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 PdCl 2 (PPh 3 ) 2 with 0.5 M aqueous Na 2 CO 3 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 Cs 2 CO 3 in CH 3 CN:DMF (1:1). Some of the 2,5-disubstituted pyrimidines have shown moderate in vitro cytotoxic activity against HeLa cell line.
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