Process for preparing 2',2'-difluoronucleosides
US5434254A · kind A · utility
13Cited by
5References
4Claims
0Family size
Assignee
Inventors
Key dates
| Filing date | Apr 19, 1993 |
| Grant date | Jul 18, 1995 |
| Priority date | — |
| Expiry date | Apr 19, 2013 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H19/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 .alpha./.beta. anomeric ratio, and processes for selectively isolating .beta.-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 .alpha./.beta. mixture.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.