摘要
研究了雷米普利中间体2-苯甲酰氨基-3(2-氧代环戊基)丙酸乙酯的合成工艺,以苯甲酰胺和丙酮酸乙酯为原料,在催化剂作用下进行脱水缩合,得到2-苯甲酰氨基丙烯酸乙酯;再与烯胺进行加成反应,得到2-苯甲酰氨基-3(2-氧代环戊基)丙酸乙酯。分别考察了缩合反应中反应溶剂、催化剂、阻聚剂等条件对反应收率的影响。结果表明,以甲苯作溶剂,苯甲酰胺、丙酮酸乙酯、对甲苯磺酸、对羟基苯甲醚的摩尔比为1.0:0.9:0.1:0.001,总收率达到43.2%以上。该工艺具有收率较高、工艺简单、环境友好等特点,具有较好的产业化应用前景。
The paper studied the synthesis process of the intermediate of Ramipril, ethyl 2-benzamido-3-(2-oxocyclopentyl)propanoate. Firstly, 2-benzoyl amino ethyl acrylate was synthesized from benzamide and ethyl pyruvate via dehydration condensation reaction under the action of catalyst. Then, ethyl 2-benzamido-3-(2-oxocyclopentyl)propanoate was obtained via addition reaction with enamine. The effect of solvent, catalyst, inhibitor and other conditions in condensation reaction on the reaction yield were investigated respectively. Results showed that when toluene as solvent, mole ratio of benzamide, ethyl pyruvate, p-toluene sulfonic acid and p-hydroxy benzoic ether was 1.0:0.9:0.1:0.001, the total yield reached above 43.2%. The process had better prospect for industrial application due to its advantages of good yield, simple process, and environmental protection.
出处
《化工生产与技术》
CAS
2015年第3期12-14,8,共3页
Chemical Production and Technology