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公开(公告)号：US20200071259A1
公开(公告)日：2020-03-05
申请号：US16163623
申请日：2018-10-18
发明人： Weiming Xu , Pengfei Zhang , Dongxiang Feng , Lianzhi Tao
IPC分类号： C07C213/08
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%.
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公开(公告)号：US11161809B2
公开(公告)日：2021-11-02
申请号：US16854143
申请日：2020-04-21
发明人： Weiming Xu , Wanmei Li , Lianzhi Tao , Pengfei Zhang , Hongyun Shen , Dongxiang Feng
IPC分类号： C07C315/02 , C07C253/22 , C07C317/46 , C07C255/35
摘要： The disclosure provides processes for preparing 5-fluoro-2-methyl-1-(4-methylthiobenzylidene)-3-indanacetonitrile and for preparing sulindac, relating to the field of medicine. The former comprises mixing 6-fluoro-2-methyl-1-indanone, cyanoacetic acid, a first organic solvent and an acetic acid-based catalyst to proceed with a first condensation reaction to give a first condensation reaction solution, which contains 5-fluoro-2-methyl-3-indanacetonitrile; and mixing the first condensation reaction solution, per se, with a base, a second organic solvent and 4-(methylthio)benzaldehyde to proceed with a second condensation reaction to give 5-fluoro-2-methyl-1-(4-methylthiobenzylidene)-3-indanacetonitrile. The process is a one-pot process without separation of 5-fluoro-2-methyl-3-indanacetonitrile from the solvent, shortening the synthetic route, simplifying the preparation process and improving the 5-fluoro-2-methyl-1-(4-methylthiobenzylidene)-3-indanacetonitrile yield.
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