromoethyl, 1-fluoro ethyl, 2-fluoro ethyl, 2,2-two fluoro ethyls, 2,2,2-trifluoroethyl, 2-chloro-2-fluoro ethyl, 2-chloro-2,2-two fluoro ethyls, 2,2-two chloro-2-fluoro ethyls, 2,2,2-three chloroethyls, pentafluoroethyl group and 1,1,1-trifluoropropyl-2-base;

Thiazolinyl: have 2 to 4,6 or 8 carbon atoms and at an arbitrary position on have the undersaturated straight or branched alkyl of two keys, C for example ₂-C ₆Thiazolinyl, as vinyl, the 1-acrylic, the 2-acrylic, the 1-methyl ethylene, the 1-cyclobutenyl, the 2-cyclobutenyl, the 3-cyclobutenyl, 1-methyl isophthalic acid-acrylic, 2-methyl isophthalic acid-acrylic, 1-methyl-2-acrylic, 2-methyl-2-acrylic, the 1-pentenyl, the 2-pentenyl, the 3-pentenyl, the 4-pentenyl, 1-methyl isophthalic acid-cyclobutenyl, the 2-methyl-1-butene thiazolinyl, the 3-methyl-1-butene base, 1-methyl-2-butene base, 2-methyl-2-butene base, 3-methyl-2-butene base, 1-methyl-3-cyclobutenyl, 2-methyl-3-cyclobutenyl, 3-methyl-3-cyclobutenyl, 1,1-dimethyl-2-acrylic, 1,2-dimethyl-1-acrylic, 1,2-dimethyl-2-acrylic, 1-ethyl-1-acrylic, 1-ethyl-2-acrylic, the 1-hexenyl, the 2-hexenyl, the 3-hexenyl, the 4-hexenyl, the 5-hexenyl, 1-methyl-1-pentene thiazolinyl, 2-methyl-1-pentene thiazolinyl, 3-methyl-1-pentene thiazolinyl, the 4-methyl-1-pentene base, 1-methyl-2-pentenyl, 2-methyl-2-pentenyl, 3-methyl-2-pentenyl, 4-methyl-2-pentenyl, 1-methyl-3-pentenyl, 2-methyl-3-pentenyl, 3-methyl-3-pentenyl, 4-methyl-3-pentenyl, 1-methyl-4-pentenyl, 2-methyl-4-pentenyl, 3-methyl-4-pentenyl, 4-methyl-4-pentenyl, 1,1-dimethyl-2-cyclobutenyl, 1,1-dimethyl-3-cyclobutenyl, 1,2-dimethyl-1-cyclobutenyl, 1,2-dimethyl-2-cyclobutenyl, 1,2-dimethyl-3-cyclobutenyl, 1,3-dimethyl-1-cyclobutenyl, 1,3-dimethyl-2-cyclobutenyl, 1,3-dimethyl-3-cyclobutenyl, 2,2-dimethyl-3-cyclobutenyl, 2,3-dimethyl-1-cyclobutenyl, 2,3-dimethyl-2-cyclobutenyl, 2,3-dimethyl-3-cyclobutenyl, 3,3-dimethyl-1-cyclobutenyl, 3,3-dimethyl-2-cyclobutenyl, 1-ethyl-1-cyclobutenyl, 1-ethyl-2-cyclobutenyl, 1-ethyl-3-cyclobutenyl, 2-ethyl-1-cyclobutenyl, 2-ethyl-2-cyclobutenyl, 2-ethyl-3-cyclobutenyl, 1,1,2-trimethyl-2-acrylic, 1-ethyl-1-methyl-2-acrylic, 1-ethyl-2-methyl isophthalic acid-acrylic and 1-ethyl-2-methyl-2-acrylic;

Alkynyl: have 2 to 4,6 or 8 carbon atoms and at an arbitrary position on have the straight or branched alkyl of triple bond, C for example ₂-C ₆Alkynyl, as acetenyl, the 1-propinyl, 2-propynyl, the 1-butynyl, the 2-butynyl, the 3-butynyl, 1-methyl-2-propynyl, the 1-pentynyl, the valerylene base, the 3-pentynyl, the 4-pentynyl, 1-methyl-2-butynyl, 1-methyl-3-butynyl, 2-methyl-3-butynyl, 3-methyl isophthalic acid-butynyl, 1,1-dimethyl-2-propynyl, 1-ethyl-2-propynyl, 1-hexin base, 2-hexin base, 3-hexin base, 4-hexin base, 5-hexin base, 1-methyl-valerylene base, 1-methyl-3-pentynyl, 1-methyl-4-pentynyl, 2-methyl-3-pentynyl, 2-methyl-4-pentynyl, 3-methyl-1-pentene alkynyl, 3-methyl-4-pentynyl, 4-methyl-1-pentene alkynyl, 4-methyl-valerylene base, 1,1-dimethyl-2-butynyl, 1,1-dimethyl-3-butynyl, 1,2-dimethyl-3-butynyl, 2,2-dimethyl-3-butynyl, 3,3-dimethyl-1-butynyl, 1-ethyl-2-butynyl, 1-ethyl-3-butynyl, 2-ethyl-3-butynyl and 1-ethyl-1-methyl-2-propynyl;

Cycloalkyl: have the monocyclic saturated hydrocarbon group base of 3 to 6 carboatomic ring atoms, as cyclopropyl, cyclobutyl, cyclopenta and cyclohexyl;

Cycloalkenyl group: have 3 to 8 carboatomic ring atoms and have the monocycle non-aromatic hydrocarbon base of at least one two key, as cyclopentene-1-base, cyclohexene-1-base, ring heptan-1,3-diene-1-base;

Alkoxy carbonyl: (CO-) be connected to alkoxy base (as mentioned above) on the skeleton with 1 to 6 carbon atom by carbonyl;

Oxygen base alkylidene oxygen base: have 1 to 3 CH ₂The unbranched chain of the divalence of group, wherein two chemical valences all are connected on the skeleton by oxygen atom, for example OCH ₂O, OCH ₂CH ₂O and OCH ₂CH ₂CH ₂O;

Contain one to four heteroatomic five to ten yuan saturated or undersaturated heterocycle of part that is selected from oxygen, nitrogen and sulphur: except that carboatomic ring atom, also contain one to three nitrogen-atoms and/or oxygen or sulphur atom or one or two oxygen and/or the monocycle of sulphur atom or the heterocycles (heterocyclic radical) of two rings; If this ring contains a plurality of oxygen atoms, these oxygen atoms direct neighbor not then; Oxyranyle for example, aziridinyl, the 2-tetrahydrofuran base, the 3-tetrahydrofuran base, the 2-tetrahydro-thienyl, the 3-tetrahydro-thienyl, the 2-pyrrolidinyl, the 3-pyrrolidinyl, the 3-isoxazole alkyl, the 4-isoxazole alkyl, the 5-isoxazole alkyl, 3-isothiazole alkyl, 4-isothiazole alkyl, 5-isothiazole alkyl, the 3-pyrazolidinyl, the 4-pyrazolidinyl, the 5-pyrazolidinyl, 2-oxazole alkyl, 4-oxazole alkyl, 5-oxazole alkyl, the 2-thiazolidinyl, the 4-thiazolidinyl, the 5-thiazolidinyl, the 2-imidazolidinyl, the 4-imidazolidinyl, 1,2,4-oxadiazole alkane-3-base, 1,2,4-oxadiazole alkane-5-base, 1,2,4-thiadiazolidine-3-base, 1,2,4-thiadiazolidine-5-base, 1,2,4-triazolidine-3-base, 1,3,4-oxadiazole alkane-2-base, 1,3,4-thiadiazolidine-2-base, 1,3,4-triazolidine-2-base, 2,3-dihydrofuran-2-base, 2,3-dihydrofuran-3-base, 2,4-dihydrofuran-2-base, 2,4-dihydrofuran-3-base, 2,3-dihydro-thiophene-2-base, 2,3-dihydro-thiophene-3-base, 2,4-dihydro-thiophene-2-base, 2,4-dihydro-thiophene-3-base, 2-pyrrolin-2-base, 2-pyrrolin-3-base, 3-pyrrolin-2-base, 3-pyrrolin-3-base, 2-isoxazoline-3-base, 3-isoxazoline-3-base, 4-isoxazoline-3-base, 2-isoxazoline-4-base, 3-isoxazoline-4-base, 4-isoxazoline-4-base, 2-isoxazoline-5-base, 3-isoxazoline-5-base, 4-isoxazoline-5-base, 2-isothiazoline-3-base, 3-isothiazoline-3-base, 4-isothiazoline-3-base, 2-isothiazoline-4-base, 3-isothiazoline-4-base, 4-isothiazoline-4-base, 2-isothiazoline-5-base, 3-isothiazoline-5-base, 4-isothiazoline-5-base, 2,3-pyrazoline-1-base, 2,3-pyrazoline-2-base, 2,3-pyrazoline-3-base, 2,3-pyrazoline-4-base, 2,3-pyrazoline-5-base, 3,4-pyrazoline-1-base, 3,4-pyrazoline-3-base, 3,4-pyrazoline-4-base, 3,4-pyrazoline-5-base, 4,5-pyrazoline-1-base, 4,5-pyrazoline-3-base, 4,5-pyrazoline-4-base, 4,5-pyrazoline-5-base, 2,3-dihydro-oxazole-2-base, 2,3-dihydro-oxazole-3-base, 2,3-dihydro-oxazole-4-base, 2,3-dihydro-oxazole-5-base, 3,4-dihydro-oxazole-2-base, 3,4-dihydro-oxazole-3-base, 3,4-dihydro-oxazole-4-base, 3,4-dihydro-oxazole-5-base, the 2-piperidyl, the 3-piperidyl, the 4-piperidyl, 1,3-diox-5-base, the 2-THP trtrahydropyranyl, the 4-THP trtrahydropyranyl, the 2-tetrahydro-thienyl, 3-hexahydro-pyridazine base, 4-hexahydro-pyridazine base, 2-hexahydropyrimidine base, 4-hexahydropyrimidine base, 5-hexahydropyrimidine base, the 2-piperazinyl, 1,3,5-Hexahydrotriazine-2-base and 1,2,4-Hexahydrotriazine-3-base;

Contain one to four heteroatomic five to ten membered aromatic heterocycle that are selected from oxygen, nitrogen and sulphur: the heteroaryl of monocycle or two rings, for example

- Contain 5 of one to four nitrogen-atoms or one to three nitrogen-atoms and sulphur or oxygen atom Unit's heteroaryl:Except that carbon atom, also can contain one to four nitrogen-atoms or one to three nitrogen-atoms and sulphur or oxygen atom 5 yuan of heteroaryls as annular atoms, 2-furyl for example, the 3-furyl, the 2-thienyl, the 3-thienyl, the 2-pyrrole radicals, the 3-pyrrole radicals, the 3-isoxazolyl, the 4-isoxazolyl, the 5-isoxazolyl, the 3-isothiazolyl, the 4-isothiazolyl, the 5-isothiazolyl, the 3-pyrazolyl, the 4-pyrazolyl, the 5-pyrazolyl, the 2-oxazolyl, the 4-oxazolyl, the 5-oxazolyl, the 2-thiazolyl, the 4-thiazolyl, the 5-thiazolyl, the 2-imidazole radicals, the 4-imidazole radicals, 1,2,4-oxadiazole-3-base, 1,2,4-oxadiazole-5-base, 1,2,4-thiadiazoles-3-base, 1,2,4-thiadiazoles-5-base, 1,2,4-triazole-3-base, 1,3,4-oxadiazole-2-base, 1,3,4-thiadiazoles-2-base and 1,3,4-triazole-2-base;

- The benzo that contains one to three nitrogen-atoms or nitrogen-atoms and oxygen or sulphur atom 5 yuan of heteroaryls that condense:Following 5 yuan of heteroaryls, wherein except that carbon atom, also can contain one to four nitrogen-atoms or one to three nitrogen-atoms and sulphur or oxygen atom as annular atoms, and two adjacent carboatomic ring atoms or nitrogen and the adjacent carboatomic ring atom fourth-1 that can be replaced by nitrogen-atoms by one or two carbon atom wherein wherein, 3-diene-1,4-two basic bridgings;

- Connect and 5 yuan of heteroaryls that contain one to four nitrogen-atoms perhaps pass through nitrogen by nitrogen The 5 yuan of benzo-fused heteroaryls that connect and contain one to three nitrogen-atoms:Following 5 yuan of heteroaryls, wherein except that carbon atom, also can contain one to four nitrogen-atoms or one to three nitrogen-atoms as annular atoms, and two adjacent carboatomic ring atoms or nitrogen and the adjacent carboatomic ring atom fourth-1 that can be replaced by nitrogen-atoms by one or two carbon atom wherein wherein, 3-diene-1,4-two basic bridgings, wherein these rings can be connected on the skeleton by one of azo-cycle atom, described 5 yuan of heteroaryls are 1-pyrrole radicals, 1-pyrazolyl, 1 for example, 2,4-triazol-1-yl, 1-imidazole radicals, 1,2,3-triazoles-1-base, 1,3, the 4-triazol-1-yl;

- 6 yuan of heteroaryls that wherein contain one to three or one to four nitrogen-atoms:Except that carbon atom, also can contain one to three or one to four nitrogen-atoms 6 yuan of heteroaryl groups as annular atoms, 3-pyridazinyl, 4-pyridazinyl, 2-pyrimidine radicals, 4-pyrimidine radicals, 5-pyrimidine radicals, 2-pyrazinyl, 1,3,5-triazines-2-base and 1 for example, 2,4-triazine-3-base.

Formula I and Ia compound can be by known generally method preparations.The feasible route of the Ib compound of a kind of synthetic wherein Y=N and Z=CH is illustrated in scheme 1.At this, each symbol as above defines.R ⁶As above definition.In addition, R ⁶Also can represent wherein each symbol group C (R as defined above ¹⁴) ₂A.

Scheme 1

R when wherein, synthesizing Ia type compound ⁶Be C (R ¹⁴) ₂A.

Synthetic (the Houben-Weyl on the books in the literature of the thiazole compound that II and III type replace, Methoden der Organischen Chemie[organic chemistry method], volume E6b, Hetarene III/Teil 2, Thieme Verlag 1994, the 1-361 pages or leaves; Also can be referring to WO-A 2005/012298 especially; WO-A 2004/056368; WO-A 2001/072745).Thus, for example, thiazole II can carry out condensation and synthesize by α-Lu Daitong that will suitably replace and the thioamides that suitably replaces or (randomly N-replaces) thiocarbamide according to the Hantzsch method.Perhaps, these thiazoles can prepare by using phosphorus pentasulfide for example that α-acylamino-ketone is carried out cyclizative condensation (modification that Robinson-Gabriel is synthetic).Thiazole-5-ylmethyl ketone III can obtain by for example the unsubstituted thiazole compound of 5-being carried out the Friedel-Crafts acidylate.

Perhaps, the thiazole of III type-5-ylmethyl ketone can be by following thiazolyl-5-carboxylic acid derivates preparation; The various routes of realizing this purpose have been recorded in the document and (for example the methyl Grignard reagent have been added to the iron catalytic addition reaction on the phosgene: J.Org.Chem.2004,69,3943; The methyl Grignard reagent is added to addition reaction on the Weinreb acid amides: Synlett 1999,1091; Malonate is added on the phosgene, carries out two decarboxylic reaction: Tetrahedron 1992,48,9233 subsequently; The methyl Grignard reagent is added to addition reaction on the nitrile: J.Am.Chem.Soc.1956,78,2141).

In condensation reaction, thiazolyl ketone III reacts with the compound of the methylene with activation, obtains enamino ketone IV (Chem.Ber.1964,97,3397).In this way the preparation 1,3-dicarbapentaborane equivalent can carry out condensation to obtain pyrimidines i b with guanidine V or its salt then.

If guanidine V that replaces or corresponding guanidinesalt can by make suitable amine and cyanamide by in a kind of suitable solvent such as ethanol, be adapted at stoichiometric inorganic acid such as red fuming nitric acid (RFNA) or concentrated hydrochloric acid in the presence of heat to react and prepare that (US 1972/3681459; US 1975/3903159; US 1976/3076787).

Perhaps, compounds ib can be by 2, and the dibasic thiazole-5-carboxylic acid derivative of 4-VI synthesizes (scheme 2).

Scheme 2

Wherein, when synthesizing Ia type compound, R ⁶Be C (R ¹⁴) ₂A; Alkyl independently of one another=branched or unbranched C ₁-C ₄Alkyl.

Derivative VI can be by making 2-halo-1,3-dicarbonyl compound such as 2-halo-3-keto ester, 2-halo-3-ketone nitrile or 2-halo malonate nitrile carry out condensation reaction and obtain (Houben-Weyl, Methoden der Organischen Chemie[organic chemistry method], volume E6b, Hetarene III/Teil 2, Thieme Verlag 1994, the 1-361 pages or leaves).

The present invention also provides VIII type intermediate.Equally, the invention provides the conversion process that VIII type intermediate is converted into compounds ib.This method is applicable to and particularly prepares Compound I a and I.

For this reason, the thiazole carboxylic acid can be converted into corresponding phosgene VII (J.Chem.Soc.Perkin.Trans.I1982 for example, 159 by known method; J.Heterocycl.Chem.1985,22,1621; J.Med.Chem.1999,42,5064; J.Fluorine Chem.2004,125,1287).These materials at room temperature are converted into corresponding trialkylsilkl acetylenic ketone VIII (Org.Lett.2003,5,3451 then under the Sonogashira condition; Synthesis2003,2815).Preferred palladium catalyst is (Ph ₃P) ₂PdCl ₂Preferred co-catalyst is CuI.Preferred stoichiometric additive alkali is a triethylamine.The Sonogashira reaction is preferably implemented in THF, but the also suitable reaction medium of doing of acetonitrile or other solvent---as ether or the like---.

In addition, alternative route of preparation trialkylsilkl acetylenic ketone is recorded in the document and ((trimethyl silyl) lithium acetylide is added to addition reaction on the Weinreb acid amides: Synth.Commun.1993,23,487; The Friedel-Crafts acylation reaction of two (trimethyl silyl) acetylene: J.Org.Chem.1973,38,2254; Stille coupling reaction with tributyl (trimethyl silyl alkynyl) stannane: J.Org.Chem.1982,47,2549).

Trialkylsilkl acetylenic ketone VIII carries out condensation reaction with guanidine V or its salt then, to obtain target compound Ib.For this reason, raw material---just use for example guanidinesalt of potash of additive alkali---a kind of suitable solvent for example in DMF or the 2-methyl cellosolve, at 100 ℃ of reaction 4-20h down.In addition, it is admissible using other solvent (for example alcohols) and other additive alkali.

Perhaps, the trialkylsilkl acetylenic ketone can prepare under the Sonogashira condition, and this condensation reaction that obtains aminopyrimidine can be implemented with one pot of method (one-pot process); For this reason, after coupling reaction is implemented, add a kind of cosolvent such as methyl alcohol if necessary, and make this mixture back flow reaction some hrs (Org.Lett.2003,5,3451; Synthesis2003,2815).

Obtain compound (I) and (Ia) like this, condition is that among two symbol Y or the Z represents nitrogen-atoms and the remaining optional carbon atom that replaces of another symbology.

It is known or can be by obtaining with method like the document category by document to implement the needed thiazole carboxylic acid ester VI of the inventive method.The reaction that obtains thiazole phosgene VII is implemented by literature method.Trialkyl silane ketone (silanone) VIII obtains in the mode that is similar to literature method.Guanidine V obtains by literature method equally.

Noble metal catalyst and a kind of co-catalyst that method of the present invention preferably uses a kind of routine to be used for this reaction are implemented.Preferred palladium catalyst is (Ph ₃P) ₂PdCl ₂Preferred co-catalyst is CuI.

Method of the present invention preferably uses one or more thinners to implement.Suitable diluent is nearly all inert organic solvents.These inert organic solvents preferably include the aliphatic hydrocarbon and the aromatic hydrocarbons of optional halo, for example pentane, hexane, heptane, cyclohexane, benzinum, gasoline, raw gasoline, benzene,toluene,xylene, carrene, ethlyene dichloride, chloroform, carbon tetrachloride, chlorobenzene and o-dichlorohenzene; Ether, as diethyl ether and butyl oxide, glycol dimethyl ether and diethylene glycol dimethyl ether, oxolane is with diox; Ketone is as acetone, methyl. ethyl ketone, methyl. and nezukone or methyl. isobutyl ketone; Ester is as methyl acetate or ethyl acetate; Nitrile, for example acetonitrile or propionitrile; Acid amides, for example dimethyl formamide, dimethylacetylamide and N-Methyl pyrrolidone and dimethyl sulfoxide (DMSO), sulfolane and hexamethyl phosphoric triamide.Preferred oxolane, diethyl ether or the acetonitrile of using.

Reaction temperature in the inventive method can change in wide relatively scope.In general, this method is implemented under 0 ℃ to 250 ℃, preferred 10 ℃ to 65 ℃ temperature.

If use guanidinesalt, the method for preparation formula Ib compound then of the present invention preferably uses one or more reaction promoters to implement.

If the inorganic or organic alkali or the acid acceptor of---suitable---routine that suitable reaction promoter is.These alkali or acid acceptor preferably include the acetate of alkali metal or alkaline earth metal, amides, carbonate, bicarbonate, hydride, hydroxide or alkoxide, sodium acetate for example, potassium acetate or calcium acetate, lithium amide, sodium amide, amination potassium or amination calcium, sodium carbonate, potash or calcium carbonate, sodium bicarbonate, saleratus or calcium bicarbonate, lithium hydride, sodium hydride, hydrofining or calcium hydride, lithium hydroxide, sodium hydroxide, potassium hydroxide or slaked lime, sodium methoxide, caustic alcohol, just or sodium isopropylate, just, different, the second month in a season or sodium tert-butoxide, perhaps potassium methoxide, potassium ethoxide, just or potassium isopropoxide, just, different, the second month in a season or potassium tert-butoxide; In addition, also has for example trimethylamine of alkaline organic nitrogen compound, triethylamine, tripropyl amine (TPA), tri-n-butylamine, ethyl diisopropyl amine, N, the N-dimethylcyclohexylam,ne, dicyclohexylamine, the ethyl dicyclohexylamine, N, accelerine, N, the N-dimethyl benzylamine, pyridine, the 2-methyl-, the 3-methyl-, the 4-methyl-, 2, the 4-dimethyl-, 2, the 6-dimethyl-, 3, the 4-dimethyl-and 3, the 5-lutidines, aldehydecollidine, 4-dimethylaminopyridine, the N-methyl piperidine, 1,4-diazabicyclo [2.2.2] octane (DABCO), 1,5-diazabicyclo [4.3.0] ninth of the ten Heavenly Stems-5-alkene (DBN) or 1,8 diazabicyclo [5.4.0], 11 carbon-7-alkene (DBU).The preferred potash that uses.

Method of the present invention preferably uses one or more thinners to implement.Suitable diluent is nearly all inert organic solvents.These inert organic solvents preferably include the aliphatic hydrocarbon and the aromatic hydrocarbons of optional halo, for example pentane, hexane, heptane, cyclohexane, benzinum, gasoline, raw gasoline, benzene,toluene,xylene, carrene, ethlyene dichloride, chloroform, carbon tetrachloride, chlorobenzene and o-dichlorohenzene; Ether, as diethyl ether and butyl oxide, glycol dimethyl ether and diethylene glycol dimethyl ether, oxolane is with diox; Ketone is as acetone, methyl. ethyl ketone, methyl. and nezukone or methyl. isobutyl ketone; Ester is as methyl acetate or ethyl acetate; Nitrile, for example acetonitrile or propionitrile; Acid amides, for example dimethyl formamide, dimethylacetylamide and N-Methyl pyrrolidone and dimethyl sulfoxide (DMSO), sulfolane and hexamethyl phosphoric triamide.Yet, also can use alcohol, for example methyl alcohol, ethanol, propyl alcohol, isopropyl alcohol, butanols, isobutanol, 2-methyl cellosolve.Preferred dimethyl formamide and 2-methyl cellosolve.

In the inventive method, reaction temperature can change in wide relatively scope.In general, this method is implemented under 0 ℃ to 250 ℃, preferred 10 ℃ to 120 ℃ temperature.

The inventive method is under atmospheric pressure implemented usually.Yet, also can under the pressure of elevated pressure or reduction, implement.

In order to implement the inventive method, needed raw material uses with about equimolar amounts usually under the various situations.Yet, also can be relatively excessively use under the various situations a kind of in the used component in a large number.Post processing is implemented (seeing preparation embodiment) with conventional method separately in the inventive method.

The analog of the 2-4-Disubstituted pyridine of I or Ia type (Z and Y are carbon) can be by the known method of document synthetic (J.Med.Chem.2003,46 (15), 3230-3244; J.Med.Chem.1985,28 (11), 1628-36; US 6218537).

The analog of the dibasic 1,3,5-triazines of 2-4-of I or Ia type (Z and Y are nitrogen) also can synthetic (Heterocycles 1992,34 (5), 929-35 by the known method of document; Austr.J.Chem.1981,34 (3), 623-34).

The isomer of the dibasic pyrimidine of 4-6-of I or Ia type (Y is a carbon) also can be synthetic by the known method of document (J.Heterocycl Chem.1980,17 (7), 1385-7).

The synthetic of bridging compound (bridged compound) Ic also can be finished by known method.A kind of feasible synthetic route (is being also recorded in WO 2005/005438) shown in the scheme 3:

Scheme 3

Ring-type 1,3-diketone IX or commercially availablely get or can easily obtain by the method for putting down in writing in the document.Heterocycle 1, the synthetic for example J.Org.Chem.1977 that is recorded in of 3-diketone, (R in 42,1163 _a-R _b=-O-CH ₂-or-S-CH ₂-).Suitable ring-type 1, the bromination of 3-diketone is recorded in J.Chem.Soc.1965, and 353; J.Chem.Soc.Perkin Trans.I 1987,2153 or Z.Chem.1967 in 7,422, and obtain corresponding 2-bromination ring-type 1,3-diketone X, and the reaction of this compounds X and thioamides or thiocarbamide is to obtain corresponding thiazole XI then.As the replaceable scheme of bromination, also can implement to use SOCl ₂The chlorination of carrying out is recorded in J.Prakt.Chem.1963,20 (5-6), in 285 or Tetrahedron Lett.1967,34,3331.Formoxyl can be by for example Ethyl formate, reaction under alkali condition are introduced with formic acid derivates.Obtain in this way 1,3-dicarbonyl compound XII can with amidine or guanidine V or the direct condensation of its salt; This reaction is recorded in for example Gazz.Chim.Ital.1973, in 103,1063.Perhaps, this acyl compounds can at first be converted into enamine ketone (Chem.Ber.1964,97,3397), can carry out condensation with amidine or guanidine V or its salt then.Fully aromatization or undersaturated compound can for example obtain by oxidation.

