2-alkoxycarbonyl-3-phenylpropionate derivant-synthesis and uses thereof of novel ace inhibitor

Abstract

An angiotensin converting enzyme (ACE) inhibitor is mainly used for treating diseases such as hypertension, congestive heart failure, myocardial infarction, renal dysfunction, etc. The existing medicines in the market comprise captopril, enalapril, benazepril, and the like, which have obvious adverse reactions such as severe dry cough, parageusia, proteinuria, hematuria, hypotension, and the like, and the medicines have some adverse reactions that threaten life such as acute thrombocytopenia, hyperkalemia, severe arrhythmia and renal failure. The invention relates to a technical scheme for chemosynthesis of a 2-alkoxycarbonyl-3-phenylpropionic acid ester derivative with the characteristic of the structural general formula I and provides a 2-alkoxycarbonyl-3-phenylpropionic acid ester derivative with the characteristic of the structural general formula I and the derivative is taken as an ACE inhibitor for treating diseases such as hypertension, congestive heart failure, myocardial infarction and renal dysfunction, and lowering blood sugar and blood lipid, etc. R1, R2, R3 and R4 are -H, C1-3-alkyl, C1-3-alkenylnyl, C1-3-alkoxy, aryloxy, arylalkoxyl, heterocycles, heteroarylalkyl, acyl, acyloxy, hydroxy C1-3-alkyl, hydroxy, amino, halogen, nitro, cyano, formyl, acylamino, C1-3-alkyamino, C1-3-alkoxycarbonylamino, C1-3-alkylcarbonylamino, C1-3-alkylsulfonyl and arylsulfonyl.

Description

technical field [0001] The present invention relates to the synthesis and application of novel ACE inhibitors. Specifically, the present invention relates to the synthesis of 2-alkoxycarbonyl-3-phenylpropionate derivatives and their application in the treatment of diseases such as hypertension. technical background [0002] ACE inhibitors are mainly used in the treatment of hypertension, congestive heart failure, myocardial infarction, renal dysfunction and other diseases. The drugs that have been marketed include: captopril, enalapril, berapril Lee (benazepril) and so on. Although these drugs have good clinical therapeutic effects, there are obvious adverse reactions of these drugs, among which severe dry cough, abnormal taste, proteinuria, hematuria and hypotension are the most common; there are also some adverse reactions that may be life-threatening Such as: acute thrombocytopenia, hyperkalemia, severe arrhythmia and renal failure. Therefore, it is very necessary to f...

AI Technical Summary

Problems solved by technology

Although these drugs have good clinical therapeutic effects, there are obvious adverse reactions of these drugs, among which severe dry cough, abnormal taste, proteinuria, hematuria and hypotension are the most common; there are also some adverse reactions that may be life-threatening Examples: acute thrombocytopenia, hyperkalemia, severe cardiac arrhythmias, and renal failure

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