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    • 9. 发明授权
    • Process for the preparation of an oxazolidinecarboxylic acid which is useful for preparing therapeutically active taxoids
    • 可用于制备治疗活性紫杉烷的恶唑烷羧酸的制备方法
    • US06444825B1
    • 2002-09-03
    • US08564345
    • 1995-12-14
    • Jean-Dominique BourzatAlain Commerçon
    • Jean-Dominique BourzatAlain Commerçon
    • C07D26302
    • C07D263/04C07D305/14
    • 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.
    • 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。