Process for obtaining Cizolirtine and its enantiomers
    2.
    发明授权
    Process for obtaining Cizolirtine and its enantiomers 失效
    获得Cizolirtine及其对映异构体的方法

    公开(公告)号:US07109349B2

    公开(公告)日:2006-09-19

    申请号:US11041637

    申请日:2005-01-24

    IPC分类号: C07D231/12

    CPC分类号: C07D231/12

    摘要: A process is described for the preparation of a precursor alcohol of Cizolirtine, (±)-2-[phenyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethylethanamine and its enantiomers. The process involves the asymmetric addition of a metalated phenyl reagent to a pyrazolcarbaldehyde in the presence of a chiral ligand to yield chiral alcohols. The chiral alcohols are further O-alkylated to yield Cizolirtine or its enantiomers.

    摘要翻译: 描述了制备Cizolirtine(±)-2- [苯基(1-甲基-1H-吡唑-5-基)甲氧基] -N,N-二甲基乙胺及其对映异构体的前体醇的方法。 该方法包括在手性配体存在下将金属化苯基试剂不对称加成到吡唑甲醛中以产生手性醇。 手性醇进一步O-烷基化以得到西来甜胺或其对映异构体。

    Process for obtaining enantiomers of thienylazolylalcoxyethanamines
    9.
    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:US07078531B2

    公开(公告)日:2006-07-18

    申请号:US11041638

    申请日:2005-01-24

    IPC分类号: C07D231/12

    CPC分类号: C07D409/06

    摘要: 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 in general for thienylazolylalcoxyethanamines and their enantiomers. The process involves asymmetric addition of a metalated thienyl reagent to a pyrazolcarbaldehyde in the presence of a chiral ligand to yield chiral alcohols. The chiral alcohols are further O-alkylated to yield the corresponding pharmaceutically active thienylazolylalcoxyethanamines.

    摘要翻译: 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,通常用于噻吩并噻唑基醛乙氧基胺及其对映异构体。 该方法包括在手性配体的存在下将金属化噻吩试剂不对称加成到吡唑甲醛中以产生手性醇。 手性醇进一步O-烷基化,得到相应的药学活性噻吩并噻唑基乙醇胺。