盐酸非那嗪奈的合成

Synthesis of Fenazinel Dihydrochloride

盐酸非那嗪奈是我院发现的抗缺氧性脑卒中的新化合物,正在进行临床研究。本文报道了一条适宜放大合成的工艺路线,用1-甲酰哌嗪与苯甲酰甲基氯缩合,经碱水解得苯甲酰甲基哌嗪,再与N-氯乙酰苄胺经缩合、酸化、重结晶得盐酸非那嗪奈,总收率约42%(以1-甲酰哌嗪计)。

Fenazinel dihydrochloride is a new anti-stroke agent discovered by SIPI, and is in phase Ⅰ clinical trial. In this paper, a scalable synthesis of fenazinel dihydrochloride is described. 1-Formylpiperazine was reacted with phenacyl chloride, followed by hydrolysis to give phenacylpiperazine, which was subjected to condensation with N-chloroacetylbenzylamine to afford the target with an overall yield of about 42 % （based on 1-formylpiperazine）.