利可君合成工艺的改进  

Process Improvement on Synthesis of Leucogen

作　　者：陆强[1] 王艳艳[2] 

机构地区：[1]江苏苏北人民医院,江苏扬州225001 [2]江苏联合职业技术学院连云港中医药分院,江苏连云港222006

出　　处：《食品与药品》2012年第2期110-112,共3页Food and Drug

摘　　要：目的改进利可君合成工艺。方法以胱氨酸、苯乙酸乙酯和甲酸乙酯为原料,以还原铁粉为催化剂合成L-半胱氨酸盐酸盐,以石油醚为溶剂在超声条件下合成α-甲酰基苯乙酸乙酯,两者以乙醇为溶剂环合反应制备利可君。结果 L-半胱氨酸盐酸盐收率99.51%,c-甲酰基苯乙酸乙酯反应时间4h,收率92.6%,利可君合成总收率75.3%。结论以胱氨酸为原料降低了合成成本,超声条件下合成α-甲酰基苯乙酸乙酯缩短了生产周期,收率提高9.2%,利可君总收率比化统工艺提高了22.5%～27.2%,以乙醇为溶剂环合,生产更安全环保。Objective To improve the synthesis process of leucogen. Methods With cystine, ethyl phenylacetate and ethyl formate as the material, L-cysteine hydrochtoride was synthesized with iron as catalyst. Ethyl α-formylphenylacetate was prepared with the solvent of benzene on the condition of ultrasonic. Leucogen was synthesized by the cyclization reaction of L-cysteine hydrochloride with ethyl α-formylphenylacetate in the solvent of alcohol. Results The yield of L-cysteine hydrochloride was 99.51%. The reaction time of ethyl α-formylphenylacetate was 4 h, and the yield was 92.6%. The total yield of leucogen was 75.3%. Conclusion The cost of synthesis can be decreased with the material of cystine. The reaction time of ethyl α-formylphenylacetate can be shortened and the yield can be increased by 9.2% on the condition of ultrasonic. The total yield of leucogen can be increased 22.5%427.2% with the manufacture process of more safety and environmental protection.

关 键 词：利可君 胱氨酸 苯乙酸乙酯 合成 改进 

分 类 号：R914.5[医药卫生—药物化学]