A method for preparing atorvastatin key intermediate l1 by a solvent-free method

An atorvastatin, solvent-free technology, applied in the field of pharmaceutical chemical synthesis, can solve the problems of complex post-processing, difficult solvent recovery, long reaction time, etc., and achieve the effect of shortening reaction time, short reaction time and high conversion rate
CN110372677BInactive Publication Date: 2021-01-05ZHEJIANG HAISEN PHARMACY CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG HAISEN PHARMACY CO LTD
Publication Date
2021-01-05
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a novel method for preparing an atorvastatin key intermediate L1 through a solvent-free method and belongs to the technical field of drug chemical synthesis. The novel method comprises the following steps that M4 and A9 are taken as raw materials, under the effects of a phase transfer catalyst and an acid catalyst, constant-temperature stirring melting reaction is directlyconducted for 5-7 hours under the solvent-free condition, the reaction temperature is 80-140 DEG C, water distribution is conducted in the reaction process, after reaction is completed, cooling is conducted, then recrystallization is conducted, and thus the atorvastatin key intermediate L1 is obtained. According to the novel method, the phase transfer catalyst and the acid catalyst are adopted, aparent nucleus M4 and a chiral side chain A9 are subjected to stirring melting reaction under the solvent-free condition, after reaction, recrystallization is conducted directly through ethyl alcohol / water, and thus L1 is obtained; and as for the process, the reaction time can be shortened to be 5 h, the conversion rate can reach up to 90%, operation and aftertreatment are easy, no mixed solvent is recovered, pollution is reduced remarkably, and the method is suitable for amplification production.
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Description

technical field

[0001] The invention relates to the technical field of chemical synthesis of medicines, in particular to a method for preparing atorvastatin key intermediate L1 by a solvent-free method. Background technique

[0002] Atorvastatin is a statin hypolipidemic drug jointly developed by WarnerLambert Company and Pfizer Company of the United States. It can strongly inhibit the activity of hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase. It is a potent HMG-CoA reductase inhibitor, which can significantly reduce the content of total cholesterol and low-density lipoprotein cholesterol. It has the characteristics of strong lipid-lowering effect, high safety, and less toxic and side effects. Because atorvastatin is the world's first drug with a sales volume exceeding 10 billion U.S. dollars, it has a very broad application prospect, so it is favored by people, and the huge economic benefits stimulate researchers to continuously improve and enhance its technological ...

Claims

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