Patent ID: 9133132
Filing Date: 2015-09-15
Classification: A61K,A61P,C07D

Abstract:
1. A method for the preparation of a rosuvastatin product, which method is one of the following methods I or II: I) for the preparation of rosuvastatin TBA salt of Formula (III) which comprises reacting a rosuvastatin ester of Formula (II) wherein R represents methyl, ethyl or tert-butyl, in a polar solvent with 1.5 to 5 molar equivalents of tert-butylamine in aqueous solution at a temperature between 10° C. and the boiling point of the solvent; or II) for the preparation of crystalline Form II rosuvastatin TBA salt of Formula (III), which comprises suspending a rosuvastatin ester of Formula (II), wherein R represents methyl, ethyl or tert-butyl, in water, adding an aqueous solution of equimolar amount of tert-butylamine at a temperature between 10 and 50° C., optionally repeating the addition of tert-butylamine within 2 to 24 hours one to five times by adding the aqueous solution of 0.1 to 0.5 molar equivalents of tert-butylamine each time, removing the separated solids from the solution after 72 to 96 hours and isolating the thus obtained crystalline Form II rosuvastatin TBA salt of Formula (III).