- A formyl rosuvastatin salts calcium intermediate preparation method
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The invention discloses a preparation method of a formoxyl rosuvastatin calcium intermediate. With 2-methyl-3-carbonyl valeronitrile, 4-fluorobenzaldehyde and urea as raw materials, the formoxyl rosuvastatin calcium intermediate 4-(4-fluorophenyl)-2-hydroxy-6-isopropyl-5-formoxyl-2-(N-methyl-N-methylsulfonyl) pyrimidine is synthesized by reactions such as cyclization, oxidation, N-substitution and reduction. Compared with an existing method, the method has the advantages that reaction conditions are mild, the used reagent is relatively cheap and the yield is high.
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- IMPROVED PROCESS FOR PREPARING STATIN PRECURSOR
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The present invention relates to a process for preparing a statin precursor, which process comprises a first reaction step, wherein a hydroxy-pyrimidine-carbonitrile is reacted with an organic sulfonyl halide to form the sulfonate-pyrimidine-carbonitrile; a second reaction step, wherein the sulfonate-pyrimidine-carbonitrile is reacted with N-methylmethane sulfonamide to form a pyrimidinyl-sulfonamide; and optionally a third reaction step, wherein the pyrimidinyl-sulfonamide is reacted with a reducing agent. All steps are conducted in toluene as the main solvent.
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Page/Page column 11
(2016/12/22)
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- Method for preparing rosuvastatin intermediate and intermediate compound (by machine translation)
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The invention discloses a preparation method of a rosuvastatin intermediate: 4-(4-fluorobenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonyl amino) pyrimidine-5-formonitrile. The method comprises the following steps: carrying out a reaction on ethyl isobutyrate and acetonitrile to generate isobutyryl acetonitrile; and then carrying out cyclization, methylation, reduction, oxidization and substitution on isobutyryl acetonitrile and p-fluoro benzaldehyde as well as thiourea to prepare the intermediate. The 4-(4-fluorobenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonyl amino) pyrimidine-5-formonitrile prepared by the method is low in cost, simple to react, high in yield and easy to realize industrialized production.
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- PROCESS FOR PREPARATION OF ROSUVASTATIN CALCIUM
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Disclosed is the process for the preparation of 4-(fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)-5-formyl-pyrimidine of formula (I), which is the intermediate of rosuvastatin calcium. Purification of substantially pure acetonide protected tert-butyl ester of rosuvastatin (II) and its use for the preparation of substantially pure amorphous rosuvastatin calcium are also disclosed.
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