A kind of method for preparing rosuvastatin intermediate

A technology for rosuvastatin and intermediates, applied in the field of pharmaceutical intermediates, can solve the problems of long reaction time, expensive catalyst, low yield, etc., reduce the generation of by-products, have a good prospect for industrial production, and reduce production costs Effect
CN105175345BActive Publication Date: 2018-05-22SHANGHAI INST OF TECH
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF TECH
Publication Date
2018-05-22

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Abstract

The invention discloses a method for preparing a rosuvastatin midbody. The method comprises the steps of weighing lewis acid MgCl<2>, aromatic aldehyde, isobutyryl acetate and thiourea, wherein the mole ratio of aromatic aldehyde to isobutyryl acetate to thiourea is 1:1-1.5:1-2.0, and the mole number of a lewis acid catalyst accounts for 5-20% of the total mole number of aromatic aldehyde, isobutyryl acetate and thiourea; adding aromatic aldehyde, isobutyryl acetate, thiourea and the lewis acid catalyst MgCl<2> into a reaction vessel, adopting 1, 4-dioxane as solvent, stirring the mixture and raising the temperature, after the reaction is conducted sufficiently, getting a reaction solution to be subjected to cooling, washing, extraction, drying, filtration and reduced pressure distillation, then conducting column chromatography isolation, and obtaining the rosuvastatin midbody, namely 4-(4-fluoro-phenyl)-6-isopropyl-2-thiocarbonyl-1, 4-dihydropyrimidine-5-acetate. By means of the method, the rosuvastatin midbody high in purity can be obtained, the catalyst is low in price and easy to obtain, reutilization can be conducted, and the production cost is lowered.
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Description

technical field

[0001] The invention belongs to the field of organic chemistry, in particular to a pharmaceutical intermediate, specifically a preparation of rosuvastatin intermediate 4-(4-fluorophenyl)-6-isopropyl-2-thiocarbonyl-1 , 4-dihydropyrimidine-5-carbonate method. Background technique

[0002] Cardiovascular disease is a major disease that seriously endangers human health. The etiology of cardiovascular and cerebrovascular diseases mainly comes from atherosclerosis, which is mostly manifested as hyperlipidemia, leading to coronary heart disease and hypertension. Statins have become the representative varieties of cardiovascular and cerebrovascular drugs because of their high efficiency and low toxicity. Among them, rosuvastatin calcium was developed by AstraZeneca and was the latest statin drug approved for marketing in Europe in 2002. The results of clinical trials show that its effect on treating cardiovascular drugs is better than that of other statins (such as...

Claims

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