Begin with 2-methyl-4-(beta-hydroxy carbonyl ethyl) thiazolyl-5-carboxylic acid or 2-methyl-4-(beta-hydroxy carbonyl butyl) thiazolyl-5-carboxylic acid XIII, synthetic (the J.Prakt.Chem.1963 on the books of XI type thiazolyl ketone precursor, 20 (5-6), 285-90).Be summarized in the scheme 4.

Scheme 4

The present invention is used for the method for preparation formula Ic compound and preferably uses one or more reaction promoters to implement.

If the inorganic or organic alkali or the acid acceptor of---suitable---routine that suitable reaction promoter is.These alkali or acid acceptor preferably include the acetate of alkali metal or alkaline earth metal, amides, carbonate, bicarbonate, hydride, hydroxide or alkoxide, sodium acetate for example, potassium acetate or calcium acetate, lithium amide, sodium amide, amination potassium or amination calcium, sodium carbonate, potash or calcium carbonate, sodium bicarbonate, saleratus or calcium bicarbonate, lithium hydride, sodium hydride, hydrofining or calcium hydride, lithium hydroxide, sodium hydroxide, potassium hydroxide or slaked lime, sodium methoxide, caustic alcohol, just or sodium isopropylate, just, different, the second month in a season or sodium tert-butoxide, perhaps potassium methoxide, potassium ethoxide, just or potassium isopropoxide, just, different, the second month in a season or potassium tert-butoxide; In addition, also has for example trimethylamine of alkaline organic nitrogen compound, triethylamine, tripropyl amine (TPA), tri-n-butylamine, ethyl diisopropyl amine, N, the N-dimethylcyclohexylam,ne, dicyclohexylamine, the ethyl dicyclohexylamine, N, accelerine, N, the N-dimethyl benzylamine, pyridine, the 2-methyl-, the 3-methyl-, the 4-methyl-, 2, the 4-dimethyl-, 2, the 6-dimethyl-, 3, the 4-dimethyl-and 3, the 5-lutidines, aldehydecollidine, 4-dimethylaminopyridine, the N-methyl piperidine, 1,4-diazabicyclo [2.2.2] octane (DABCO), 1,5-diazabicyclo [4.3.0] ninth of the ten Heavenly Stems-5-alkene (DBN) or 1,8 diazabicyclo [5.4.0], 11 carbon-7-alkene (DBU).

Method of the present invention preferably uses one or more thinners to implement.Suitable diluent is nearly all inert organic solvents.These inert organic solvents preferably include the aliphatic hydrocarbon and the aromatic hydrocarbons of optional halo, for example pentane, hexane, heptane, cyclohexane, benzinum, gasoline, raw gasoline, benzene,toluene,xylene, carrene, ethlyene dichloride, chloroform, carbon tetrachloride, chlorobenzene and o-dichlorohenzene; Ether, as diethyl ether and butyl oxide, glycol dimethyl ether and diethylene glycol dimethyl ether, oxolane is with diox; Ketone is as acetone, methyl. ethyl ketone, methyl. and nezukone or methyl. isobutyl ketone; Ester is as methyl acetate or ethyl acetate; Nitrile, for example acetonitrile or propionitrile; Acid amides, for example dimethyl formamide, dimethylacetylamide and N-Methyl pyrrolidone and dimethyl sulfoxide (DMSO), sulfolane and hexamethyl phosphoric triamide.

In the inventive method, reaction temperature can change in wide relatively scope.Generally speaking, this method is implemented under 0 ℃ to 250 ℃, preferred 10 ℃ to 185 ℃ temperature.

In order to implement the inventive method, needed raw material uses with about equimolar amounts usually under the various situations.Yet, also can be relatively excessively use under the various situations a kind of in the required component in a large number.Post processing is implemented (seeing preparation embodiment) with conventional method separately in the inventive method.

With with the similar mode of known method, also can by the 5-bromethiazole that replaces or 5-iodo thiazole XIV---be referred to herein as 5-halo thiazole---and the optional pyrimidine XV that replaces prepares Id type compound.In this pyrimidine XV, R ¹⁰As above definition.A kind of feasible synthetic route is illustrated in scheme 5.

Scheme 5

Some 5-halo thiazole XIV is known, and perhaps they are by carrying out bromination with conventional method to known thiazole compound or iodate prepares (Organikum, the 21st edition, Wiley-VCH, 2001).At first, use metal or metallorganic (metal organyl) for example n-BuLi 5-halo thiazole XIV is metallized.Then the organo-metallic compound that obtains is joined among the corresponding 2-Chloropyrimide XV, form dihydro-pyrimidin.By with oxidant for example 4,5-two chloro-3,6-dioxo hexamethylene-1,4-diene-1,2-dintrile (DDQ) reaction, the dihydro-pyrimidin that obtains by aromatization again to obtain pyrimidine XVI (J.Heterocyclic Chem.1990,27,1393; J.Org.Chem.1988,53,4137).Pyrimidine XVI then by conventional method under the condition of acid, alkalescence or metal catalytic, also can be under the condition that does not have catalyzer if suitable, react with the amine of formula XVII, obtain target compound Id (Houben-Weyl, Methodender organischen Chemie; J.Med.Chem.2004,47,4716-4730; J.Med.Chem.2004,47,2724-2727, Org.Lett.2002,4,3481-3484; GB2369359; WO 2002/096888).XVI type intermediate is new.This method is also by the invention provides.Especially, this method is suitable for preparing Ia and I compound.

The 2-Chloropyrimide of formula XV is known and/or can be prepared (Houben-Weyl, Methoden der organischen Chemie) by known method.

The suitable diluent that is used to implement the inventive method first step is all inert organic solvents.These inert organic solvents preferably include aliphatic hydrocarbon, alicyclic or aromatic hydrocarbons, for example benzinum, hexane, heptane, cyclohexane, hexahydrotoluene, benzene,toluene,xylene or naphthalane; Halogenated hydrocarbons, for example chlorobenzene, dichloro-benzenes, carrene, chloroform, carbon tetrachloride, dichloroethane or trichloroethanes; Ether is as diethyl ether, diisopropyl ether, methyl. tertbutyl ether, methyl-tert-amyl ether, diox, oxolane, 1,2-dimethoxy-ethane, 1,2-diethoxyethane or anisole; Ketone is as acetone, butanone, methyl. isobutyl ketone or cyclohexanone; Nitrile, for example acetonitrile, propionitrile, just or isobutyronitrile or benzonitrile; Acid amides, N for example, dinethylformamide, N,N-dimethylacetamide, formanilide, N-Methyl pyrrolidone or hexamethyl phosphoric triamide.

In the first step of the inventive method, be used to make metallized suitable metal of 5-halo thiazole XIV or metallorganic, except that n-BuLi, also can be all metals or the metallorganic that are applicable to the preparation metallorganic.These metals or metallorganic preferably include the metal of first and second main groups in the periodic table, for example lithium or magnesium, perhaps its metallorganic, for example lithium methide, phenyl lithium, the second month in a season or tert-butyl lithium or methyl magnesium bromine.

Be applicable to the oxidant that in the first step of the inventive method, dihydro-pyrimidin is carried out again aromatisation, remove 4,5-two chloro-3,6-dioxo hexamethylene-1,4-diene-1 outside the 2-dintrile (DDQ), also has other oxidant.These oxidants preferably include other quinones, and for example 2,3,5,6-tetrachloro [1,4] benzoquinones (chloranil); N-halo imidodicarbonic diamide, for example N-bromosuccinimide; Sulphur or selenium; With the group that photochemistry, radiochemistry or hot mode produce, especially be the group at those oxygen atom places, as hydroxyl, hydroperoxyl or alkoxy base.

The suitable diluent that is used to implement second step of the inventive method is all organic solvents.These organic solvents preferably include aliphatic hydrocarbon, alicyclic or aromatic hydrocarbons, for example benzinum, hexane, heptane, cyclohexane, hexahydrotoluene, benzene,toluene,xylene or naphthalane; Halogenated hydrocarbons, for example chlorobenzene, dichloro-benzenes, carrene, chloroform, carbon tetrachloride, dichloroethane or trichloroethanes; Alcohol, for example methyl alcohol, ethanol, normal propyl alcohol, isopropyl alcohol, n-butanol, isobutanol; Water; Ether is as diethyl ether, diisopropyl ether, methyl. tertbutyl ether, methyl. and tert-amyl ether, diox, oxolane, 1,2-dimethoxy-ethane, 1,2-diethoxyethane or anisole; Ketone is as acetone, butanone, methyl. isobutyl ketone or cyclohexanone; Nitrile, for example acetonitrile, propionitrile, just or isobutyronitrile or benzonitrile; Acid amides, N for example, dinethylformamide, N,N-dimethylacetamide, formanilide, N-Methyl pyrrolidone or hexamethyl phosphoric triamide, the perhaps mixture of they and water.

In second step of the inventive method,, in the presence of a kind of suitable acid acceptor, implement if suitable.Suitable acid acceptor is the inorganic or organic alkali of all routines.These alkali preferably include the hydride of alkali metal or alkaline earth metal, hydroxide, amides, alkoxide, acetate, carbonate or bicarbonate, sodium hydride for example, sodium amide, the diisopropylaminoethyl lithium, sodium methoxide, caustic alcohol, potassium tert-butoxide, sodium hydroxide, potassium hydroxide, sodium acetate, sodium carbonate, potash, saleratus, sodium bicarbonate or ammonium carbonate, and tertiary amine, as trimethylamine, triethylamine, tri-n-butylamine, N, accelerine, N, N-dimethyl-benzylamine, pyridine, the N-methyl piperidine, N-methylmorpholine, N, the N-dimethyl aminopyridine, diazabicyclo octane (DABCO), diazabicyclo-nonene (DBN) or diazabicyclo endecatylene (DBU).

If suitable, second step of the inventive method also can implement in the presence of a kind of suitable acid.Suitable acid is preferably inorganic acid example hydrochloric acid or sulfuric acid, and organic acid such as formic acid, acetate, 4-toluene sulfonic acide or ascorbic acid.

If suitable, second step of the inventive method also can implement in the presence of a kind of appropriate catalyst.Appropriate catalyst especially is palladium salt or complex compound.What be preferred for this purpose is that palladium bichloride, acid chloride, four (triphenyl phasphine) close palladium or two (triphenyl phasphine) palladium chloride.For palladium complex, also can be by palladium salt and complex compound part are separately added in the reaction to make its generation in reactant mixture.Preferred part is an organic phosphorus compound.Mode that can example is mentioned following compound: triphenyl phasphine, three-o-tolyl phosphine, 2,2 '-two (diphenylphosphino)-1,1 '-dinaphthalene, dicyclohexylphosphontetrafluoroborate biphenyl, 1, two (diphenylphosphino) butane of 4-, two diphenylphosphino ferrocene, two (tert-butyl group phosphino-) biphenyl, two (cyclohexyl phosphino-) biphenyl, 2-dicyclohexyl phosphino--2 ' N, N-dimethylamino biphenyl, tricyclohexyl phosphine, tri-butyl phosphine, 2,2 '-two diphenylphosphine bases (phosphanyl)-[1,1 '] dinaphthalene (binaphthalenyl), 4, the two diphenylphosphine base dibenzofuran of 6-.Yet, also can be without part.

The reaction temperature that is used to implement the inventive method can change in wide relatively scope.Generally speaking, this method-100 ℃ to 150 ℃, preferred-80 ℃ to 110 ℃, extremely especially preferred-80 ℃ to 70 ℃ temperature, implement.

The inventive method is under atmospheric pressure implemented usually.Yet, also can---be generally 0.1 crust---and implement down at the pressure of elevated pressure or reduction to 10 crust.

The compounds of this invention has strong microbiocidal activity, can be used to prevent and treat harmful microorganism in the protection of crop protection neutralization materials, as fungi and bacterium.

Fungicide can be used to prevent and treat for example plasmodiophora brassicae (Plasmodiophoromycete), oomycetes (Oomycete), chytrid (Chytridiomycete), zygomycete (Zygomycete), sac fungi (Ascomycete), basidiomycetes (Basidiomycete) and imperfect fungus (Deuteromycete) in crop protection.

Bactericide can be used to prevent and treat for example pseudomonad (Pseudomonadaceae), rhizobium (Rhizobiaceae), enterobacteria (Enterobacteriaceae), corynebacterium (Corynebacteriaceae) and streptomycete (Streptomycetaceae) in crop protection.

Thiazole compound of the present invention has extraordinary fungicidal properties, can be used for preventing and treating phytopathogenic fungi, for example plasmodiophora brassicae, oomycetes, chytrid, zygomycete, sac fungi, basidiomycetes and imperfect fungus etc.

As an example but some cause the pathogene of fungal disease and bacteriosis so that unrestriced mode can propose to be included into above-mentioned generic name:

Yellow unit cell (Xanthomonas) bacterial classification, for example pathogenic mutation (Xanthomonas campestris pv.oryzae) of xanthomonas campestris paddy rice;

False unit cell (Pseudomonas) bacterial classification, for example pathogenic mutation (Pseudomonas syringae pv.lachrymans) of pseudomonas syringae cucumber;

Ou Wenshi (Erwinia) bacterial classification is for example separated starch Erwinia (Erwiniaamylovora);

By the disease that the powdery mildew pathogene causes, described pathogene for example

Bu Shi Erysiphe (Blumeria) bacterial classification, for example grass family Bu Shi powdery mildew (Blumeriagraminis);

Podosphaera (Podosphaera) bacterial classification, for example white cross hair list softgel shell (Podosphaera leucotricha);

Single softgel shell belongs to (Sphaerotheca) bacterial classification, for example garden balsam list softgel shell (Sphaerothecafuliginea);

Uncinula (Uncinula) bacterial classification, for example grape snag shell (Uncinula necator);

By the disease that the rust pathogene causes, described pathogene for example

Glue Rust (Gymnosporangium) bacterial classification, for example Gymnosporangiumsabinae;

Camel spore rust belongs to (Hemileia) bacterial classification, for example coffee camel spore rest fungus (Hemileiavastatrix);

Layer rest fungus (Phakopsora) bacterial classification, for example yam bean layer rest fungus (Phakopsorapachyrhizi) and mountain horseleech layer bacterium (Phakopsora meibomiae);

Handle rest fungus (Puccinia) bacterial classification, for example Puccinia recondita (Puccinia recondita);

Uromyces (Uromyces) bacterial classification, for example wart top uromyce (Uromycesappendiculatus);

By the disease that Oomycete class pathogene causes, described pathogene for example

Dish downy mildew (Bremia) bacterial classification, for example lettuce dish downy mildew (Bremia lactucae);

Downy mildew (Peronospora) bacterial classification, for example pea downy mildew (Peronospora pisi) or Cruciferae downy mildew (P.brassicae);

Epidemic disease mould (Phytophthora) bacterial classification, for example phytophthora infestans (Phytophthorainfestans);

Axle downy mildew (Plasmopara) bacterial classification, for example grape is given birth to axle downy mildew (Plasmoparaviticola);

False downy mildew (Pseudoperonospora) bacterial classification, the false downy mildew (Pseudoperonosporacubensis) of for example careless false downy mildew (Pseudoperonospora humuli) or Cuba;

Rotten mould (Pythium) bacterial classification, for example ultimate corruption mould (Pythium ultimum);

The sick disease of leaf spot blight that causes by for example following pathogene and leaf withering,

Alternaria (Alternaria) bacterial classification, for example early blight chain lattice spore (Alternariasolani);

Cercospora (Cercospora) bacterial classification, Li such as Chard dish are given birth to tail spore (Cercosporabeticola);

Cladiosporum bacterial classification, for example Cladiosporium cucumerinum;

Cochliobolus belongs to (Cochliobolus) bacterial classification, for example standing grain cochliobolus (Cochliobolussativus) (conidial form: De Shi mould (Drechslera), Syn: the long spore bacterium (Helminthosporium) that wriggles);

Colletotrichum (Colletotrichum) bacterial classification, for example Colletotrichumlindemuthanium;

Cycloconium bacterial classification, for example Cycloconium oleaginum;

Between the seat shell belong to (Diaporthe) bacterial classification, seat shell (Diaporthe citri) between citrus for example;

Elsinoe (Elsinoe) bacterial classification, for example citrus Elsinochrome (Elsinoefawcettii);

Coil long spore and belong to (Gloeosporium) bacterial classification, for example please the long spore of colour disk (Gloeosporiumlaeticolor);

Small cluster shell belongs to (Glomerella) bacterial classification, for example encloses small cluster shell (Glomerellacingulata);

Ball seat Pseudomonas (Guignardia) bacterial classification, for example grape Guignardia (Guignardiabidwelli);

Leptosphaeria (Leptosphaeria) bacterial classification, for example Leptosphaeria maculans;

Magnaporthe bacterial classification, for example Magnaporthe grisea;

Mycosphaerella (Mycosphaerella) bacterial classification, for example standing grain green-ball chamber bacterium (Mycosphaerelle graminicola);

Phaeosphaeria bacterial classification, for example Phaeosphaeria nodorum;

Nuclear cavity Pseudomonas (Pyrenophora) bacterial classification, for example round nuclear cavity bacteria (Pyrenophorateres);

Ramularia (Ramularia) bacterial classification, for example Ramularia collo-cygni;

Rhynchosporium spp (Rhynchosporium) bacterial classification, for example rye beak spore (Rhynchosporiumsecalis);

The pin spore belongs to (Septoria) bacterial classification, for example Septoria apii (Septoria apii);

Nuclear coral Pseudomonas (Typhula) bacterial classification, for example meat spore nuclear coral bacterium (Typhula incarnata);

Venturia (Venturia) bacterial classification, for example apple black star bacteria (Venturiainaequalis);

It is harmful by root and stem disease that for example following pathogene causes,

Corticium bacterial classification, for example Corticium graminearum;

Fusarium (Fusarium) bacterial classification, for example sharp sickle spore (Fusarium oxysporum);

Gaeumannomyces bacterial classification, for example Gaeumannomyces graminis;

Rhizoctonia (Rhizoctonia) bacterial classification, for example Rhizoctonia solani Kuhn (Rhizoctoniasolani);

Tapesia bacterial classification, for example Tapesia acuformis;

Thiclaviopsis (Thielaviopsis) bacterial classification, for example thielaviopsis sp (Thielaviopsisbasicola);

The multiple Honoka preface and panicled spike (the comprising corncob) disease that cause by for example following pathogene,

Alternaria bacterial classification, for example Alternaria kind (Alternaria spp.);

Aspergillus (Aspergillus) bacterial classification, for example aspergillus flavus (Aspergillus flavus);

Cladosporium (Cladosporium) bacterial classification, for example Cladosporium spp.;

Claviceps (Claviceps) bacterial classification, for example ergot (Claviceps purpurea);

The Fusarium bacterial classification, for example yellow sickle spore (Fusarium culmorum);

Gibberella (Gibberella) bacterial classification, for example Gibberella zeae (Gibberella zeae);

Monographella bacterial classification, for example Monographella nivalis;

By the disease that smut causes, described smut for example

Sphacelotheca bacterial classification, for example Sphacelotheca reiliana;

Tilletia (Tilletia) bacterial classification, for example wheat net fungus tilletia (Tilletiacaries);

Urocystis (Urocystis) bacterial classification, for example latent bar smut (Urocystisocculta);

Smut (Ustilago) bacterial classification, for example naked smut (Ustilago nuda);

The fruit rot that causes by for example following pathogene,

Aspergillus bacterium, for example aspergillus flavus;

Botrytis (Botrytis) bacterial classification, for example Botrytis cinerea (Botrytis cinerea);

Penicillium (Penicillium) bacterial classification, for example penicillium expansum (Penicilliumexpansum);

Sclerotinia (Sclerotinia) bacterial classification, for example sclerotinite (Sclerotiniasclerotiorum);

Verticilium bacterial classification, for example Verticilium alboatrum;

That the kind that is caused by for example following pathogene passes and soil passes rots and wilting disease and seedling disease,

The Fusarium bacterial classification, for example yellow sickle spore;

Phytophthora kind, for example Phytophthora cactorum (Phytophthora cactorum);

Rhizoctonia bacterial classification, for example Rhizoctonia solani Kuhn;

Bulbil belongs to (Sclerotium) bacterial classification, for example Sclerotium rolfsii (Sclerotiumrolfsii);

The ulcer, mycoceicidum and the broom disease that cause by for example following pathogene,

Nectria (Nectria) bacterial classification, for example Nectria galligena;

The atrophy disease that causes by for example following pathogene,

Chain sclerotinia sclerotiorum belongs to (Monilinia) bacterial classification, for example drupe chain sclerotinia sclerotiorum (Monilinialaxa);

The deformity of leaf, flower and the fruit that causes by for example following pathogene,

Exoascus (Taphrina) bacterial classification, for example peach external capsule bacterium (Taphrina deformans);

The degeneration disease of the woody plant that causes by for example following pathogene,

Esca bacterial classification, for example Phaemoniella clamydospora;

The flower that causes by for example following pathogene and the disease of seed,

Botrytis bacterial classification, for example Botrytis cinerea;

The plant tuber disease that causes by for example following pathogene,

Rhizoctonia bacterial classification, for example Rhizoctonia solani Kuhn.

Reactive compound of the present invention also shows the effect of strong enhancing plant.Therefore, they are applicable to and transfer the resistance of inside plants at the harmful microorganism invasion and attack.

In the present invention, the implication that plant strengthens (induction of resistance) compound is interpreted as some materials like this, they can stimulating plant the system that resists, thereby make treated plant when inserting harmful microorganism subsequently, show significant resistance at these microorganisms.

In the present invention, the harmful microbe implication is interpreted as phytopathogenic fungi and bacterium.Therefore compound of the present invention also is used in the invasion and attack that protective plant in a period of time after the processing is avoided described pathogene.After handling plant with reactive compound, the time that obtains this protection generally continues 1 to 10 day, preferred 1 to 7 day.

Reactive compound shows good plant tolerance under the required concentration of controlling plant diseases, make it possible to ground plant parts, in-vitro propagate strain (propagation stock) and seed and soil are handled.

Reactive compound of the present invention can good especially effect be used to prevent and treat the cereal disease, the disease that causes by powdery mildew (Erysiphe) bacterial classification, handle rest fungus bacterial classification and fusarium (Fusaria) bacterial classification for example, the rice disease, the disease that causes by pears spore (Pyricularia) and rhizoctonia for example, and the disease in the plantation of viticulture, fruits and vegetables, for example by Botrytis, Venturia (Venturia), single softgel shell belongs to and the Podosphaera bacterial classification causes disease.

Reactive compound of the present invention also is suitable for improving the output of crop.In addition, they also show hypotoxicity and good plant tolerance.

If suitable, concentration that reactive compound of the present invention also can be certain and rate of application are used for coordinate plant growth, and are used to prevent and treat animal pest as weed killer herbicide.If suitable, they also can be used as the intermediate or the parent of synthetic other reactive compound.

According to the present invention, can handle all plants and plant parts (part).Here the implication of plant is interpreted as all plants and plant population, for example need and unwanted wild plant or crop plants (comprising naturally occurring crop plants).Crop plants can be by conventional breeding and optimum seeking method or the plant that obtains by biotechnology and gene engineering method or the combination by described method; comprise genetically modified plants, also comprise the plant cultivars that is subjected to or is not subjected to plant seedling power (plantbreeders ' certificate) protection.The implication of plant parts is interpreted as all grounds of plant and underground position and organ, and for example bud, leaf, Hua Jigen, the example that can mention be leaf, needle (needle), stem, do, flower, fruit body, fruit, seed, root, stem tuber and rhizome.Plant parts also comprises harvested material and asexual and sexual propagation thing, for example seedling, stem tuber, rhizome, cutting and seed.

The processing that reactive compound used according to the invention carries out plant and plant parts, directly carry out or undertaken according to conventional treatment method by acting on its environment, habitat or storage areas, described conventional treatment method comprises for example immersion liquid, spraying, evaporation, atomizing (atomizing), broadcasts sowing, brushes (brushing-on), and under the situation of breeding thing, particularly seed, also comprise applying one or more layers.

In material protection, compound of the present invention can be used for the safeguard industries material and avoids harmful microbe invasion and attack and destruction.

The implication of industrial materials is interpreted as Manufactured non-living body (non-living) material that is equipped with to be used for industry among the present invention.For example, being intended to by reactive compound of the present invention protection can be that tackifier, sizing material, paper and cardboard, textile, leather, timber, coating and plastic products, cooling lubricant (cooling lubricant) and other can be subjected to the material of microbiological attack or destruction with the industrial materials of avoiding microorganism and changing or destroy.May be subjected to the production equipment parts of microbial reproduction infringement, for example the chilled(cooling) water return (CWR) also can be mentioned in the scope of material to be protected.The industrial materials that can mention in the scope of the invention are preferably tackifier, sizing material, paper and cardboard, leather, timber, coating, cooling lubricant and heat-transfer fluid, preferred especially timber.

The made industrial materials that can mention take place to degrade or the microorganism of change is, for example bacterium, fungi, saccharomycete, algae and mucus biology.Reactive compound of the present invention preferably acts on fungi, especially fade fungi and wood-rotting fungi (basidiomycetes) and mucus biology and algae of mould, timber.

