Method for preparing amlodipine

A technology of amlodipine and ground level meter, which is applied in the field of medicine and chemical industry, can solve the problems of high boiling point, easy explosion, disproportionation reaction, etc., and achieve the effects of good solvent stability, low cost and low toxicity
CN101544597AActive Publication Date: 2009-09-30北京天衡药物研究院有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
北京天衡药物研究院有限公司
Publication Date
2009-09-30

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Abstract

The present invention relates to a method for preparing a novel S-(-)-amlodipine, and especially to a novel method for preparing S-(-)-amlodipine through the resolution of racemic amlodipine. The N,N-dimethylformamide (DMF) is used as a dissolvent. The L-(+)-tartaric acid is used as a resolving agent. Not only can the excellent resolving effect be obtained, but also the cost is low and safety is excellent.
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Description

technical field

[0001] The present invention relates to a new preparation method of S-(-)-amlodipine, in particular to a new method for preparing S-(-)-amlodipine by splitting racemic amlodipine, which belongs to medicine chemical industry. Background technique

[0002] Amlodipine is a calcium antagonist clinically used in the treatment of hypertension and stable angina. According to Arrowsmiith, J.E.; etal.J.Med.chem (1956) 29; 1696-1702 report, its pharmacologically active main ingredient is S-(-)-amlodipine, and its calcium ion antagonistic activity is about R-(+) -1000 times of amlodipine, 2 times of racemate; Young, J.W., WO93 / 10779 reported that using S-(-)-amlodipine can reduce acral edema, headache and dizziness compared to using racemic amlodipine and other side effects. Therefore, the use of S-(-)-amlodipine to treat hypertension and stable angina pectoris has a good market prospect. The chemical structural formula of amlodipine is as follows:

[0003] [0...

Claims

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