Peter Dr Andres

A new synthesis of 5-trifluoromethyluracil

Abstract 5-Trifluoromethyluracil, an important intermediate for the preparation of the antiviral trifluridine, is obtained by chlorinating thymine to give the new 2,4-dichloro-5-trichloromethylpyrimidine. Reacting the latter with hydrogen fluoride yields the new 2, 4-difluoro-5-trifluoromethylpyrimidine, and hydrolysis with water gives 5-trifluoromethyluracil in high purity and good yield.

Synthese von α-Fluoracrylsäure und Derivaten

Zusammenfassung Three new routes to derivatives of α-fluoracrylic acid, including a laboratory synthesisand a large-scale method, are reported. The processes are (i) addition of elementaryfluorine to acrylic esters and subsequent elimination of HF; (ii) addition of difluorocarbeneto isopropenyl methyl ether, oxidation via ring opening and dehalogenation; and (iii)‘nitrofluorination’ of 2,3-dichloropropene, hydrolysis and dechlorination.