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US 2002/0002288 A1Published application
Process for purifying lovastatin and simvastatin with reduced levels of dimeric impurities
AssigneeBiogal Gyogyszergyar Rt.
InventorsVilmos Keri, Ilona Forgas
Life of this patent
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Abstract
A process reducing the levels of dimeric impurities in a statin to less than 0.08% by treatment of a statin containing more than 0.08% dimeric impurities with a mild base in a suitable solvent mixture.
Claims19
A process for reducing the dimeric impurities in Lovastatin or Simvastatin comprising:
- a) dissolving or suspending Lovastatin or Simvastatin containing greater than 0.08% dimeric impurities in a solvent mixture;
- b) treating said solution or suspension with a mild base;
- and
- c) isolating Lovastatin or Simvastatin containing less than about 0.08% dimeric imputities.
1 more element
A process for a statin selected from the group consisting of Lovastatin or Simvastatin comprising:
- a) dissolving or suspending the statin in the solvent comprising 1-70% or an alcohol selected from the group consisting of Methanol, Ethanol, i-Propanol, n-Propanol, i-Butanol, n-Butanol, t-Butanol and a mixture thereof;
- and a second solvent selected from the group dichloromethane, dichloroethane, chloroform, carbon tetrachloride, acetonitrile, petroleum ether, heptane, hexane, cyclohexane, acetone, butyl-methyl keton, methyl acetate, ethyl acetate, propyl acetate, i-butyl acetate, n-butyl acetate, t-butyl acetate, methyl formate, ethyl formate, propyl formate;
- and a mixture of said solvents;
- b) adding a mild base selected from the group aliphatic mono- or di- or triamines, aromatic amines, ammonium hydroxide, ammonia gas, an aqueous solution of any of the foregoing, and mixtures thereof;
- c) treating of the solution;
- and
- d) isolating lovastatin or simvastatin from said solvent mixture by crystallization or precipitation, at about −20° C. to about +25° C.
4 more elements
Dependencies are inferred from the claim text.