| 摘要 |
PURPOSE:The one-step reaction between 2-halo-3,3,3-trifluoropropene, a urea derivative and carbon monoxide is effected in the presence of a base and Pd catalyst to give the titled compound used as a drug with low-toxic carcinostatic and antiviral activity. CONSTITUTION:The reaction between 2-halo-3,3,3-trifluoropropene, a urea derivative of formula II (R<1>, R<2> are H, alkyl, aromatic radical) such as urea or methylurea carbon monoxide is carried out in the presence of a base such as triethylamine or pyridine and a palladium catalyst such as dichlorobis(triphenylphosphine)palladium, preferably in a solvent such as N,N-dimethylformamide, to give a 5-trifluoromethyldihydrouracyl derivative of formula III such as 5-trifluoromethyl-5,6-dihydrouracil. |
