| 摘要 |
Benzofuryl and benzothienyl alkyl amides (I), their enantiomers, diastereoisomers, and salts with acids and bases are new. The benzofuryl and benzothienyl derivatives (I) are new: a = saturated or unsaturated bond; W' = O or S; B' = 1-6C alkylene (optionally substituted by one or more 1-6C alkyl, 1-6C alkoxy, OH, carboxy, and/or 1-6C alkoxy carbonyl); R = H, OH, R', or OR'; R' = 1-6C alkyl or trihaloalkyl sulfonyl, 2-6C alkenyl or alkynyl, 3-7C cycloalkyl, aryl, biphenyl, or heteroaryl (all optionally substituted); either G1 = halogen, 1-6C trihaloalkyl sulfonyloxy, COOH, CHO, CN, R1, -CO-R1, or -O-CO-R1; R1 = 1-6C alkyl, 2-6C alkenyl or alkynyl, 3-7C cycloalkyl, aryl, biphenyl or heteroaryl (all optionally substituted); when G11 = H or; G11+R = 5-7C saturated or unsaturated oxygen-containing ring (optionally substituted by 1-6C alkyl, 1-6C alkoxy, OH, oxo, COOH, or 1-6C alkoxycarbonyl) or G1 = H; when G11 = 1-6C trihaloalkyl sulfonyloxy, COOH, CHO, CN, R1, -CO-R1, or -O-CO-R1; G2 = (i), (ii), or (iii); X = O or S; R2 = H or 1-6C alkyl; R20 - R22 = 1-6C alkyl, 2-6C alkenyl or alkynyl, 3-7C cycloalkyl, aryl, biphenyl, or heteroaryl (all optionally substituted) provided that: when G2 = (iii) in which R22 is not aryl, heteroaryl or biphenyl, then G1 or G11 is heteroaryl other than pyridyl, 1-6C alkyl, 1-6C alkylheteroaryl (other than pyridyl), COR1, or O-CO-R1; when G2 = (i) or (ii) in which R20 and R21 are not aryl, biphenyl or heteroaryl, and G1 is other than heteroaryl or naphthyl, and R is H, then B' is a methylene or ethylene chain (optionally substituted); when G2 = (i) or (ii) in which R20 and R21 are not aryl, or heteroaryl, and when R and G1 are both H, then G11 is other than 1-6C alkyl, 3-7C cycloalkyl (optionally substituted by halogen, OH) or 1-6C alkyl (optionally substituted by halogen, OH or 1-6C alkoxy or 3-7C cycloalkyl (optionally substituted by halogen or OH)); when G2 = (i) or (ii) in which R20 and R21 are not aryl, or heteroaryl, and G1 is H and R is OR', R' being other than heteroaryl, then G11 is other than 1-6C alkyl, 2-6C alkenyl, or 2-6C alkynyl; when G2 = either (ii) with R21 being other than 2-6C alkenyl or alkynyl or (i) with R20 being cycloalkyl (optionally substituted by halogens), OH, 1-6C alkoxy, or 1-6C alkyl (optionally substituted by 3-7C cycloalkyl (optionally substituted by halogens, OH or 1-6C alkoxy), then G11 is other than 1-6C alkyl, and G1 is other than halogen, 1-6C alkyl, 1-6C alkylphenyl, or phenyl; and when G2 = (ii), X is S and B' is ethylene, then R21 is other than aryl; aryl = phenyl or naphthyl; heteroaryl = mono or bicyclic (optionally substituted). An Independent claim is also included for the preparation of (I). |
