Process for preparation of chiral 3-amino-pyrrolidine and analogous
bicyclic compounds
    1.
    发明授权
    Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds 失效
    手性3-氨基 - 吡咯烷和类似双环化合物的制备方法

    公开(公告)号:US5837868A

    公开(公告)日:1998-11-17

    申请号:US974206

    申请日:1997-11-19

    摘要: A process for the preparation of chiral 3-aminopyrrolidine and analogous bicyclic derivatives from dihydroxy olefins by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylation of the intermediate with an alkyl or alkenyl magnesium halide, then pyrrolidine ring formation by condensation with an arylmethylamine, subsequent chiral replacement of a ring hydroxyl group with an amino group with further protection thereof, optional additional substitution closing of the second ring, and hydrogenolysis to remove a ring-nitrogen protecting group.

    摘要翻译: 通过用异丙醇钛,光学活性酒石酸酯和叔丁基过氧化氢处理二羟基烯烃手性3-氨基吡咯烷和类似双环衍生物的方法,然后用烷基或链烯基卤化镁随后烷基化中间体,然后 通过与芳基甲胺缩合形成吡咯烷环,随后进一步保护具有氨基的环羟基的手性取代,任选的第二环的另外的取代封闭,以及氢解除去环 - 氮保护基。

    Process for preparation of chiral 3-amino-pyrrolidine and analogous
bicyclic compounds
    2.
    发明授权
    Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds 失效
    手性3-氨基 - 吡咯烷和类似双环化合物的制备方法

    公开(公告)号:US5703244A

    公开(公告)日:1997-12-30

    申请号:US754641

    申请日:1996-11-21

    摘要: A process for the preparation of chiral 3-aminopyrrolidine and analogous bicyclic derivatives from dihydroxy olefins by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylation of the intermediate with an alkyl or alkenyl magnesium halide, then pyrrolidine ring formation by condensation with an arylmethylamine, subsequent chiral replacement of a ring hydroxyl group with an amino group with further protection thereof, optional additional substitution closing of the second ring, and hydrogenolysis to remove a ring-nitrogen protecting group.

    摘要翻译: 通过用异丙醇钛,光学活性酒石酸酯和叔丁基过氧化氢处理二羟基烯烃手性3-氨基吡咯烷和类似双环衍生物的方法,然后用烷基或链烯基卤化镁随后烷基化中间体,然后 通过与芳基甲胺缩合形成吡咯烷环,随后进一步保护具有氨基的环羟基的手性取代,任选的第二环的另外的取代封闭,以及氢解除去环 - 氮保护基。