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目的采用新的方法合成桂利嗪的顺式杂质(Z)-1-二苯甲基-4-(3-苯基-2-丙烯基)哌嗪。方法以3-苯基-2-丙炔-1-醇为原料,经过H_2/林德拉催化剂还原、甲磺酰氯氯代,最后与二苯甲基哌嗪发生缩合反应得到目标化合物。结果与结论目标化合物的结构经ESI-MS和~1H-NMR谱确证,3步总收率为41.6%。该合成路线收率较高,操作简便。
OBJECTIVE To synthesize the cis-impurity (Z) -1-benzhydryl-4- (3-phenyl-2-propenyl) piperazine of cinnarizine by a novel method. Methods 3-Phenyl-2-propyn-1-ol was used as a starting material and was reduced by H 2 / Lindlar catalyst and chlorinated with methanesulfonyl chloride. Finally, the target compound was obtained by condensation reaction with benzhydrylpiperazine. Results and Conclusion The structures of target compounds were confirmed by ESI-MS and ~ 1H-NMR spectra. The total yield of 3 steps was 41.6%. The synthetic route yield higher, easy to operate.