FIELD: organic chemistry, biochemistry, chemical technology, pharmacy.
SUBSTANCE: invention relates to (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(me-thylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dih-ydroxyhept-6-enoic acid crystalline salts wherein salt represents ammonium, methyl ammonium, ethyl ammonium, diethanol ammonium, tris-(hydroxymethyl)methyl ammonium, benzyl ammonium, 4-methoxybenzyl ammonium, lithium or magnesium salt possessing property of HMG CoA-reductase inhibitor. Also, invention relates to a pharmaceutical composition comprising crystalline salt in mixture with a pharmaceutically acceptable diluting agent or vehicle an to a method for preparing crystalline salt. Method involves addition of corresponding amine or a base to a solution of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(me-thylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-dihydro-xyhept-6-enoic acid in acetonitrile or ethyl acetate medium. The advantage of crystalline salts involves the possibility for enhancing purity and homogenicity of compounds, the possibility for re-crystallization and preparing the pure amorphous form and enhancing stability of the form.
EFFECT: improved preparing method.
15 cl, 9 dwg, 10 ex
Title |
Year |
Author |
Number |
METHOD OF PRODUCING ROSUVASTATIN CALCIUM SALT (E) -7-[4-(4-FLUOROPHEHYL)-6-ISOPROPYL-2-[METHYL(METHYLSULPHONYL)AMINO]PYRIMIDIN-5-YL](3R,5S)-3,5-DIHYDROXYHEPT-6-ENOIC ACID AND CRYSTALLINE INTERMEDIATE PRODUCTS THEREOF |
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|
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|
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