卡维地洛制备工艺改进研究  

Improvent of synthesis process for carvedilol

作　　者：方惠珍 宋旭莹 

机构地区：[1]浙江金华康恩贝生物制药有限公司新药研发部,浙江金华321016

出　　处：《中国医药导报》2011年第18期76-77,共2页China Medical Herald

摘　　要：目的:研究卡维地洛的合成并进行工艺改进。方法:以4-羟基咔唑为起始原料,经过缩合、氢解脱除苄基得到目标产物,反应过程采用薄层层析进行监控。结果:该反应总收率为48.3%。目标产物经红外光谱、核磁共振及元素分析确证了其化学结构。结论:改进后的工艺,反应条件温和,质量和收率有较大的提高,环境污染小,适合工业化生产。Objective： To study and improve the synthesis of carvedilol.Methods： Carvediol was high effectively synthesized from 4-hydroxy carbazole by condensation with epichlorohydrin,N-[2-（2-methoxy-phenoxy）ethyl]benzylamine;debenzylated by catalytic hydrogenation.Results： The overall yield was 48.3%.The chemical structures of target product were characterized by IR,NMR and element analysis.Conclusion： This synthetic route is simple and suitable for industrialized production with lower cost,lower pollution and higher yield.

关 键 词：4-羟基咔唑 卡维地洛 缩合反应 脱苄基反应 

分 类 号：R914.5[医药卫生—药物化学]