Process for producing 5-perfluoroalkyluracil derivatives

摘要

A novel process is provided for producing a 5-perfluoroalkyl-5,6-dihydrouracil represented by General Formula (1): (where R1 and R2 are independently hydrogen, methyl, or ethyl, and Rf is a perfluoroalkyl of 1 to 10 carbons). The process comprises reacting alpha -perfluoroalkylacrylic acid represented by General Formula (2): CH2=C(Rf)-COOH(2) with a urea derivative represented by General Formula (3): R1NHCONHR2(3) in the presence of acetic anhydride with formed acetic acid being removed out of the reaction system during the reaction. The alpha -perfluoroalkylacrylic acid may be added successively. A process for producing a 5-perfluoroalkyl-5-bromo-6-hydrouracil by General Formula (4) is also provided: (where R1, R2, and Rf are as defined above) wherein the reaction of a 5-perfluoroalkyl-5,6-dihydrouracil produced by the above process with bromine is conducted in water as the solvent. The process of the present invention can be industrially conducted safely and simply at a high yield.