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US 5,202,029 AGranted
Process for purification of HMG-CoA reductase inhibitors
AssigneeCaron Kabushiki Kaisha
InventorsPeter N. Haytko, Arthur S. Wildman, Jr.
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Abstract
A process for the purification of an HMG-CoA reductase inhibitor employing preparative high performance liquid chromatography is described.
Claims10
A process for purifying a crude HMG-CoA reductase inhibitor which comprises:
- (1) placing a solution of the crude HMG-CoA reductase inhibitor on a high performance liquid chromatography column wherein the column is packed with silica optionally coated with a stationary phase selected from the group consisting of a triorganosilyl, a cyanoorganosilyl and a polystyrene-divinylbenzene copolymer with an organosilyl, or the column is packed with a porous graphitic carbon;
- (2) eluting the crude HMG-CoA reductase inhibitor with a solvent mixture comprising:
- (a) an organic solvent selected from the group consisting of acetonitrile, methanol, ethanol, acetone, tetrahydrofuran, isopropanol, ethyl acetate, methylene chloride and chloroform, or a mixture thereof and optionally
- (b) water or an aqueous solution selected from the group consisting of phosphoric acid and acetic acid;
- (3) removing a portion of the solvent mixture from the eluted HMG-CoA reductase inhibitor;
- and
- (4) treating the eluted HMG-CoA reductase inhibitor with water to crystallize a purified HMG-CoA reductase inhibitor of purity .gtoreq.99.5%.
4 more elements
A process for purifying a crude HMG-CoA reductase inhibitor which comprises:
- (1) placing a solution of the crude HMG-CoA reductase inhibitor on a high performance liquid chromatography column wherein the column is packed with silica optionally coated with a stationary phase selected from the group consisting of triorganosilyl, a cyanoorganosilyl and a polystyrene-divinylbenzene copolymer with an organosilyl, or the column is packed with a porous graphitic carbon;
- (2) eluting with a solvent mixture comprising:
- (a) an organic solvent selected from the group consisting of acetonitrile, methanol, ethanol, acetone, tetrahydrofuran, isopropanol, ethyl acetate, methylene chloride and chloroform, or a mixture thereof and optionally,
- (b) water or an aqueous solution selected from the group consisting of phosphoric acid and acetic acid;
- and
- (3) removing about 60 to 65% of the solvent mixture to crystallize a purified HMG-CoA reductase inhibitor of purity .gtoreq.99.5%.
3 more elements
Dependencies are inferred from the claim text.