马来酸依那普利的合成与表征

Synthesis and Chafaracterization of Enalapril Maleate

研究了由3-苯甲酰丙烯酸乙酯和L-丙氨酸苄酯对甲苯磺酸盐缩合并用Pd/C催化加氢还原合成N-[(S)-1-(乙氧羰基)-3-苯丙基]-L-丙氨酸,再用双(三氯甲基)碳酸酯进行酰氯化,最后与L-脯氨酸直接缩合成盐获得马来酸依那普利的新方法。产品总收率为50%。对产品结构进行了表征。

Enalapril Maleate was prepared from N - [（S） - 1 - （ethoxycarbonyl） - 3 - phenylpropyl] - L- alanine and L - proline by through chloroformylation use BTC. The intermediate was synthesized from Ethyl - 3 - benzoyl acrylate and L - Phenylalanine benzyl esterp - toluenesulfonate salt. Varied factors which affected the reaction were studied. The overall yieldof the product is 50 %.