Patent ID: 6680382
Filing Date: 2004-01-20
Classification: C07H

Abstract:
A stereoselective procedure process for the preparation 2-chloro-9-(2â€²-deoxy-2â€²-fluoro-&bgr;-D-arabinofuranosyl) adenine comprising:(1) reacting 3,5-O-dibenzoyl-2-deoxy-2-fluoro-&agr;-D-arabinofuranosyl bromide with a 2-chloroadeinine potassium salt of the formula: â€ƒwherein the exocyclic amino group of said 2-chloroadenine potassium salt is not protected, in the presence of a solvent mixture comprising t-amyl alcohol, dichloroethane and acetonitrile to form 2-chloro-9-(3â€²,5â€²-O-dibenzoyl-2â€²-deoxy-2â€²-fluoro-&bgr;-D-arabinofuranosyl) adenine; (2) deprotecting said 2-chloro-9-(3â€²,5â€²-O-dibenzoyl-2â€²-deoxy-2â€²-fluoro-&bgr;-D-arabinofuranosyl)adenine to from 2-chloro-9-(2â€²-deoxy-2â€²-fluoro-&bgr;-D-arabinofuranosyl) adenine; and (3) isolating said 2-chloro-9-(2â€²-deoxy-2-fluoro-&bgr;-D-arabinofuranosyl) adenine to form a composition comprising 2-chloro-9-(2â€²-deoxy-2-fluoro-&bgr;-D-arabinofuranosyl) adenine.