Process for the preparation of a water soluble mono-lysine salt of ((2R,3R)-3 (4-(4-cyanophenyl)thiazol-2-yl)-2-(2,4 difluorophenyl)-1-(1H-1,1,2,4-triazol-1 yl)butan-2-yloxy)methyl dihydrogen phosphate

Abstract

A process for the preparation of a water soluble mono-lysine salt of the following formula: said method comprising: (a) reacting a compound of formula B: with a compound of formula III’:wherein Pr of formula III’ represents a hydroxyl-protecting group; said reaction is in an inert organic solvent in the presence of base at a temperature of from about 25oC to 50oC to form a first intermediate of formula IV’: wherein Pr of formula IV’ represents a hydroxyl-protecting group; (b) removing the protecting groups Pr of formula IV’ with organic solvent to form a second intermediate of formula V’: (b) reacting said second intermediate of formula V’ with lysine in a solvent at a pH in the range of 4.2-5.5 to produce said mono-lysine salt.