A Study of the Synthesis of 5-Fluorouracil

Author: Hung-cheh Chiang(Institute of Chemistry College of Sciences)

Abstract：

5-Fluorouracil is one of the anticancer drugs in clinical use. After checking the documentation about synthetic methods and patents, we found two improved methods to be valid and economical. The synthetic methods are (1) Duschinsky method : To the potassium ethoxide in ether solution were added ethyl-fluoro-acetate and ethyl formate. The reaction mixture was allowed to react wity alkyl-thiourea salt to form 5-fluorouracil. After repetition of this method no product was obtained though 17.3% yield was reported. The improved method was to proceed the reaction in sodium methoxide toluene solution instead of ether solution, and it gave the tatal yield up to 22.7% (2) Kaes method: To the sodium methoxide in toluene solution were addid ethylfluoroacetate and methylformate. The reaction mixture was allowed to dehydrate with Guanidine to give 5-fluorouracil, with a total yield of 28.3% (doc. 28 -33%).

《Full Text》