5-Fluorouracil(5-FU) was an antimetabolite of the pyrimidine analogue type,which was frequently used for treating colorectal,gastric tract,and liver carcinomas etc.However,the clinical applications of 5-FU were greatl...5-Fluorouracil(5-FU) was an antimetabolite of the pyrimidine analogue type,which was frequently used for treating colorectal,gastric tract,and liver carcinomas etc.However,the clinical applications of 5-FU were greatly limited by its myelosuppression,and strong intestinal toxicity.Consequently,numerous research efforts had focused on the discovery of suitable carrier-linked prodrugs with high efficiency and low toxicity.In order to decline the toxicity of 5-FU,we synthesized 2-(5-fluorouracil-1-yl-acetamido) acetic acid by liquid coupling reaction with 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride(EDC·HCl) and 1-hydroxybenzotriazole(HOBt) as a coupling reagent.And the structures of the synthesized compounds were assigned by 1H NMR,13C NMR,mass spectrometry,and infrared spectroscopy,etc.展开更多
文摘5-Fluorouracil(5-FU) was an antimetabolite of the pyrimidine analogue type,which was frequently used for treating colorectal,gastric tract,and liver carcinomas etc.However,the clinical applications of 5-FU were greatly limited by its myelosuppression,and strong intestinal toxicity.Consequently,numerous research efforts had focused on the discovery of suitable carrier-linked prodrugs with high efficiency and low toxicity.In order to decline the toxicity of 5-FU,we synthesized 2-(5-fluorouracil-1-yl-acetamido) acetic acid by liquid coupling reaction with 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride(EDC·HCl) and 1-hydroxybenzotriazole(HOBt) as a coupling reagent.And the structures of the synthesized compounds were assigned by 1H NMR,13C NMR,mass spectrometry,and infrared spectroscopy,etc.
