PREPARATION OF NONCRYSTALLINE CALCIUM ATORVASTATIN Russian patent published in 2008 - IPC C07D207/34 

FIELD: technological processes.

SUBSTANCE: method of atorvastatin preparation in noncrystalline form includes: a) preparation of solution that contains intermediate compound of the following formula (I) in nonhydroxyl dissolvant: , where A stands for generic protective group or separate protective groups for dihydroxygroup, and B stands for protective group for carboxyl group; b) removal of protection from dihydroxygroup; c) removal of protection from carboxyl group; at that sequence of stages b) and c) may be reverse; d) solution concentration approximately to half or less of initial volume; e) addition of water volume, which is excessive in comparison with volume of concentrated solution; f) addition of dissolvent that poorly mixes or does not mix with water and in which calcium atorvastatin does not dissolve or dissolves poorly, and the volume of this dissolvent is approximately equal to or more than water volume that was added to stage e); g) optional operation of mixing and division into two phases; h) neutralization of water phase; i) conversion of atorvastatin in the form of dihydroxycarboxylic acid into pharmaceutically acceptable form of salt; and j) creation of calcium atorvastatin deposit, which is obtained by conversion to mentioned pharmaceutically acceptable form of salt.

EFFECT: improves stages of calcium atorvastatin preparation out of atorvastatin lactone form.

22 cl, 1 dwg, 2 ex