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1. 发明授权

US06833461B2 Process for preparing simvastatin 失效
标题翻译：辛伐他汀的制备方法
公开(公告)号：US06833461B2
公开(公告)日：2004-12-21
申请号：US10468852
申请日：2003-08-25
申请人： Chung Il Hong , Jung Woo Kim , Hee Jong Shin , Tae Won Kang , Dong Ock Cho
发明人： Chung Il Hong , Jung Woo Kim , Hee Jong Shin , Tae Won Kang , Dong Ock Cho
IPC分类号： C07D30930
CPC分类号： C07D309/30 , Y02P20/55
摘要： The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following sequential processes comprising: (i) hydrolysis of lovastatin as starting material with potassium t-butoxide in an organic solvent and small amount of water under a mild reaction condition, followed by lactonization of the obtained solid intermediate with preventing from formation of by-products; (ii) protection of an alcohol group with t-butyldimethylsilyl group which can be easily removed with concentrated hydrochloric acid without the formation of by-products; (iii) acylation of the obtained protected intermediate with acyloxytriphenyl phosphonium salt as an acylating agent under a mild reaction condition; and (iv) removal of the silyl protective group with a concentrated hydrochloric acid. The present invention is to provide the improved process of preparing simvastatin expressed by formula 1 environmentally sound, economically efficient, and industrially useful.
摘要翻译：本发明涉及一种制备辛伐他汀的改进方法，更具体地说，涉及通过进行以下顺序方法制备具有高产率和高纯度的式1所表达的辛伐他汀的改进方法，包括：（i）将洛伐他汀作为原料与钾叔丁醇在有机溶剂和少量水中，在温和的反应条件下，然后将所得固体中间体内酯化，防止副产物的形成; （ii）用叔丁基二甲基甲硅烷基保护醇基，其可以用浓盐酸容易地除去而不形成副产物; （iii）在温和的反应条件下用酰氧基三苯基鏻盐作为酰化剂酰化所得保护的中间体; 和（iv）用浓盐酸除去甲硅烷基保护基。本发明提供了由式1表达的辛伐他汀的改进方法，其在环境无害，经济有效和工业上有用。

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