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1. 发明授权

US08658811B2 Process for the preparation of docetaxel, its intermediates, and methods for preparation thereof 有权
标题翻译：多西他赛制剂的制备方法，其中间体及其制备方法
公开(公告)号：US08658811B2
公开(公告)日：2014-02-25
申请号：US12741714
申请日：2009-05-22
申请人： Xin Shen , Huaxing Zhan , Jidong Yang , Xiao He , Fuxing Lin , Shaohong Wu
发明人： Xin Shen , Huaxing Zhan , Jidong Yang , Xiao He , Fuxing Lin , Shaohong Wu
IPC分类号： C07D407/00 , C07D493/00
CPC分类号： C07D305/14 , C07C269/04 , C07C269/06 , C07C271/22 , Y02P20/55
摘要： Described is a process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained from step a to prepare compound 5; c) removing one tert-butoxycarbonyl of compound 5 obtained from step b to prepare compound 6; d) removing one acetyl of compound 6 obtained from step c to prepare compound 1; wherein, R1 represents tert-butyl dimethyl silyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl or methoxymethyl, Boc is tert-butoxycarbonyl, Ac is acetyl, and Ph is phenyl. Also disclosed are intermediates of docetaxel and methods for preparation thereof.
摘要翻译：描述了制备多西紫杉醇1的方法，包括以下步骤：a）化合物2和3的羟基酰化反应得到化合物4; b）由步骤a获得的化合物4的羟基的脱保护基团R1，以制备化合物5; c）除去由步骤b获得的化合物5的一个叔丁氧基羰基，制备化合物6; d）除去由步骤c获得的化合物6的一个乙酰基，制备化合物1; 其中，R1表示叔丁基二甲基甲硅烷基，三乙基甲硅烷基，乙氧基乙基，四氢吡喃基，三氯乙氧基羰基或甲氧基甲基，Boc是叔丁氧基羰基，Ac是乙酰基，Ph是苯基。还公开了多西他赛的中间体及其制备方法。

2. 发明申请

US20100311991A1 PROCESS FOR THE PREPARATION OF DOCETAXEL, ITS INTERMEDIATES, AND METHODS FOR PREPARATION THEREOF 有权
标题翻译：制备DOCETAXEL及其中间体的方法及其制备方法
公开(公告)号：US20100311991A1
公开(公告)日：2010-12-09
申请号：US12741714
申请日：2009-05-22
申请人： Xin Shen , Huaxing Zhan , Jidong Yang , Xiao He , Fuxing Lin , Shaohong Wu
发明人： Xin Shen , Huaxing Zhan , Jidong Yang , Xiao He , Fuxing Lin , Shaohong Wu
IPC分类号： C07D305/14 , C07C271/66 , C07C269/06
CPC分类号： C07D305/14 , C07C269/04 , C07C269/06 , C07C271/22 , Y02P20/55
摘要： The present invention disclosed an process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained from step a to prepare compound 5; c) removing one tert-butoxycarbonyl of compound 5 obtained from step b to prepare compound 6; d) removing one acetyl of compound 6 obtained from step c to prepare compound 1; wherein, R1 represents tert-butyl dimethyl silyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl or methoxymethyl, Boc is tert-butoxycarbonyl, Ac is acetyl, and Ph is phenyl. The present invention also disclosed intermediates of docetaxel and methods for preparation thereof. In the methods for preparation of the present invention, the protective groups used are easy to be removed, the purification of the intermediates is easy, the cost is lower, the yield and the purity are higher, and the processes can be scaled to commercial implementation.
摘要翻译：本发明公开了一种制备多西紫杉醇1的方法，包括以下步骤：a）化合物2和3的羟基酰化反应得到化合物4; b）由步骤a获得的化合物4的羟基的脱保护基团R1，以制备化合物5; c）除去由步骤b获得的化合物5的一个叔丁氧基羰基，制备化合物6; d）除去由步骤c获得的化合物6的一个乙酰基，制备化合物1; 其中，R1表示叔丁基二甲基甲硅烷基，三乙基甲硅烷基，乙氧基乙基，四氢吡喃基，三氯乙氧基羰基或甲氧基甲基，Boc是叔丁氧基羰基，Ac是乙酰基，Ph是苯基。本发明还公开了多西紫杉醇的中间体及其制备方法。在本发明的制备方法中，所使用的保护基团易于除去，中间体的纯化容易，成本低，产率和纯度高，并且可以将其扩展到商业实施。

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