Method for preparing atorvastatin calcium intermediate

A technology of atorvastatin calcium and intermediates, which is applied in the field of pharmaceutical organic synthesis, can solve the problems of reduced condensation reaction yield, poor solubility, heterogeneous system, etc. rate increase effect
CN102766136AInactive Publication Date: 2012-11-07ZHEJIANG HONGYUAN PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ZHEJIANG HONGYUAN PHARMA
Publication Date
2012-11-07
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a method for preparing atorvastatin calcium intermediate and belongs to the technical field of drug organic synthesis. The method includes the following steps: 1) a compound A and a compound B are mixed according to weight ratio of 1:1.5-2.0; 2) tetrahydrofuran and n-butyl ether are added in the material obtained in the step 1) according to weight ratio of the compound A, the tetrahydrofuran and the n-butyl ether as 1:6-10:6-10 and stirred evenly; 3) trimethylacetic acid occupying 15-25% of the weight of the compound A is added in the material obtained in the step 2), and backflow reaction is performed at the temperature of 94-96 DEG C to obtain a compound C; 4) concentration of the compound C is detected in a reaction process, triethylamine or tert-butylamine is added equivalently in two batches, total addition of the triethylamine is 7-13% of the weight of the compound A, and total addition of the tert-butylamine is 12.8-24% of the weight of the compound A. The method for preparing the atorvastatin calcium intermediate can improve conversion rate of products and reduce pollutant generated in reaction remarkably.
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Description

technical field

[0001] The invention belongs to the technical field of pharmaceutical organic synthesis, and in particular relates to a method for preparing an atorvastatin calcium intermediate. Background technique

[0002] Atorvastatin Calcium is a drug originally developed by the pharmaceutical giant Pfizer. This drug is a new type of HMG-CoA reductase inhibitor, which can effectively reduce blood lipids. Favored by people, so the prospect of the drug is extremely broad.

[0003] The synthetic route of the key intermediate compound C of atorvastatin calcium in the prior art is as follows:

[0004]

[0005] Wherein the chemical name of compound A is: (4R, Cis)-6-aminoethyl-2,2-dimethyl-1,3-dioxolane-tert-butyl acetate; the chemical name of compound B is: 4 -Fluoro-a-(2-methyl-1-oxypropyl)-γ-oxygen-N,β-diphenyl-benzenebutyramide; Compound C chemical name: (4R-cis)-6-[2 -[2-(4-fluorophenyl)-5-(1-isopropyl)-3-phenyl-4-[(aniline)carbonyl]-1H-pyrrol-1-yl]ethyl]-2, tert-b...

Claims

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