Patent ID: 8063213
Filing Date: 2011-11-22
Classification: A61P,C07D

Abstract:
1. A process for the formation of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl (methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, comprising the steps a) to g): a) reacting a (1-6C)alkyl ester of (E)-(6-{2-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl}(4R,6S)-2,2-dimethyl[1,3]dioxan-4-yl) acetic acid in a water miscible organic solvent with aqueous acid at a temperature of 30-50° C.; b) reacting the resulting solution with an aqueous alkali metal hydroxide and optionally washing the resulting aqueous alkali metal salt solution with a suitable organic solvent; c) adjusting the pH of the resulting solution to between pH 9 and pH 10.5 by addition of aqueous hydrochloric acid; d) removing the water miscible organic solvent; e) optionally filtering the resulting mixture; f) adding a water soluble calcium salt to the filtrate so as to form (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt; and g) isolating the product of step f).