盐酸左布诺洛尔的合成工艺改进  

Improved Process on the Synthesis of Levobunolol Hydrochloride

作　　者：陈登辉[1] 饶志威[2] 左文果[1] 钟大猷[1] 李宗桃[1] 

机构地区：[1]武汉大学药学院组合生物合成与新药发现教育部重点实验室,湖北武汉430071 [2]南华大学药物药理研究所,湖南衡阳422101

出　　处：《合成化学》2013年第5期630-633,共4页Chinese Journal of Synthetic Chemistry

摘　　要：以回收的盐酸左布诺洛尔废料为原料,经NaOH碱化,HBr水解得5-羟基-α-萘满酮(2);2经醚化、氨化、用右旋酒石酸拆分得到盐酸左布诺洛尔,其结构经1H NMR和IR确证。2的回收率90%,总收率80.6%。5-Hydroxy-1-tetralone（2） was recovered by alkalization with NaOH and hydrolysis with 48％ HBr solution on bunolol waste.Levobunolol hydrochloride was synthesized by etherification with epichlorohydrin,ammoification with tert-butylamine and resolution using d-tartrate from 2.The structures were confirmed by 1H NMR and IR.Recovery rate of 2 was 90％ and the total yield was 80.6％.

关 键 词：盐酸左布诺洛尔 光学拆分 合成 废料利用 工艺改进 

分 类 号：R914.5[医药卫生—药物化学] O625.4[医药卫生—药学]