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Polycyclic fused quinazolinones with anti-malarial activity were synthesized through tert-butyl hydro-peroxide(TBHP)-mediated oxidative decarboxylative cyclization between commercially available isatins and cyclic amines in one step.The reaction pro-ceeds smoothly in water without additional transition-metal catalyst,acid and base.The newly synthesized products were evaluated to exhibit moderate to good anti-malarial activity against chloroquine drug-sensitive Plasmodium falciparum 3D7 strain.Additionally,this method also provides direct ap-proach to Rutaecarpine in good yield.