| 摘要 |
Benzofuran carboxamide and thioamide derivatives of formula (I) and their salts are new. Z = CO or CS; R1 = alkoxy optionally substituted by 1 or more halo, OH or thioalkyl; R2, R3 = H, R6, OR10, COR6, C(=NOR6)R6, alkyl-C(=NOR6)R6, alkyl-C(=NOH)R6, C(=NOH)R6, halo, NR8R9, CF3, CN, CO2H, CO2R10, CONH2, CONHR6 or CON(R6)2; R4 = H, arylalkyl, heteroaryl-alkyl, heterocyclo-alkyl, S(O)mR10 or alkyl optionally substituted by 1 or more hydroxy, alkoxy, CO2R7, SO2NR11R12, CONR11R12, CN, carbonyl oxygen, NR8R9, COR10 or S(O)nR10; R5 = aryl, heteroaryl, heterocyclyl, arylalkyl, heteroaryl-alkyl or heterocyclo-alkyl; in R4 and/or R5, aryl/heteroaryl/heterocyclyl are optionally substituted by 1 or more alkyl-R13 or R13; R6 = R10 optionally substituted by R14; R7 = H, alkyl, arylalkyl, heteroaryl-alkyl or heterocyclo-alkyl; R8 = H, aryl, heteroaryl, heterocyclyl, alkyl, cycloalkyl, arylalkyl, heteroaryl-alkyl, heterocyclo-alkyl, alkylcarbonyl, alkoxycarbonyl, arylsulphonyl, heteroaryl-sulphonyl, heterocyclo-sulphonyl, arylcarbonyl, heteroaryl-carbonyl, heterocyclo-carbonyl or alkylsulphonyl; R10 = alkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, arylalkyl, heteroaryl-alkyl or heterocyclo-alkyl; R9, R11, R12 = H or R10; R13 = alkyl optionally substituted by halo, alkoxy optionally substituted by halo, aryl, heteroaryl, heterocyclyl, OH, aryloxy, heteroaryloxy, heterocyclo-oxy, arylalkyloxy, heteroaryl-alkyloxy, heterocyclo-alkyloxy, CO2R7, CONR11R12, SO2NR11R12, halo, CN, NR8R9, COR10, S(O)nR10 or carbonyl oxygen; R14 = OH, carbonyl oxygen, OR10, NR8R9, CN, CO2H, CO2R10, CONR11R12 or COR10; m = 1 or 2; and n = 0-2. |
