Method for obtaining S-(-)-amlodipine in splitting manner

A technology of amlodipine and dichloromethane, which is applied in the field of optical separation to obtain S--amlodipine, can solve problems such as pollution, surplus, and difficulty in reaching clinical medical standards, and achieve simple preparation process and shortened reaction time Effect
CN101654429AActive Publication Date: 2010-02-24JIANGXI SHIMEI PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
JIANGXI SHIMEI PHARM CO LTD
Publication Date
2010-02-24

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Abstract

The invention relates to a method for obtaining S-(-)-amlodipine in a splitting manner. The method comprises the following steps: dissolving racemic amlodipine and D-tartaric acid into a mixed cosolvent containg dimethylsulfoxide and urea to carry out a complex reaction, carrying out alkaline treatment, solvent-out crystallization and the like on the S-(-)-amlodipine, the D-tartaric acid and the urea complexes solid sedimentation obtained after the complex reaction is finished, and then obtaining S-(-)-amlodipine pure crystal. The method introduces the other chiral auxiliary reagent-urea in the prior dimethylsulfoxide solution, thus the racemic amlodipine can better react with a splitting agent D-tartaric acid in the cosolvent containing the dimethylsulfoxide and urea, the reaction time islargely shortened, and the reaction does not have special requirements on the water content of the used solvent; the enantiomeric purity of the obtained levamlodipine is over than 99% and the rate ofrecovery is over than 80%. The method can be applied to preparing the intermediate of other chiral medicaments basically meeting the standard of the medical industry, is simple and provides a betterprospect for the preparation of various agents by the amlodipine single enantiomer.
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Description

technical field

[0001] The invention relates to a method for obtaining S-(-)-amlodipine by optical resolution, which belongs to the downstream separation field of medicinal chemistry. Background technique

[0002] Amlodipine (Amlodipine), trade name Norvasc, is a kind of calcium antagonist developed and listed by Pfizer Company of the United States, because of its remarkable curative effect, gentle onset of effect, long drug effect time (with 24h long-acting effect) and patient's It is well tolerated and widely used clinically. As a third-generation calcium antagonist, amlodipine effectively overcomes the shortcomings of the second-generation calcium antagonists, such as unstable blood pressure reduction and large adverse reactions, and has been recognized as a safe and effective drug by the US FDA.

[0003] The chemical structure of amlodipine is shown below:

[0004]

[0005] Amlodipine

[0006] Since its molecular structure contains a chiral carbon atom, it has a pa...

Claims

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