Process for obtaining enantiomers of thienylazolylalcoxyethanamines
    7.
    发明授权
    Process for obtaining enantiomers of thienylazolylalcoxyethanamines 失效
    获得噻吩并噻唑基乙酰胺的对映异构体的方法

    公开(公告)号:US06979742B1

    公开(公告)日:2005-12-27

    申请号:US11041639

    申请日:2005-01-24

    CPC classification number: C07D409/06

    Abstract: A process is described for the preparation of a precursor alcohol of (±)-2-[thienyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethyletanamine, and more generally for thyenylazolylalcoxyethanamines and their enantiomers. The process involves the asymmetric reduction of a prochiral ketone in the presence of a chiral ruthenium (II) catalyst system comprising at least a bidentate phosphorous-containing ligand and a diamine ligand to yield chiral alcohols. The chiral alcohols are further O-alkylated to yield corresponding pharmaceutically active ethanamines.

    Abstract translation: 描述了制备(±)-2- [噻吩基(1-甲基-1H-吡唑-5-基)甲氧基] -N,N-二甲基乙胺的前体醇的方法,更通常用于甲烯基薁基乙氧基胺及其对映异构体 。 该方法包括在手性钌(II)催化剂体系存在下不对称还原前手性酮,所述手性钌(II)催化剂体系包含至少二齿含磷配体和二胺配体,以产生手性醇。 手性醇进一步O-烷基化以产生相应的药学活性乙胺。

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