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US 5,296,589 AGranted
Hydrogenation of 2-fluoro-9-(2,3,5-tri-o-benzyl-beta-D-arabinofuranosyl)adenine
AssigneeAsh Stevens, Inc.
InventorPeter Blumbergs
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Abstract
A process for the preparation of 2-fluoro-9-beta-D-arabinofuranosyl purine (VII) by a reaction of palladium chloride and hydrochloric acid with 2-fluoro-9-(2,3,5-tribenzyl-beta-D-arabinofuranosyl)adenine (VI) at elevated pressures in a solvent for (VI) is described. The reaction is rapid, economical and efficient.
Claims6
A process for the preparation of 9-beta-D-arabinofuranosyl-2-fluoroadenine (VII) which consists essentially of:
- (a) reacting a mixture of 2-fluoro-9-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl)adenine (VI) dissolved in a non-reactive solvent for (VI), with hydrogen and a molar amount of palladium chloride less than (VI) and concentrated hydrochloric acid in a molar excess to (VI) such that the weight of palladium chloride is between about 3 and 15% by weight of (VI) in a sealed vessel at elevated pressure above atmospheric pressure between about 30 and 50 psig to produce (VII) in the reaction mixture;
- (b) removing the palladium chloride from the reaction mixture;
- (c) neutralizing the reaction mixture;
- and
- (d) separating 2-fluoro-9-beta-D-arabinofuranosyl adenine from the reaction mixture.
2 more elements
Dependencies are inferred from the claim text.