Microorganism with the subordinate can be proposed as an example:

Alternaria (Alternaria), chain lattice spore (Alternaria tenuis) for example,

Aspergillus (Aspergillus), aspergillus niger (Aspergillus niger) for example,

Cupreum (Chaetomium), chaetomium globosum (Chaetomium globosum) for example,

Coniophora, the full lead fungi (Coniophora puetaha) of powder for example,

Lentinus (Lentinus), Lentinus tigrinus bacterium (Lentinus tigrinus) for example,

Penicillium (Penicillium), Penicillum glaucum (Penicillium glaucum) for example,

Bracket fungus (Polyporus), for example variegated bracket fungus (Polyporusversicolor),

Aureobasidium (Aureobasidium), Aureobasidium pullulans (Aureobasidiumpullulans) for example,

Nuclear stem point genus (Sclerophoma), Sclerophoma pityophila for example,

Trichoderma (Trichoderma), Trichoderma viride (Trichoderma viride) for example,

Escherichia (Escherichia), colon bacillus (Escherichiacoli) for example,

Pseudomonas (Pseudomonas), pseudomonas aeruginosa (Pseudomonasaeruginosa) for example,

Staphylococcus (Staphylococcus), for example staphylococcus aureus (Staphylococcus aureus).

Reactive compound of the present invention can be converted into conventional formulation according to its concrete physics and/or chemical property, the cooling of for example microcapsule formulations in solution, emulsion, suspending agent, pulvis, foaming agent, paste, granule, aerosol, polymer and the seed coating composition, and ULV and atomizing (fogging) preparation of heating.

Described preparation prepares in a known way, for example reactive compound is mixed with filler, promptly mixes with liquid flux, pressurized liquefied gas and/or solid carrier, can choose the use surfactant wantonly simultaneously, i.e. emulsifier and/or dispersant and/or blowing agent.If used filler is a water, for example also can use organic solvent as secondary solvent.Basically, the liquid flux of Shi Heing is: aromatic compounds, for example dimethylbenzene, toluene or Fluhyzon; Chlorinated aromatics or chlorination aliphatic hydrocarbon, for example chlorobenzene, vinyl chloride or carrene; Aliphatic hydrocarbon, for example cyclohexane or paraffin are as petroleum distillate; Alcohol, for example butanols or ethylene glycol and ether thereof and ester; Ketone, for example acetone, methyl. ethyl ketone, methyl. isobutyl ketone or cyclohexanone; Intensive polar solvent, for example dimethyl formamide or dimethyl sulfoxide (DMSO); Or water.The implication of liquefaction gaseous state filler or carrier is interpreted as being the liquid of gaseous state, for example aerosol propellant, for example halogenated hydrocarbons, perhaps butane, propane, nitrogen and carbonic acid gas under normal temperature and atmospheric pressure.The solid carrier that is fit to is: the natural minerals of Fen Suiing for example, as kaolin, clay, talcum, chalk, quartz, attapulgite, montmorillonite or diatomite; And the synthetic mineral of pulverizing, for example finely divided silica, aluminium oxide and silicate.The solid carrier that is applicable to granule is: for example pulverize the also natural rock of classification, for example calcite, float stone, marble, sepiolite and dolomite; Or synthetic inorganic and organic powder particles, and organic particle, for example wood sawdust, coconut husk, corncob and tobacco stem.The emulsifier and/or the blowing agent that are fit to are: for example nonionic and anion emulsifier, for example polyoxyethylene fatty acid ester, polyoxyethylene aliphatic alcohol ether---for example alkylaryl polyglycol ether, alkylsulfonate, alkyl sulfate, arylsulphonate or protein hydrolysate.The dispersant that is fit to is: for example lignin sulfite waste liquor and methylcellulose.

Can use tackifier in the preparation; carboxymethyl cellulose for example; and the natural and synthetic polymer of powder, particle or latex form---for example gum Arabic, polyvinyl alcohol and polyvinyl acetate, or natural phospholipid---for example cephalin and lecithin, and synthetic phospholipid.Other additive that can add is mineral oil and vegetable oil.

Can use colouring agent, inorganic pigment for example---for example iron oxide, titanium oxide and Prussian blue, and organic dyestuff---for example alizarin dyes, azo dyes and metal phthalocyanine dyestuff, and micronutrient---for example molysite, manganese salt, boron salt, mantoquita, cobalt salt, molybdenum salt and zinc salt.

Each preparation generally comprises the reactive compound of 0.1 to 95 weight %, preferred 0.5 to 90 weight %.

Reactive compound of the present invention also can itself or its preparation form mix use with known fungicide, bactericide, miticide, nematocide or insecticide, for example to enlarge activity profile or to prevent to produce resistance.Obtain synergistic effect in many cases, that is, the activity of mixture is greater than the activity of each independent component.

Suitable blending ingredients is for example following compound:

Fungicide:

1. nucleic acid synthetic inhibitor

M 9834 (benalaxyl), smart M 9834 (benalaxyl-M), bupirimate (bupirimate), chiralaxyl, clozylacon, dimethirimol (dimethirimol), the phonetic phenol of second (ethirimol), furalaxyl (furalaxyl), dislike mould spirit (hymexazol), efficient metalaxyl (mefenoxam), metalaxyl (metalaxyl), efficient metalaxyl (metalaxyl-M), ofurace (ofurace), Wakil (oxadixyl), oxolinic acide (oxolinic acid)

2. mitosis and cell division inhibitor

Benomyl (benomyl), carbendazim (carbendazim), the mould prestige of second (diethofencarb), furidazol (fuberidazole), Pencycuron (pencycuron), probenazole (thiabendazole), thiophanate-methyl (thiophanate-methyl), zoxamide (zoxamide)

3. the inhibitor of respiratory chain

3.1 composite I

Fluorine mepanipyrim (diflumetorim)

3.2 composite I I

Boscalid (boscalid), carboxin (carboxin), fenfuram (fenfuram), flutolanil (flutolanil), furan pyrrole bacterium amine (furametpyr), seed dressing amine (furmecyclox), mebenil (mepronil), oxycarboxin (oxycarboxin), pyrrole metsulfovax (penthiopyrad), thiophene fluorine bacterium amine (thifluzamide)

3.3 composite I II

Indazole flusulfamide (amisulbrom), Fluoxastrobin (azoxystrobin), cyanogen frost azoles (cyazofamid), ether bacterium amine (dimoxystrobin), enestrobin, Famoxate (famoxadone), Fenamidone (fenamidone), fluoxastrobin (fluoxastrobin), kresoxim-methyl (kresoxim-methyl), SSF 126 (metominostrobin), orysastrobin (orysastrobin), ZEN 90160 (picoxystrobin), pyraclostrobin (pyraclostrobin), oxime bacterium ester (trifloxystrobin)

3.4 uncoupler (decoupler)

Karathane (dinocap), fluazinam (fluazinam), methyl karathane (methyldinocap)

3.5ATP formation inhibitor

Fentin acetate (fentin acetate), triphenyl tin chloride (fentinchloride), fentin hydroxide (fentin hydroxide), silicon metsulfovax (silthiofam)

4. amino acid and protein biosynthesis inhibitor

Amine puts out (andoprim), blasticidin-S (blasticidin-S), cyprodinil (cyprodinil), kasugarnycin (kasugamycin), kasugarnycin one hydrochloride hydrate (kasugamycin hydrochloride hydrate), mepanipyrim (mepanipyrim), phonetic mould amine (pyrimethanil)

5. signal transduction inhibitor

Fenpiclonil (fenpiclonil), fludioxonil (fludioxonil), benzene oxygen quinoline (quinoxyfen)

6. lipid and film synthetic inhibitor

Chlozolinate (chlozolinate), iprodione (iprodione), procymidone (procymidone), vinclozolin (vinclozolin)

Pyrazophos (pyrazophos), edifenphos (edifenphos), iprobenfos (iprobenfos) (IBP), Isoprothiolane (isoprothiolane)

Tolelofos-methyl (tolclofos-methyl), biphenyl

Iodocarb, Propamocarb (propamocarb), propamocarb (propamocarbhydrochloride)

7. ergosterol biosynthesis inhibitor

Fenhexamid (fenhexamid),

Oxygen ring azoles (azaconazole), bitertanol (bitertanol), bromuconazole (bromuconazole), Cyproconazole (cyproconazole), diclobutrazol (diclobutrazole), Difenoconazole (difenoconazole), alkene azoles alcohol (diniconazole), alkene azoles alcohol-M (diniconazole-M), fluorine ring azoles (epoxiconazole), etaconazole (etaconazole), RH-7592 (fenbuconazole), Fluquinconazole (fluquinconazole), flurprimidol (flurprimidol), Flusilazole (flusilazole), Flutriafol (flutriafol), furconazole (furconazole), furconazole_cis (furconazole-cis), own azoles alcohol (hexaconazole), glyoxalin (imibenconazole), plant bacterium azoles (ipconazole), metconazole (metconazole), nitrile bacterium azoles (myclobutanil), paclobutrazol (paclobutrazol), penconazole (penconazole), propiconazole (propiconazole), prothioconazoles (prothioconazole), pyrifenox (pyrifenox), simeconazoles (simeconazole), Tebuconazole (tebuconazole), tetraconazole (tetraconazole), triazolone (triadimefon), Triadimenol (triadimenol), triticonazole (triticonazole), uniconazole P (uniconazole), voriconazole (voriconazole)

Press down mould azoles (imazalil), IMAZALIL (imazalil sulphate), evil imidazoles (oxpoconazole), Fenarimol (fenarimol), flurprimidol (flurprimidol), nuarimol (nuarimol), pyrifenox (pyrifenox), triforine (triforine), pefurazoate (pefurazoate), Prochloraz (prochloraz), fluorine bacterium azoles (triflumizole), alkene frost benzyl azoles (viniconazole)

Cartap (aldimorph), dodemorph (dodemorph), dodemorph acetate, fenpropidin (fenpropidin), butadiene morpholine (fenpropimorph), tridemorph (tridemorph), volution bacterium amine (spiroxamine),

Naftifine (naftifine), pyributicarb (pyributicarb), Terbinafine (terbinafine)

8. cell wall synthetic inhibitor

Benzene metsulfovax (benthiavalicarb), dimethomorph (dimethomorph), flumorph (flumorph), iprovalicarb (iprovalicarb), polyoxin (polyoxins), Polyoxin (polyoxorim), valida (validamycin A)

9. melanin biosynthesis inhibitor

Ring propionyl imines (capropamid), two chlorine zarilamid (diclocymet), zarilamid (fenoxanil), Rabcide (phthalide), pyroquilon (pyroquilon), tricyclazole (tricyclazole)

10. induction of resistance material

Diazosulfide (acibenzolar-S-methyl), probenazole (probenazole), tiadinil (tiadinil)

11. have the active material of multidigit point

Bordeaux mixture, difoltan (captafol), captan (captan), tpn (chlorothalonil), mantoquita is for example: Kocide SD, copper naphthenate, copper oxychloride (copperoxychloride), copper oxide, copper sulphate, copper 8-hydroxyquinolinate (oxine copper), dichlofluanid (dichlofluanid), dithianon (dithianone), dodine (dodine), the dodine free alkali, ferbam (ferbam), fluorine folpet (fluorofolpet), folpet (folpet), the hot salt (guazatine) of biguanides, guazatine acetate (guazatineacetate), iminoctadine (iminoctadine), biguanides octyl benzene sulfonate (iminoctadine albesilate), iminoctadine triacetate (iminoctadinetriacetate), mancopper (mancopper), mancozeb (mancozeb), maneb (maneb), Carbatene (metiram, metiram zinc), Propineb (propineb), sulphur and sulphur preparation comprise: calcium polysulfide, tmtd (thiram), Tolylfluanid (tolylfluanid), zineb (zineb), ziram (ziram)

12. the material of unknown mechanisms

Amibromdol, benthiozole (benthiazole), bethoxazin, capsimycin (capsimycin), carvol (carvon), chinomethionat (chinomethionat), chloropicrin (chloropicrin), cufraneb (cufraneb), cyflufenamid (cyflufenamid), frost urea cyanogen (cymoxanil), dazomet (dazomet), debacarb (debacarb), antiphen (dichlorophen), diclomezin (diclomezin), botran (dicloran), difenzoquat (difenzoquat), difenzoquat methylsulfuric acid ester (difenzoquatmethylsulphate), diphenylamines (diphenylamine), ferimzone (ferimzone), fluorine acyl bacterium amine (flumetover), fluorine Boscalid (fluopicolide), fluoromide (fluoroimide), flusulfamide (flusulphamide), phosethyl-Al (fosetyl-aluminium), triethylphosphine acid calcium (fosetyl-calcium), triethylphosphine acid sodium (fosetyl-sodium), hexachloro-benzene (hexachlorobenzene), oxine (8-hydroxyquinolinsulphate), people's metamycin (irumamycin), methasulfocarb (methasulphocarb), Trapex (methyl isothiocyanate), metrafenone (metrafenone), midolthromycin (mildiomycin), myprozine (natamycin), Sankel (nickel dimethyldithiocarbamate), nitrothalisopropyl (nitrothal-isopropyl), octhilinone (octhilinone), oxamocarb, oxyfenthiin, pentachlorophenol (pentachlorophenol) and salt thereof, 2-phenylphenol and salt thereof, phosphorous acid and salt thereof, disease is spent spirit (piperalin), Propamocarb ethyl phosphine hydrochlorate (propamocarb fosetylate), propanosin-sodium, the third oxygen quinoline (proquinazid), pyrrolnitrin (pyrrolnitrin), Quintozene (quintozen), tecloftalam (tecloftalam), tecnazene (tecnazen), triazoxide (triazoxid), trichlamide (trichlamid), zarilamid (zarilamid) and

2-amino-4-methyl-N-phenyl-5-thiazole carboxamides,

2-chloro-N-(2,3-dihydro-1,1,3-trimethyl-1H-indenes-4-yl)-3-pyridine carboxamide,

3-[5-(4-chlorphenyl)-2,3-dimethyl isoxazole alkane-3-yl] pyridine,

Suitable-1-(4-chlorphenyl)-2-(1H-1,2,4-triazol-1-yl) suberol,

2,4-dihydro-5-methoxyl group-2-methyl-4-[[[[1-[3-(trifluoromethyl) phenyl] ethylidene] amino] the oxygen base] methyl] phenyl]-3H-1,2,3-triazole-3-ketone,

1-(2,3-dihydro-2,2-dimethyl-1H-indenes-1-yl)-1H-imidazoles-5-methyl formate,

2-[[[cyclopropyl [(4-methoxyphenyl) imino group] methyl] sulfenyl] methyl] phenyl-3-methoxy-methyl acrylate,

3-(4-chlorphenyl)-3-{[N-(isopropoxy carbonyl) valyl] amino } methyl propionate,

4-chloro-α-third alkynyloxy group-N-[2-[3-methoxyl group-4-(2-third alkynyloxy group) phenyl] ethyl] phenyl acetamide,

2-(2-{[6-(3-chloro-2-methylphenoxy)-5-fluorine pyrimidine-4-yl] the oxygen base } phenyl)-2-(methoxyimino)-N-methylacetamide,

(2S)-and N-[2-[4-[[3-(4-chlorphenyl)-2-propynyl] the oxygen base]-the 3-methoxyphenyl] ethyl]-3-methyl-2-[(mesyl) amino] butyramide,

5-chloro-7-(4-methyl piperidine-1-yl)-6-(2,4, the 6-trifluorophenyl) [1,2,4] triazols [1,5-a] pyrimidine,

5-chloro-6-(2,4, the 6-trifluorophenyl)-N-[(1R)-1,2,2-trimethyl propyl group] [1,2,4] triazol [1,5-a] pyrimidine-7-amine,

5-chloro-N-[(1R)-1, the 2-dimethyl propyl]-6-(2,4, the 6-trifluorophenyl) [1,2,4] triazols [1,5-a] pyrimidine-7-amine,

N-[1-(5-bromo-3-chloropyridine-2-yl) ethyl]-2,4-two chloro-nicotinamides,

N-(5-bromo-3-chloropyridine-2-yl) methyl-2,4-two chloro-nicotinamides,

N-[1-(5-bromo-3-chloropyridine-2-yl) ethyl]-2-fluoro-4-iodine vitamin PP,

2-butoxy-6-iodo-3-propyl group chromene-4-ketone,

N-[2-(4-{[3-(4-chlorphenyl) third-2-alkynes-1-yl] the oxygen base }-the 3-methoxyphenyl) ethyl]-N-2-(mesyl) valine amide,

N-{ (Z)-[(cyclo propyl methoxy) imino group] [6-(difluoro-methoxy)-2,3-difluorophenyl] methyl }-the 2-phenyl-acetamides,

N-(4-chloro-2-nitrobenzophenone)-N-ethyl-4-methyl benzenesulfonamide,

N-(3-ethyl-3,5,5-trimethylcyclohexyl)-3-formoxyl amino-2-hydroxybenzamide,

2-[[[[1-[3-(1-fluoro-2-phenylethyl) oxygen base] phenyl] ethylidene] amino] the oxygen base] methyl]-α-(methoxyimino)-N-methyl-α-phenyl acetamide,

N-{2-[3-chloro-5-(trifluoromethyl) pyridine-2-yl] ethyl }-2-(trifluoromethyl) benzamide,

N-(3 ', 4 '-two chloro-5-fluorine biphenyl-2-yls)-3-(difluoromethyl)-1-methyl isophthalic acid H-pyrazole-4-carboxamide,

N-(6-methoxyl group-3-pyridine radicals) cyclopropane carboxamide,

1-[(4-methoxyl group phenoxy group) methyl]-2,2-dimethyl propyl-1H-imidazoles-1-formic acid,

O-[1-[(4-methoxyl group phenoxy group) methyl]-2, the 2-dimethyl propyl]-1H-imidazoles-1-bamic acid,

2,3,5,6-tetrachloro-4-(methyl sulphonyl) pyridine,

3,4,5-three chloro-2,6-pyridine dintrile.

Bactericide:

Bronopol (bronopol), antiphen, trichloromethyl pyridine (nitrapyrin), Sankel, kasugarnycin, octhilinone, furancarboxylic acid (furancarboxylicacid), terramycin (oxytetracyclin), probenazole, streptomycin (streptomycin), tecloftalam, copper sulphate and other copper agent.

Insecticide/miticide/nematocide:

1. acetylcholinesterase (AChE) inhibitor

1.1 carbamates (alanycarb (alanycarb) for example, Aldicarb (aldicarb), aldoxycarb (aldoxycarb), allyxycarb (allyxycarb), aminocarb (aminocarb), azamethiphos (azamethiphos), bendiocarb (bendiocarb), Benfuracard micro (benfuracarb), metalkamate (bufencarb), butacarb (butacarb), butocarboxim (butocarboxim), butanone sulfone prestige (butoxycarboxim), carbaryl (carbaryl), carbofuran (carbofuran), carbosulfan (carbosulfan), cloethocarb (chloethocarb), Resistox (coumaphos), Surecide (cyanofenphos), cynock (cyanophos), dimetilan (dimetilan), ethiofencarb (ethiofencarb), Bassa (fenobucarb), fenothiocarb (fenothiocarb), Carzol (formetanate), furathiocarb (furathiocarb), Mobucin (isoprocarb), metham-sodium (metam-sodium), methiocarb (methiocarb), Methomyl (methomyl), meta-tolyl-N-methylcarbamate (MTMC) (metolcarb), oxamyl (oxamyl), Aphox (pirimicarb), Carbamult (promecarb), unden (propoxur), the two prestige (thiodicarb) of sulphur, thiofanox (thiofanox), triaguron (triazamate), Landrin (trimethacarb), XMC (XMC), Meobal (xylylcarb))

1.2 organophosphorus compounds (orthene accephate (acephate) for example; Azamethiphos Zuo Ding phosphorus (azamethiphos); The cotton phosphorus of azinphos-methyl/Yi (aziphos (methyl ,-ethyl)); Rilariol (bromophos-ethyl); Xiu benzene alkene phosphorus (bromfenvinfos (methyl)); Special Pyrimitate (butathiofos); Cadusafos (cadusafos); Carbophenothion (carbophenothion); Chlorine oxygen earth worm chlorine phosphorus (chlorethoxyfos); Chlorfenviphos (chlorfenvinphos); Chlormephos (chlormephos); Chlorpyrifos-methyl (chlorpyrifos-methyl); Chlopyrifos; Ying poison phosphorus; Surecide; Cynock; Chlorfenviphos (chlorfenvinphos); Demeton-methyl (demeton-s-methyl); Feng inhales phosphorus (demeton-s-methylsulphon); Dialifos (dialifos); Diazinon (diazinon); Dichlofenthion (dichlofenthion); DDVP (dichlorvos)/DDVP); Carbicron (dicrotophos); Rogor (dimethoate); Dimethylvinphos (dimethylvinphos); Salithion (dioxabenzofos); Disulfoton (disulfoton); EPN (EPN); Ethodan (ethion); Phonamiphos (ethoprophos); Etrimfos (etrimfos); Famphur (famphur); Fenamiphos (fenamiphos); Fenifrothion (fenitrothion); Fensulfothion (fensulfothion); Entex (fenthion); Bi fluorine sulphur phosphorus (flupyrazofos); Dyfonate (fonofos); Formothion (formothion); Fosmethilan (fosmethilan); Thiazolone phosphorus (fosthiazate); Heptenophos (heptenophos); Iodfenphos (iodofenphos); IBP (iprobenfos); Isazofos (isazofos); Yi willow phosphorus (isofenphos); The o-isopropyl salicylate; Isoxathion (isoxathion); Malathion (malathion); Afos (mecarbam); Methacrifos (methacrifos); Acephatemet (methamidophos); Methidathion (methidathion); Menite (mevinphos); Azodrin (monocrotophos); 2-dichloroethylk dimethyl phosphate (naled); Flolimat (omethoate); Oxydemeton_methyl (oxydemeton-methyl); Parathion-methyl/parathion (parathion (methyl/-ethyl)); Phenthoate dimephenthoate cidial (phenthoate); Thimet (phorate); Phosalone (phosalone); Phosmet (phosmet); Phosphamidon (phosphamidon); Yi the third phosphorus prestige (phosphocarb); Phoxim (phoxim); Pirimiphos-methyl/Diothyl (pirimiphos (methyl/-ethyl)); Profenofos (profenofos); Kayaphos (propaphos); Propetamphos (propetamphos); Toyodan (prothiofos); Prothoate (prothoate); Bi Zuo sulphur phosphorus (pyraclofos); Pyridaphethione (pyridaphenthion); Da sulphur phosphorus (pyridathion); Quinalphos (quinalphos); Cadusafos (sebufos); Sulfotep (sulfotep); Sulprofos (sulprofos); Butyl pyrimidine phosphorus (tebupirimfos); Swebate (temephos); Terbufos (terbufos); Ravap (tetrachlorvinphos); Thiometon (thiometon); Hostathion (triazophos); Metrifonate (trichlorfon); Vamidothion (vamidothion).

