| 摘要 |
Benzodioxin and benzoxathiin derivatives of formula (I), their enantiomers, diastereoisomers, and salts with acids and bases are new: X, Y = S, O, CHq, CHSO or SO2, such that X, Y may not both be CHq; q = 0-2; Z = O or CH2; n = 0-4; A = -NR1R2 or a group -C(=T')NR6R7; R1 = H or 1-6C alkyl; R2 = -C(=T)R3; T = O or S; R3 = R'3 or -NR4R5; R'3 = H, 1-6C alkyl, 2-6C alkenyl, 1-6C alkynyl (sic), 3-8C cycloalkyl, cycloalkyl alkyl (all optionally substituted), or aryl or aralkyl; R4 = H or 1-6C alkyl; R5 = H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, cycloalkyl, cycloalkyl alkyl (all optionally substituted) or aryl or arylalkyl; T' = O or S; R6 = H or 1-6C alkyl; R7 = H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, cycloalkyl or cycloalkyl alkyl (all optionally substituted) or aryl or arylalkyl; R = H, 1-6C alkyl (optionally substituted), aryl or aralkyl; Ring A = optionally substituted by one or more halo, OH, 1-6C alkyl or alkoxy, CN, NO2, NH2 or trihaloalkyl; arylalkyl = 1-6C alkyl substituted by aryl; cycloalkyl alkyl = 1-6C alkyl substituted by 3-8C cycloalkyl; provided that when X, Z both = CH2, R = H, and A = NR1R2, then Y is not O; and when Z = O, n is not zero, and when Z = O and n = 1, then A is not CONEt2; when Z = CH2, n = 1, A = -NR1CSNR4R5, then R2 is not aryl; and when X = Y = O, the dotted lines in ring A are single bonds, R = H or CH2OH, then A is not NR1R2a; R2a = benzoyl (optionally substituted). |
