【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。更多还原

【Abstract】 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.更多还原