2. sodium channel modulators/current potential gated sodium channel blocking agent

2.1 pyrethroid (the fluorine ester third chrysanthemum ester (acrinathrin) for example, allyl alkene pyrethrins (d-is suitable-and anti-, d-is anti-) (allethrin (d-cis-trans, d-trans)), β-betacyfluthrin (beta-cyfluthrin), fluorine chlordiphenyl chrysanthemum ester (bifenthrin), bioallethrin Dtrans allethrin (bioallethrin), bioallethrin Dtrans allethrin-S-cyclopenta isomer, bioethanomethrin, biopermethrin (biopermethrin), biological benzyl furan bioresmethrin (bioresmethrin), dichloro alkyne valerate (chlovaporthrin), along cypermethrin (cis-cypermethrin), along Chryson resmethrin (cis-resmethrin), along permethrin (cis-permethrin), cyhalothrin (clocythrin), cycloprothrin (cycloprothrin), cyfloxylate (cyfluthrin), cyhalothrin (cyhalothrin), cypermethrin (α-, β-, θ-, ζ-) (cypermethrin (alpha-, beta-, theta-, zeta-)), phenylate cypermethrin (cyphenothrin), DDT, decis (deltamethrin), empenthrin (1R-isomer) (empenthrin (1R-isomer)), high S-sumicidin (esfenvalerate), ether chrysanthemum ester (etofenprox), fenfluthrin (fenfluthrin), fenpropathrin (fenpropathrin), fenpirithrin (fenpyrithrin), cyanogen penta is killed chrysanthemum ester (fenvalerate), brofluthrinate (flubrocythrinate), flucythrinate (flucythrinate), trifluoropropyl benzyl oxide chrysanthemum ester (flufenprox), flumethrin (flumethrin), taufluvalinate (fluvalinate), fubfenprox, gamma-cyhalothrin (gamma-cyhalothrin), miaow alkynes miaow chrysanthemum ester (imiprothrin), kadethrin (kadethrin), λ-gamma cyhalothrin (lambda-cyhalothrin), methoxy benzyl Flumethrin (metofluthrin), permethrin (suitable-, instead-) (permethrin (cis-, trans-)), phenothrin (1R-transisomer) (phenothrin (1R-trans isomer), dextrorotation alkynes acetone chrysanthemum ester (prallethrin), third Flumethrin (profluthrin), protrifenbute, anti-Chryson (pyresmethrin), Chryson resmethrin (resmethrin), kadethrin (RU 15525), silafluofene (silafluofen), taufluvalinate (tau-fluvalinate), tefluthrin (tefluthrin), terallethrin (terallethrin), tetramethrin (1R-isomer) (tetramethrin (1R-isomer)), tralomethrin (tralomethrin), transfluthrin (transfluthrin), brofluthrinate (ZXI 8901), pyrethrin (pyrethrin, pyrethrum)

2.2 oxadiazine class (for example indenes worm prestige (indoxacarb))

3. acetyl choline receptor agonists/antagonist

3.1 chlorine nicotine (chloronicotinyls)/anabasine (neonicotinoid) (for example Acetamiprid (acetamiprid), thiophene worm amine (clothianidin), MTI-446 (dinotefuran), Imidacloprid (imidacloprid), Nitenpyram (nitenpyram), Nithiazine (nithiazine), thiophene worm quinoline (thiacloprid), thiophene worm piperazine (thiamethoxam))

3.2 nicotine (nicotine), bensultap (bensultap), cartap (cartap)

4. acetylcholine receptor modulators

4.1 multiple killing teichomycin (spinosyn) class (for example pleocidin (spinosad))

5.GABA gate chloride channel antagonist

5.1 cyclic diolefine organochlorine class (for example toxaphene (camphechlor), Niran (chlordane), 5a,6,9,9a-hexahydro-6,9-methano-2,4 (endosulfan), lindane (gamma-HCH), hexachlorcyclohexane (HCH), heptachlor (heptachlor), lindane (lindane), methoxychlor (methoxychlor))

5.2fiprol class (for example acetoprole, second worm nitrile (ethiprole), fluorine worm nitrile (fipronil), fluorine pyrazoles worm (vaniliprole))

6. chloride channel activator class

6.1Mectin class (Avermectin (abamectin, avermectin), emaricin (emamectin), emamectin-benzoate (emamectin-benzoate), Olivomitecidin (ivermectin), more visit rhzomorph (milbemectin), milbemycin (milbemycin)) for example

7. juvenile hormone analogies class

(for example difenolan (diofenolan), protect young ether (epofenonane), fenoxycarb (fenoxycarb), hydroprene (hydroprene), kinoprene (kinoprene), methoprene (methoprene), pyrrole propyl ether (pyriproxifen), triprene (triprene))

8. ecdysone agonist/agent interfering class (disruptor)

8.1 diacyl hydrazide class (for example encircling worm hydrazides (chromafenozide), chlorine worm hydrazides (halofenozide), methoxyfenozide (methoxyfenozide), worm hydrazides (tebufenozide))

9. chitin biosynthesis inhibitor

9.1 benzoyl area kind (for example two three flufenoxurons (bistrifluron), fluorine pyridine urea (chlorfluazuron), diflubenzuron (diflubenzuron), fluazuron (fluazuron), flucycloxuron (flucycloxuron), flufenoxuron (flufenoxuron), fluorine bell urea (hexaflumuron), Acarus tritici urea (lufenuron), fluorine uride (novaluron), noviflumuron (noviflumuron), penfluron (penfluron), fluorobenzene urea (teflubenzuron), kill bell urea (triflumuron))

9.2 Buprofezin (buprofezin)

9.3 fly eradication amine (cyromazine)

10. oxidative phosphorylation inhibitor, ATP agent interfering class

10.1 butyl ether urea (diafenthiuron)

10.2 organic tin (for example azoles ring tin (azocyclotin), plictran (cyhexatin), fenbutatin oxide (fenbutatin-oxide))

11. by interrupting the oxidative phosphorylation uncoupler class that the H-proton gradient works

11.1 pyroles (for example capillary (chlorfenapyr))

11.2 dinitro benzene phenols (for example binapacryl (binapacryl), dinobuton (dinobuton), karathane (dinocap), dnoc (DNOC))

12. site I (Site-I) electronics transfer inhibitor class

12.1METI class (for example fenazaquin (fenazaquin), azoles mite ester (fenpyroximate), pyrimidifen (pyrimidifen), pyridaben (pyridaben), tebufenpyrad (tebufenpyrad), azoles insect amide (tolfenpyrad))

12.2 Hydramethylnon Bait (hydramethylnon)

12.3 dicofol (dicofol)

13. site II electronics transfer inhibitor class

13.1 rotenone (rotenone)

14. site III electronics transfer inhibitor class

Mite quinone (acequinocyl), fluacrypyrim (fluacrypyrim) 14.1 go out

15. the microorganism agent interfering class of insect gut film

Bacillus thuringiensis,Bt (Bacillus thuringiensis) bacterial strain

16. lipogenesis inhibitor class

16.1 tetronic acid class (for example spiral shell mite ester (spirodiclofen), Spiromesifen (spiromesifen))

16.2 (for example 3-(2 for tetramates acids (tetramic acids), the 5-3,5-dimethylphenyl)-8-methoxyl group-2-oxo-1-azaspiro [4.5] last of the ten Heavenly stems-3-alkene-4-base ethyl carbonate ester (another name: carbonic acid 3-(2, the 5-3,5-dimethylphenyl)-8-methoxyl group-2-oxo-1-azaspiro [4.5] last of the ten Heavenly stems-3-alkene-4-base ethyl ester, the CAS number of registration: 382608-10-8) and carbonic acid suitable-3-(2, the 5-3,5-dimethylphenyl)-8-methoxyl group-2-oxo-1-azaspiro [4.5] last of the ten Heavenly stems-3-alkene-4-base ethyl ester (CAS number of registration: 203313-25-1)

17. benzamide type

(for example flonicamid (flonicamid))

18. octopaminergic agonist class

(for example Amitraz (amitraz))

19. magnesium stimulates the atpase inhibitor class

(for example alkynes mite spy (propargite))

20. phthalyl amine

(N for example ²-[1,1-dimethyl-2-(methyl sulphonyl) ethyl]-3-iodo-N ¹-[2-methyl-4-[1,2,2,2-tetrafluoro-1-(trifluoromethyl) ethyl] phenyl]-1,2-benzenedicarboxamide (CAS number of registration: 272451-65-7, Flubendiamide (flubendiamide))

21. the similar thing of nereistoxin

(for example thiocyclam oxalate (thiocyclam hydrogen oxalate), dimehypo (thiosultap-sodium))

22. biologic product class, steroids or pheromones class

(for example nimbin (azadirachtin), bacillus kind (Bacillus spec.), Beauveria kind (Beauveria spec.), Pherocon CM (codlemone), green muscardine fungus belong to kind of (Metarrhizium spec.), a paecilomyces kind (Paecilomyces spec.), enemy Bei Te (thuringiensin), Verticillium dahliae genus kind of (a Verticillium spec.))

23. have the reactive compound class of unknown or the indeterminate mechanism of action

23.1 fumigant class (for example aluminum phosphate, Celfume, vikane)

23.2 selectivity food refusal agent class (for example ice crystal (cryolite), flonicamid, pyrrole aphid ketone (pymetrozine))

23.3 mite growth inhibitor class (for example four mite piperazines (clofentezine), second mite azoles (etoxazole), Hexythiazox (hexythiazox))

23.4amidoflumet, benclothiaz, Citrazon (benzoximate), Bifenazate (bifenazate), fenisobromolate (bromopropylate), Buprofezin (buprofezin), chinomethionat, galecron (chlordimeform), chlorobenzilate (chlorobenzilate), chloropicrin, clothiazoben, cycloprene, fourth fluorine mite ester (cyflumetofen), CGA 183893 (dicyclanil), fenoxacrim, fluorine nitre diphenylamines (fentrifanil), thiazole mite (flubenzimine), flufenerim, fluorine mite piperazine (flutenzin), gossyplure (gossyplure), Hydramethylnon Bait (hydramethylnone), japonilure, metoxadiazone (metoxadiazone), oil, Butacide (piperonyl butoxide), potassium oleate, pyrafluprole, pyridalyl (pyridalyl), pyriprole, sulfluramid (sulfluramid), tetradiphon (tetradifon), kill mite thioether (tetrasul), triarathene (thiarathene), synergy alkynes ether (verbutin)

Also have in addition compound propyl carbamic acid-3-aminomethyl phenyl ester (meta-tolyl-N-methylcarbamate (MTMC) Z (tsumacideZ)),

Compound 3-(5-chloro-3-pyridine radicals)-8-(2,2,2-trifluoroethyl)-8-azabicyclo [3.2.1] octane-3-nitrile (CAS number of registration 185982-80-3) and corresponding 3-endo isomer (CAS number of registration 185984-60-5) (referring to WO 96/37494, WO 98/25923),

And the preparation that contains plant extracts, nematode, fungi or the virus of killing insect active.

With other known activity compound such as weed killer herbicide, perhaps the mixture with fertilizer and growth regulator, safener and/or chemical information compound also is feasible.

In addition, formula of the present invention (I) compound also has extraordinary antifungi activity.They have the antifungi activity profile of non-constant width, especially at dermatophyte (dermatophyte) and saccharomycete, mould and two-phase (diphasic) fungi is (for example at Mycotoruloides (Candida) bacterial classification such as Candida albicans (Candida albicans), Candida glabrata (Candidaglabrata)) and acrothesium floccosum (Epidermophyton floccosum), aspergillus bacterial classification such as aspergillus niger and aspergillus fumigatus (Aspergillus fumigatus), trichophyton (Trichophyton) bacterial classification such as alpha fungus (Trichophyton mentagrophytes), Microsporon (Microsporon) bacterial classification such as microsporum canis (Microsporon canis) and Microsporon audouinii.Enumerate these moulds and never represent overlayable mould spectrum is limited, and only for it is carried out the example explanation.

Reactive compound can itself, its dosage form or use by the type of service of formulation preparation, described type of service is for example promptly used solution, suspending agent, wetting powder, paste, soluble powder, pulvis and the granule of (ready-to-use).Use in the usual way and carry out, for example by pouring, spraying, atomizing, broadcast sowing, dust, foam use, sprinkling etc.In addition, also can use reactive compound, perhaps active agent preparations or reactive compound itself are expelled in the soil by ultralow amount method.Also can handle the seed of plant.

When using reactive compound of the present invention as bactericide, rate of application can change in the scope of relative broad according to using type.In the processing to plant parts, the reactive compound rate of application is generally 0.1 to 10000g/ha (hectare), and preferred 10 to 1000g/ha.For seed pelleting, the reactive compound rate of application is generally 0.001 to 50g every kilogram of seed, preferred 0.01 to 10g every kilogram of seed.In the processing to soil, the reactive compound rate of application is generally 0.1 to 10000g/ha, and preferred 1 to 5000g/ha.

As mentioned above, can handle all plants and its position according to the present invention.In a preferred embodiment, handled wild plant kind and plant cultivars, or---for example hybridized or the protoplast fusion---plant species and plant cultivars of acquisition, and the position of described plant species and cultivated species by the biological breeding method of routine.In a further preferred embodiment,---suitable also can combine---and the genetically modified plants and plant cultivars (genetically modified organisms) and the position thereof that obtain with conventional method if handled by gene engineering.Term " position " or " position of plant " or " plant parts " are explained as above.

Particularly preferably, the plant of the plant cultivars that is commercially available separately or using is handled according to the present invention.The implication of plant cultivars is interpreted as the plant with new features (" feature ") by conventional breeding, mutagenesis or recombinant DNA technology acquisition.They can be cultivated species, mutation, biotype (biotype) or genotype.

According to plant variety or plant cultivars, its plantation place and growth conditions (soil, weather, vegetation period, nutrition), processing of the present invention also can produce superadditivity (superadditive) (" working in coordination with ") effect.Thus, for example, can obtain to surpass the following effect of actual desired: can reduce the rate of application of spendable material of the present invention and composition and/or widen its activity profile and/or improve its activity, improve plant growing, improve high temperature or cold tolerance, raising arid or water or soil salt content tolerance, improve the quality of blooming, make simpler and easy, the hasting of maturity of gathering, raising gather output, improve the quality of the product of gathering and/or improve its nutritive value, improve the bin stability and/or the processing characteristics of the product of gathering.

Preferably the genetically modified plants that can handle according to the present invention or plant cultivars (promptly obtaining by gene engineering) are included in all plants of having accepted genetic material in the genetic modification, and described genetic material is given described plant with particularly advantageous useful properties (" feature ").The example of described characteristic is to improve plant growing, improve high temperature or cold tolerance, raising arid or water or soil salt content tolerance, improve the quality of blooming, make gather simpler and easy, hasting of maturity, raising output, improve the quality of the product of gathering and/or improve its nutritive value, improve the bin stability and/or the processing characteristics of the product of gathering.Need further example with ben described characteristic for improving plant to noxious animal and harmful microbe resistance, for example to the resistance of insect, acarid, phytopathogenic fungi, bacterium and/or virus, and improve the tolerance of plant to some weeding active compound.The example of the genetically modified plants that can mention is important crop plants, such as grain (wheat, rice), corn, soybean, potato, cotton, tobacco, rape and fruit plant (fruit is apple, pears, citrus fruit and grape), ben is corn, soybean, potato, cotton, tobacco and rape.Ben feature is by form toxin in plant corpus, particularly the toxin that is formed in plant corpus by the genetic material (for example by gene C ryIA (a), CryIA (b), CryIA (c), CryIIA, CryIIIA, CryIIIB2, Cry9c, Cry2Ab, Cry3Bb and CryIF and combination thereof) from bacillus thuringiensis,Bt improves the resistance (hereinafter referred to as " Bt plant ") of plant to insect, arachnid, nematode and slug and snail.Ben feature is also for improving plant to fungi, bacterium and viral resistance by systemic acquired resistance (SAR), systemin, phytoalexin, releaser and resistant gene and corresponding marking protein and toxin.Also ben being characterized as improved the tolerance of plant to some weeding active compound, for example imidazolone type, sulfonylurea, glyphosate (glyphosate) or phosphino-triein (phosphinotricin) (for example " PAT " gene).The gene of giving described required feature separately also can exist with the form that mutually combines in the genetically modified plants body.The example of " the Bt plant " that can mention is that commercially available brand name is YIELD

(for example corn, cotton, soybean),

(for example corn),

(cotton),

(cotton) and

The corn variety of (potato), cotton variety, soybean varieties and potato kind.The example of the plant with herbicide tolerant that can mention is that commercially available brand name is Roundup

(having glyphosate tolerant, for example corn, cotton, soybean), Liberty

(having phosphino-triein tolerance, for example rape),

(having imidazolinone-tolerant) and

Corn variety, cotton variety and the soybean varieties of (having the sulfonylureas tolerance, for example corn).The plant with Herbicid resistant that can mention (breeding is to have the plant of herbicide tolerant in a usual manner) comprises that also name is called

Commercially available kind (for example corn).Certainly, more than narration also is applicable to have plant cultivars described hereditary feature or that still wait to develop hereditary feature, and described plant cultivars will be developed and/or goes on the market in future.

Above-mentioned plant can be handled with general formula of the present invention (I) compound or active compound combinations in particularly advantageous mode according to the present invention.The preferable range of above-mentioned reactive compound or mixture also is applicable to the processing to these plants.Ben for plant being handled with concrete compound or the mixture that proposes of the present invention.

The preparation of reactive compound of the present invention and purposes are illustrated by following examples example, but are not restricted to these embodiment.

Embodiment

Embodiment 95:2-methyl-N-(3-nitrobenzophenone)-4,5-dihydro [1,3] thiazole is [4,5-h] quinazoline-8-amine also

A) 2-methyl-7-oxo-4,5,6, the 7-tetrahydro benzothiazol:

80g (419mmol) 2-bromo-hydroresorcinol (Z.Chem.1967,7,422) and 31.46g (419mmol) thioacetamide are dissolved in the 600ml pyridine, and under 50 ℃, stir and spend the night.Then this mixture is cooled to room temperature, adding 600ml concentration is 10% NaCl solution, and with the dichloromethane extraction of this mixture with 3 * 250ml.Separate organic facies, be 10% NaCl solution washing with the concentration of 2 * 200ml, and use dried over sodium sulfate.Except that desolvating, the kermesinus grease that obtains gluing distills under high vacuum this grease with Rotary Evaporators.Under 96 ℃ (0.2mbar), obtain two kinds of cuts of 25.3g (purity is 100%) and 6.2g (purity is 90%) respectively.(gross production rate is 44%).logP(HCOOH)＝1.08

B) 8-formoxyl-2-methyl-7-oxo-4,5,6, the 7-tetrahydro benzothiazol:

At first 11g (275mmol) sodium hydride (with the form of 60% dispersion in the oil) is put in the 400ml ether, and slowly dropwise added 40ml methyl alcohol.Hydrogen select stop after, add 44.44ml (550mmol) Ethyl formate, add 18.4g (110mmol) 2-methyl-7-oxo-4,5,6 subsequently, the solution of 7-tetrahydro benzothiazol in the 100ml diethyl ether.Stir 16h under this reactant mixture room temperature, add 500ml concentration then and be 10% hydrochloric acid.Separate organic facies, and wash water with 3 * 500ml ethyl acetate.The dry organic facies that merges makes it clarification and it is concentrated with Rotary Evaporators.The alkane grease on upper strata (paraffin oil) is used n-hexane extraction, is dissolved in product in the ethyl acetate and carries out concentrating again.(purity is 77% to obtain 8.5g; 33mmol) rufous oily crude product (30% productive rate), this crude product is not further purified and is used for next step.logP(HCOOH)＝1.36

C) 2-methyl-N-(3-nitrobenzophenone)-4,5-dihydro [1,3] thiazole is [4,5-h] quinazoline-8-amine also:

With 403mg (2.06mmol) 8-formoxyl-2-methyl-7-oxo-4,5,6,7-tetrahydro benzothiazol and 500mg (2.06mmol) 3-nitrobenzophenone guanidine nitrate is dissolved among the 5ml DMF, adds 285mg (2.06mmol) K ₂CO ₃And at 100 ℃ of following this mixture 3h that stir.Then this mixture is cooled to room temperature and pours in the water.(Nutschfilter) leaches solid with nutsch filter, washes with water and drying.Obtain 106mg (13%, 0.23mmol is in purity 85%) ecru solid.logP(HCOOH)＝2.79

Embodiment 216:4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-nitrobenzophenone) pyrimidine-2-amine

A) 3-dimethylamino-1-(2-cyclohexyl-4-methylthiazol-5-yl) propenone:

With 4.2g (18.8mmol) 5-acetyl group-2-cyclohexyl-4-methylthiazol and 24.9ml (188mmol) N, the dinethylformamide dimethyl-acetal stirs 12h down at 100 ℃.This mixture is evaporated to dried with Rotary Evaporators, and separates residue with silica gel chromatograph.Obtain 5.1g product (purity is 81%) like this.logP(HCOOH)＝2.44

B) 4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-nitrobenzophenone) pyrimidine-2-amine:

With 200mg (0.58mmol) 3-dimethylamino-1-(2-cyclohexyl-4-methylthiazol-5-yl) propenone and 141mg (0.58mmol) 3-nitrobenzophenone guanidine nitrate and 61.6mg (0.58mmol) Na ₂CO ₃Together in the 5ml 2-methyl cellosolve, stir down 18h at 100 ℃.Mixture with heat filters then, the filter cake washing with acetone, and filtrate concentrates with Rotary Evaporators.With residue and acetone and methyl. 1: 1 mixture of tertbutyl ether grinds, and suction filtration goes out resulting crystal and dry.Obtain 85mg product (purity is 99%) like this.logP(HCOOH)＝4.63

Embodiment 874:5-chloro-4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine

A) 2,5-two chloro-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine

Under constant argon gas stream, with the 4.8g in the 50ml diethyl ether (25mmol) 5-bromo-2, the 4-dimethylthiazole is cooled to-70 ℃.Under this temperature, the form of 9.7ml (25mmol) n-BuLi with the hexane solution of 2.6 molar concentrations dropwise added with 30 minutes.This mixture is stirred half an hour under-70 ℃ again.With 3.45g (23mmol) 2, the 40ml diethyl ether solution of 5-dichloro pyrimidine dropwise adds, and stirs this mixture 30 minutes.Make resulting suspension be warming up to 0 ℃ in one hour, use 0.52g (29mmol) the water all standing reaction among the 20ml THF then.To be dissolved in the 5.67g (25mmol) 4 of 100ml THF then, 5-two chloro-3,6-dioxy hexamethylene-1,4-diene-1, the solution of 2-dintrile (DDQ) dropwise joins this mixture.This mixture is warming up to 20 ℃, stirs and also be cooled to 0 ℃ once more in 15 minutes.29ml (58mmol) 2N sodium hydrate aqueous solution is joined in this solution, and stirred this mixture 5 minutes down at 0 ℃.Separate organic facies, through dried over sodium sulfate and concentrated.With 2-methoxyl group-2-methylpropane is that flowing phase is carried out the silica gel chromatograph purifying, obtain 3.9g (theoretical value 63%) purity and be 97% (HPLC) 2,5-two chloro-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine.logP(HCOOH)＝2.47

B) 5-chloro-4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine

With the 0.112g (0.43mmol) 2 in 6.9ml (1.72mmol) the 0.25N hydrochloric acid, 5-two chloro-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine and 0.316g (1.72mmol) 3,4, the 5-trimethoxy-aniline stirred one hour under 150 ℃ and 15bar in the micro-wave oven of 250W.After the cooling, with this mixture of 2 * 5ml ethyl acetate extraction.Merge organic facies, through dried over sodium sulfate and concentrated.Obtaining 0.11g (theoretical value 52%) purity like this is 5-chloro-4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine of 82% (HPLC).logP(HCOOH)＝2.82

With with the similar mode of said method, obtained or also can obtain formula listed in the following table 1 (I) and (Ia) compound.

Table 1

Embodiment	IUPAC (IUPAC) name	logP
Embodiment	IUPAC (IUPAC) name	logP	1	1-(3-{[2-(tert-butylamine)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) ethyl ketone	2.18*
2	1-(3-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	2.14**	1		2.18*
2		2.14**	3	1-(3-{[4-(2-amino-1,3-thiazoles-5-yl) pyrimidine-2-yl] amino } phenyl) ethyl ketone
4	1-(3-{[4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	1.47*	3
4		1.47*	5	1-(3-{[4-(2-amino-4-sec-butyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone
6	1-(3-{[4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	4.11*	5
6		4.11*	7	1-(3-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	2.88*
8	1-(3-{[4-(2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-yl] amino } phenyl) ethyl ketone		7		2.88*
8			9	1-(3-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	2.7*
10	1-(3-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	3.1*	9		2.7*
10		3.1*	11	1-(3-{[4-(2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-yl] amino } phenyl) ethyl ketone	2.57*
12	1-(3-{[4-(4-chloro-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone		11		2.57*
12			13	1-(3-{[4-(4-cyclopropyl-2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone
14	1-(3-{[4-(4-cyclopropyl-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone		13
14			15	1-(3-{[4-(4-methoxyl group-2-methyl isophthalic acid, 3-thiazole-5-

	Base) pyrimidine-2-base] amino } phenyl) ethyl ketone
	Base) pyrimidine-2-base] amino } phenyl) ethyl ketone		16	1-(3-{[4-(4-methyl-2-phenyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone
17	1-(3-{[4-(4-sec-butyl-2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone		16
17			18	1-(3-{[4-(4-sec-butyl-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone
19	1-[3-(2-[(2-hydroxyl-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] ethyl ketone		18
19			20	1-[3-(2-[(2-methoxyl group-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] ethyl ketone
21	1-[3-(2-[(oxolane-2-ylmethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] ethyl ketone		20
21			22	1-[3-(4-[2-(cyclopropylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone
23	1-[3-(4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	1.91*	22
23		1.91*	24	1-[3-(4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.38*
25	1-[3-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.25*	24		2.38*
25		2.25*	26	1-[3-(4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	3.02*
27	1-[3-(4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	1.62*	26		3.02*
27		1.62*	28	1-[3-(4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.99*

29	1-{3-[(2-amino-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } ethyl ketone
29			30	1-{3-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } ethyl ketone	2.29*
31	1-{3-[(4-{2-[(2-hydroxyl-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone		30		2.29*
31			32	1-{3-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone
33	1-{3-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone		32
33			34	The 1-{3-[(4-{2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone
35	1-{3-[(4-{2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone		34
35			36	1-{3-[(4-{4-cyclopropyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone
37	1-{3-[(4-{4-cyclopropyl-2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone		36
37			38	1-{3-[(4-{4-cyclopropyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone
39	1-{3-[(4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone	1.82*	38
39		1.82*	40	1-{3-[(4-{4-sec-butyl-2-[(2-methoxyl group-1-methyl

	Ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone
		41	1-{3-[(4-{4-sec-butyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone
42	2-(8-[(3,4,5-trimethoxyphenyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl } amino) third-1-alcohol	41
42		43	2-(the 8-[(3-chlorphenyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl } amino) third-1-alcohol
44	2-(the 8-[(3-methoxyphenyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl } amino) third-1-alcohol	43
44		45	2-(the 8-[(3-nitrobenzophenone) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl } amino) third-1-alcohol
46	2-(8-[(4-fluoro-3-aminomethyl phenyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl } amino) third-1-alcohol	45
46		47	2-(the 8-[(4-fluorophenyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl } amino) third-1-alcohol
48	2-(8-[(6-methoxypyridine-3-yl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl } amino) third-1-alcohol	47
48		49	2,2,2-three fluoro-N-(5-{2-[(3,4,5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
50	2,2,2-three fluoro-N-(5-{2-[(3-hydroxy phenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide	49
50		51	2,2,2-three fluoro-N-(5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
52	2-[(4-methyl-5-{2-[(3,4, the 5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) amino] third-1-	51

	Alcohol
	Alcohol		53	2-[(4-methyl-5-{2-[(3-nitrobenzophenone) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) amino] third-1-alcohol
54	The 2-[(5-{2-[(3-chlorphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) amino] third-1-alcohol		53
54			55	The 2-[(5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) amino] third-1-alcohol
56	2-[(5-{2-[(4-fluoro-3-aminomethyl phenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) amino] third-1-alcohol		55
56			57	The 2-[(5-{2-[(4-fluorophenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) amino] third-1-alcohol
58	2-[(5-{2-[(6-methoxypyridine-3-yl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) amino] third-1-alcohol		57
58			59	2-[(8-anilino--4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl) amino] third-1-alcohol
60	2-{[5-(2-anilino-pyrimidine-4-yl)-4-methyl isophthalic acid, the 3-thiazol-2-yl] amino } third-1-alcohol		59
60			61	2-chloro-N1, N1-dimethyl-N4-{4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl] pyrimidine-2-base } benzene-1, the 4-diamines	2.74*
62	2-chloro-N4-[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-base]-N1, N1-dimethyl benzene-1,4-diamines	2.06*	61		2.74*
62		2.06*	63	2-chloro-N4-[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-N1, N1-dimethyl benzene-1,4-diamines	2.59*
64	2-chloro-N4-[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-N1, N1-dimethyl benzene-1,4-diamines	2.72*	63		2.59*
64		2.72*	65	2-chloro-N4-{4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-base }-N1, N1-dimethyl benzene-1,4-diamines	2.04*
66	The 2-methoxy ethyl-(4-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) carbamate		65		2.04*

67	The 2-methoxy ethyl-(4-{[4-(2-amino-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) carbamate
67			68	The 2-methoxy ethyl-(4-{[4-(2-amino-4-cyclopropyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) carbamate
69	The 2-methoxy ethyl-(4-{[4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate	1.4*	68
69		1.4*	70	The 2-methoxy ethyl-(4-{[4-(2-amino-4-sec-butyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) carbamate
71	The 2-methoxy ethyl-(4-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate	2.51*	70
71		2.51*	72	The 2-methoxy ethyl-(4-{[4-(2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) carbamate
73	The 2-methoxy ethyl-(4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate	2.36*	72
73		2.36*	74	The 2-methoxy ethyl-(4-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate	2.67*
75	The 2-methoxy ethyl-(4-{[4-(2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate		74		2.67*
75			76	The 2-methoxy ethyl-(4-{[4-(4-cyclopropyl-2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) carbamate
77	The 2-methoxy ethyl-(4-{[4-(4-cyclopropyl-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate		76
77			78	2-methoxy ethyl-(4-{[4-(4-sec-butyl-2-ethyl

