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    • 2. 发明专利
    • Method for producing 3-aralkyloxypyrrolidine derivative
    • 用于生产3-芳基甲基吡咯烷衍生物的方法
    • JP2008169225A
    • 2008-07-24
    • JP2008060163
    • 2008-03-10
    • Kaneka Corp株式会社カネカ
    • TAKEDA TOSHIHIROONUKI MASATOSHIKISHIMOTO SHIGEMI
    • C07D207/12
    • C07D207/12Y02P20/55
    • PROBLEM TO BE SOLVED: To provide a method for producing a 3-aralkyloxypyrrolidine derivative which is important for producing pharmaceuticals and the like, and a method for simply and efficiently producing a high purity 3-aralkyloxypyrrolidine derivative on a commercial scale. SOLUTION: The 3-aralkyloxypyrrolidine derivative is prepared in the form of a crystal by reacting an N-protected-3-hydroxypyrrolidine with an aralkyl halide in the presence of a base and a metal halide and/or a phase transfer catalyst to convert into an N-protected-3-aralkyloxypyrrolidine, deprotecting the N-protecting group to convert into a 3-aralkyloxypyrrolidine derivative, subsequently treating the product in a polar solvent-containing solvent. COPYRIGHT: (C)2008,JPO&INPIT
    • 待解决的问题:提供一种制备药物等重要的3-芳烷氧基吡咯烷衍生物的方法,以及以商业规模简单有效地制备高纯度3-芳烷氧基吡咯烷衍生物的方法。 解决方案:通过在碱和金属卤化物和/或相转移催化剂的存在下使N-保护的3-羟基吡咯烷与芳烷基卤化物反应制备3-芳烷氧基吡咯烷衍生物,其结晶形式为 转化成N-保护的3-芳烷氧基吡咯烷,将N-保护基脱保护,转化为3-芳烷氧基吡咯烷衍生物,随后在含极性溶剂的溶剂中处理该产物。 版权所有(C)2008,JPO&INPIT