Design And Synthesis Of Phthalides Piperazine Compounds

In this thesis, the design and synthesis of novel compouds with phthalide piperazidine as their framework, were studied.The etiological factors of cerebral apoplexy and development of its curative were introduced briefly. The novel multitarget stroke drug butyl phthalide and N-methyl-D-aspartic acid (NMDA) receptor antagonists were described in detail in the paper. Based on the structure-activty relationship(SAR) of NMDA receptor antagonists, with butyl phthalide as the leading compoud, aryl acetyl piperazidine and phenylcarbamoyl peperazidine groups were introduced at the 3 position. And twenty-one new compouds which had not been reported in the literatures were designded. Starting from phthalic anhydride and malonic acid, target compounds were synthesized through a eight-step procedure as addition, methylation, bromination, piperizine substitution, reduction, hydrolization, cyclization, substitution. The structures of the target compounds were confirmed by MS and ~1H-NMR.The pharmacological evaluation of these target compounds is in proces.