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    • 3. 发明申请
    • PROCESS FOR SYNTHESIZING 4-SUBSTITUTED AZETIDINONE DERIVATIVE
    • 合成4-取代的AZETIDINONE衍生物的方法
    • WO1994018163A1
    • 1994-08-18
    • PCT/JP1994000195
    • 1994-02-10
    • SUNTORY LIMITEDISHIGURO, MasajiNAKATSUKA, TakashiTANAKA, RieSHIMAMOTO, TetsuoYOSHIDA, Takuro
    • SUNTORY LIMITED
    • C07D205/08
    • C07D205/08
    • The invention relates to a process for synthesizing a 4-substituted azetidinone derivative represented by the general formula (3) (wherein OR1 represents a protected hydroxyl group; CO2R3 represents an esterified carboxyl group; and X and Y represent each independently alkyl, alkenyl, aralkyl, aryl, alkylthio, alkoxy, heterocycle, acyl, amino, hydrogen or halogen, or alternatively X and Y are combined together to represent cycloalkan-2-on-2-yl) by the reaction of an azetidinone derivative represented by general formula (1) (wherein OR1 is as defined above; and R2 represents alkyl, alkenyl or aryl) with an ester compound represented by general formula (2): (wherein CO2R3, X and Y are each as defined above) in the presence of zinc and copper compounds. The invention relates also to a compound represented by general formula (3) and further to a compound prepared by decarboxylating the compound (3), both being useful as an intermediate for synthesizing antibacterial carbapenem compounds.
    • 本发明涉及一种合成由通式(3)表示的4-取代氮杂环丁酮衍生物的方法(其中OR 1表示被保护的羟基; CO 2 R 3表示酯化羧基; X和Y各自表示烷基,烯基,芳烷基 ,芳基,烷硫基,烷氧基,杂环,酰基,氨基,氢或卤素,或者X和Y组合在一起代表环烷-2- -2-基),通过通式(1)表示的氮杂环丁酮衍生物 )(其中OR 1如上所定义; R 2表示烷基,烯基或芳基)与通式(2)表示的酯化合物:(其中CO 2 R 3,X和Y各自如上所定义)在锌和铜存在下 化合物。 本发明还涉及由通式(3)表示的化合物,还涉及通过使化合物(3)脱羧制备的化合物,两者都可用作合成抗菌碳青霉烯化合物的中间体。