| 摘要 |
Dimethyl-(3-aryl-but-3-enyl)amine compounds of formula (I) and their salts, as enantiomers or racemates, are new. R1 = 1-5C alkyl; R2, R3 = H or 1-5C alkyl; or R1+R2 = (CH2)2, (CH2)3, (CH2)4, (CH2)2CHR7 or CH2-CHR7-CH2; R4, R6 = H, OH, 1-4C alkyl, 1-4C alkoxy, benzyloxy, CF3, OCF3, Cl, F or OR8; R5 = CHF2 or as for R4; provided that two of R4-R6 = H; or R4 = H and R5+R6 = CH=CH-C(OR10)=CH; or R4+R5 = CH=C(R9)-O and R6 = H; R7 = 1-8C alkyl, 3-8C cycloalkyl, 1-4C alkoxy, benzyloxy, CF3, Cl or F; R8 = phenyl, pyridyl, thienyl, thiazolyl (all optionally substituted), CO-T or PO(OR)2; T = 1-5C alkyl, 1-5C alkoxy, C6H4-R11, CHR12-NHR13 or NH-C6H3(R14)2; R = 1-4C alkyl; R9 = H or 1-4C alkyl; R10 = H or 1-3C alkyl; R11 = (1-3C alkyl)carbonyloxy in the o-position, or CH2N(R15)2 in the m- or p- position; R12, R13 = H, 1-6C alkyl or 3-8C cycloalkyl; or R12+R13 = (CH2)n; n = 3-8; R14 = independently H, OH, 1-7C alkyl , 1-7C alkoxy, phenyl, aryloxy, CF3, Cl or F; R15 = R; or N(R15)2 = morpholino; provided that the racemate (I; R1+R2 = (CH2)3; R3, R4, R6 = H; R5 = OMe) is excluded. |
