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以四氢吡咯为原料,与氯乙酰氯反应生成N-(2-氯乙酰基)四氢吡咯;以(E)-3,4,5-三甲氧基肉桂酸为原料,与1,1-羰基二咪唑反应生成活性酯后再与N-叔丁氧羰基哌嗪反应,生成物经过脱保护得到关键中间体1-(3,4,5-三甲氧基肉桂酰基)哌嗪盐酸盐;再经烃化反应制备桂哌奇特游离碱,与马来酸成盐得到目标化合物。产品结构经1H NMR确认,总收率为46%。该合成工艺简便、合理、可行,适合工业化生产。
Using tetrahydropyrrole as starting material and reacting with chloroacetyl chloride to produce N- (2-chloroacetyl) tetrahydropyrrole; (E) -3,4,5-trimethoxycinnamic acid as raw material and 1,1- Carbonyldiimidazole reaction of active ester and then N-tert-butoxycarbonylpiperazine reaction, the product was deprotected to obtain the key intermediate 1- (3,4,5-trimethoxy cinnamoyl) piperazine hydrochloride; Then by the alkylation reaction to prepare cinepazide free base, with maleic acid salt to obtain the target compound. The product structure was confirmed by 1H NMR with a total yield of 46%. The synthesis process is simple, reasonable and feasible, suitable for industrial production.