	-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) carbamate
		79	The 2-methoxy ethyl-(4-{[4-(4-sec-butyl-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate
80	The 2-methoxy ethyl-[4-(4-[2-(acetyl amine)-1,3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] carbamate	79
80		81	The 2-methoxy ethyl-[4-(4-[2-(acetyl amine)-4-cyclopropyl-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] carbamate
82	The 2-methoxy ethyl-[4-(4-[2-(acetyl amine)-4-sec-butyl-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] carbamate	81
82		83	The 2-methoxy ethyl-[4-(4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] carbamate
84	The 2-methoxy ethyl-and 4-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } carbamate	83
84		85	The 2-methoxy ethyl-and the 4-[(4-{2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } carbamate
86	The 2-methoxy ethyl-and 4-[(4-{2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } carbamate	85
86		87	The 2-methoxy ethyl-and the 4-[(4-{2-[(trifluoroacetyl group) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } carbamate
88	The 2-methoxy ethyl-and 4-[(4-{4-cyclopropyl-2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base)	87

	Amino] phenyl } carbamate
	Amino] phenyl } carbamate		89	The 2-methoxy ethyl-and 4-[(4-{4-cyclopropyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } carbamate
90	The 2-methoxy ethyl-and 4-[(4-{4-cyclopropyl-2-[(trifluoroacetyl group) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } carbamate		89
90			91	The 2-methoxy ethyl-and 4-[(4-{4-sec-butyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } carbamate
92	The 2-methoxy ethyl-and 4-[(4-{4-sec-butyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } carbamate		91
92			93	The 2-methoxy ethyl-and 4-[(4-{4-sec-butyl-2-[(trifluoroacetyl group) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } carbamate
94	2-methyl-N-(3,4, the 5-trimethoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	2.18*	93
94		2.18*	95	2-methyl-N-(3-nitrobenzophenone)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	2.79*
96	2-methyl-N-phenyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	2.48*	95		2.79*
96		2.48*	97	3-(2-[(2-hydroxyl-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenol
98	3-(2-[(2-methoxyl group-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenol		97
98			99	3-(2-[(oxolane-2-ylmethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenol
100	3-(4-[2-(cyclopropylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenol		99

101	3-(4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenol	1.97*
101		1.97*	102	3-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenol	1.82*
103	3-(4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenol	2.52*	102		1.82*
103		2.52*	104	3-(4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenol
105	3-(4-methyl-5-{2-[(3,4,5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-1,3-oxazolidine-2-ketone		104
105			106	3-(4-methyl-5-{2-[(3-nitrobenzophenone) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-1,3-oxazolidine-2-ketone
107	3-(5-{2-[(3-acetylphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-1,3-oxazolidine-2-ketone		106
107			108	3-(5-{2-[(3-acetylphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-the 4-methyl isophthalic acid, 3-Evil azoles alkane-2-ketone
109	3-(5-{2-[(3-chlorphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-1,3-oxazolidine-2-ketone		108
109			110	3-(5-{2-[(3-chlorphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
111	3-(5-{2-[(3-hydroxy phenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-1,3-oxazolidine-2-ketone		110
111			112	3-(5-{2-[(3-hydroxy phenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
113	3-(5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-1,3-oxazolidine-2-		112

	Ketone
	Ketone	114	3-(5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-the 4-methyl isophthalic acid, 3-Evil azoles alkane-2-ketone
115	3-(5-{2-[(4-fluoro-3-aminomethyl phenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-1,3-oxazolidine-2-ketone	114
115		116	3-(5-{2-[(4-fluoro-3-aminomethyl phenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-the 4-methyl isophthalic acid, 3-Evil azoles alkane-2-ketone
117	3-(5-{2-[(4-fluorophenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-1,3-oxazolidine-2-ketone	116
117		118	3-(5-{2-[(4-fluorophenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
119	3-(5-{2-[(4-hydroxy phenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-1,3-oxazolidine-2-ketone	118
119		120	3-(5-{2-[(4-hydroxy phenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
121	3-(5-{2-[(6-methoxypyridine-3-yl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-1,3-oxazolidine-2-ketone	120
121		122	3-(5-{2-[(6-methoxypyridine-3-yl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl)-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
123	3-(8-anilino--4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl)-1,3-oxazolidine-2-ketone	122
123		124	3-(8-anilino--4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl)-4-methyl isophthalic acid, 3-oxazolidine-2-ketone
125	3-[(2-amino-4,5-dihydro [1,3] thiazole [4,5-h] quinoline azoles	124

	Quinoline-8-yl) amino] phenol
	Quinoline-8-yl) amino] phenol		126	3-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenol	1.77*
127	3-[(4-{2-[(2-hydroxyl-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenol		126		1.77*
127			128	3-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenol
129	3-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenol	1.53*	128
129		1.53*	130	The 3-[(4-{2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenol
131	3-[(4-{2-[(oxolane-2-ylmethyl) amino]-1,3-thiazole-5-yl } pyrimidine-2-base) amino] phenol		130
131			132	3-[(4-{4-cyclopropyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenol
133	3-[(4-{4-cyclopropyl-2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenol		132
133			134	3-[(4-{4-cyclopropyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenol
135	3-[(4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenol		134
135			136	3-[(4-{4-sec-butyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenol
137	3-[(4-{4-sec-butyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenol		136
137			138	3-[5-(2-anilino-pyrimidine-4-yl)-4-methyl isophthalic acid, the 3-thiazol-2-yl]-1,3-oxazolidine-2-ketone
139	3-[5-(2-anilino-pyrimidine-4-yl)-4-methyl isophthalic acid, the 3-thiazol-2-yl]-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone		138

140	3-{[2-(tert-butylamine)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenol
140			141	3-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-yl] amino } phenol	1.84*
142	3-{[4-(2-amino-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenol		141		1.84*
142			143	3-{[4-(2-amino-4-cyclopropyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenol
144	3-{[4-(2-amino-4-sec-butyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenol		143
144			145	3-{[4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzoic acid	3.27*
146	3-{[4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol	3.33*	145		3.27*
146		3.33*	147	3-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzoic acid	2.27*
148	3-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol	2.24*	147		2.27*
148		2.24*	149	3-{[4-(2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenol
150	3-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol	2.12*	149
150		2.12*	151	3-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol	2.42*
152	3-{[4-(2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol		151		2.42*
152			153	3-{[4-(4-cyclopropyl-2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenol
154	3-{[4-(4-cyclopropyl-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol		153
154			155	3-{[4-(4-methyl-2-phenyl-1,3-thiazoles-5-yl) pyrimidine

	-2-yl] amino } phenol
	-2-yl] amino } phenol	156	3-{[4-(4-sec-butyl-2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenol
157	3-{[4-(4-sec-butyl-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol	156
157		158	3-{8-[(3,4, the 5-trimethoxyphenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone
159	The 3-{8-[(3-acetylphenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone	158
159		160	The 3-{8-[(3-acetylphenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
161	The 3-{8-[(3-chlorphenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone	160
161		162	The 3-{8-[(3-chlorphenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
163	The 3-{8-[(3-hydroxy phenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone	162
163		164	The 3-{8-[(3-hydroxy phenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
165	The 3-{8-[(3-methoxyphenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone	164
165		166	The 3-{8-[(3-methoxyphenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
167	The 3-{8-[(3-nitrobenzophenone) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone	166
167		168	3-{8-[(4-fluoro-3-aminomethyl phenyl) amino]-4, the 5-dihydro

	[1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone
			169	3-{8-[(4-fluoro-3-aminomethyl phenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
170	The 3-{8-[(4-fluorophenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone	1.34*	169
170		1.34*	171	The 3-{8-[(4-fluorophenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
172	The 3-{8-[(4-hydroxy phenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone		171
172			173	The 3-{8-[(4-hydroxy phenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
174	3-{8-[(6-methoxypyridine-3-yl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone		173
174			175	3-{8-[(6-methoxypyridine-3-yl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-the 4-methyl isophthalic acid, 3-oxazolidine-2-ketone
176	4-(2-[(2-hydroxyl-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenol		175
176			177	4-(2-[(2-methoxyl group-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenol
178	4-(2-[(oxolane-2-ylmethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenol		177
178			179	4-(4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) benzonitrile	2.57*
180	4-({ 4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-	1.67*	179		2.57*

	Base] pyrimidine-2-base } amino) phenol
	Base] pyrimidine-2-base } amino) phenol		181	4-(4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) benzonitrile
182	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.1**	181
182		2.1**	183	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine	2.64*
184	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(3-nitrobenzophenone) pyrimidine-2-amine	2.61**	183		2.64*
184		2.61**	185	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(4-fluoro-3-aminomethyl phenyl) pyrimidine-2-amine	3.07*
186	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(4-fluorophenyl) pyrimidine-2-amine	2.65*	185		3.07*
186		2.65*	187	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	2.09*
188	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-[3-(trifluoromethyl) phenyl] pyrimidine-2-amine	3.3**	187		2.09*
188		3.3**	189	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-[4-(trifluoromethyl) phenyl] pyrimidine-2-amine	3.56*
190	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine	2.4**	189		3.56*
190		2.4**	191	4-(2-amino-1,3-thiazoles-5-yl)-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine
192	4-(2-amino-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		191
192			193	4-(2-amino-1,3-thiazoles-5-yl)-N-(3-chlorphenyl) pyrimidine-2-amine
194	4-(2-amino-1,3-thiazoles-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine		193
194			195	4-(2-amino-4-cyclopropyl-1,3-thiazoles-5-yl)-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine

196	4-(2-amino-4-cyclopropyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
196			197	4-(2-amino-4-cyclopropyl-1,3-thiazoles-5-yl)-N-(3-chlorphenyl) pyrimidine-2-amine
198	4-(2-amino-4-cyclopropyl-1,3-thiazoles-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine		197
198			199	4-(2-amino-4-cyclopropyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine
200	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine		199
200			201	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	1.51*
202	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3, the 4-Dimethoxyphenyl) pyrimidine-2-amine	1.28*	201		1.51*
202		1.28*	203	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-chloro-4-methoxyphenyl) pyrimidine-2-amine	1.63*
204	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-chlorphenyl) pyrimidine-2-amine	1.78*	203		1.63*
204		1.78*	205	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine
206	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-nitrobenzophenone) pyrimidine-2-amine	1.5**	205
206		1.5**	207	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-fluoro-3-aminomethyl phenyl) pyrimidine-2-amine	l.68*
208	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-fluorophenyl) pyrimidine-2-amine	1.56*	207		l.68*
208		1.56*	209	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[3-(trifluoromethyl) phenyl] pyrimidine-2-amine	1.97*
210	4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	1.51*	209		1.97*
210		1.51*	211	4-(2-amino-4-sec-butyl-1,3-thiazoles-5-

	Base)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
	Base)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		212	4-(2-amino-4-sec-butyl-1,3-thiazoles-5-yl)-N-(3-chlorphenyl) pyrimidine-2-amine
213	4-(2-amino-4-sec-butyl-1,3-thiazoles-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine		212
213			214	4-(2-amino-4-sec-butyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine
215	4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	3.97*	214
215		3.97*	216	4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-nitrobenzophenone) pyrimidine-2-amine	4.63*
217	4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	3.86*	216		4.63*
217		3.86*	218	4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[4-(trifluoromethyl) phenyl] pyrimidine-2-amine	5.62*
219	4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	4.65*	218		5.62*
219		4.65*	220	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(2,3-dihydro-1,4-benzo dioxine-6-yl) pyrimidine-2-amine	2.91*
221	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine	3.71*	220		2.91*
221		3.71*	222	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.77*
223	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3, the 4-Dimethoxyphenyl) pyrimidine-2-amine	2.6*	222		2.77*
223		2.6*	224	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine	3.28*
225	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-nitrobenzophenone) pyrimidine-2-amine	3.29*	224		3.28*
225		3.29*	226	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-	3.71*

	Fluoro-3-aminomethyl phenyl) pyrimidine-2-amine
	Fluoro-3-aminomethyl phenyl) pyrimidine-2-amine		227	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-fluorophenyl) pyrimidine-2-amine	3.31*
228	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	2.53*	227		3.31*
228		2.53*	229	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[3-(trifluoromethyl) phenyl] pyrimidine-2-amine	4.04*
230	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[4-(trifluoromethyl) phenyl] pyrimidine-2-amine	4.2*	229		4.04*
230		4.2*	231	4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	3.26*
232	4-(2-ethyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		231		3.26*
232			233	4-(2-ethyl-1,3-thiazoles-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine
234	4-(2-ethyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine		233
234	4-(2-ethyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine		235	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.61*
236	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine	3*	235		2.61*
236		3*	237	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-nitrobenzophenone) pyrimidine-2-amine	3.14*
238	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-fluoro-3-aminomethyl phenyl) pyrimidine-2-amine		237		3.14*
238			239	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-fluorophenyl) pyrimidine-2-amine	3.1*
240	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	2.33*	239		3.1*
240		2.33*	241	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[3-(trifluoromethyl) phenyl] pyrimidine-2-amine	3.85*

242	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[4-(trifluoromethyl) phenyl] pyrimidine-2-amine
242			243	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	3.07*
244	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.99*	243		3.07*
244		2.99*	245	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine	3.5*
246	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-nitrobenzophenone) pyrimidine-2-amine	3.55*	245		3.5*
246		3.55*	247	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	2.76*
248	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[3-(trifluoromethyl) phenyl] pyrimidine-2-amine	4.3*	247		2.76*
248		4.3*	249	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[4-(4-methyl piperazine-1-yl) phenyl] pyrimidine-2-amine	1.71*
250	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[4-(trifluoromethyl) phenyl] pyrimidine-2-amine		249		1.71*
250			251	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	3.55*
252	4-(2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		251		3.55*
252			253	4-(2-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine
254	4-(4-chloro-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		253
254			255	4-(4-chloro-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-chlorphenyl) pyrimidine-2-amine
256	4-(4-chloro-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine		255

257	4-(4-cyclopropyl-2-ethyl-1,3-thiazoles-5-yl)-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine
257			258	4-(4-cyclopropyl-2-ethyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
259	4-(4-cyclopropyl-2-ethyl-1,3-thiazoles-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine		258
259			260	4-(4-cyclopropyl-2-ethyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine
261	4-(4-cyclopropyl-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine		260
261			262	4-(4-cyclopropyl-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
263	4-(4-cyclopropyl-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine		262
263			264	4-(4-cyclopropyl-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine
265	4-(4-methoxyl group-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		264
265			266	4-(4-methoxyl group-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine
267	4-(4-methyl isophthalic acid, 3-thiazole-5-yl)-N-[3-(trifluoromethyl) phenyl] pyrimidine-2-amine	3.14*	266
267		3.14*	268	4-(4-methyl-2-phenyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
269	4-(4-methyl-2-phenyl-1,3-thiazoles-5-yl)-N-(3-nitrobenzophenone) pyrimidine-2-amine		268
269			270	4-(4-methyl-2-phenyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine
271	4-(4-sec-butyl-2-ethyl-1,3-thiazoles-5-yl)-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine		270
271			272	4-(4-sec-butyl-2-ethyl-1,3-thiazoles-5-

	Base)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
	Base)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		273	4-(4-sec-butyl-2-ethyl-1,3-thiazoles-5-yl)-N-(3-chlorphenyl) pyrimidine-2-amine
274	4-(4-sec-butyl-2-ethyl-1,3-thiazoles-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine		273
274			275	4-(4-sec-butyl-2-ethyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine
276	4-(4-sec-butyl-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine		275
276			277	4-(4-sec-butyl-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
278	4-(4-sec-butyl-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-chlorphenyl) pyrimidine-2-amine		277
278			279	4-(4-sec-butyl-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-methoxyphenyl) pyrimidine-2-amine
280	4-(4-sec-butyl-2-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine		279
280			281	4-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenol	1.41*
282	4-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenol		281		1.41*
282			283	4-[(4-{2-[(2-hydroxyl-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenol
284	4-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenol	1.4*	283
284		1.4*	285	4-[(4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenol
286	4-[2-(cyclopropylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		285
286			287	4-[2-(cyclopropylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-methoxyphenyl) pyrimidine-2-amine

288	4-[2-(cyclopropylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine
288			289	4-[2-(cyclopropylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-fluoro-3-aminomethyl phenyl) pyrimidine-2-amine
290	4-[2-(cyclopropylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-phenyl pyrimidine-2-amine	1.96*	289
290		1.96*	291	4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	3.43*
292	4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-phenyl pyrimidine-2-amine	3.88*	291		3.43*
292		3.88*	293	4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-methoxyphenyl) pyrimidine-2-amine	1.98*
294	4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-fluoro-3-aminomethyl phenyl) pyrimidine-2-amine	2.22*	293		1.98*
294		2.22*	295	4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.36*
296	4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-methoxyphenyl) pyrimidine-2-amine	2.67*	295		2.36*
296		2.67*	297	4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine
298	4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	2.13*	297
298		2.13*	299	4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-[3-(trifluoromethyl) phenyl] pyrimidine-2-amine	3.41*
300	4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-[4-(trifluoromethyl) phenyl] pyrimidine-2-amine	3.59*	299		3.41*
300		3.59*	301	4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-phenyl pyrimidine-2-amine	3.01*
302	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		301		3.01*
302			303	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-	2.99*

	Base]-N-(3-chlorphenyl) pyrimidine-2-amine
	Base]-N-(3-chlorphenyl) pyrimidine-2-amine		304	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-methoxyphenyl) pyrimidine-2-amine	2.4*
305	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine	2.63*	304		2.4*
305		2.63*	306	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-fluoro-3-aminomethyl phenyl) pyrimidine-2-amine	2.7*
307	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-fluorophenyl) pyrimidine-2-amine	2.54*	306		2.7*
307		2.54*	308	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	2.04*
309	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-phenyl pyrimidine-2-amine	2.42*	308		2.04*
309		2.42*	310	4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	3.02*
311	4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine	3.5*	310		3.02*
311		3.5*	312	4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-phenyl pyrimidine-2-amine	3.45*
313	4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	1.53*	312		3.45*
313		1.53*	314	4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine
315	4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl]-N-phenyl pyrimidine-2-amine	1.61*	314
315		1.61*	316	4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.76*
317	4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl]-N-[4-(trifluoromethyl) phenyl] pyrimidine-2-amine	4.37*	316		2.76*
317		4.37*	318	4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl]-N-phenyl pyrimidine-2-amine	3.34*

319	4-{[2-(tert-butylamine)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenol
319			320	4-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-yl] amino } benzonitrile
321	4-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-yl] amino } phenol	1.62*	320
321		1.62*	322	4-{[4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzonitrile
323	4-{[4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol	0.93*	322
323		0.93*	324	4-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol	2.01*
325	4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzoic acid	2.16*	324		2.01*
325		2.16*	326	4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzonitrile
327	4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol	1.88*	326
327		1.88*	328	4-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzonitrile
329	4-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenol	2.18*	328
329		2.18*	330	4-{2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
331	4-{2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-(3-methoxyphenyl) pyrimidine-2-amine		330
331			332	4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	1.85*
333	4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl	2.03*	332		1.85*

	-1,3-thiazoles-5-yl }-N-(3-methoxyphenyl) pyrimidine-2-amine
			334	4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(3-nitrobenzophenone) pyrimidine-2-amine	2.2*
335	4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	Jan 65	334		2.2*
335		Jan 65	336	4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-phenyl pyrimidine-2-amine
337	The 4-{2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		336
337			338	The 4-{2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl }-N-(3-methoxyphenyl) pyrimidine-2-amine
339	The 4-{2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl }-N-phenyl pyrimidine-2-amine		338
339			340	4-{2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
341	4-{2-[cyclopropyl (methyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-phenyl pyrimidine-2-amine	2.43*	340
341		2.43*	342	4-{4-cyclopropyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine
343	4-{4-cyclopropyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine		342
343			344	4-{4-cyclopropyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-(3-methoxyphenyl) pyrimidine-2-amine
345	4-{4-cyclopropyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-phenyl pyrimidine-2-amine		344
345			346	4-{4-cyclopropyl-2-[(2-methoxy ethyl) amino]-1,3-

	Thiazole-5-yl }-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine
			347	4-{4-cyclopropyl-2-[(2-methoxy ethyl) amino]-1,3-thiazole-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
348	4-{4-cyclopropyl-2-[(2-methoxy ethyl) amino]-1,3-thiazole-5-yl }-N-(3-methoxyphenyl) pyrimidine-2-amine		347
348			349	4-{4-cyclopropyl-2-[(2-methoxy ethyl) amino]-1,3-thiazole-5-yl }-N-phenyl pyrimidine-2-amine
350	4-{4-cyclopropyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine		349
350			351	4-{4-cyclopropyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
352	4-{4-cyclopropyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(3-methoxyphenyl) pyrimidine-2-amine		351
352			353	4-{4-cyclopropyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-phenyl pyrimidine-2-amine
354	4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	1.8*	353
354		1.8*	355	4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(3-nitrobenzophenone) pyrimidine-2-amine	2.13*
356	4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-phenyl pyrimidine-2-amine	1.87*	355		2.13*
356		1.87*	357	4-{4-methyl-2-[methyl (phenyl) amino]-1,3-thiazoles-5-yl }-N-phenyl pyrimidine-2-amine	3.21*
358	4-{4-sec-butyl-2-[(2-methoxyl group-1-Methylethyl) ammonia		357		3.21*

	Base]-1,3-thiazoles-5-yl }-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine
		359	4-{4-sec-butyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
360	4-{4-sec-butyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-(3-chlorphenyl) pyrimidine-2-amine	359
360		361	4-{4-sec-butyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-(3-methoxyphenyl) pyrimidine-2-amine
362	4-{4-sec-butyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl }-N-phenyl pyrimidine-2-amine	361
362		363	4-{4-sec-butyl-2-[(2-methoxy ethyl) amino]-1,3-thiazole-5-yl }-N-phenyl pyrimidine-2-amine
364	4-{4-sec-butyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(2, the 5-Dimethoxyphenyl) pyrimidine-2-amine	363
364		365	4-{4-sec-butyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine
366	4-{4-sec-butyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(3-chlorphenyl) pyrimidine-2-amine	365
366		367	4-{4-sec-butyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-(3-methoxyphenyl) pyrimidine-2-amine
368	4-{4-sec-butyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl }-N-phenyl pyrimidine-2-amine	367
368		369	4-methyl-3-(4-methyl-5-{2-[(3,4,5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-

	Base)-1,3-oxazolidine-2-ketone
	Base)-1,3-oxazolidine-2-ketone		370	4-methyl-3-(4-methyl-5-{2-[(3-nitrobenzophenone) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-1,3-oxazolidine-2-ketone
371	4-methyl-3-{8-[(3,4, the 5-trimethoxyphenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl]-1,3-oxazolidine-2-ketone		370
371			372	4-methyl-3-{8-[(3-nitrobenzophenone) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl }-1,3-oxazolidine-2-ketone
373	5-(2-anilino-pyrimidine-4-yl)-N, N, 4-trimethyl-1,3-thiazole-2-formamide	2.72*	372
373		2.72*	374	Ethyl-3-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzoic ether	3.56*
375	Ethyl-3-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzoic ether	3.83*	374		3.56*
375		3.83*	376	Ethyl-4-(4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) benzoic ether
377	Ethyl-4-(4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) benzoic ether		376
377			378	Ethyl-4-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } benzoic ether
379	Ethyl-4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzoic ether		378
379			380	Methyl-(4-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) carbamate	1.84**
381	Methyl-(4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate		380		1.84**
381			382	Methyl-(4-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate
383	Methyl-[4-({ 4-[4-methyl-2-(methyl amine)-1,3-thiazoles		382

	-5-yl] pyrimidine-2-base } amino) phenyl] carbamate
	-5-yl] pyrimidine-2-base } amino) phenyl] carbamate		384	Methyl-and 4-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } carbamate	1.92*
385	N-(2,3-dihydro-1,4-benzo dioxine-6-yl)-2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	2.19*	384		1.92*
385		2.19*	386	N-(2,3-dihydro-1,4-benzo dioxine-6-yl)-2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine
387	N-(2,3-dihydro-1,4-benzo dioxine-6-yl)-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	2.34*	386
387		2.34*	388	N-(2,3-dihydro-1,4-benzo dioxine-6-yl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	2.7*
389	N-(2,3-dihydro-1,4-benzo dioxine-6-yl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.16*	388		2.7*
389		3.16*	390	N-(2,3-dihydro-1,4-benzo dioxine-6-yl)-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.49*
391	N-(2, the 5-Dimethoxyphenyl)-4-(2,4-dimethyl-1,3-thiazole-5-yl) pyrimidine-2-amine	3.03*	390		2.49*
391		3.03*	392	N-(2, the 5-Dimethoxyphenyl)-4-(2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine
393	N-(2, the 5-Dimethoxyphenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine		392
393			394	N-(2, the 5-Dimethoxyphenyl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine
395	N-(2, the 5-Dimethoxyphenyl)-4-(2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine		394

396	N-(2, the 5-Dimethoxyphenyl)-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine
396			397	N-(2, the 5-Dimethoxyphenyl)-4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] pyrimidine-2-amine
398	N-(2, the 5-Dimethoxyphenyl)-4-{2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine		397
398			399	N-(2, the 5-Dimethoxyphenyl)-4-{2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine
400	N-(2, the 5-Dimethoxyphenyl)-4-{2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine		399
400			401	N-(3, the 4-difluorophenyl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.95*
402	N-(3, the 4-Dimethoxyphenyl)-2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	1.95*	401		3.95*
402		1.95*	403	N-(3, the 4-Dimethoxyphenyl)-4-(2,4-dimethyl-1,3-thiazole-5-yl) pyrimidine-2-amine	2.16*
404	N-(3, the 4-Dimethoxyphenyl)-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.23*	403		2.16*
404		2.23*	405	N-(3, the 4-Dimethoxyphenyl)-4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl] pyrimidine-2-amine	2.78*
406	N-(3, the 5-Dimethoxyphenyl)-4-(2,4-dimethyl-1,3-thiazole-5-yl) pyrimidine-2-amine	2.64*	405		2.78*
406		2.64*	407	N-(3, the 5-Dimethoxyphenyl)-4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl] pyrimidine-2-amine	3.39*
408	N-(3-{[2-(2-oxo-1,3-oxazolidine-3-yl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) acetamide		407		3.39*
408			409	N-(3-{[2-(2-oxo-1,3-oxazolidine-3-yl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) Methanesulfomide
410	N-(3-{[2-(4-methyl-2-oxo-1,3-oxazolidine-3-		409

