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.