Studies on Synthesis of Novel Triazolalkyl Tagged Trifluoromethyl Substituted Pyrimidine Derivatives and their Evaluation for Cytotoxic Activity

The 2-amino-6-trifluoromethyl-3H-pyrimidin-4-one 1 was propargylated to give two regioisomers 2, 3 in definite proportions. Both regioisomers 2 and 3 were independently reacted with alkyl, aryl or cycloalkyl substituted azides under Sharpless conditions and were obtained exclusively 1,4–disubstituted triazole tagged trifluoromethyl substituted pyrimidine derivatives 4 and 5 respectively. All the final products were evaluated for cytotoxic activity against four cancer cell lines and promising compounds were identified.