摘要:
A stereoselective anion glycosylation process for preparing β anomer enriched 2'-deoxy-2',2'-difluoronucleosides by reacting an αanomer enriched 2-deoxy-fluoro-1-halo carbohydrate with at least a molar equivalent of a nucleobase salt in an inert solvent.
摘要:
A process for separating an anomeric mixture of alpha and beta 2-deoxy-2,2-difluoro-D-ribofuranosyl-1-alkylsulfonates by contacting the anomeric mixture with a solvent; heating; adding a countersolvent; and lowering the temperature.
摘要:
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 α/β anomeric ratio, and processes for selectively isolating β-2′-deoxy-2′,2′-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 α/β mixture.
摘要:
57 7β-Amino-3-(1-pyridiniummethyl)-3-cephem-4-carboxylate dihydrochloride salt is obtained as the crystalline dihydrate directly from the N-deacylation reaction mixture by mixing said reaction mixture with acetonitrile, acetone or isopropyl alcohol, each containing 5% to 10% water.
摘要:
N-chlorophthalimide, N-chlorosuccinimide, and N-chloroglutarimide are prepared by contacting the corresponding imide with molecular chlorine under substantially non-aqueous conditions in an inert organic solvent in the presence of a polyvinylpyridine copolymer.