Synthesis and cytotoxic evaluation for some new 2,5-disubstituted pyrimidine derivatives for anticancer activity
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An efficient synthetic approach for 2,5-disubstituted pyrimidines has been reported. The desired 2,5-substituted pyrimidines were obtained by Suzuki coupling of 2-substituted benzyloxy-5-bromopyrimidines with various aryl boronic acids in the presence catalytic amount of PdCl2(PPh3)2 with 0.5 M aqueous Na2CO3 in water at 80 °C. 2-Benzyloxy-5-bromopyrimidines were synthesized, in turn by the reaction of 2-chloro-5-bromopyrimidine with substituted benzyl alcohols in the presence of Cs2CO3 in CH3CN:DMF (1:1). Some of the 2,5-disubstituted pyrimidines have shown moderate in vitro cytotoxic activity against HeLa cell line.
Keywords2-Chloro-5-bromopyrimidine Cesium carbonate Green synthesis HeLa cell line PdCl2(PPh3)2
The authors are highly thankful to Department of Chemistry, Acharya Nagarjuna University, Nagarjunanagar, Guntur, and Andhra Pradesh, India for constant encouragement.
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