Polycyclic fused quinazolinones with anti‐malarial activity were synthesized through tert‐butyl hydroperoxide (TBHP)‐mediated oxidative decarboxylative cyclization between commercially available isatins and cyclic amines in one step. The reaction proceeds 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 approach to Rutaecarpine in good yield.

中文翻译：

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TBHP介导的水中氧化脱羧环化：直接和可持续获得抗疟疾多环融合喹唑啉酮和芸苔芸香碱

第一步，通过叔丁基氢过氧化物（TBHP）介导的氧化性脱羧环化反应合成具有抗疟疾活性的多环稠合喹唑啉酮。该反应可在水中顺利进行，而无需额外的过渡金属催化剂，酸和碱。对新合成的产品进行了评估，显示出对氯喹药物敏感性恶性疟原虫3D7菌株具有中等至良好的抗疟疾活性。另外，该方法还提供了直接的方法以高产率生产鲁他卡平。