公开(公告)号：WO1998022437A1

公开(公告)日：1998-05-28

申请号：PCT/US1997021081

申请日：1997-11-18

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  WANG, Wei-bo ,  LI, Qun ,  CHU, Daniel, T. ,  HASVOLD, Lisa, Anne

IPC: C07D207/14

CPC classification number: C07D207/14 ,  C07D455/02 ,  C07D471/04 ,  Y02P20/55

Abstract: A process for the preparation of chiral 3-aminopyrrolidine of formula (I) and analogous bicyclic derivatives of formula (II) from dihydroxy olefins such as for the formula: HO-CH2-CH=CH-CH2-OAr 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.

Abstract translation: 通过用异丙醇钛处理从二羟基烯烃如式HO-CH2-CH = CH-CH2-OAr制备式（I）的手性3-氨基吡咯烷和式（Ⅱ）的类似双环衍生物的方法， 光学活性酒石酸酯和叔丁基过氧化氢，然后用烷基或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，随后进一步用氨基取代环羟基 其保护，第二环的任选的另外的取代封闭，以及氢解以除去环 - 氮保护基。