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    • 1. 发明公开
    • 세팔로스포린 유도체의 신규한 제조 방법
    • 制造CEPHOROSPORIN衍生物的新工艺
    • KR1020010049719A
    • 2001-06-15
    • KR1020000038364
    • 2000-07-05
    • 에프. 호프만-라 로슈 아게
    • 스푸르파울트릭케스게오르크
    • C07D501/48
    • C07D501/00Y02P20/55
    • PURPOSE: Provided is a novel process for the manufacture of cephalosporin derivatives to offer easier access to pharmacologically useful cephalosporins. CONSTITUTION: Cephalosporin derivatives are represented by the formula(I), wherein R1 is an amino protecting group, R2 is a carboxy protecting group and R is hydrogen, lower alkyl, lower alkoxy, cycloalkyl, cycloalkenyl, cycloalkyl-lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; the lower alkyl, cycloalkyl, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl and the heterocyclyl moieties being unsubstituted or substituted with at least one group selected from carboxy, amino, aminoethyl, carbamoyl, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen and trifluoromethyl. The manufacturing method comprises the steps of: converting a phosphonium salt of the formula(II) into the corresponding ylide of the formula(III); reacting it with aldehyde of the formula(IV).
    • 目的:提供一种用于制造头孢菌素衍生物以提供更容易获得药理学上有用的头孢菌素的新方法。 构成:头孢菌素衍生物由式(I)表示,其中R1是氨基保护基,R2是羧基保护基,R是氢,低级烷基,低级烷氧基,环烷基,环烯基,环烷基 - 低级烷基,低级烯基, 低级炔基,芳基,芳基 - 低级烷基,杂环基或杂环基 - 低级烷基; 低级烷基,环烷基,低级烯基,环烯基,低级炔基,芳基 - 低级烷基,芳基和杂环基部分是未取代的或被至少一个选自羧基,氨基,氨基乙基,氨基甲酰基,硝基,氰基,低级烷基, 低级烷氧基,羟基,卤素和三氟甲基。 制造方法包括以下步骤:将式(II)的鏻盐转化成式(III)的相应的叶立德; 使其与式(IV)的醛反应。