Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines
US5347017A · kind A · utility
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Key dates
| Filing date | Jul 7, 1993 |
| Grant date | Sep 13, 1994 |
| Priority date | — |
| Expiry date | Jul 7, 2013 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D207/09
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
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.
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