匹维溴铵的合成

Synthesis of pinaverium bromide

目的研究肠易激综合征治疗药物匹维溴铵的合成工艺。方法以诺卜醇为起始原料,与4-(2-氯乙基)吗啉缩合,氢化后再与2-溴-4,5-二甲氧基溴苄反应制得目标化合物。结果以诺卜醇计三步反应总收率83.3%,目标化合物的结构经元素分析、红外、核磁共振氢谱、核磁共振碳谱、DEPT-135、HMQC和HMBC、质谱确证。结论该方法条件温和、操作简单、收率高,适合工业化生产。

Objective To investigate the synthetic process for irritable bowel syndrome（IBS） treating agent pinaverium bromide（I）. Methods Pinaverium bromide was prepared by three steps from nopol via condensation, hydrogenation and condensation. Results Pinaverium bromide was synthesized in overall yield of 83.3% and its structure was confirmed by elementary analysis, IR, ^1H-NMR, ^13C-NMR, DEPT-135, HMQC, HMBC and ESI-MS. Conclusions The synthetic process has advantages of high yield, lower cost, mild reaction conditions and simple work-up. It is suitable for industrial production.