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    • 4. 发明授权
    • Process for synthesizing 4-substituted azetidinone derivatives
    • 合成4-取代的氮杂环丁酮衍生物的方法
    • US06867297B1
    • 2005-03-15
    • US09178594
    • 1998-10-26
    • Masaji IshiguroTakashi NakatsukaRie TanakaTetsuo ShimamotoTakuro Yoshida
    • Masaji IshiguroTakashi NakatsukaRie TanakaTetsuo ShimamotoTakuro Yoshida
    • C07D205/08
    • C07D205/08
    • An azetidinone derivative represented by the general formula (1) (wherein OR1 is a protected hydroxyl group; R2 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group or a substituted or unsubstituted aromatic group) is reacted with an ester compound represented by the formula (2) (wherein CO2R3 is an esterified carboxyl group; X and Y are the same or different and represent individually a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted alkyloxy group, a substituted or unsubstituted alkenyloxy group, a substituted or unsubstituted aralkyloxy group, a substituted or unsubstituted aryloxy group, a substituted or unsubstituted silyloxy group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic-thio group, a substituted or unsubstituted heterocyclic-oxy group, a substituted or unsubstituted acyl group, a substituted or unsubstituted ester group, a substituted or unsubstituted thio ester group, a substituted or unsubstituted amide group, a substituted or unsubstituted amino group, a hydrogen atom or halogen atom, or are taken together with each other to form a substituted or unsubstituted cycloalkan-2-on-1-yl group) in the presence of zinc and copper compounds to synthesis a 4-substituted azetidinone derivative represented by the formula (3) (wherein OR1, CO2R3, X and Y are as defined above).
    • 由通式(1)表示的氮杂环丁酮衍生物(其中OR 1为保护的羟基; R2为取代或未取代的烷基,取代或未取代的烯基或取代或未取代的芳族基团)与表示的酯化合物 通式(2)(其中CO 2 R 3是酯化的羧基; X和Y相同或不同,分别代表取代或未取代的烷基,取代或未取代的烯基,取代或未取代的芳烷基,取代或未取代的芳烷基, 未取代的芳基,取代或未取代的烷硫基,取代或未取代的链烯硫基,取代或未取代的芳烷硫基,取代或未取代的芳硫基,取代或未取代的烷氧基,取代或未取代的烯氧基,取代或未取代的 芳烷氧基,取代或未取代的芳氧基,取代基 取代或未取代的杂环基,取代或未取代的杂环硫基,取代或未取代的杂环氧基,取代或未取代的酰基,取代或未取代的酯基,取代或未取代的硫代 酯基,取代或未取代的酰胺基,取代或未取代的氨基,氢原子或卤素原子,或彼此一起形成取代或未取代的环烷烃-2-基-1-基) 存在锌和铜化合物以合成由式(3)表示的4-取代的氮杂环丁酮衍生物(其中OR1,CO2R3,X和Y如上定义)。