	Base)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) acetamide
			411	N-(3-{[2-(4-methyl-2-oxo-1,3-oxazolidine-3-yl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) Methanesulfomide
412	N-(3-{[2-(tert-butylamine)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) acetamide		411
412			413	N-(3-{[2-(tert-butylamine)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) Methanesulfomide
414	N-(3-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) acetamide	1.96*	413
414		1.96*	415	N-(3-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) acetamide	2.05*
416	N-(3-chloro-4-methoxyphenyl)-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	2.88*	415		2.05*
416		2.88*	417	N-(3-chloro-4-methoxyphenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine
418	N-(3-chloro-4-methoxyphenyl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine		417
418			419	N-(3-chloro-4-methoxyphenyl)-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.91*
420	N-(3-chlorphenyl)-2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	3.33*	419		2.91*
420		3.33*	421	N-(3-chlorphenyl)-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	3.11**
422	N-(3-chlorphenyl)-4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.94*	421		3.11**
422		3.94*	423	N-(3-chlorphenyl)-4-(2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine
424	N-(3-chlorphenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.72*	423

425	N-(3-chlorphenyl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	4.25*
425		4.25*	426	N-(3-chlorphenyl)-4-(2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine
427	N-(3-chlorphenyl)-4-(4-cyclopropyl-2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine		426
427			428	N-(3-chlorphenyl)-4-(4-cyclopropyl-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine
429	N-(3-chlorphenyl)-4-(4-methoxyl group-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine		428
429			430	N-(3-chlorphenyl)-4-(4-methyl-2-phenyl-1,3-thiazoles-5-yl) pyrimidine-2-amine
431	N-(3-chlorphenyl)-4-[2-(cyclopropylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine		430
431			432	N-(3-chlorphenyl)-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	3.24*
433	N-(3-chlorphenyl)-4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine	4.03*	432		3.24*
433		4.03*	434	N-(3-chlorphenyl)-4-[4-methyl-2-(methyl amine)-1,3-thiazole-5-yl] pyrimidine-2-amine	2.03*
435	N-(3-chlorphenyl)-4-[4-methyl-2-(methyl mercapto)-1,3-thiazole-5-yl] pyrimidine-2-amine	4.08*	434		2.03*
435		4.08*	436	N-(3-chlorphenyl)-4-{2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine
437	N-(3-chlorphenyl)-4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	2.47*	436
437		2.47*	438	N-(3-chlorphenyl)-4-{2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine
439	N-(3-chlorphenyl)-4-{2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine		438
439			440	N-(3-chlorphenyl)-4-{4-cyclopropyl-2-[(2-methoxyl group

	-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine
			441	N-(3-chlorphenyl)-4-{4-cyclopropyl-2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine
442	N-(3-chlorphenyl)-4-{4-cyclopropyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine		441
442			443	N-(3-chlorphenyl)-4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine	2.36*
444	N-(3-methoxyphenyl)-2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	2.59*	443		2.36*
444		2.59*	445	N-(3-methoxyphenyl)-4-(2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine
446	N-(3-methoxyphenyl)-4-(4-methyl-2-phenyl-1,3-thiazole-5-yl) pyrimidine-2-amine		445
446			447	N-(3-methoxyphenyl)-4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine
448	N-(3-methoxyphenyl)-4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] pyrimidine-2-amine		447
448			449	N-(3-methoxyphenyl)-4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl] pyrimidine-2-amine	3.33*
450	N-(3-methoxyphenyl)-4-{2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine		449		3.33*
450			451	N-(3-methoxyphenyl)-4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine	1.94*
452	N-(4-{[2-(2-oxo-1,3-oxazolidine-3-yl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) acetamide		451		1.94*
452			453	N-(4-{[2-(2-oxo-1,3-oxazolidine-3-yl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) Methanesulfomide
454	N-(4-{[2-(4-methyl-2-oxo-1,3-oxazolidine-3-		453

	Base)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) acetamide
			455	N-(4-{[2-(4-methyl-2-oxo-1,3-oxazolidine-3-yl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) Methanesulfomide
456	N-(4-{[2-(tert-butylamine)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) acetamide	1.72*	455
456		1.72*	457	N-(4-{[2-(tert-butylamine)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) Methanesulfomide
458	N-(4-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) acetamide	1.62*	457
458		1.62*	459	N-(4-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) acetamide	2.0*
460	N-(4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) acetamide	1.88*	459		2.0*
460		1.88*	461	N-(4-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) acetamide	2.15*
462	N-(4-chlorphenyl)-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	3.09**	461		2.15*
462		3.09**	463	N-(4-chlorphenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.72*
464	N-(4-chlorphenyl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	4.25*	463		3.72*
464		4.25*	465	N-(4-chlorphenyl)-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	3.29*
466	N-(4-chlorphenyl)-4-[4-methyl-2-(methyl amine)-1,3-thiazole-5-yl] pyrimidine-2-amine		465		3.29*
466			467	N-(4-cyclopropyl-5-{2-[(2,5-Dimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide
468	N-(4-cyclopropyl-5-{2-[(2,5-Dimethoxyphenyl) ammonia		467

	Base] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
	Base] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide		469	N-(4-cyclopropyl-5-{2-[(3,4,5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide
470	N-(4-cyclopropyl-5-{2-[(3,4,5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide		469
470			471	N-(4-cyclopropyl-5-{2-[(3-hydroxy phenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide
472	N-(4-cyclopropyl-5-{2-[(3-hydroxy phenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide		471
472			473	N-(4-cyclopropyl-5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide
474	N-(4-cyclopropyl-5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide		473
474			475	N-(4-fluoro-3-aminomethyl phenyl)-2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	2.94*
476	N-(4-fluoro-3-aminomethyl phenyl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine		475		2.94*
476			477	N-(4-fluoro-3-aminomethyl phenyl)-4-(4-methyl-2-phenyl-1,3-thiazoles-5-yl) pyrimidine-2-amine
478	N-(4-fluoro-3-aminomethyl phenyl)-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	3.14*	477
478		3.14*	479	N-(4-fluoro-3-aminomethyl phenyl)-4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine
480	N-(4-fluoro-3-aminomethyl phenyl)-4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] pyrimidine-2-amine		479
480			481	N-(4-fluoro-3-aminomethyl phenyl)-4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl] pyrimidine-2-amine	3.89*
482	N-(4-fluoro-3-aminomethyl phenyl)-4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } phonetic	2.19*	481		3.89*

	Pyridine-2-amine
	Pyridine-2-amine		483	N-(4-fluoro-3-aminomethyl phenyl)-4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine	2.03*
484	N-(4-fluorophenyl)-2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	2.62*	483		2.03*
484		2.62*	485	N-(4-fluorophenyl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.58*
486	N-(4-fluorophenyl)-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.8*	485		3.58*
486		2.8*	487	N-(4-fluorophenyl)-4-[4-methyl-2-(methyl amine)-1,3-thiazole-5-yl] pyrimidine-2-amine
488	N-(4-fluorophenyl)-4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	2.0*	487
488		2.0*	489	N-(4-fluorophenyl)-4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine	2.1*
490	N-(4-methyl-5-{2-[(3,4,5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide		489		2.1*
490			491	N-(4-methyl-5-{2-[(3-nitrobenzophenone) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
492	N-(4-sec-butyl-5-{2-[(2,5-Dimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide		491
492			493	N-(4-sec-butyl-5-{2-[(2,5-Dimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
494	N-(4-sec-butyl-5-{2-[(3,4,5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide		493
494			495	N-(4-sec-butyl-5-{2-[(3,4,5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
496	N-(4-sec-butyl-5-{2-[(3-chlorphenyl) amino] pyrimidine		495

	-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide
	-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide	497	N-(4-sec-butyl-5-{2-[(3-chlorphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
498	N-(4-sec-butyl-5-{2-[(3-hydroxy phenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide	497
498		499	N-(4-sec-butyl-5-{2-[(3-hydroxy phenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
500	N-(4-sec-butyl-5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide	499
500		501	N-(4-sec-butyl-5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
502	N-(5-{2-[(2,5-Dimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide	501
502		503	N-(5-{2-[(2,5-Dimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide
504	N-(5-{2-[(3,4,5-trimethoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide	503
504		505	N-(5-{2-[(3-acetylphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide
506	N-(5-{2-[(3-acetylphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide	505
506		507	N-(5-{2-[(3-acetylphenyl) amino] pyrimidine-4-yl }-4-cyclopropyl-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide
508	N-(5-{2-[(3-acetylphenyl) amino] pyrimidine-4-yl }-4-cyclopropyl-1,3-thiazoles-2-yl) acetamide	507
508		509	N-(5-{2-[(3-acetylphenyl) amino] pyrimidine-4-yl }-4-sec-butyl-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide
510	N-(5-{2-[(3-acetylphenyl) amino] pyrimidine-4-	509

	Base }-4-sec-butyl-1,3-thiazoles-2-yl) acetamide
	Base }-4-sec-butyl-1,3-thiazoles-2-yl) acetamide		511	N-(5-{2-[(3-chlorphenyl) amino] pyrimidine-4-yl }-1, the 3-thiazol-2-yl)-2,2, the 2-trifluoroacetamide
512	N-(5-{2-[(3-chlorphenyl) amino] pyrimidine-4-yl }-1, the 3-thiazol-2-yl) acetamide		511
512			513	N-(5-{2-[(3-chlorphenyl) amino] pyrimidine-4-yl }-4-cyclopropyl-1,3-thiazoles-2-yl)-2,2, the 2-trifluoroacetamide
514	N-(5-{2-[(3-chlorphenyl) amino] pyrimidine-4-yl }-4-cyclopropyl-1,3-thiazoles-2-yl) acetamide		513
514			515	N-(5-{2-[(3-chlorphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) acetamide	2.49**
516	N-(5-{2-[(3-hydroxy phenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide		515		2.49**
516			517	N-(5-{2-[(3-hydroxy phenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) acetamide
518	N-(5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-1,3-thiazoles-2-yl) acetamide		517
518			519	N-(5-{2-[(3-methoxyphenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) acetamide
520	N-(5-{2-[(4-fluoro-3-aminomethyl phenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) acetamide		519
520			521	N-(6-methoxypyridine-3-yl)-2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	2.01*
522	N-(6-methoxypyridine-3-yl)-4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl] pyrimidine-2-amine	2.67*	521		2.01*
522		2.67*	523	N-(6-methoxypyridine-3-yl)-4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine	1.57*
524	N, N-dimethyl-N '-4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl] and pyrimidine-2-base } benzene-1, the 4-diamines	1.75*	523		1.57*
524		1.75*	525	N-[3-(2-[(2-hydroxyl-1-Methylethyl) and amino]-4,5-

	Dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] acetamide
			526	N-[3-(2-[(2-hydroxyl-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] Methanesulfomide
527	N-[3-(2-[(2-methoxyl group-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] acetamide		526
527			528	N-[3-(2-[(2-methoxyl group-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] Methanesulfomide
529	N-[3-(2-[(oxolane-2-ylmethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] acetamide		528
529			530	N-[3-(2-[(oxolane-2-ylmethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] Methanesulfomide
531	N-[3-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.57*	530
531		1.57*	532	N-[3-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] Methanesulfomide	1.57*
533	N-[3-(4-[4-methyl-2-(2-oxo-1,3-oxazolidine-3-yl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide		532		1.57*
533			534	N-[3-(4-[4-methyl-2-(2-oxo-1,3-oxazolidine-3-yl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] Methanesulfomide
535	N-[3-(4-[4-methyl-2-(4-methyl-2-oxo-1,3-oxazolidine-3-yl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide		534
535			536	N-[3-({ 4-[4-methyl-2-(4-methyl-2-oxo-1,3-

	Oxazolidine-3-yl)-and 1,3-thiazoles-5-yl] pyrimidine-2-base } amino) phenyl] Methanesulfomide
			537	N-[3-(amino methyl) phenyl]-4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	1.45*
538	N-[4-(2-[(2-hydroxyl-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] acetamide		537		1.45*
538			539	N-[4-(2-[(2-hydroxyl-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] Methanesulfomide
540	N-[4-(2-[(2-methoxyl group-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] acetamide		539
540			541	N-[4-(2-[(2-methoxyl group-1-Methylethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] Methanesulfomide
542	N-[4-(2-[(oxolane-2-ylmethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] acetamide		541
542			543	N-[4-(2-[(oxolane-2-ylmethyl) and amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl } amino) phenyl] Methanesulfomide
544	N-[4-(4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.8*	543
544		1.8*	545	N-[4-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.75*
546	N-[4-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] Methanesulfomide	1.83*	545		1.75*
546		1.83*	547	N-[4-(4-[4-methyl-2-(2-oxo-1,3-oxazolidine-3-yl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide

548	N-[4-(4-[4-methyl-2-(2-oxo-1,3-oxazolidine-3-yl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] Methanesulfomide
548			549	N-[4-(4-[4-methyl-2-(4-methyl-2-oxo-1,3-oxazolidine-3-yl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide
550	N-[4-(4-[4-methyl-2-(4-methyl-2-oxo-1,3-oxazolidine-3-yl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] Methanesulfomide		549
550			551	N '-[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-yl]-N, N-dimethyl benzene-1,3-diamines	1.75*
552	N '-[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-yl]-N, N-dimethyl benzene-1,4-diamines	1.41*	551		1.75*
552		1.41*	553	N '-[4-(2-cyclohexyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-N, N-dimethyl benzene-1,4-diamines	2.38*
554	N '-[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-N, N-dimethyl benzene-1,3-diamines	2.19*	553		2.38*
554		2.19*	555	N '-[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-N, N-dimethyl benzene-1,4-diamines	1.63*
556	N-[5-(2-anilino-pyrimidine-4-yl)-1,3-thiazoles-2-yl]-2,2, the 2-trifluoroacetamide		555		1.63*
556			557	N-[5-(2-anilino-pyrimidine-4-yl)-1,3-thiazoles-2-yl] acetamide
558	N-[5-(2-anilino-pyrimidine-4-yl)-4-cyclopropyl-1, the 3-thiazol-2-yl]-2,2, the 2-trifluoroacetamide		557
558			559	N-[5-(2-anilino-pyrimidine-4-yl)-4-cyclopropyl-1, the 3-thiazol-2-yl] acetamide
560	N-[5-(2-anilino-pyrimidine-4-yl)-4-methyl isophthalic acid, the 3-thiazol-2-yl] acetamide	2.09*	559
560		2.09*	561	N-[5-(2-anilino-pyrimidine-4-yl)-4-sec-butyl-1, the 3-thiazol-2-yl]-2,2, the 2-trifluoroacetamide

562	N-[5-(2-anilino-pyrimidine-4-yl)-4-sec-butyl-1, the 3-thiazol-2-yl] acetamide
562			563	N-{3-[(2-amino-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } acetamide
564	N-{3-[(2-amino-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } Methanesulfomide		563
564			565	N-{3-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } acetamide	1.71*
566	N-{3-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } Methanesulfomide		565		1.71*
566			567	N-{3-[(4-{2-[(2-hydroxyl-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } acetamide
568	N-{3-[(4-{2-[(2-hydroxyl-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } Methanesulfomide		567
568			569	N-{3-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } acetamide	1.47*
570	N-{3-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } Methanesulfomide	1.57*	569		1.47*
570		1.57*	571	N-{3-[(4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } acetamide
572	N-{3-[(4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } Methanesulfomide		571
572			573	N-{4-[(2-amino-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } Methanesulfomide
574	N-{4-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h]	1.56*	573

	Quinazoline-8-yl) amino] phenyl } acetamide
	Quinazoline-8-yl) amino] phenyl } acetamide		575	N-{4-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } Methanesulfomide	1.79*
576	N-{4-[(4-{2-[(2-hydroxyl-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } acetamide		575		1.79*
576			577	N-{4-[(4-{2-[(2-hydroxyl-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } Methanesulfomide
578	N-{4-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } acetamide	1.43*	577
578		1.43*	579	N-{4-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } Methanesulfomide
580	N-{4-[(4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } acetamide	1.39*	579
580		1.39*	581	N-{4-[(4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } Methanesulfomide
582	N2-(2-methoxyl group-1-Methylethyl)-N8-(3,4, the 5-trimethoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines		581
582			583	N2-(2-methoxyl group-1-Methylethyl)-N8-(3-methoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
584	N2-(2-methoxyl group-1-Methylethyl)-N8-(3-nitrobenzophenone)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines		583
584			585	N2-(2-methoxyl group-1-Methylethyl)-N8-(6-methoxyl group pyrrole

	Pyridine-3-yl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
		586	N2-(2-methoxyl group-1-Methylethyl)-N8-phenyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
587	N2-(tert-butyl group)-N8-(3,4, the 5-trimethoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	586
587		588	N2-(tert-butyl group)-N8-(3-chlorphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
589	N2-(tert-butyl group)-N8-(3-methoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	588
589		590	N2-(tert-butyl group)-N8-(3-nitrobenzophenone)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
591	N2-(tert-butyl group)-N8-(4-fluoro-3-aminomethyl phenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	590
591		592	N2-(tert-butyl group)-N8-(4-fluorophenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
593	N2-(tert-butyl group)-N8-(6-methoxypyridine-3-yl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	592
593		594	N2-(tert-butyl group)-N8-phenyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
595	N2-(oxolane-2-ylmethyl)-N8-(3,4, the 5-trimethoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	594
595		596	N4-[4-(1-acetyl group-2,3-dihydro-1H-indoles-5-yl) pyrimidine-2-base]-2-chloro-N1, N1-dimethyl benzene-1,4-diamines
597	N8-(3,4, the 5-trimethoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	596
597		598	N8-(3-chlorphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
599	N8-(3-chlorphenyl)-N2-(oxolane-2-Ji Jia	598

	Base)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
		600	N8-(3-methoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
601	N8-(3-methoxyphenyl)-N2-(oxolane-2-ylmethyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	600
601		602	N8-(3-nitrobenzophenone)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
603	N8-(3-nitrobenzophenone)-N2-(oxolane-2-ylmethyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	602
603		604	N8-(4-fluoro-3-aminomethyl phenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
605	N8-(4-fluoro-3-aminomethyl phenyl)-N2-(2-methoxyl group-1-Methylethyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	604
605		606	N8-(4-fluoro-3-aminomethyl phenyl)-N2-(oxolane-2-ylmethyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
607	N8-(4-fluorophenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	606
607		608	N8-(4-fluorophenyl)-N2-(2-methoxyl group-1-Methylethyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
609	N8-(4-fluorophenyl)-N2-(oxolane-2-ylmethyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	608
609		610	N8-(4-fluorophenyl)-N2, N2-dimethyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	1.78*
611	N8-(6-methoxypyridine-3-yl)-4,5-dihydro [1,3] thiophene	610		1.78*

	Azoles [4,5-h] quinazoline-2, the 8-diamines
	Azoles [4,5-h] quinazoline-2, the 8-diamines		612	N8-(6-methoxypyridine-3-yl)-N2-(oxolane-2-ylmethyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
613	N8-phenyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines		612
613			614	N8-phenyl-N2-(oxolane-2-ylmethyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines
615	N-1,3-benzo dioxole-5-base-2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-amine	2.25*	614
615		2.25*	616	N-1,3-benzo dioxole-5-base-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	2.44*
617	N-1,3-benzo dioxole-5-base-4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	2.96*	616		2.44*
617		2.96*	618	N-1,3-benzo dioxole-5-base-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	2.77*
619	N-1,3-benzo dioxole-5-base-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.25*	618		2.77*
619		3.25*	620	N-1,3-benzo dioxole-5-base-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.47*
621	N-acetyl group-N-(3-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) acetamide	1.87*	620		2.47*
621		1.87*	622	N-acetyl group-N-(3-{ acetyl group [4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) acetamide	2.39*
623	N-phenyl-4-{2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine		622		2.39*
623			624	The tert-butyl group-(3-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) carbamate	2.87*
625	The tert-butyl group-(4-{[4-(2,4-dimethyl-1,3-thiazoles-5-	2.7**	624		2.87*

	Base) pyrimidine-2-base] amino } benzyl) carbamate
	Base) pyrimidine-2-base] amino } benzyl) carbamate		626	The tert-butyl group-(4-{[4-(2-amino-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } benzyl) carbamate
627	The tert-butyl group-(4-{[4-(2-amino-4-cyclopropyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } benzyl) carbamate		626
627			628	The tert-butyl group-(4-{[4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) carbamate	1.86*
629	The tert-butyl group-(4-{[4-(2-amino-4-sec-butyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } benzyl) carbamate		628		1.86*
629			630	The tert-butyl group-(4-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) carbamate	3.46*
631	The tert-butyl group-(4-{[4-(2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } benzyl) carbamate		630		3.46*
631			632	The tert-butyl group-(4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) carbamate	3.26*
633	The tert-butyl group-(4-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) carbamate	3.68*	632		3.26*
633		3.68*	634	The tert-butyl group-(4-{[4-(2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) carbamate
635	The tert-butyl group-(4-{[4-(4-cyclopropyl-2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } benzyl) carbamate		634
635			636	The tert-butyl group-(4-{[4-(4-cyclopropyl-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) carbamate
637	The tert-butyl group-(4-{[4-(4-sec-butyl-2-ethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } benzyl) carbamate		636
637			638	The tert-butyl group-(4-{[4-(4-sec-butyl-2-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) carbamate
639	The tert-butyl group-[3-(4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) benzyl] carbamate	2.94*	638
639		2.94*	640	The tert-butyl group-[4-({ 4-[2-(acetyl amine)-1,3-thiazoles-5-

	Base] pyrimidine-2-base } amino) benzyl] carbamate
	Base] pyrimidine-2-base } amino) benzyl] carbamate	641	The tert-butyl group-[4-(4-[2-(acetyl amine)-4-cyclopropyl-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) benzyl] carbamate
642	The tert-butyl group-[4-(4-[2-(acetyl amine)-4-sec-butyl-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) benzyl] carbamate	641
642		643	The tert-butyl group-[4-(4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) benzyl] carbamate	2.99*
644	The tert-butyl group-and 4-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate	643		2.99*
644		645	The tert-butyl group-and the 4-[(4-{2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate
646	The tert-butyl group-and 4-[(4-{2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate	645
646		647	The tert-butyl group-and the 4-[(4-{2-[(trifluoroacetyl group) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate
648	The tert-butyl group-and 4-[(4-{4-cyclopropyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate	647
648		649	The tert-butyl group-and 4-[(4-{4-cyclopropyl-2-[(2-methoxy ethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate
650	The tert-butyl group-and 4-[(4-{4-cyclopropyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate	649

651	The tert-butyl group-and 4-[(4-{4-cyclopropyl-2-[(trifluoroacetyl group) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate
651			652	The tert-butyl group-and 4-[(4-{4-sec-butyl-2-[(2-methoxyl group-1-Methylethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate
653	The tert-butyl group-and 4-[(4-{4-sec-butyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate		652
653			654	The tert-butyl group-and 4-[(4-{4-sec-butyl-2-[(trifluoroacetyl group) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] benzyl } carbamate
655	N2, N2-dimethyl-N8-(3,4, the 5-trimethoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	1.67*	654
655		1.67*	656	Methyl-(4-{[4-(2-amino-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate	1.31*
657	N-{4-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } Methanesulfomide	1.53*	656		1.31*
657		1.53*	658	The tert-butyl group-[3-(4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) benzyl] carbamate	1.99*
659	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-phenyl-1,3,5-triazines-2-amine		658		1.99*
659			660	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl-1,3,5-triazines-2-amine
661	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl-1,3,5-triazines-2-amine		660
661			662	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl)-1,3,5-triazines-2-amine
663	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-		662

	Base)-N-(3,4, the 5-trimethoxyphenyl)-1,3,5-triazines-2-amine
			664	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl)-1,3,5-triazines-2-amine
665	N-(3-acetylphenyl)-N-[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] acetamide	2.43*	664
665		2.43*	666	N-[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-N-(3,4, the 5-trimethoxyphenyl) acetamide	2.53*
667	N-[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-yl]-N-(3,4, the 5-trimethoxyphenyl) acetamide	1.9*	666		2.53*
667		1.9*	668	N-[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-phenyl acetanilide,Phenacetylaniline	2.33*
669	N-[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-N-(3,4, the 5-trimethoxyphenyl) acetamide	2.19*	668		2.33*
669		2.19*	670	N-acetyl group-N-(3-{ acetyl group-[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzyl) acetamide	Feb 39
671	N-(3-acetylphenyl)-N-[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] acetamide	2.23*	670		Feb 39
671		2.23*	672	Methyl-(4-{[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate	2.51*
673	1-{4-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } ethyl ketone	2.36*	672		2.51*
673		2.36*	674	2-chloro-N4-[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-base]-N1, N1-dimethyl benzene-1,4-diamines	2*
675	N-[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-yl]-N-(3,4, the 5-trimethoxyphenyl) acetamide	1.9*	674		2*
675		1.9*	676	N-(3-acetylphenyl)-N-[4-(2-cyclopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] acetamide	2.43*
677	N-(4-fluorophenyl)-4-{2-[(2-methoxy ethyl) ammonia	1.9*	676		2.43*

