A method for continuously preparing rosuvastatin intermediates using a microchannel modular reaction device

A microchannel module, rosuvastatin technology, applied in organic chemistry, chemical recovery, etc., can solve the problems of many by-products, difficulty in purification, and low yield, so as to increase yield, shorten reaction time, and reduce solvent consumption volume effect
CN109796414BActive Publication Date: 2022-05-20CHINA PHARM UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CHINA PHARM UNIV
Publication Date
2022-05-20

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Abstract

The invention discloses a method for continuously preparing rosuvastatin intermediates by adopting a microchannel modular reaction device. The isopropanol solution of p-fluorobenzaldehyde and the isopropanol solution of methyl isobutyryl acetate are prepared in acetic acid and piperidine Under catalysis, react in the first microreactor to generate the first product; the first product and the free isopropanol solution of S-methyl isothiourate react in the second microreactor to generate the second product; the second The product is reacted with an acetone solution of potassium permanganate and acetic acid in the third microreactor to obtain the third product; finally the third product is reacted with methylamine ethanol solution in the fourth microreactor to obtain the rosuvastatin intermediate. The invention has low toxicity and pollution, low production cost, good product quality, high profit, environmental protection, energy saving and high efficiency, and has the potential of industrial scale-up.
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Description

technical field

[0001] The invention relates to a method for preparing an intermediate of statin blood lipid-lowering drug rosuvastatin, in particular to a method for preparing an important intermediate of rosuvastatin 4-(4-fluorophenyl)- Method for methyl 6-isopropyl-2-(methylamino)pyrimidine-5-carboxylate. Background technique

[0002] Rosuvastatin, chemical name (3R,5S,6E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methyl-methylsulfonyl-amino)- Pyrimidin-5-yl]-3,5-dihydroxy-6-heptenoic acid, which is a selective hydroxymethylglutaryl coenzyme (HMG-CoA) reductase inhibitor, competes for HMG-CoA reductase, Thereby reducing cholesterol biosynthesis and causing increased clearance of cholesterol from the blood. The main site of action of rosuvastatin is the liver-the target organ for lowering cholesterol. It increases the number of receptors on the surface of liver LDL cells, promotes the absorption and catabolism of LDL, and inhibits the hepatic synthesis of VLDL, thereby reduci...

Claims

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