发明名称 Process for production of optically active-3-amino-2-hydroxypropionic cyclopropylamide derivatives and salts thereof
摘要 An objective of the present application is to provide an industrially practicable method for producing an optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof from an inexpensive easily-available starting material. The derivative or salt thereof is useful as an intermediate for a medicine. It is also intended by the present application to provide a useful intermediate of the derivative. The objective is attained by the following method. First, an easily-available 2-halo-3-oxopropionic acid derivative is asymmetrically reduced, and then epoxidated to produce an optically-active epoxycarboxylic acid derivative. Next, the derivative is converted into an optically-active epoxyamide derivative by reaction with cyclopropylamine, and then reacted with a nitrile to obtain an optically-active oxazolinamide derivative. Subsequently, selective acid solvolysis of the oxazoline skeleton gives the optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof.
申请公布号 US2010048909(A1) 申请公布日期 2010.02.25
申请号 US20070227788 申请日期 2007.05.22
申请人 KANEKA CORPORATION 发明人 MORI KOHEI;NISHIYAMA AKIRA;TAOKA NAOAKI;MORIYAMA DAISUKE;NAGASHIMA NOBUO
分类号 C07D263/12;C07C237/06;C07D303/38 主分类号 C07D263/12
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