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Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-

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专利名称:Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted- pyrrolidines

发明人:Victor Fedij,Mark J. Suto,James N.

Wemple,James R. Zeller

申请号:US08/0884申请日:19930707公开号:US05347017A公开日:19940913

摘要:The process for the preparation of chiral 3-(1-amino-1,1- bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridineand quinolone antibacterial agents which comprises reacting readily available chiral 1-substituted-3-pyrrolidinols to their corresponding chiral sulfonate esters; converting thesulfonate esters to chiral 1-substituted-3-cyanopyrrolidines having an inverse

configuration, and then dialkylating the chiral cyanopyrrolidines with alkyl lithium in thepresence of a Lewis acid without racemization at the asymmetric carbon atom isdescribed.

申请人:WARNER-LAMBERT COMPANY

代理人:Ronald S. Daignault,Charles W. Ashbrook

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