Method for synthesizing statins compounds

A technology of simvastatin and methylation, applied in the field of preparation of statin compounds
CN101190907AInactive Publication Date: 2008-06-04马群力 +1

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
马群力
Publication Date
2008-06-04
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a novel synthesis method of statin compounds, in particular to a preparation method of methylation reaction of Simvastatin (2,2-dimethylbutyric acid-8-((4R, 6R)-6-(2-((1s, 2s, 6R, 8S, 8aR)-1,2,6,7,8,8-a-hexahydro-8-hydroxy-2,6-dimethyl-1-naphthyl)ethyl))tetrahydrochysene-4-hydroxy-2H-pyran-2-ketone ester) and analogues thereof. The method consists of the reaction of Lovastatin amido disiloxane and methylating agent.
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Description

technical field

[0001] The invention relates to a method for preparing statin compounds, in particular to a method for synthesizing simvastatin. In the process of preparing simvastatin, lovastatin is used as a raw material, and lovastatin is formed by ring opening under the action of primary or secondary amines Amide; then use tert-butyl dimethyl chlorosilane and other protective agents such as hexaalkyl disiloxane to protect the hydroxyl to obtain lovastatin amide disiloxane. The present invention is to use this as raw material methylation reaction to form Simvastatin A new preparation method of statin amide disiloxane and simvastatin amide disiloxane deprotection under acid catalysis, hydrolysis under alkaline conditions to form simvastatin acid, and finally ring-closing lactonization to form simvastatin. The chemical name of simvastatin is: 2,2-dimethylbutyric acid-8-{(4R,6R)-6-(2-[(1s,2s,6R,,8S,8aR)-1,2,6 ,7,8,-a-hexahydro-8-hydroxy-2,6-dimethyl-1-naphthyl]ethyl)}tetrahyd...

Claims

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