| 摘要 |
The method for preparing N-(2-halopropionyl)-proline derivatives of formula (I), used as an inhibitor against angiotensin and antihypertensive agent, is presented. Thus, 4.1g of proline benzylester is dissolved in 20ml of chloroform and the above mixture is cooled in water-ice bath. Then, 1.7g 2-bromopropionyl chloride is dropped slowly in 15ml of chloroform containing proline ester. The above mixture is stirred at 25≦̸C C for 2 hrs and the obtained chloroform layer is washed with water three times, evaporated and purified. In (I), R1 is H, C1-10 lower alkyl or aryl; R2 and R3 are each H, C1-4 alkyl, aryl, amino or cyano; X is Cl, Br or I.
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