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    Paclitaxel trihydrates and methods of making thereof
    7.
    发明授权
    Paclitaxel trihydrates and methods of making thereof 有权
    紫杉醇三水合物及其制备方法

    公开(公告)号：US08633240B2

    公开(公告)日：2014-01-21

    申请号：US13486229

    申请日：2012-06-01

    申请人： James K. Harper ,  David M. Grant

    发明人： James K. Harper ,  David M. Grant

    IPC分类号： C07D305/00 ,  A61K31/335

    CPC分类号： C07D305/14

    摘要： Novel paclitaxel trihydrates. The paclitaxel trihydrates described herein are obtained by recrystallizing paclitaxel from a water/alcohol solution. Such recrystallization is known in the art to yield the one previously known paclitaxel crystalline trihydrate polymorph. Formation of the novel paclitaxel trihydrates described herein is induced by subjecting paclitaxel trihydrate crystals to an elevated pressure. As evidenced by NMR spectra, the novel paclitaxel trihydrates described herein have three-dimensional structures and/or water coordination geometry structures that are distinct from any previously known paclitaxel trihydrate.

    摘要翻译： 新型紫杉醇三水合物。 本文所述的紫杉醇三水合物通过从水/醇溶液中重结晶紫杉醇获得。 这种重结晶在本领域中是已知的，以产生一种先前已知的紫杉醇结晶三水合物多晶型物。 本文所述的新型紫杉醇三水合物的形成是通过使紫杉醇三水合物晶体升高的压力而诱导的。 如通过NMR光谱所证明的，本文所述的新型紫杉醇三水合物具有与任何先前已知的紫杉醇三水合物不同的三维结构和/或水配位几何结构。

    Preparation of taxanes from 9-dihydro-13-acetylbaccatin III
    9.
    发明授权
    Preparation of taxanes from 9-dihydro-13-acetylbaccatin III 有权
    9-二氢-13-乙酰浆果赤霉素III的紫杉烷类的制备

    公开(公告)号：US08263793B2

    公开(公告)日：2012-09-11

    申请号：US11909973

    申请日：2006-03-30

    申请人： Gaetan Caron ,  Mettilda Lourdusamy

    发明人： Gaetan Caron ,  Mettilda Lourdusamy

    IPC分类号： A01N43/02 ,  A61K31/335 ,  C07D305/00 ,  C07D407/00 ,  C07D493/00 ,  C07C69/74

    CPC分类号： C07D305/14 ,  Y02P20/55

    摘要： The present invention relates to a new process for the preparation of 9-dihydrobaccatin III intermediates as useful precursors for the preparation of paclitaxel, 1, docetaxel, 2, and analogues thereof. More particularly, the process comprises the steps of (i) concomitantly deacetylating esters at the 10-position and 13-position of 9-dihydro-13-acetylbaccatin III to form 9-dihydro-10-deacetylbaccatin III; (ii) protecting a hydroxy group at the 7-position of 9-dihydro-10-deacetylbaccatin III; and (iii) acylating a hydroxy group at the 10-position to form a compound of formula II.

    摘要翻译： 本发明涉及作为制备紫杉醇，1，多西他赛，2及其类似物的有用前体的9-二氢浆果赤霉素III中间体的制备新方法。 更具体地说，该方法包括以下步骤：（i）在9-二氢-13-乙酰浆果赤霉素III的10位和13位上伴随脱乙酰化以形成9-二氢-10-脱乙酰基浆果赤霉素III; （ii）保护9-二氢-10-脱乙酰基浆果赤霉素Ⅲ的7-位的羟基; 和（iii）在10位上酰化羟基以形成式II化合物。