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盐酸左布诺洛尔的合成工艺改进

Improved Process on the Synthesis of Levobunolol Hydrochloride
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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％.
作者 陈登辉 饶志威 左文果 钟大猷 李宗桃
机构地区 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 南华大学药物药理研究所
出处 《合成化学》 CAS CSCD 北大核心 2013年第5期630-633,共4页 Chinese Journal of Synthetic Chemistry
关键词 盐酸左布诺洛尔 光学拆分 合成 废料利用 工艺改进 Levobunolol hydrochloride optical resolution synthesis waste solution utilization process improvement
分类号 R914.5 [医药卫生—药物化学] O625.4 [理学—有机化学]
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参考文献7

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二级参考文献8

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合成化学
2013年 第5期

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