Preparation method of N-carboxyalkyl dipeptide type angiotensin converting enzyme inhibitor

A technology of carboxyalkyl dipeptide type and angiotensin, which is applied in chemical instruments and methods, dipeptide, cardiovascular system diseases, etc., can solve the problem of overdose, and achieve the effect of simple and efficient process
CN1429835AInactive Publication Date: 2003-07-16SHANGHAI INST OF PHARMA IND CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI INST OF PHARMA IND CO LTD
Publication Date
2003-07-16
Estimated Expiration
Not applicable · inactive patent
Patent Text Reader

Abstract

A process for preparing N-carboxyalkyl dipeptide type angiotensin converting enzyme (ACE) depressant (such as enalapril maleate, ramipril, etc) includes such steps as preparing N-carboxylic acid anhydride from bis (trichloromethyl) carbonate, and coupling with relative alpha-amino acid.
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Description

technical field

[0001] The invention relates to a preparation method of an angiotensin-converting enzyme (ACE) inhibitor of N-carboxyalkyl dipeptide structure type. Background technique

[0002] N-carboxyalkyl dipeptide structure type Angiotensin-converting enzyme (ACE) inhibitors are a class of safe and effective drugs for the treatment of hypertension and congestive heart failure, including enalapril maleate and lisinopril, which are best-selling in the world Drugs play an important role in cardiovascular drugs. Its structural general formula is as follows: where: R 1 =C 3 h 7 -; R 2 =CH 3 -; CF 3 CONH(CH 2 ) 3 CH 2 -; NH 2 (CH 2 ) 3 CH 2 -R 3 = H, C 2 h 5

[0003] Existing many patent literatures have reported the preparation method of this type of medicine at present, as: reports such as Jerry WSkiles (Organic Preparations and Procedures International, 1988,20 (2): 109-115) by first preparing N-carboxylic anhydride (N-CarboxyAnhydride, NCA), the...

Claims

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