Studies on Synthesis of Novel Triazolalkyl Tagged Trifluoromethyl Substituted Pyrimidine Derivatives and their Evaluation for Cytotoxic Activity
Gannarapu Malla Reddy,
Royya Naresh Kumar,
Anugu Chandrashekar Reddy,
Loka Reddy Velatooru,
Janapala Venkateswara Rao,
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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