FIELD: chemistry.
SUBSTANCE: invention relates to an improved method of producing rosuvastatin calcium salt (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulphonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid, which is useful as inhibitor of HMG-CoA-reductase. The method involves: a) acid hydrolysis of the acetal protective group in compound with formula 
,
where A is an acetal or ketal protective group and R is (2-6C)alkyl, and separation of the obtained crystalline compound with formula 
; b) possible recrystallisation of formula (8) compound; c) hydrolysis of the ester group in formula (8) compound, obtaining hydroxycarboxylate derivative (9) (where M is hydrogen or metal counter ion, different from calcium) or compound with formula (1); and 
, 
.
EFFECT: invention also relates to crystalline intermediate compounds with formulae 7, 8 and 10.
17 cl, 11 dwg
| Title |
Year |
Author |
Number |
| CRYSTALLINE FORM OF CALCIUM SALT OF BIS-[(E)-7-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULPHONYL)AMINO]-PYRIMIDIN-5-YL](3R, 5S)-3, 5-DIHYDROXYHEPT-6-ENOIC ACID |
2004 |
- But Rebekka Dzhejn
- Sittern Piter Ehntoni
- Krabb Dzheffri Norman
- Khorberi Dzhon
- Dzhouns Dejvid Uin Kalvert
|
RU2363697C2 |
| METHOD OF PRODUCING CALCIUM SALT (E)-7-[4-(4-FLUOROPHENYL)-6-ISOPROYL-2-[METHYL(METHYSUFONYL)AMINO]PYRIMIDIN-5-YL](3R,5S)3,5-DIHYDROXYHEPT-6-ENOIC ACID (ROSUVASTATIN CALCIUM SALT) |
2004 |
- Krabb Dzheffri Norman
- Khorberi Dzhon
- Tejlor Najdzhel Filip
|
RU2361864C2 |
| 7-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2- [METHYL(METHYLSULFONYL)AMINO]PYRIMIDIN -5-YL]-(3R,5S)-3,5-DIHYDROXYHEPT-6-ENOIC ACID CRYSTALLINE SALTS, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION |
2001 |
- Tehjlor Najdzhel Filip
- Okada Tetsuo
|
RU2265599C2 |
| CRYSTALLINE HYDRATED FORM OF BIS-[(E)-7-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]-PYRIMIDINE-5-YL]-(3R,5S)-3,5-DIHYDROXYHEPT-6-ENOIC ACID] CALCIUM SALT, METHOD FOR ITS PREPARING, PHARMACEUTICAL COMPOSITION, METHOD FOR ITS PREPARING AND METHOD FOR TREATMENT |
1999 |
|
RU2236404C2 |
| METHOD OF ROSUVASTATIN CALCIUM SALT PREPARATION |
2003 |
- Khorberi Dzhon
- Tejlor Najdzhel Filip
|
RU2326871C2 |
| TERTIARY BUTYL-(E)-(6-{2-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]-PYRIMIDINE-5-YL}-(4R,6S)-2,2-DIMETHYL[1,3]DIOXANE-4-YL]ACETATE AND METHOD FOR ITS PREPARING, DIPHENYL-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]-PYRIMIDINE-5-YLMETHYL]PHOSPHINE OXIDE, METHODS FOR PREPARING (E)-7-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]-PYRIMIDINE-5-YL]-(3R,5S)-3,5-DIHYDROXYHEPT-6-ENOIC ACID AND ITS DERIVATIVES |
2000 |
- Koike Kharuo
- Kabaki Mikio
- Tehjlor Najdzhel Filip
- Dioratsio Lui Dzhozef
|
RU2243969C2 |
| PHARMACEUTICAL COMPOSITIONS COMPRISING INHIBITOR OF HMG-REDUCTASE |
2000 |
- Krikmor Dzhozef Richard
- Uigginz Norman Al'Fred
|
RU2206324C1 |
| APPLICATION OF ROSUVASTATIN (ZD-4522) IN TREATING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA |
2001 |
- Rehjza Ali
- Khatchinson Khauard Dzherard
|
RU2294744C2 |
| PHARMACEUTICAL COMPOSITION COMPRISING INHIBITOR OF HMG-COA- REDUCTASE |
2000 |
- Krikmor Dzhozef Richard
- Vidzhins Norman Alfred
|
RU2264210C2 |
| APPLICATION OF 3-HYDROXY-3-METHTYLGLUTARYL-COENZYME A REDUCTASE INHIBITORS IN PRODUCING MEDICINAL AGENT FOR TREATMENT OF DIABETIC NEUROPATHY |
2000 |
- Kehmeron Norman Judzhin
- Kotter Mehri Ehnn
|
RU2239456C2 |
