达比加群酯的合成工艺改进  

Study on the Synthesis of Dabigatran Etexilate

作　　者：孟洪光 焦淑清[1] 张立宇[1] 吴连贺 乔越[1] 

机构地区：[1]佳木斯大学药学院,黑龙江佳木斯154007

出　　处：《精细化工中间体》2016年第3期32-34,共3页Fine Chemical Intermediates

基　　金：佳木斯大学研究生科技创新项目(LZR2015_023)

摘　　要：以3-[(3-氨基-4-甲胺基苯甲酰基)(吡啶-2-基)-氨基]丙酸乙酯和N-(4-氰基苯基)氨基乙酸为起始原料,经酰胺化、环合、醇解、胺解和酰化等制得达比加群酯,总收率约68.8%。该工艺操作简单,收率高,具有工业化生产前景。The dabigatran etexilate was synthesized using 3-[（3-amino-4-methylaminobenzoyl）pyridin-2-ylamino] ethyl propionate and N-（4-cyanophenyl）-glycine as the starting materials through a series of reactions including amidation, cyclization, alcoholysis, aminolysis and acylation with an overall yield of about 68.8%. This synthetic route for dabigatran etexilate has the advantages of simple operation and high yield and is suitable for industrial production.

关 键 词：3-[(3-氨基-4-甲胺基苯甲酰基)(吡啶-2-基)-氨基]丙酸乙酯 N-(4-氰基苯基)氨基乙酸 达比加群酯 血栓栓塞 

分 类 号：R973.2[医药卫生—药品]