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Preparation method of rosuvastatin calcium

A technology of rosuvastatin calcium and its compound, which is applied in the field of medicinal chemistry, can solve the problems of high cost and high price of compound IV, and achieve the effects of cheap raw materials, less pollution and mild conditions

Inactive Publication Date: 2012-08-01
湖南欧亚药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] (Red-Al), the price of these two reducing agents is relatively high, so the cost of compound IV is high

Method used

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  • Preparation method of rosuvastatin calcium
  • Preparation method of rosuvastatin calcium
  • Preparation method of rosuvastatin calcium

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Embodiment Construction

[0052] In order to make the technical means, creative features, work flow, and use methods of the present invention achieve the purpose and effect easily understood, the present invention will be further described below in conjunction with specific embodiments.

[0053]

[0054]

[0055] V VI

[0056]

[0057] Ⅳ Ⅱ

[0058]

[0059]Ⅵ Ⅲ

[0060]

[0061] Ⅱ Ⅲ

[0062] Ⅶ Ⅷ

[0063]

[0064] Ⅰ

[0065] Compound V and compound VI can be purchased directly or synthesized with reference to existing literature reports.

[0066] Synthesis of Compound IV:

[0067] Add 762 grams of compound V (2.00mol) and 2,500 milliliters of butyl acetate into the reaction flask, under stirring, cool to 10°C, add 152 grams of sodium borohydride (4.00mol) in batches, continue stirring at this temperature for 30 minutes, and then Lower to 0...

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Abstract

The invention discloses a preparation method of rosuvastatin calcium. The method comprises the following steps of: synthesizing an important intermediate, i.e., [4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-mesyl amino)pyrimidine-5-radical]methanol (compound IV); and preparing the rosuvastatin calcium (compound I). The method has the advantages of readily available raw materials, high stereoselectivity, high yield and suitability for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a preparation method of rosuvastatin calcium. Background technique [0002] Rosuvastatin calcium (Rosuvastatin calcium), the chemical name is (+)-(3R,5S)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl- N-methylsulfonylamino)pyrimidin-5-yl]-3,5-dihydroxy-6(E)-calcium heptenoate was developed by Shionogi (Osaka Shionogi Company) in Japan and transferred to the company in April 1998 British AstraZeneca company, in August 2003 was approved by the US FDA for listing. Rosuvastatin calcium can reduce elevated LDL-cholesterol, total cholesterol, triglyceride and ApoB, and increase HDL-cholesterol. Judging from the existing clinical verification results and the comparison of similar products, rosuvastatin calcium has the advantages of high efficiency, low toxicity, and small side effects. Drugs, the market prospect is very good. [0003] [0004] I [0005] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/42
Inventor 林开朝
Owner 湖南欧亚药业有限公司
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