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    Process for the preparation of an oxazolidinecarboxylic acid which is useful for preparing therapeutically active taxoids
    7.
    发明授权
    Process for the preparation of an oxazolidinecarboxylic acid which is useful for preparing therapeutically active taxoids 失效
    可用于制备治疗活性紫杉烷的恶唑烷羧酸的制备方法

    公开(公告)号：US06444825B1

    公开(公告)日：2002-09-03

    申请号：US08564345

    申请日：1995-12-14

    申请人： Jean-Dominique Bourzat ,  Alain Commerçon

    发明人： Jean-Dominique Bourzat ,  Alain Commerçon

    IPC分类号： C07D26302

    CPC分类号： C07D263/04 ,  C07D305/14

    摘要： A method for preparing an oxazolidinecarboxylic acid of general formula (I), which is useful for preparing therapeutically active taxoids of general formula (III), from an oxazolidinecarboxylic acid of general formula (II). In formulae (I), (II) and (III), R is a hydrogen atom or an acetyl radical; R1 is a benzyl radical or a radical of the general formula R2—O—CO—, wherein R2 is an optionally substituted alkyl radical, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl; each of R3 and R4, which are the same or different, is hydrogen, alkyl, alkoxy, optionally substituted aryl or optionally substituted aralkyl, or together they form a 4-7 membered ring; R5 is alkenyl, alkynyl, phenyl, formyl, alkanoyl, aroyl, hydroxymethyl, carboxy or alkyloxycarbonyl; and R′ is a hydrogen atom or an alkali or alkaline-earth metal atom or an alkyl radical with 1-4 carbon atoms optionally substituted by phenyl radical.

    摘要翻译： 一种制备通式（I）的恶唑烷羧酸的方法，其可用于由通式（II）的恶唑烷羧酸制备通式（III）的治疗活性紫杉烷类。 在式（I），（II）和（III）中，R是氢原子或乙酰基; R 1是苄基或通式R 2 -O-CO-的基团，其中R 2是任选取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基; R 3和R 4各自相同或不同，为氢，烷基，烷氧基，任选取代的芳基或任选取代的芳烷基，或一起形成4-7元环; R5是烯基，炔基，苯基，甲酰基，烷酰基，芳酰基，羟甲基，羧基或烷氧基羰基; 并且R'是氢原子或碱金属或碱土金属原子或任选被苯基取代的具有1-4个碳原子的烷基。

    Methods of preparing new taxoids and pharmaceutical compositions containing them
    9.
    发明授权
    Methods of preparing new taxoids and pharmaceutical compositions containing them 失效
    制备新紫杉烷和含有它们的药物组合物的方法

    公开(公告)号：US06232477B1

    公开(公告)日：2001-05-15

    申请号：US09528448

    申请日：2000-03-17

    申请人： Hervé Bouchard ,  Jean-Dominique Bourzat ,  Alain Commerçon

    发明人： Hervé Bouchard ,  Jean-Dominique Bourzat ,  Alain Commerçon

    IPC分类号： C07D30514

    CPC分类号： C07D305/14

    摘要： Methods of preparing new taxoids of general formula (I) are presented: in which: R4 represents an alkanoyloxy radical in which the alkanoyl portion contains 2 to 6 carbon atoms in an unbranched or branched chain, this radical unsubstituted or substituted with one or more halogen atoms, an alkoxy radical containing 1 to 4 carbon atoms, or alternatively R4 represents a cycloalkanoyloxy radical in which the cycloalkanoyl portion contains 4 to 8 carbon atoms, or alternatively R4 represents a benzoyloxy radical; R5 represents an alkoxy radical containing 1 to 4 carbon atoms, substituted by an alkylthio radical containing 1 to 4 carbon atoms; and Z represents a hydrogen atom or a radical of general formula:

    摘要翻译： 提供了制备通式（I）的新紫杉烷的方法：其中：R4表示烷酰氧基，其中链烷酰基部分在无支链或支链上含有2-6个碳原子，该未取代的基团或被一个或多个卤素 原子，含有1至4个碳原子的烷氧基，或者R4表示环烷酰氧基，其中环烷酰基部分含有4至8个碳原子，或者R4表示苯甲酰氧基; R5表示含有1至4个碳原子的烷氧基 被含有1至4个碳原子的烷硫基取代; 和Z表示氢原子或通式如下的基团：