Novel Method for the Preparation of Stavudine Polymorphic Form I and Form II

摘要

A novel method for the preparation of stavudine polymorphic form I and form II is described. 5′-acetate-2′,3′-diacetyl-5-methyluridine is reacted with catalytic amounts of sodium methoxide in a C1-C4 alcoholic solvent, resulting in crude stavudine form II. Crude stavudine form II can be converted into polymorphic stavudine form I by slurry at reflux in isopropanol, without isolating or purifying the crude stavudine form II.