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    • 5. 发明授权
    • Process for preparing optically active oxazolidinone derivative
    • 光学活性恶唑烷酮衍生物的制备方法
    • US06403804B1
    • 2002-06-11
    • US09456950
    • 1999-12-07
    • Kenzo SumiTakashi ImaiShigeru MitsuhashiHideki NaraTakashi Miura
    • Kenzo SumiTakashi ImaiShigeru MitsuhashiHideki NaraTakashi Miura
    • C07D26304
    • C07D263/20C07D263/22C07D263/24
    • Disclosed is a process for preparing an optically active oxazolidinone derivative comprising allowing hydrazine to react on an optically active ester having a hydroxyl group at the 3-position which is represented by formula (II): wherein R1 represents a lower alkyl group having 1 to 4 carbon atoms, a phenyl group, a methoxymethyl group, a benzyloxymethyl group, a benzyloxycarbonylaminomethyl group which may have a substituent or substituents on the benzene ring thereof, an acylaminomethyl group having 3 to 10 carbon atoms, or an alkyloxycarbonylaminomethyl group having 3 to 6 carbon atoms; R2 and R3, which may be the same or different, each represent a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a phenyl group, an acetylaminomethyl group, a benzoylaminomethyl group, or a benzyl group; and * indicates an asymmetric carbon atom, and subjecting the resulting hydrazide to Curtius rearrangement.
    • 公开了一种制备光学活性恶唑烷酮衍生物的方法,其包括使肼在由式(II)表示的3-位具有羟基的光学活性酯上反应:其中R1表示具有1-4个碳原子的低级烷基 碳原子,苯基,甲氧基甲基,苄氧基甲基,苯环上可以具有取代基的苄氧羰基氨基甲基,碳原子数3〜10的酰氨基甲基或碳原子数3〜6的烷氧基羰基氨基甲基 原子 R 2和R 3可以相同或不同,分别表示氢原子,碳原子数1〜4的低级烷基,苯基,乙酰氨基甲基,苯甲酰基氨基甲基或苄基。 和*表示不对称碳原子,并将所得酰肼进行柯氏重排。