发明名称 |
Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines |
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 naphthyridine and quinolone antibacterial agents which comprises reacting readily available chiral 1-substituted-3-pyrrolidinols to their corresponding chiral sulfonate esters; converting the sulfonate esters to chiral 1-substituted-3-cyanopyrrolidines having an inverse configuration, and then dialkylating the chiral cyanopyrrolidines with alkyl lithium in the presence of a Lewis acid without racemization at the asymmetric carbon atom is described.
|
申请公布号 |
US5347017(A) |
申请公布日期 |
1994.09.13 |
申请号 |
US19930088464 |
申请日期 |
1993.07.07 |
申请人 |
WARNER-LAMBERT COMPANY |
发明人 |
FEDIJ, VICTOR;SUTO, MARK J.;WEMPLE, JAMES N.;ZELLER, JAMES R. |
分类号 |
C07D207/09;(IPC1-7):C07D207/50 |
主分类号 |
C07D207/09 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|