PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF

摘要

The present invention relates to novel compound having strong antitumor activities of general formula (I), wherein R1 and R2 are independently hydrogen, substituted or unsubstituted C1-C8 alkyl, substituted or unsubstituted C3-C6 cycloalkyl, substituted or unsubstituted C2-C8 unsaturated alkyl, ketone, substituted or unsubstituted aryl, substituted or unsubstituted C1-C4 alkoxy, substituted or unsubstituted arylhydroxy, substituted or unsubstituted amino, C1-C4 lower ester, C1-C4 lower thioester, thiol, substituted or unsubstituted carboxyl, epoxy, substituted or unsubstituted C1C4 lower thioalkoxy; or R1 and R2 are fused to form C3-C4 saturated or unsaturated chain; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, C1-C4 lower ester, C1-C4 lower alkyl, C1-C4 lower thioalkyl, substituted or unsubstituted C3-C6 cycloalkyl, C1-C4 lower alkoxy, C1-C4 lower thioalkoxy, substituted or unsubstituted aryl, substituted or unsubstituted lower arylalkoxy, substituted or unsubstituted lower alkylamino, or lower alkyl substituted or unsubstituted carbamate; or among R3, R4, R5, R6 and R7, two adjacent groups are bonded with each other to form 1,2-phenylene or 2,3naphthylene; X is oxygen, sulfur, or substituted or unsubstituted imino; Y is bonded at the 3-position or 4-position of the aromatic ring part wherein Y is oxygen or -NR8- (wherein, R8 is the same with the above-mentioned R3); Z is hydroxy, C1-C4 lower alkoxy, C1-C4 lower thioalkoxy, substituted or unsubstituted aryloxy, C1-C4 lower alkylamino, substituted or unsubstituted cycloamino containing 1-5 nitrogen atoms; A is nitrogen or -CH=; its pharmaceutically acceptable acid addition salts and process for the preparation thereof.