ES412248A1 - O2,2-anhydro-1- beta-d-arabino-furanosyl-cytosine derivatives methods for their preparation and related procedures - Google Patents

Abstract

A process for the preparation of pharmaceutically acceptable salts of derivatives of O2,2'-anhydrol- (3'-O-acyl-β -D-arabinofuranosyl) cytosine, which consists of treating the corresponding salts of the formula: **(See formula)** where R1 and R2 are independently selected from the group consisting of hydrogen, lower alkyl, aryl or lower alkylaryl; R3 is selected from the group consisting of lower alkyl or cycloalkyl of 3 to 6 ring atoms or a heterocycle of 5 to 7 ring atoms and containing the 2 ring heteroatoms independently selected from the group consisting of oxygen, nitrogen and sulfur; X is halogen or another pharmaceutically acceptable anion, Z is the group (see formula) where R6 is hydrogen, halogen, lower alkyl, hydroxyalkyl lower, trifluoromethyl, azido, nitro, amino, lower alkyl or acylamino, and R7 is hydrogen or methyl and where when Z is (see formula), then R1 and R2 are independently selected from the group consisting of hydrogen or lower alkyl, one of the radicals R4 or R5 is lower alkyl or aryl and the other is hydrogen, lower alkyl or aryl or R4 and R5 joined to the Carbon atoms to which they are attached form a cycloalkyl group containing 4 to 8 ring atoms or a heterocycle of 5 to 7 ring atoms containing one or two heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur, in a hydroxylic solvent containing an amount of a strong mineral or organic acid sufficient to provide an acidic solution of about 0.01 to 0.5 molar, at temperatures ranging from about 0 to 40ºC and for about 0.5 to 5 hours. (Machine-translation by Google Translate, not legally binding)