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.
Keywords: Alkylation, Propargyl bromide, 3H-pyrimidin-4-one, Regioisomers, Sharpless conditions, Triazoles.
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