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1. 发明申请

WO1998008832A1 PROCESS FOR PREPARING PACLITAXEL 审中-公开
标题翻译：制备PACLITAXEL的方法
公开(公告)号：WO1998008832A1
公开(公告)日：1998-03-05
申请号：PCT/KR1997000157
申请日：1997-08-25
申请人： HANMI PHARM. CO., LTD. , KIM, Kyoung, Soo , CHAI, Ki, Byung , MOON, Young, Ho , LEE, Kwang, Ok , KIM, Nam, Du , HA, Tae, Hee , SHIN, Jung, Ae , LEE, Gwan, Sun , KIM, Wan, Joo
发明人： HANMI PHARM. CO., LTD.
IPC分类号： C07D305/14
CPC分类号： C07D263/04 , C07D305/14 , C07D413/12 , Y02P20/55
摘要： The present invention relates to a process for preparing paclitaxel represented by formula (1) characterized in that: (a) an oxazolidine derivative represented by formula (2) or its salt in which X represents halogen, is coupled with a 7-trihaloacetyl-baccatin III represented by formula (3) in which R1 represents trihaloacetyl, in a solvent in the presence of a condensing agent to produce an oxazolidine substituent-containing taxane represented by formula (4) in which X and R1 are each as previously defined; (b) the oxazolidine ring is opened in a solvent in the presence of an acid, and the product thus obtained is reacted with benzoyl chloride in the presence of a base to produce a protected paclitaxel wherein the hydroxy group at 7-position is protected with trihaloacetyl group represented by formula (5) in which R1 is as previously defined; (c) then the protecting group at 7-position is removed by ammonia or a salt of ammonia with a weak acid in a solvent.
摘要翻译：本发明涉及一种制备由式（1）表示的紫杉醇的方法，其特征在于：（a）由式（2）表示的恶唑烷衍生物或其中X表示卤素的盐与7-三卤代乙酰基浆果赤霉素（3）表示的化合物，其中R 1表示三卤代乙酰基，在溶剂中，在缩合剂存在下制备由式（4）表示的含恶唑烷取代基的紫杉烷，其中X和R 1各自如上所定义; （b）在酸存在下，在溶剂中打开恶唑烷环，将得到的产物与苯甲酰氯在碱的存在下反应，得到保护的紫杉醇，其中7位的羟基被由式（5）表示的三卤代乙酰基，其中R 1如前所定义; （c）然后在溶剂中用氨或氨与弱酸将7位保护基除去。

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