| 摘要 |
Hexahydro-chromeno-Ä3,4-cÜ-pyrrole derivatives of formula (I), their enantiomers, diastereoisomers and salts are new. m = 0-3; n = 0-3; n+m = 2 or 3; p = 1-6; the junction between rings B and C is trans; X = CN or -CONR4R5; R4, R5 = H, 1-6C alkyl, 3-7C cycloalkyl or optionally substituted aryl; A = sigma bond or -NR-CO-, -CO-NR-, -NR-SO2-, or -SO2-NR-; R = H or 1-6C alkyl; R1, R2 = H or 1-6C alkyl; R3 = H or phenyl, naphthyl or heteroaryl (all optionally substituted by one or more halo, 1-6C alkyl or alkoxy, OH, CN, NH2, NO2, COOH, 1-6C perhaloalkyl, sulphonyl, acylamino, 1-6C alkylsulphonyl, or 1-6C alkyl sulphonylamino), aryl or heteroaryl (both substituted by A'-Cy), 2-indolinon-5-yl, or, when A is a sigma bond, aryloxy or arylthio; A' = sigma bond or 1-6C alkylene or alkenylene, (in which one C atom may be replaced by O or S), -NR-CO-, -CO-NR-, -NR-SO2-, or -SO2-NR-; Cy = aryl or heteroaryl (optionally substituted); provided that when n = 0, then m is other than 2, when n = 1, R1, R2 = H, A = sigma bond and p = 1, then R3 is not phenyl nor pyridyl, when n = 1, R1 & R2 = H, A = sigma bond, R3 is not H, when n = 1, R1 & R2 = H, A = -NH-CO-, then R3 is other than H, phenyl, naphthyl, thienyl, furyl, pyrrolyl, pyridyl, (all optionally substituted by one or more halo, trihalomethyl, alkoxy or OH). |
