Patent ID: 8058424
Filing Date: 2011-11-15
Classification: C07H

Abstract:
1. A method of preparing 5-azacytidine comprising the steps of: a) reacting 5-azacytosine with at least one silylating reagent in a dry organic solvent to yield a silylated 5-azacytosine having the structure: wherein each R b) contacting the reaction mixture of Step a) with trimethylsilyl trifluoromethanesulfonate and a compound having the structure; wherein each R c) contacting the reaction mixture of Step b) with an aqueous quenching composition and extracting the quenched reaction mixture; d) removing substantially all of the solvent in the extract of Step c); e) deprotecting the product in the extract of Step c) with sodium methoxide in methanol to yield 5-azacytidine; and f) recrystallizing the 5-azacytidine product of Step e) from a solvent system comprising dimethylsulfoxide.