卡维地洛制备工艺改进研究

Improvent of synthesis process for carvedilol

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.