Semi-synthesis of taxane derivatives using metal alkoxides and oxazinones
    82.
    发明公开
    Semi-synthesis of taxane derivatives using metal alkoxides and oxazinones 失效
    Teilsynthese von Taxanderivaten mittels Metallalkoxiden und Oxazinonen。

    公开(公告)号:EP0568203A1

    公开(公告)日:1993-11-03

    申请号:EP93302650.2

    申请日:1993-04-05

    发明人: Holton, Robert A.

    IPC分类号: C07D305/14 C07D265/04

    CPC分类号: C07D305/14 C07D265/06

    摘要: A process for preparing taxane derivatives such as taxol by providing a metal alkoxide having the bi, tri-, or tetracylic taxane nucleus, reacting the metal alkoxide with an oxazinone to form an intermediate, and converting the intermediate to the taxane derivative.

    摘要翻译: 通过提供具有双,三或四环紫杉烷核的金属醇盐,使金属醇盐与恶嗪酮反应形成中间体,并将中间体转化成紫杉烷衍生物,制备紫杉酚衍生物如紫杉醇的方法。

    Method for preparation of taxol using an oxazinone
    85.
    发明公开
    Method for preparation of taxol using an oxazinone 失效
    Methode zur Herstellung von Taxol unter Verwendung von Oxazinon。

    公开(公告)号:EP0428376A1

    公开(公告)日:1991-05-22

    申请号:EP90312366.9

    申请日:1990-11-13

    发明人: Holton, Robert A.

    IPC分类号: C07D265/04 C07D305/14

    摘要: Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula:
    wherein R₁ is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR₇ wherein R₇ is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R₂ and R₅ are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR₈ wherein R₈ is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R₃ and R₆ are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl and heteroaryl.

    摘要翻译: 制备紫杉醇中间体的方法,包括使醇与具有下式的嗪嗪酮接触:其中R 1为芳基,杂芳基,烷基,烯基,炔基或OR 7,其中R 7为烷基,烯基,炔基,芳基或杂芳基; R2和R5独立地选自氢,烷基烯基,炔基,芳基,杂芳基和OR8,其中R8是烷基,烯基,炔基,芳基,杂芳基或羟基保护基; 并且R 3和R 6独立地选自氢,烷基,烯基,炔基,芳基和杂芳基。