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    • 46. 发明专利
    • Method for producing hexahydrofurofuranol derivative
    • 生产十六氢呋喃醇衍生物的方法
    • JP2012158595A
    • 2012-08-23
    • JP2012066509
    • 2012-03-23
    • Sumitomo Chemical Co Ltd住友化学株式会社
    • WATANABE YOSUKEIKEMOTO TETSUYA
    • C07D493/04C07B61/00
    • C07B53/00C07C45/30C07C45/72C07C47/198C07D493/04Y02P20/55C07C47/277
    • PROBLEM TO BE SOLVED: To provide a method for efficiently and inexpensively producing a compound represented by formula (IV) (preferably an optically active substance) in an industrial scale without using ozone oxidation or a strongly toxic reagent and without requiring optical resolution.SOLUTION: The compound (IV) is produced by reacting a compound (I) with a compound (II) in the presence of an optionally substituted cyclic secondary amine to obtain a compound (III) and sequentially or simultaneously eliminating the protective groups (Rand R) of the hydroxy groups of the compound (III), and then cyclizing the Rand R-eliminated compound. (In formulas, Rand Rare each independently a protective group of a hydroxy group).
    • 要解决的问题:提供一种在不使用臭氧氧化或强毒性试剂并且不需要光学拆分的情况下以工业规模有效且廉价地制备由式(IV)表示的化合物(优选光学活性物质)的方法 。 解决方案:化合物(Ⅳ)是通过使化合物(Ⅰ)与化合物(Ⅱ)在任意取代的环状仲胺存在下进行反应,得到化合物(Ⅲ),顺序或同时地除去保护基 (III)的羟基的(R 1 和R 2 ),然后环化R 1 和R 2 - 所有化合物。 (在式中,R 1 和R 2 各自独立地为羟基的保护基)。 版权所有(C)2012,JPO&INPIT