Preparation of an enantiomeric mixture of erythro and threo...

Details Preparation of an enantiomeric mixture of erythro and threo... Preparation of an enantiomeric mixture of erythro and threo...

C - Chemistry, Metallurgy

07

D

260/362, 260/366

C07D 307/33 (2006.01) C07H 19/073 (2006.01)

Patent

CA 1331194

ABSTRACT The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleo- sides 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 addi- tion salt thereof, from the 1:1 .alpha./.beta. mixture.

616613

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