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RU98122366A - IMPROVED METHOD OF LACTONIZATION IN OBTAINING STATINS - Google Patents

IMPROVED METHOD OF LACTONIZATION IN OBTAINING STATINS

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Publication number
RU98122366A
RU98122366A RU98122366/04A RU98122366A RU98122366A RU 98122366 A RU98122366 A RU 98122366A RU 98122366/04 A RU98122366/04 A RU 98122366/04A RU 98122366 A RU98122366 A RU 98122366A RU 98122366 A RU98122366 A RU 98122366A
Authority
RU
Russia
Prior art keywords
formula
reaction mixture
obtaining
lactonization
statins
Prior art date
Application number
RU98122366/04A
Other languages
Russian (ru)
Other versions
RU2214407C2 (en
Inventor
Ятендра Кумар
Раджеш Кумар Тапер
С.М.Дилип Кумар
Джаг Мохан Кханна
Original Assignee
Рэнбакси Лабораториз Лтд.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US09/064,285 external-priority patent/US5917058A/en
Application filed by Рэнбакси Лабораториз Лтд. filed Critical Рэнбакси Лабораториз Лтд.
Publication of RU98122366A publication Critical patent/RU98122366A/en
Application granted granted Critical
Publication of RU2214407C2 publication Critical patent/RU2214407C2/en

Links

Claims (11)

1. Способ получения соединения формулы I
Figure 00000001

где R представляет
Figure 00000002

где R1 представляет Н или CH3,
включающий обработку соединения формулы II
Figure 00000003

где Z представляет водород, катион металла, или NH4 и R является таким, как определено выше, слабой органической кислотой в отсутствие сильной кислоты при температуре ниже 55°С с получением реакционной смеси и извлечение указанного соединения формулы I из указанной реакционной смеси.1. The method of obtaining the compounds of formula I
Figure 00000001

where R represents
Figure 00000002

where R 1 represents H or CH 3 ,
comprising treating a compound of formula II
Figure 00000003

where Z is hydrogen, a metal cation, or NH 4 and R is, as defined above, a weak organic acid in the absence of a strong acid at a temperature below 55 ° C. to obtain a reaction mixture and recovering said compound of formula I from said reaction mixture. 2. Способ по п. 1, отличающийся тем, что указанная слабая органическая кислота является уксусной кислотой. 2. The method according to p. 1, characterized in that said weak organic acid is acetic acid. 3. Способ по п. 1, отличающийся тем, что дополнительно включает добавление к указанной реакционной смеси антирастворителя, что вызывает осаждение указанного соединения формулы I из указанной реакционной смеси. 3. The method according to p. 1, characterized in that it further comprises adding to the specified reaction mixture an anti-solvent, which causes the precipitation of the specified compounds of formula I from the specified reaction mixture. 4. Способ по п. 3, отличающийся тем, что указанное соединение формулы I осаждается из указанной реакционной смеси в виде кристаллического продукта. 4. The method according to p. 3, characterized in that said compound of formula I is precipitated from said reaction mixture as a crystalline product. 5. Способ по п. 3, отличающийся тем, что указанный антирастворитель является водой, гексаном, гептаном или циклогексаном. 5. The method according to p. 3, characterized in that said anti-solvent is water, hexane, heptane or cyclohexane. 6. Способ по п. 3, отличающийся тем, что указанный антирастворитель является водой. 6. The method according to p. 3, characterized in that said anti-solvent is water. 7. Способ по п. 2, отличающийся тем, что Z представляет Na, K или NH4.7. The method according to p. 2, characterized in that Z represents Na, K or NH 4 . 8. Способ по п. 1, отличающийся тем, что Z представляет NH4.8. The method according to p. 1, characterized in that Z represents NH 4 . 9. Способ по п. 1, отличающийся тем, что его проводят при температуре около 25-45oС.9. The method according to p. 1, characterized in that it is carried out at a temperature of about 25-45 o C. 10. Способ по п. 1, отличающийся тем, что его проводят при температуре около 35-40oС.10. The method according to p. 1, characterized in that it is carried out at a temperature of about 35-40 o C. 11. Способ по п. 1, отличающийся тем, что его проводят в течение примерно 5-7 ч. 11. The method according to p. 1, characterized in that it is carried out for about 5-7 hours
RU98122366/04A 1998-04-22 1998-12-09 Improved method for lactonization in preparing statins RU2214407C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/064,285 US5917058A (en) 1997-10-28 1998-04-22 Process of lactonization in the preparation of statins
US09/064,285 1998-04-22

Publications (2)

Publication Number Publication Date
RU98122366A true RU98122366A (en) 2000-09-27
RU2214407C2 RU2214407C2 (en) 2003-10-20

Family

ID=22054869

Family Applications (1)

Application Number Title Priority Date Filing Date
RU98122366/04A RU2214407C2 (en) 1998-04-22 1998-12-09 Improved method for lactonization in preparing statins

Country Status (9)

Country Link
EP (1) EP0955297B9 (en)
AT (1) ATE264849T1 (en)
DE (1) DE69823333T2 (en)
DK (1) DK0955297T3 (en)
ES (1) ES2217485T3 (en)
HU (1) HUP9802936A3 (en)
PT (1) PT955297E (en)
RU (1) RU2214407C2 (en)
ZA (1) ZA9810764B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001034590A1 (en) 1999-11-11 2001-05-17 Biocon India Limited Process for manufacturing simvastatin and the novel intermediates
US6573385B1 (en) 1999-11-11 2003-06-03 Biocon India Limited Process for manufacturing simvastatin and novel intermediates thereof
SI21235A (en) * 2001-05-18 2003-12-31 Aurobindo Pharma Limited A process for lactonization to produce simvastatin
KR100407758B1 (en) * 2001-08-27 2003-12-01 씨제이 주식회사 Process of lactonization in the preparation of statins
US6603022B1 (en) 2002-05-10 2003-08-05 Biocon India Limited Process for manufacturing Simvastatin and novel intermediates thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4820850A (en) * 1987-07-10 1989-04-11 Merck & Co., Inc. Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof
US4916239A (en) * 1988-07-19 1990-04-10 Merck & Co., Inc. Process for the lactonization of mevinic acids and analogs thereof
US5159104A (en) * 1991-05-01 1992-10-27 Merck & Co., Inc. Process to simvastatin ester
US5393893A (en) * 1993-11-08 1995-02-28 Apotex, Inc. Process for producing simvastatin and analogs thereof

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