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    • 1. 发明申请
    • PROCESS FOR PREPARING PACLITAXEL
    • 制备PACLITAXEL的方法
    • WO1998008832A1
    • 1998-03-05
    • PCT/KR1997000157
    • 1997-08-25
    • HANMI PHARM. CO., LTD.KIM, Kyoung, SooCHAI, Ki, ByungMOON, Young, HoLEE, Kwang, OkKIM, Nam, DuHA, Tae, HeeSHIN, Jung, AeLEE, Gwan, SunKIM, Wan, Joo
    • HANMI PHARM. CO., LTD.
    • C07D305/14
    • C07D263/04C07D305/14C07D413/12Y02P20/55
    • 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.
    • 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。