	Base]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine
			678	The 4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-phenyl pyrimidine-2-amine	1.82*
679	The 4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	1.74*	678		1.82*
679		1.74*	680	N-(3-chlorphenyl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	2.28*
681	The 4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(3-methoxyphenyl) pyrimidine-2-amine	1.86*	680		2.28*
681		1.86*	682	The N-{3-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } acetamide	1.36*
683	The N-{4-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } acetamide	1.35*	682		1.36*
683		1.35*	684	N-[3-(4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.26*
685	1-[3-(4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	1.89*	684		1.26*
685		1.89*	686	4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine	2.34*
687	N-(3-chlorphenyl)-4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.62*	686		2.34*
687		2.62*	688	4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-phenyl pyrimidine-2-amine	1.98*
689	The 1-{3-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone	1.69*	688		1.98*
689		1.69*	690	The 3-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenol	1.38*
691	The N-{4-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl	1.39*	690		1.38*

	-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } Methanesulfomide
			692	4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-(4-fluoro-3-aminomethyl phenyl) pyrimidine-2-amine	4.43*
693	Methyl-[4-(4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] carbamate	2.7*	692		4.43*
693		2.7*	694	Methyl-[4-(4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] carbamate	3.04*
695	N-(3-chlorphenyl)-4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine	4.51*	694		3.04*
695		4.51*	696	4-(4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenol	2.39*
697	4-(4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenol	2.64*	696		2.39*
697		2.64*	698	N-[4-(4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	2.26*
699	N-[4-(4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	2.58*	698		2.26*
699		2.58*	700	2-chloro-N1, N1-dimethyl-N4-{4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-base } benzene-1, the 4-diamines	2.88*
701	2-chloro-N4-{4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-base }-N1, N1-dimethyl benzene-1,4-diamines	3.46*	700		2.88*
701		3.46*	702	3-(4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenol	2.84*
703	N-1,3-benzo dioxole-5-base-4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine	3.21*	702		2.84*
703		3.21*	704	N-1,3-benzo dioxole-5-base-4-[2-(two	3.63*

	Methyl amine)-and 4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine
			705	N-(3, the 4-difluorophenyl)-4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine	3.76*
706	N-(3, the 5-Dimethoxyphenyl)-4-[2-methyl-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine	3.41*	705		3.76*
706		3.41*	707	N-(3, the 5-Dimethoxyphenyl)-4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine	3.85*
708	4-[4-(difluoromethyl)-2-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.61*	707		3.85*
708		2.61*	709	1-[3-(4-[4-(difluoromethyl)-2-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.64*
710	4-[4-(difluoromethyl)-2-methyl isophthalic acid, 3-thiazole-5-yl]-N-phenyl pyrimidine-2-amine	2.97*	709		2.64*
710		2.97*	711	4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino }-N-(2-methoxy ethyl) benzamide	2.09*
712	Methyl-[3-(4-[4-methyl-2-(methyl mercapto)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) benzyl] carbamate	2.16*	711		2.09*
712		2.16*	713	4-(4-methyl-2-pyridin-3-yl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.56*
714	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-pyridin-3-yl pyrimidine-2-amine	1.35*	713		2.56*
714		1.35*	715	4-(4-methyl-2-pyridin-3-yl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine	3.04*
716	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-pyridine-3-yl pyrimidines-2-amine	0.98*	715		3.04*
716		0.98*	717	1-(4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	2.6*
718	N-(3, the 4-3,5-dimethylphenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.71*	717		2.6*

719	N-(3, the 5-Dimethoxyphenyl)-4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine	2.02*
719		2.02*	720	1-{4-[(4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } pyrrolidin-2-one	1.6*
721	N-[6-(2,2-dimethyl propoxyl group) pyridin-3-yl]-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	4.23*	720		1.6*
721		4.23*	722	N-(8-anilino--4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl) acetamide	1.83*
723	N-{3-[(2-acetylaminohydroxyphenylarsonic acid 4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } acetamide	1.38*	722		1.83*
723		1.38*	724	N-[8-(the 3-[(methyl sulphonyl) and amino] phenyl } amino)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl] acetamide	1.54*
725	The 4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-phenyl pyrimidine-2-amine	1.81*	724		1.54*
725		1.81*	726	N-(3-chlorphenyl)-4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	2.28*
727	1-{4-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } pyrrolidin-2-one	1.94*	726		2.28*
727		1.94*	728	1-{4-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } pyrrolidin-2-one	1.64*
729	1-{4-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone	1.92*	728		1.64*
729		1.92*	730	N-{8-[(3,4, the 5-trimethoxyphenyl) amino]-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2-yl } acetamide	1.76*
731	4-(4-methyl-2-morpholine-4-base-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine	2.25*	730		1.76*

732	Methyl-[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] carbanilate	2.59*
732		2.59*	733	1-(4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) fourth-1-ketone	3.5*
734	1-(3-{[4-(4-methyl-2-pyridin-3-yl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	2.56*	733		3.5*
734		2.56*	735	4-(4-methyl-2-morpholine-4-base-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.07*
736	1-(3-{[4-(4-methyl-2-morpholine-4-base-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	2.16*	735		2.07*
736		2.16*	737	N-(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) benzene-1, the 4-diamines	1.68*
738	The 1-{3-[(4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone	1.75*	737		1.68*
738		1.75*	739	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3, the 5-Dimethoxyphenyl) pyrimidine-2-amine	2.44*
740	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(2,3-dihydro-1,4-benzo dioxine-6-yl) pyrimidine-2-amine	2.11*	739		2.44*
740		2.11*	741	1-[4-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] pyrrolidin-2-one	1.96*
742	1-[4-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.35*	741		1.96*
742		2.35*	743	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3, the 4-Dimethoxyphenyl) pyrimidine-2-amine	2*
744	N-1,3-benzo dioxole-5-base-4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.14*	743		2*
744		2.14*	745	N-(3-chlorphenyl)-4-(4-methyl-2-morpholine-4-base-1,3-thiazole-5-yl) pyrimidine-2-amine	2.99*
746	4-(4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl]	1.11*	745		2.99*

	Pyrimidine-2-base } amino) phenol
	Pyrimidine-2-base } amino) phenol		747	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(5-picoline-3-yl) pyrimidine-2-amine	1.41*
748	1-(4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) pyrrolidin-2-one	2.24*	747		1.41*
748		2.24*	749	1-(4-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) pyrrolidin-2-one	1.99*
750	N-(4-fluoro-3-aminomethyl phenyl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	2.04*	749		1.99*
750		2.04*	751	The 1-{4-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone	1.72*
752	The 1-{4-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } pyrrolidin-2-one	1.51*	751		1.72*
752		1.51*	753	1-{3-[(2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl) amino] phenyl } pyrrolidin-2-one	2.01*
754	4-(4-[4-methyl-2-(methyl amine)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) the phenylacetic acid ester	1.73*	753		2.01*
754		1.73*	755	N-(3, the 4-difluorophenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.44*
756	N-(3, the 4-difluorophenyl)-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	2.99*	755		3.44*
756		2.99*	757	N-(3-chlorphenyl)-4-[4-(difluoromethyl)-2-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	1.41*
758	The tert-butyl group-[4-(4-[4-(difluoromethyl)-2-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) benzyl] carbamate	3.2*	757		1.41*
758		3.2*	759	N-(2, the 4-difluorophenyl)-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	2.8*
760	N-(2, the 4-difluorophenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	3.27*	759		2.8*

761	1-[4-(4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] pyrrolidin-2-one	1.6*
761		1.6*	762	N-[3-(4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.42*
763	4-(4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenol	1.8*	762		1.42*
763		1.8*	764	N-(3, the 5-Dimethoxyphenyl)-4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.73*
765	3-methoxy-propyl-4-(4-[2-(methoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) benzoic ether	2.63*	764		2.73*
765		2.63*	766	4-(4-methyl-2-propyl group-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine	3.49*
767	1-(3-{[4-(4-methyl-2-propyl group-1,3-thiazoles-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	3.04*	766		3.49*
767		3.04*	768	4-(4-methyl-2-propyl group-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.93*
769	1-[4-(4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	3.44*	768		2.93*
769		3.44*	770	1-[4-(4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] pyrrolidin-2-one	2.99*
771	1-[3-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] pyrrolidin-2-one	1.93*	770		2.99*
771		1.93*	772	1-{3-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } pyrrolidin-2-one	1.68*
773	N8-(4-fluorophenyl)-N2-(2-methoxy ethyl)-N2-methyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	1.94*	772		1.68*

774	4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(2,2,3,3-tetrafluoro-2,3-dihydro-1,4-benzo dioxine-6-yl) pyrimidine-2-amine	3.6*
774		3.6*	775	1-[3-(4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] pyrrolidin-2-one	3.07*
776	N2-(3-methoxy-propyl)-N2-methyl-N8-(3,4, the 5-trimethoxyphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	1.89*	775		3.07*
776		1.89*	777	4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-(4-fluorophenyl) pyrimidine-2-amine	3.96*
778	4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-(4-iodophenyl) pyrimidine-2-amine	4.88*	777		3.96*
778		4.88*	779	N-(2,2-two fluoro-1,3-benzo dioxole-5-yl)-4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine	4.72*
780	4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-(2,2,3,3-tetrafluoro-2,3-dihydro-1,4-benzo dioxine-6-yl) pyrimidine-2-amine	5.28*	779		4.72*
780		5.28*	781	The 4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(3-nitrobenzophenone) pyrimidine-2-amine	1.97*
782	1-[3-(4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] pyrrolidin-2-one	1.65*	781		1.97*
782		1.65*	783	4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	3.17*
784	The 4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	1.45*	783		3.17*
784		1.45*	785	4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	1.55*
786	4-(2-phenyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	3.37*	785		1.55*

787	N-phenyl-4-(2-phenyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	3.97*
787	N-phenyl-4-(2-phenyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	3.97*	788	4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(4-methoxyphenyl) pyrimidine-2-amine	2.34*
789	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-methoxyphenyl) pyrimidine-2-amine	2.78*	788		2.34*
789		2.78*	790	5-{[4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-yl] amino }-the 2-metoxyphenol	1.79*
791	5-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino }-the 2-metoxyphenol	2.09*	790		1.79*
791		2.09*	792	4-[2-(4-chlorphenyl)-1,3-thiazoles-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	4.12*
793	4-[2-(4-chlorphenyl)-1,3-thiazoles-5-yl]-N-phenyl pyrimidine-2-amine	4.85*	792		4.12*
793		4.85*	794	N-(2,4 dichloro benzene base)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	4.9*
795	N-(3-chlorphenyl)-4-[2-(4-chlorphenyl)-1,3-thiazoles-5-yl] pyrimidine-2-amine	5.57*	794		4.9*
795		5.57*	796	Ethyl-(4-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) carbamate	2.18*
797	N5-(4-fluorophenyl)-N2, N2-dimethyl-8H-[1,3] thiazole [4 ', 5 ': 4,5] cyclopenta [1,2-d] pyrimidine-2, the 5-diamines	1.56*	796		2.18*
797		1.56*	798	N-(4-fluorophenyl)-4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.36*
799	4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-methyl-3-nitro phenyl) pyrimidine-2-amine	2.68*	798		2.36*
799		2.68*	800	N-(3, the 4-Dimethoxyphenyl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	1.55*
801	N-(3, the 5-Dimethoxyphenyl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	1.96*	800		1.55*

802	N-1,3-benzo dioxole-5-base-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	1.65*
802		1.65*	803	N-(2,3-dihydro-1,4-benzo dioxine-6-yl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	1.63*
804	N-(3-chloro-4-methoxyphenyl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	1.96*	803		1.63*
804		1.96*	805	2-chloro-N4-(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base)-N1, N1-dimethyl benzene-1,4-diamines	1.57*
806	The 4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(4-methyl-3-nitro phenyl) pyrimidine-2-amine	2.17*	805		1.57*
806		2.17*	807	The 4-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] benzonitrile	1.9*
808	The 4-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenol	1.22*	807		1.9*
808		1.22*	809	N-(2, the 4-difluorophenyl)-4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine	2.09*
810	N-(4-methyl-3-nitro phenyl)-4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine	2.33*	809		2.09*
810		2.33*	811	4-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) benzonitrile	2.63*
812	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-chloro-4-methoxyphenyl) pyrimidine-2-amine	2.52*	811		2.63*
812		2.52*	813	N4-{4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-base }-2-chloro-N1, N1-dimethyl benzene-1,4-diamines	2.09*
814	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(2, the 4-difluorophenyl) pyrimidine-2-amine	2.71*	813		2.09*

815	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-methyl-3-nitro phenyl) pyrimidine-2-amine	2.88*
815		2.88*	816	1-{4-[(4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone	1.83*
817	N-(3, the 4-Dimethoxyphenyl)-4-{4-methyl-2-[(oxolane-2-ylmethyl) amino]-1,3-thiazoles-5-yl } pyrimidine-2-amine	1.65*	816		1.83*
817		1.65*	818	N-(3-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) acetamide	2.26*
819	N-(3, the 4-Dimethoxyphenyl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	2.85*	818		2.26*
819		2.85*	820	1-(4-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	3.06*
821	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-methoxyphenyl) pyrimidine-2-amine	3.25*	820		3.06*
821		3.25*	822	4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-phenyl pyrimidine-2-amine	2.2*
823	4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.06*	822		2.2*
823		2.06*	824	1-[3-(4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.08*
825	N-(3-chlorphenyl)-4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	2.74*	824		2.08*
825		2.74*	826	4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-methoxyphenyl) pyrimidine-2-amine	2.22*
827	N-[3-(4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.63*	826		2.22*
827		1.63*	828	1-[4-(4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.13*
829	N-(4-fluoro-3-aminomethyl phenyl)-4-[2-(isobutylamine)-4-	2.55*	828		2.13*

	Methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine
			830	4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	1.87*
831	1-(4-{[4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) pyrrolidin-2-one	2.56*	830		1.87*
831		2.56*	832	N-(2, the 4-difluorophenyl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	1.99*
833	N-[4-(4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.58*	832		1.99*
833		1.58*	834	1-[4-(4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] pyrrolidin-2-one	1.82*
835	4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-fluorophenyl) pyrimidine-2-amine	2.32*	834		1.82*
835		2.32*	836	4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-phenyl pyrimidine-2-amine	2.2*
837	4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.04*	836		2.2*
837		2.04*	838	4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine	2.46*
839	1-[3-(4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.07*	838		2.46*
839		2.07*	840	4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-chlorphenyl) pyrimidine-2-amine	2.75*
841	4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-methoxyphenyl) pyrimidine-2-amine	2.23*	840		2.75*
841		2.23*	842	N-[3-(4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.65*
843	N-[4-(4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.59*	842		1.65*
843		1.59*	844	1-[4-(4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.2*

845	1-[4-(4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] pyrrolidin-2-one	1.8*
845		1.8*	846	4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-fluoro-3-aminomethyl phenyl) pyrimidine-2-amine	2.67*
847	4-[2-(butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	1.85*	846		2.67*
847		1.85*	848	N-[3-(4-acetyl group piperazine-1-yl)-4-fluorophenyl]-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	2.42*
849	4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-fluorophenyl) pyrimidine-2-amine	1.99*	848		2.42*
849		1.99*	850	4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	1.77*
851	N-(4-fluorophenyl)-4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	1.92*	850		1.77*
851		1.92*	852	N-(3-methoxyphenyl)-4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	1.89*
853	The N-{3-[(4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } acetamide	1.44*	852		1.89*
853		1.44*	854	The N-{4-[(4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } acetamide	1.4*
855	The 1-{4-[(4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } ethyl ketone	1.81*	854		1.4*
855		1.81*	856	The 1-{4-[(4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } pyrrolidin-2-one	1.57*
857	N-(4-fluoro-3-aminomethyl phenyl)-4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	2.11*	856		1.57*
857		2.11*	858	The 4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, the 3-thiophene	1.57*

	Azoles-5-yl }-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine
	Azoles-5-yl }-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine		859	4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine	3.99*
860	N-[3-(4-[2-(dimethyl amine)-4-(trifluoromethyl)-1,3-thiazoles-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	2.65*	859		3.99*
860		2.65*	861	The 1-{3-[(4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] phenyl } pyrrolidin-2-one	1.62*
862	N-[4-(4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] acetamide	1.33*	861		1.62*
862		1.33*	863	4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-fluoro-3-methoxyphenyl) pyrimidine-2-amine	2.99*
864	4-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino] benzsulfamide	1.49*	863		2.99*
864		1.49*	865	The 4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(3-nitrobenzophenone) pyrimidine-2-amine	2.03*
866	The 4-{2-[(3-methoxy-propyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl }-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	1.73*	865		2.03*
866		1.73*	867	1-[4-(4-[2-(dimethyl amine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	1.9*
868	4-[2-(isobutylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine	2.47*	867		1.9*
868		2.47*	869	N2, N2-dimethyl-N5-phenyl-8H-[1,3] thiazole [4 ', 5 ': 4,5] cyclopenta [1,2-d] pyrimidine-2, the 5-diamines	1.49*
870	1-(4-{[2-(dimethyl amine)-8H-[1,3] thiazole [4 ', 5 ': 4,5] cyclopenta [1,2-d] pyrimidine-5-yl] amino } phenyl) pyrrolidin-2-one	1.37*	869		1.49*

871	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(6-chloropyridine-3-yl) pyrimidine-2-amine	2.48*
871		2.48*	872	N-(6-chloropyridine-3-yl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	1.71*
873	5-chloro-4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine	3.26*	872		1.71*
873		3.26*	874	5-chloro-4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.82*
875	5-chloro-N-(3-chlorphenyl)-4-(2,4-dimethyl-1,3-thiazoles-5-yl) pyrimidine-2-amine	3.86*	874		2.82*
875		3.86*	876	5-chloro-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	3.78*
877	5-chloro-N-(4-chlorphenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	4.48*	876		3.78*
877		4.48*	878	5-chloro-N-(2-chlorphenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	4.62*
879	N '-[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-N, N-dimethyl benzene-1,4-diamines	1.56*	878		4.62*
879		1.56*	880	N '-[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base]-N, N-dimethyl benzene-1,3-diamines	1.99*
881	2-methoxy ethyl-4-{[4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } benzoic ether	2.91*	880		1.99*
881		2.91*	882	4-(the 2-tert-butyl group-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	4.24*
883	4-(the 2-tert-butyl group-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(4-fluorophenyl) pyrimidine-2-amine	4.18*	882		4.24*
883		4.18*	884	4-(the 2-tert-butyl group-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3-chlorphenyl) pyrimidine-2-amine	4.82*
885	1-(4-{[4-(the 2-tert-butyl group-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	4.22*	884		4.82*
885		4.22*	886	4-(the 2-tert-butyl group-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(6-	3.42*

	Methoxypyridine-3-yl) pyrimidine-2-amine
	Methoxypyridine-3-yl) pyrimidine-2-amine		887	1-(3-{[4-(the 2-tert-butyl group-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino } phenyl) ethyl ketone	3.66*
888	4-(the 2-tert-butyl group-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	3.48*	887		3.66*
888		3.48*	889	6-[(4-{2-[(2-methoxyl group-1-Methylethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino]-2-benzofuran-1 (3H)-ketone	1.65*
890	The 6-[(4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-base) amino]-2-benzofuran-1 (3H)-ketone	1.53*	889		1.65*
890		1.53*	891	The 2-[(5-{2-[(4-fluorophenyl) amino] pyrimidine-4-yl }-the 4-methyl isophthalic acid, the 3-thiazol-2-yl) amino] ethanol	1.5*
892	6-(4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino)-2-benzofuran-1 (3H)-ketone	2*	891		1.5*
892		2*	893	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3, the 4-3,5-dimethylphenyl) pyrimidine-2-amine	2.79*
894	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3, the 4-difluorophenyl) pyrimidine-2-amine	2.96*	893		2.79*
894		2.96*	895	4-[2-(tert-butylamine)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(4-chlorphenyl) pyrimidine-2-amine	3.13*
896	N-(3, the 4-3,5-dimethylphenyl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	2.08*	895		3.13*
896		2.08*	897	N-(3, the 4-difluorophenyl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	2.15*
898	N-(4-chlorphenyl)-4-{2-[(2-methoxy ethyl) amino]-the 4-methyl isophthalic acid, 3-thiazole-5-yl } pyrimidine-2-amine	2.24*	897		2.15*
898		2.24*	899	N-(4-fluorophenyl)-4-[2-(2-methoxy ethoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	3.12*
900	The N2-tert-butyl group-N8-(4-fluorophenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	2.22*	899		3.12*

901	4-[2-(2-methoxy ethoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-phenyl pyrimidine-2-amine	3.01*
901		3.01*	902	5-bromo-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	3.82*
903	5-chloro-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	4.27*	902		3.82*
903		4.27*	904	5-bromo-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-phenyl pyrimidine-2-amine	4.32*
905	5-bromo-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	3.29*	904		4.32*
905		3.29*	906	5-bromo-4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.85*
907	5-chloro-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	3.2*	906		2.85*
907		3.2*	908	5-bromo-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	3.65*
909	5-bromo-4-(2,4-dimethyl-1,3-thiazoles-5-yl)-N-phenyl pyrimidine-2-amine	3.3*	908		3.65*
909		3.3*	910	4-[2-(2-methoxy ethoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3,4, the 5-trimethoxyphenyl) pyrimidine-2-amine	2.53*
911	4-[2-(2-methoxy ethoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-nitrobenzophenone) pyrimidine-2-amine	3.08*	910		2.53*
911		3.08*	912	1-[3-(4-[2-(2-methoxy ethoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] ethyl ketone	2.64*
913	N-(3-chlorphenyl)-4-[2-(2-methoxy ethoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] pyrimidine-2-amine	3.57*	912		2.64*
913		3.57*	914	4-[2-(2-methoxy ethoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(3-methoxyphenyl) pyrimidine-2-amine	2.92*
915	4-[2-(2-methoxy ethoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl]-N-(6-methoxypyridine-3-yl) pyrimidine-2-amine	2.34*	914		2.92*
915		2.34*	916	1-[4-({ 4-[2-(2-methoxy ethoxy)-4-methyl	2.58*

	-1,3-thiazoles-5-yl] pyrimidine-2-base } amino) phenyl] ethyl ketone
			917	1-[4-(4-[2-(2-methoxy ethoxy)-4-methyl isophthalic acid, 3-thiazole-5-yl] and pyrimidine-2-base } amino) phenyl] pyrrolidin-2-one	2.23*
918	The N2-tert-butyl group-N8-phenyl-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	2.15*	917		2.23*
918		2.15*	919	4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl)-N-pyridin-3-yl pyrimidine-2-amine	1.51*
920	5-bromo-N-(3-chlorphenyl)-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	4.36*	919		1.51*
920		4.36*	921	4-{[5-bromo-4-(2-ethyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-base] amino }-N, the N-dimethyl benzene sulfonamide	3.36*
922	5-bromo-N-(3-chlorphenyl)-4-(2-isopropyl-4-methyl isophthalic acid, 3-thiazole-5-yl) pyrimidine-2-amine	4.9*	921		3.36*
922		4.9*	923	The N2-tert-butyl group-N8-(3-chlorphenyl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	2.99*
924	1-(4-{[2-(tert-butylamine)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) ethyl ketone	2.47*	923		2.99*
924		2.47*	925	1-(4-{[2-(tert-butylamine)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-8-yl] amino } phenyl) pyrrolidines-2-ketone	1.91*
926	The N2-tert-butyl group-N8-(6-methoxypyridine-3-yl)-4,5-dihydro [1,3] thiazole [4,5-h] quinazoline-2,8-diamines	1.95*	925		1.91*

^aThe logP value is according to EEC the 79/831st trumpeter's volume appendix V.A8 (EEC Directive 79/831Annex V.A8), use following method to measure by reversed-phase column (C18) HPLC (high performance liquid chromatography):

* temperature: 40 ℃; Flowing phase: 0.1% aqueous formic acid and acetonitrile; Linear gradient is from 10% acetonitrile to 95% acetonitrile.

* temperature: 43 ℃; Flowing phase: 0.1% phosphate aqueous solution and acetonitrile; Linear gradient is from 10% acetonitrile to 95% acetonitrile.

The known unbranched alkane-2-ketone (containing 3 to 16 carbon atoms) of each personal logP value is demarcated (based on retention time, using the linear interpolation between two specific alkane ketone to determine the logP value).

Use the UV spectrum between 190nm to 400nm to determine that the chromatographic signal maximum is the λ maximum separately.

Purposes embodiment

Embodiment A

The withered ball of grain husk chamber bacterium test (wheat)/protectiveness

Solvent: 50 weight portion N,N-dimethylacetamide

Emulsifier: 1 weight portion alkylaryl polyglycol ether

In order to prepare suitable active agent preparations,, and dope is diluted with water to desired concn with the reactive compound of 1 weight portion and the solvent and the emulsifier of described amount.

Active in order to test protection, immature plant is sprayed with described rate of application with active agent preparations.After spraying layer exsiccation, the spore suspension of plant with clever withered ball chamber bacterium (Leptosphaeria nodorum) sprayed.Make plant be statically placed in 20 ℃, relative 24h in the culturing room of atmospheric humidity 100%.

Plant is put into the greenhouse of about 20 ℃ of temperature, relative atmospheric humidity 80%.

Inoculating back 10 days assesses.The 0% expression drug effect suitable with control group, and 100% drug effect is represented not observe and is infected.

In this test, following compound of the present invention shows 70% or higher drug effect when activity compound concentration is 1000ppm:

7、62、73、151、182、190、240、244、247、251、461、742、759

Embodiment B

Fusarium graminearum test (barley)/protectiveness

Solvent: 50 weight portion N,N-dimethylacetamide

Emulsifier: 1 weight portion alkylaryl polyglycol ether

Active in order to test protection, immature plant is sprayed with described rate of application with active agent preparations.After spraying layer exsiccation, the conidial suspension of plant with Fusarium graminearum (Fusarium graminearum) sprayed.

Plant is placed about 22 ℃ of temperature under the translucent culture hood (translucent incubation hoods), the greenhouse of relative atmospheric humidity 100%.

Inoculating back 4 days assesses.The 0% expression drug effect suitable with control group, and 100% drug effect is represented not observe and is infected.

9、151、182、190、222、235、240、243、244、247、251、375、461

Embodiment C

Single softgel shell belongs to test (cucumber)/protectiveness

Solvent: 24.5 weight portion acetone

24.5 weight portion dimethylacetylamide

Emulsifier: 1 weight portion alkylaryl polyglycol ether

Active in order to test protection, immature plant is sprayed with described rate of application with active agent preparations.After spraying layer exsiccation, with the aqueous spore suspension inoculation of plant with garden balsam list softgel shell (Sphaerotheca fuliginea).Then plant is placed about 23 ℃, the relative greenhouse of atmospheric humidity about 70%.

