主权项 |
1. A thiazole compound of general formula I, wherein,R1 is one of R1a, R1b, or R1c: In which, R4a and R5a are in each occurrence independently one of: C1-C6 alkyl, tert-butoxycarbonylamino, hydrogen, halogen, hydroxyl, nitro, C3-C6 cycloalkyl, C1-C6 alkoxyl; where the C1-C6 alkoxyl can be substituted with C6-C10 aryl, amino, C1-C6 alkylamino; where the C1-C6 alkylamino can be substituted with C6-C10 aryl, or C1-C6 alkyl; where the C1-C6 alkyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkenyl; where the C2-C6 alkenyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkynyl; where the C2-C6 alkynyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or 5 to 7-membered aromatic heterocycle containing 1-3 heteroatoms selected from N, O and S; R4b and R5b are in each occurrence independently one of: hydrogen, halogen, hydroxyl, nitro, C3-C6 cycloalkyl, C1-C6 alkoxyl; where the C1-C6 alkoxyl can be substituted with C6-C10 aryl, amino, C1-C6 alkylamino; where the C1-C6 alkylamino can be substituted with C6-C10 aryl, or C1-C6 alkyl; where the C1-C6 alkyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkenyl; where the C2-C6 alkenyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkynyl; where the C2-C6 alkynyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or 5 to 7-membered aromatic heterocycle containing 1-3 heteroatoms selected from N, O and S; or, R4b and R5b together with a carbon atom to which R4b and R5b are both attached form a 3 to 10-membered cyclic hydrocarbon, or a 3 to 10-membered heterocycle containing 1 to 3 heteroatoms selected from N, O and S; R4c, R5c and R6 are in each occurrence independently one of: hydrogen, halogen, hydroxyl, nitro, C3-C6 cycloalkyl, C1-C6 alkoxyl; where the C1-C6 alkoxyl can be substituted with C6-C10 aryl, amino, or C1-C6 alkylamino; where the C1-C6 alkylamino can be substituted with C6-C10 aryl, or C1-C6 alkyl; where the C1-C6 alkyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkenyl; where the C2-C6 alkenyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or C2-C6 alkynyl; where the C2-C6 alkynyl can be substituted with hydroxyl, C1-C4 alkoxyl, fluoro, C6-C10 aryl, or 5 to 7-membered aromatic heterocycle containing 1-3 heteroatoms selected from N, O and S; R2 is hydrogen, halogen, hydroxyl, C1-C6 alkoxyl, C1-C8 alkoxyl which can be substituted with C6-C10 aryl, amino, or C1-C6 alkylamino, where the C1-C6 alkylamino can be substituted with C6-C10 aryl, C1-C6 alkyl, or C3-C6 cycloalkyl; where the C3-C6 cycloalkyl can be substituted with C1-C6 alkyl; where the C1-C6 alkyl can be substituted by one or more substituent groups independently selected from hydroxyl, C1-C4 alkoxyl, halogen, benzyloxyl, C6-C10 aryl, or C2-C6 alkenyl; where the C2-C6 alkenyl group can be substituted by one or more substituent groups independently selected from hydroxyl, C1-C4 alkoxyl, halogen, C6-C10 aryl, or C2-C6 alkynyl; where the C2-C6 alkynyl that can be substituted by one or more substituent groups independently selected from hydroxyl, C1-C4 alkoxyl, halogen, C6-C10 aryl, C6-C10 aryl; where the C6-C10 aryl can be substituted by halogen or nitro, or 5-7 membered aromatic heterocycle containing 1 to 3 heteroatoms selected from N, O and S; n is 0, 1 or 2; X is —N(R7)— orwherein R7 is hydrogen or C1-C6 alkyl;
conditional component Y is one of: —(C1-C10 alkyl)-, —(C2-C9 alkenyl)-, —(C6-C10 aryl)-, —(C1-C6 alkyl)-(C6-C10 aryl)-, —(C6-C10 aryl)-(C2-C6 alkenyl)-, —(C3-C6 cycloalkyl)-, —(C1-C5 alkyl)-C(O)—NH—(C1-C5 alkyl)-, —(C1-C5 alkyl)-C(O)—O—(C1-C5 alkyl)- or —(C1-C5 alkyl)-C(O)—O—(C2-C9 alkenyl)-; R3 is one of R3a, R3c, R3d, or R3e: R8 is hydrogen or C1-C6 alkylcarbonyl; and R9 is hydrogen or C1-C10 alkylcarbonyl. |