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Method for preparing levobunolol hydrochloride

机译:盐酸左布洛诺的制备方法

摘要

The present invention provides a method for preparing levobunolol hydrochloride. In the present invention S-1-tert-butyl-epoxy methylamine is subjected to a substitution reaction with 5-hydroxy-1-tetralone, and acidified to obtain the target product levobunolol hydrochloride. The method provided by the present invention greatly improves the regioselectivity of the reaction, avoids the occurrence of side reactions, and effectively improves the yield and optical purity of levobunolol hydrochloride, with the yield being 87.3%, and the ee value being over 99%.
机译:本发明提供了一种制备盐酸左布洛诺的方法。在本发明中,使S-1-叔丁基-环氧甲胺与5-羟基-1-四氢萘酮进行取代反应,然后酸化,得到目标产物盐酸左文诺尔。本发明提供的方法大大提高了反应的区域选择性,避免了副反应的发生,并有效提高了盐酸左布诺洛尔盐酸盐的收率和光学纯度,收率为87.3%,ee值为99%以上。

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