Inoculating back 7 days assesses.The 0% expression drug effect suitable with control group, and 100% drug effect is represented not observe and is infected.

In this test, when following formula: compound of the present invention is 100ppm at activity compound concentration, show 70% or higher drug effect:

10、244

Embodiment D

Botrytis test (beans)/protectiveness

Solvent: 24.5 weight portion acetone

24.5 weight portion dimethylacetylamide

Emulsifier: the alkylaryl polyglycol ether of 1 weight portion

In order to prepare suitable active agent preparations,, and dope is diluted to desired concn with water with the reactive compound of 1 weight portion and the solvent and the emulsifier of described amount.

Active in order to test protection, immature plant is sprayed with described rate of application with active agent preparations.After spraying layer and becoming dry, on every leaf, place and grow Botrytis cinerea the is arranged two small pieces agar of (Botrytiscinerea).Postvaccinal plant is placed about 20 ℃, the relative darkroom of atmospheric humidity 100%.

Inoculate back 2 days, infect the size in zone on the assessment leaf.The 0% expression drug effect suitable with control group, and 100% drug effect is represented not observe and is infected.

201、210、244、742、758、759、780

Embodiment E

The mould test of epidemic disease (tomato)/protectiveness

Solvent: 49 weight portion N, dinethylformamide

Emulsifier: 1 weight portion alkylaryl polyglycol ether

Active in order to test protection, immature tomato plant is sprayed with described rate of application with active agent preparations.Handle after 1 day,, make plant under relative moisture 100%, 20 ℃, leave standstill 24h then the spore suspension inoculation of plant with phytophthora infestans (Phytophthora infestans).Then plant is placed about 96%, the about 20 ℃ phytotron (climatized chamber) of temperature of relative atmospheric humidity.

In this test, when following formula: compound of the present invention is 500ppm at activity compound concentration, show 70% or higher drug effect:

69、73、182、186、201、203、210、235、239、243、247、251、321、324、327、329、460、628、630

Embodiment F

Pears spore test (rice)/protectiveness

Solvent: 28.5 weight portion acetone

Emulsifier: 1.5 weight portion alkylaryl polyglycol ethers

In order to prepare suitable active agent preparations,, and the emulsifier of dope water and described amount is diluted to desired concn with the reactive compound of 1 weight portion and the solvent of described amount.

Active in order to test protection, immature rice plants is sprayed with described rate of application with active agent preparations.Handle after 1 day, with the aqueous spore suspension inoculation of plant with Magnaporthe grisea (Pyricularia oryzae).Then plant is placed relative atmospheric humidity 100%, 25 ℃ greenhouse.

In this test, following example number compound of the present invention shows 80% or higher drug effect when activity compound concentration is 500ppm:

9、235、243

Embodiment G

Rhizoctonia test (rice)/protectiveness

Solvent: 28.5 weight portion acetone

Emulsifier: 1.5 weight portion alkylaryl polyglycol ethers

Active in order to test protection, immature rice plants is sprayed with described rate of application with active agent preparations.Handle after 1 day, with the mycelium inoculation of plant with Rhizoctonia solani Kuhn (Rhizoctonia solani).Then plant is placed relative atmospheric humidity 100%, 25 ℃ greenhouse.

9、235、243、244

Embodiment H

Cochliobolus belongs to test (rice)/protectiveness

Solvent: 28.5 weight portion acetone

Emulsifier: 1.5 weight portion alkylaryl polyglycol ethers

Active in order to test protection, immature rice plants is sprayed with described rate of application with active agent preparations.Handle after 1 day, with the aqueous spore suspension inoculation of plant with palace portion's cochliobolus (Cochliobolusmiyabeanus).Then plant is placed relative atmospheric humidity 100%, 25 ℃ greenhouse.

235、243、244

Claims

1. formula (I) compound and agrochemicals active salt thereof are as the purposes of bactericide

Wherein each symbol is as giving a definition:

R ⁵Be hydrogen, the unsubstituted or C that replaces ₁-C ₈Alkyl, the unsubstituted or C that replaces ₁-C ₄Alkyl C (=O), C ₁-C ₄Alkyl OC (=O), the unsubstituted or C that replaces ₁-C ₄Alkoxyl (C ₁-C ₄) alkyl, the unsubstituted or C that replaces ₂-C ₆Thiazolinyl, the unsubstituted or C that replaces ₂-C ₆Alkynyl, C ₁-C ₆Alkyl sulphinyl, C ₁-C ₆Alkyl sulphonyl, C ₃-C ₈Cycloalkyl; The C that has 1 to 9 fluorine, chlorine and/or bromine atoms separately ₁-C ₆Haloalkyl, C ₁-C ₄Haloalkyl sulfinyl, C ₁-C ₄Halogenated alkyl sulfonyl, halo-C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl, C ₃-C ₈Halogenated cycloalkyl; Formoxyl, formoxyl-C ₁-C ₃Alkyl, (C ₁-C ₃Alkyl) carbonyl-C ₁-C ₃Alkyl, (C ₁-C ₃Alkoxyl)-carbonyl-C ₁-C ₃Alkyl; Halo-(the C that has 1 to 13 fluorine, chlorine and/or bromine atoms separately ₁-C ₃Alkyl) carbonyl-C ₁-C ₃Alkyl, halo-(C ₁-C ₃Alkoxyl) carbonyl-C ₁-C ₃Alkyl; (C ₁-C ₈Alkyl) carbonyl, (C ₁-C ₈Alkoxyl) carbonyl, (C ₁-C ₈Alkylthio group) carbonyl, (C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl) carbonyl, (C ₃-C ₆Alkene oxygen base) carbonyl, (C ₃-C ₆Alkynyloxy group) carbonyl, (C ₃-C ₈Cycloalkyl) carbonyl; (the C that has 1 to 9 fluorine, chlorine and/or bromine atoms separately ₁-C ₆Haloalkyl) carbonyl, (C ₁-C ₆Halogenated alkylthio) carbonyl, (C ₁-C ₆Halogenated alkoxy) carbonyl, (C ₃-C ₆Haloalkene oxygen base) carbonyl, (C ₃-C ₆The halo alkynyloxy group) carbonyl, (halo-C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl) carbonyl, (C ₃-C ₈Halogenated cycloalkyl) carbonyl, perhaps-CH ₂-C ≡ C-R ^1-A,-CH ₂-CH=CH-R ^1-A,-CH=C=CH-R ^1-A,-C (=O) C (=O) R ²,-CONR ³R ⁴,-CH ₂NR ⁵R ⁶, C ₁-C ₄Trialkylsilkl or C ₁-C ₄Dialkyl group one phenyl silicyl,

X is nitrogen or CR ⁸,

Y is nitrogen or CR ⁹,

Z is nitrogen or CR ¹⁰,

Perhaps

R wherein ¹³Independently of one another=hydrogen, halogen, the unsubstituted or C that replaces ₁-C ₃-alkyl, the unsubstituted or C that replaces ₁-C ₃Alkoxyl or

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

Perhaps

2. formula (I) compound and agrochemicals active salt thereof be as the purposes of bactericide, and one or more in each symbol of its Chinese style (I) have one of following listed implication:

Acetyl group, C ₂H ₅C (=O), C ₃H ₇C (=O), C ₄H ₉C (=O), CF ₃C (=O), C ₂F ₅C (=O), CH ₃OC (=O), C ₂H ₅OC (=O), C ₃H ₇OC (=O), C ₃H ₇OC (=O), C ₄H ₉OC (=O), CF ₃OC (=O), CC1 ₃OC (=O), C ₂F ₅OC (=O), CH ₂OCH ₃C ₂H ₄OCH ₃, CH=CH ₂, CH ₂CH=CH ₂, C ≡ CH, CH ₂C ≡ CH, SOCH ₃, SOC ₂H ₅, SOC ₃H ₇SO ₂CH ₃, SO ₂C ₂H ₅, SO ₂C ₃H ₇, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl; CH ₂OCF ₃C ₂H ₄OCF ₃, C=ONH ₂, SiMe ₃, SiMe ₂TBu, SiMe ₂Ph,

X is nitrogen or CR ⁸,

Y is nitrogen or CR ⁹,

Z is nitrogen or CR ¹⁰,

Wherein or Y and Z be nitrogen,

Perhaps Y is that nitrogen and Z are CR ¹⁰,

Perhaps Y is CR ⁹And Z is a nitrogen,

R ⁷Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl group; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂, COR ¹¹

Perhaps

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂

Perhaps

3. formula (I) compound and agrochemicals active salt thereof be as the purposes of bactericide, and one or more in each symbol of its Chinese style (I) have one of following implication:

R ⁵Be hydrogen, acetyl group, trifluoroacetyl group,

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

Perhaps

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

Perhaps

4. formula (I) compound and agrochemicals active salt thereof be as the purposes of bactericide, and one or more in each symbol of its Chinese style (I) have one of following implication:

R ⁵Be hydrogen, COCH ₃,

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

R ⁷Be hydrogen, methyl, 1-methyl-propyl, CF ₃, CF ₂H, cyclopropyl,

Perhaps

R wherein ¹³=hydrogen,

R ¹⁰Be hydrogen

Perhaps

R wherein ¹³=hydrogen.

5. formula (I) compound and agrochemicals active salt thereof be as the purposes of bactericide, and one or more in each symbol of its Chinese style (I) have one of following implication:

R ⁵Be hydrogen, COCH ₃, COCF ₃, COOCH ₃

X is nitrogen or CR ⁸,

R ⁸Be hydrogen, O-Me,

Y is a nitrogen,

Z is CR ¹⁰,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, cyano group, CF ₃

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

R ⁶Be methyl, ethyl, isopropyl, cyclopropyl, phenyl, 4-chlorphenyl, 3-pyridine radicals, CH ₂OCH ₃, O (CH ₂) ₂OCH ₃, S-Me, NH ₂, NHMe, NMe ₂, NHtBu, NHBu, NHiBu, N-morpholinyl, NH (CH ₂) ₂OH, NH (CH ₂) ₂OCH ₃, NH (CH ₂) ₃OCH ₃, NHCH (CH ₃) CH ₂OCH ₃, NCH ₃(CH ₂) ₂OCH ₃, NCH ₃(CH ₂) ₃OCH ₃, NHCH ₂Oxolane-2-base, N-1,3-oxazolidine-2-ketone,

R ⁷Be hydrogen, methyl, CF ₃, CF ₂H,

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge.

6. formula (I) compound and agrochemicals active salt thereof be as the purposes of bactericide, and one or more in each symbol of its Chinese style (I) have one of following implication:

R ⁵Be hydrogen, COCH ₃, COCF ₃, COOCH ₃

X is nitrogen or CR ⁸,

R ⁸Be hydrogen, O-Me,

Y is a nitrogen,

Z is CR ¹⁰,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, cyano group, CF ₃

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂-or CH ₂CH ₂Bridge,

R ⁶Be methyl, ethyl, isopropyl, cyclopropyl, phenyl, 3-pyridine radicals, CH ₂OCH ₃, O (CH ₂) ₂OCH ₃, S-Me, NH ₂, NHMe, NMe ₂, NHtBu, NHBu, NHiBu, N-morpholinyl, NH (CH ₂) ₂OH, NH (CH ₂) ₂OCH ₃, NH (CH ₂) ₃OCH ₃, NHCH (CH ₃) CH ₂OCH ₃, NCH ₃(CH ₂) ₂OCH ₃, NCH ₃(CH ₂) ₃OCH ₃, NHCH ₂Oxolane-2-base, N-1,3-oxazolidine-2-ketone,

R ⁷Be hydrogen, methyl, CF ₃, CF ₂H,

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge.

7. be used to prevent and treat the harmful microbe composition, it is characterized in that described composition except that filler and/or surfactant, also comprise at least a one or multinomial formula (I) compound according to claim 1 to 6.

8. according to the composition of claim 7, it is characterized in that described composition comprises at least a other agrochemically active compound.

9. control harmful microbe method, it is characterized in that with according to one of claim 1 to 6 or multinomial formula (I) compound administration in harmful microorganism and/or its habitat.

10. preparation is used to prevent and treat the harmful microbe method for compositions, it is characterized in that and will mix with filler and/or surfactant according to of claim 1 to 6 or multinomial formula (I) compound.

11. formula Ia compound and agrochemicals active salt thereof

Wherein each symbol is as giving a definition:

R ⁵Be hydrogen, the unsubstituted or C that replaces ₁-C ₈Alkyl, the unsubstituted or C that replaces ₁-C ₄Alkyl C (=O), C ₁-C ₄Alkyl OC (=O), the unsubstituted or C that replaces ₁-C ₄Alkoxyl (C ₁-C ₄) alkyl, the unsubstituted or C that replaces ₂-C ₆Thiazolinyl, the unsubstituted or C that replaces ₂-C ₆Alkynyl, C ₁-C ₆Alkyl sulphinyl, C ₁-C ₆Alkyl sulphonyl, C ₃-C ₈Cycloalkyl; The C that has 1 to 9 fluorine, chlorine and/or bromine atoms separately ₁-C ₆Haloalkyl, C ₁-C ₄Haloalkyl sulfinyl, C ₁-C ₄Halogenated alkyl sulfonyl, halo-C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl, C ₃-C ₈Halogenated cycloalkyl; Formoxyl, formoxyl-C ₁-C ₃Alkyl, (C ₁-C ₃Alkyl) carbonyl-C ₁-C ₃Alkyl, (C ₁-C ₃Alkoxyl)-carbonyl-C ₁-C ₃Alkyl; Halo-(the C that has 1 to 13 fluorine, chlorine and/or bromine atoms separately ₁-C ₃Alkyl) carbonyl-C ₁-C ₃-alkyl, halo-(C ₁-C ₃Alkoxyl) carbonyl-C ₁-C ₃Alkyl; (C ₁-C ₈Alkyl) carbonyl, (C ₁-C ₈Alkoxyl) carbonyl, (C ₁-C ₈Alkylthio group) carbonyl, (C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl) carbonyl, (C ₃-C ₆Alkene oxygen base) carbonyl, (C ₃-C ₆Alkynyloxy group) carbonyl, (C ₃-C ₈Cycloalkyl) carbonyl; (the C that has 1 to 9 fluorine, chlorine and/or bromine atoms separately ₁-C ₆Haloalkyl)-carbonyl, (C ₁-C ₆Halogenated alkylthio) carbonyl, (C ₁-C ₆Halogenated alkoxy) carbonyl, (C ₃-C ₆Haloalkene oxygen base) carbonyl, (C ₃-C ₆The halo alkynyloxy group) carbonyl, (halo-C ₁-C ₄Alkoxy-C ₁-C ₄Alkyl) carbonyl, (C ₃-C ₈Halogenated cycloalkyl) carbonyl, perhaps-CH ₂-C ≡ C-R ^1-A,-CH ₂-CH=CH-R ^1-A,-CH=C=CH-R ^1-A,-C (=O) C (=O) R ²,-CONR ³R ⁴,-CH ₂NR ⁵R ⁶, C ₁-C ₄Trialkylsilkl or C ₁-C ₄Dialkyl group one phenyl silicyl,

X is nitrogen or CR ⁸,

Y is nitrogen or CR ⁹,

Z is nitrogen or CR ¹⁰,

R ⁷Be hydrogen, halogen, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹, the unsubstituted or C that replaces ₁-C ₈Alkyl, the unsubstituted or C that replaces ₃-C ₆Cycloalkyl, C ₁-C ₄Trialkylsilkl, the unsubstituted or aryl that replaces or heteroaryl, COOR ¹¹, CON (R ¹¹) ₂, COR ¹¹

Perhaps

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

R ⁹Be hydrogen, halogen, N (R ¹¹) ₂, cyano group, hydroxyl, OR ¹¹, SR ¹¹, COR ¹¹, the unsubstituted or C that replaces ₁-C ₈Alkyl or C unsubstituted or that replace ₃-C ₈Cycloalkyl;

Perhaps

R ¹²Identical or different and be unsubstituted or the C that replaces ₁-C ₈Alkyl, C ₁-C ₈Haloalkyl, (CH ₂) _tOR ¹¹, C ₁-C ₄Trialkylsilkl; T=1-4 wherein

A is OR ¹⁵, SR ¹⁵, N (R ¹⁵) ₂Or C (R ¹⁶) ₃,

R ¹⁶Be hydrogen, halogen, cyano group, hydroxyl, OR independently of one another ¹¹, SR ¹¹, COR ¹¹, N (R ¹¹) ₂, the unsubstituted or C that replaces ₁-C ₈Alkyl, C ₁-C ₈Haloalkyl or C unsubstituted or that replace ₃-C ₈Cycloalkyl, (CH ₂) _uOR ¹¹U=1-4 wherein;

Perhaps

12. formula (Ia) compound and agrochemicals active salt thereof, one or more in each symbol of its Chinese style (Ia) have one of following implication:

X is nitrogen or CR ⁸,

Y is nitrogen or CR ⁹,

Z is nitrogen or CR ¹⁰,

Wherein or Y and Z be nitrogen,

Perhaps Y is that nitrogen and Z are CR ¹⁰,

Perhaps Y is CR ⁹And Z is a nitrogen,

R ⁷Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl group; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, phenyl, to the C1-phenyl, to the F-phenyl, to the Br-phenyl, to I-phenyl, p-methoxyphenyl, to Trifluoromethoxyphen-l, 2-pyridine radicals, 3-pyridine radicals, 4-pyridine radicals, 2-thienyl, 3-thienyl, SiMe ₃, COOR ¹¹, CON (R ¹¹) ₂, COR ¹¹

Perhaps

R wherein ¹³Independently of one another=hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, propyl group, 1-Methylethyl, CF ₂H, CF ₃, C ₂F ₅, OCH ₃OC ₂H ₅, OCF ₃, OC ₂F ₅Perhaps

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

Perhaps

A is OR ¹⁵, SR ¹⁵, N (R ¹⁵) ₂Or C (R ¹⁶) ₃,

Perhaps

13. formula (I is compound and agrochemicals active salt thereof a), and one or more in each symbol of its Chinese style (Ia) have one of following implication:

R ⁵Be hydrogen, acetyl group, trifluoroacetyl group,

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

R ⁷Be hydrogen, fluorine, chlorine, bromine, iodine, cyano group, hydroxyl, amino, N (R ¹¹) ₂, nitro, OR ¹¹, SR ¹¹Methyl, ethyl, propyl group, the 1-Methylethyl, butyl, the 1-methyl-propyl, the 2-methyl-propyl, 1, the 1-dimethyl ethyl, amyl group, the 1-methyl butyl, the 2-methyl butyl, the 3-methyl butyl, 2, the 2-dimethyl propyl, the 1-ethyl propyl, hexyl, 1, the 1-dimethyl propyl, 1, the 2-dimethyl propyl, the 1-methyl amyl, the 2-methyl amyl, the 3-methyl amyl, the 4-methyl amyl, 1, the 1-dimethylbutyl, 1, the 2-dimethylbutyl, 1, the 3-dimethylbutyl, 2, the 2-dimethylbutyl, 2, the 3-dimethylbutyl, 3, the 3-dimethylbutyl, the 1-ethyl-butyl, the 2-ethyl-butyl, 1,1,2-trimethyl propyl group, 1,2,2-trimethyl propyl group, 1-ethyl-1-methyl-propyl and 1-ethyl-2-methyl-propyl group; CF ₃, CF ₂H, CCl ₃, C ₂F ₅, C ₃F ₇, CF (CF ₃) ₂, cyclopropyl, cyclobutyl, cyclopenta, cyclohexyl, phenyl, to the Cl-phenyl, to the F-phenyl, to the Br-phenyl, to I-phenyl, p-methoxyphenyl, to Trifluoromethoxyphen-l, 2-pyridine radicals, 3-pyridine radicals, 4-pyridine radicals, 2-thienyl, 3-thienyl, SiMe ₃, COOR ¹¹, CO ₂Me, CO ₂Et, CO ₂Pr, CO ₂IPr, CO ₂Bu, CO ₂SecBu, CO ₂IsoBu, CO ₂TBu, CO ₂(CH ₂) ₂OH, CO ₂(CH ₂) ₂OCH ₃, CO ₂(CH ₂) ₃OH, CO ₂(CH ₂) ₃OCH ₃, CON (R ¹¹) ₂, CONHEt, CONEt ₂, CONHMe, CONMe ₂, CONHPr, CONPr ₂, CONHBu, CONHsecBu, CONHisoBu, CONHtBu, CONHCH (CH ₃) CH ₂OH, CONHCH (CH ₃) CH ₂OCH ₃, CONHCH (C ₂H ₅) CH ₂OH, CONHCH (C ₂H ₅) CH ₂OCH ₃, CONH (CH ₂) ₂OCH ₃, CONH (CH ₂) ₂OH, CONH (CH ₂) ₃OCH ₃, CONH (CH ₂) ₃OH, CONR ¹¹CH (CH ₃) CH ₂OH, COR ¹¹COMe, COEt, COPr, COiPr, COBu, COsecBu, COisoBu, COtBu, COCF ₃

Perhaps

Two geminal R ¹³Group is represented doubly linked oxygen or sulphur,

Perhaps

A is OR ¹⁵, N (R ¹⁵) ₂Or C (R ¹⁶) ₃,

Perhaps

14. formula (Ia) compound, one or more in each symbol of its Chinese style (Ia) have one of following implication:

R ⁵Be hydrogen, COCH ₃,

X is nitrogen or CR ⁸,

Y is a nitrogen,

Z is nitrogen or CR ¹⁰,

R ⁷Be hydrogen, methyl, 1-methyl-propyl, CF ₃, CF ₂H, cyclopropyl,

Perhaps

R wherein ¹³=hydrogen,

R ⁸Be hydrogen, fluorine, chlorine, cyano group, hydroxyl, nitro, OMe, CF ₃, COCH ₃, COOCH ₃, COOH, N (Me) ₂, NHCOCH ₃, NHCOCF ₃, NHSO ₂CH ₃, NHCOOCH ₃, NHCOO (CH ₂CH ₂) OCH ₃, 4-N-methyl piperazine-1-base, CH ₂NH ₂, CH ₂NHCOOCH ₃, CH ₂NHCOOtBu, methyl

R ¹⁰Be hydrogen

Perhaps

R wherein ¹³=hydrogen,

Perhaps

R ¹⁴Be hydrogen, methyl, cyclopropyl independently of one another,

A is OR ¹⁵Or C (R ¹⁶) ₃,

R ¹⁵Be ethyl,

R ¹⁶Be hydrogen,

15. formula (Ia) compound, one or more in each symbol of its Chinese style (Ia) have one of following implication:

R ⁵Be hydrogen, COCH ₃, COCF ₃, COOCH ₃,

X is nitrogen or CR ⁸,

R ⁸Be hydrogen, O-Me,

Y is a nitrogen,

Z is CR ¹⁰,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, cyano group, CF ₃

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

R ⁷Be hydrogen, methyl, CF ₃, CF ₂H,

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

Perhaps

R ¹⁴Be hydrogen, methyl, cyclopropyl independently of one another,

A is OR ¹⁵Or C (R ¹⁶) ₃,

R ¹⁵Be ethyl,

R ¹⁶Be hydrogen,

16. formula (Ia) compound, one or more in each symbol of its Chinese style (Ia) have one of following implication:

R ⁵Be hydrogen, COCH ₃, COCF ₃, COOCH ₃,

X is nitrogen or CR ⁸,

R ⁸Be hydrogen, O-Me,

Y is a nitrogen,

Z is CR ¹⁰,

R ¹⁰Be hydrogen, fluorine, chlorine, bromine, cyano group, CF ₃

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

R ⁶Be ethyl, isopropyl, CH ₂OCH ₃, cyclopropyl, 3-pyridine radicals,

R ⁷Be hydrogen, methyl, CF ₃, CF ₂H,

Perhaps

R ⁷And R ¹⁰Constitute CH together ₂Or CH ₂CH ₂Bridge,

Perhaps

R ¹⁴Be hydrogen, methyl, cyclopropyl independently of one another,

A is OR ¹⁵Or C (R ¹⁶) ₃,

R ¹⁵Be ethyl,

R ¹⁶Be hydrogen,

17. be used to prevent and treat the harmful microbe composition, it is characterized in that described composition except that filler and/or surfactant, also comprise at least a one or multinomial formula (Ia) compound according to claim 11 to 16.

18., it is characterized in that described composition comprises at least a other agrochemically active compound according to the composition of claim 17.

19. be used to prevent and treat the harmful microbe purposes according to of claim 11 to 16 or multinomial formula (Ia) compound.

20. control harmful microbe method, it is characterized in that with according to one of claim 11 to 16 or multinomial formula (Ia) compound administration in harmful microorganism and/or its habitat.

21. preparation is used to prevent and treat the harmful microbe method for compositions, it is characterized in that and will mix with filler and/or surfactant according to of claim 11 to 16 or multinomial formula (Ia) compound.

22. symbol R in the method for preparation formula (Id) compound, its Chinese style (Id) ¹, R ², R ³, R ⁴, R ⁵, R ⁶, R ⁷, R ¹⁰Have the implication of giving in claim 1 to 3 or 8 to 10 with X, it is characterized in that

A) use a kind of metal or metallorganic, halo thiazole to metallize to formula XIV in the presence of a kind of thinner,

B) if the existence that is suitably in a kind of reaction promoter down and in the presence of a kind of thinner, makes the metallic compound that obtains and the Chloropyrimide of formula XV react,

C) in the presence of a kind of oxidant, and if the existence that is suitably in a kind of reaction promoter down and in the presence of a kind of thinner, make the dihydro-pyrimidin reaction that obtains, to obtain the pyrimidine of formula XVI

With

D),, obtain formula Id compound if the existence that is suitably in a kind of metallic catalyst down and in the presence of a kind of thinner, reacts the pyrimidine of the formula XVI that obtains and the amine of formula XVII if be suitably under a kind of existence of reaction promoter

R wherein ⁶Also can be a wherein R ¹⁴With A group C (R as defined above ¹⁴) ₂A.

23. the intermediate of formula XVI

R wherein ⁶, R ⁷And R ¹⁰As above definition; R ⁶Also can be a wherein R ¹⁴With A group C (R as defined above ¹⁴) ₂A.