Process for the preparation of enantiomerically pure 3-phenyl-3-hydroxypropylamine
    1.
    发明授权
    Process for the preparation of enantiomerically pure 3-phenyl-3-hydroxypropylamine 失效
    制备对映体纯的3-苯基-3-羟基丙基胺的方法

    公开(公告)号:US06838581B2

    公开(公告)日:2005-01-04

    申请号:US10309010

    申请日:2002-12-04

    CPC classification number: C07C215/30 C07B2200/07 Y02P20/582

    Abstract: The present invention relates to an improved process for the synthesis of enantiomerically pure 3-phenyl-3-hydroxypropylamine of formula I; more particularly the present invention relates to the said process using styrene; the synthetic strategy features a Sharpless asymmetric dihydroxylation (SAD) route to the target compound, using styrene, a readily accessible starting material gives the optically pure dihydroxy compound (ee >97%; the selective monotosylation of primary alcohol, nucleophilic displacement by cyano and subsequent reduction to amino group furnishes the desired 3-phenyl-3-hydroxypropylamine in enatiomerically pure form, a key intermediate in the synthesis of variety of oxetine related anti-depressant drugs.

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