Process for and intermediates of 2',2'-difluoronucleosides
US5223608A · kind A · utility
35Cited by
5References
9Claims
0Family size
Assignee
Inventors
Key dates
| Filing date | Jul 12, 1990 |
| Grant date | Jun 29, 1993 |
| Priority date | — |
| Expiry date | Jul 12, 2010 |
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.