CRYSTALLINE FORMS VI AND VII OF ATORVASTATIN CALCIUM SALT Russian patent published in 2007 - IPC C07D207/34 

FIELD: organic chemistry, chemical technology, pharmacy.

SUBSTANCE: invention relates to a novel crystalline form of atorvastatin semicalcium salt of [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid that is characterized by the following roentgen powdery diffractogram (values of parameter d in Å): 22.52, 19.44, 11.84, 11.23, 9.58 and 4.69, and to a method for its preparing involving the following steps: (a) heating a mixture consisting of [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)-carbonyl]-1H-pyrrole-1-heptanoic acid tert.-butyl ester, acetonitrile, water and sodium peroxide in scales to temperature about 25-60°C; (b) keeping the reaction mixture from step (a) at 25-60°C for about 3-9 h; (c) addition calcium acetate semihydrate aqueous solution to the above said reaction mixture; (d) the following stirring the reaction mixture at 30-50°C for about 1-2 h; (e) filtration of the reaction solution obtained at step (d); (f) distilling off the reaction solution obtained at step (e) to yield a residue; (g) suspending a residue from step (f) in mixture of water and aliphatic nitrile solvent chosen from acetonitrile and propionitrile; (h) heating the reaction mixture obtained at stage (g) to boiling with reflux condenser for 10-18 h, and (i) isolation of atorvastatin calcium salt crystalline form obtained from step (h).

EFFECT: improved preparing method.

7 cl, 2 dwg, 3 tbl, 3 ex