An efficient synthesis of 1,4-benzodiazepin-2-ones is described by condensation between 2-aminobenzophenone and Boc-protected amino acids via microwave-assisted irradiation. This produces higher yields in shorter reaction times than with traditional methods. The antiplasmodial activity of the corresponding ferrocenyl benzodiazepines was evaluated in vitro against Plasmodium falciparum F32 (chloroquine-sensitive) and FCB1 and K1 (chloroquine-resistant) strains and gabonese clinical isolates.
描述了一种高效合成1,4-苯二氮䓬-2-酮的方法,该方法通过微波辅助照射使2-
氨基苯基酮与Boc保护的
氨基酸缩合。这种方法相比传统方法在较短的反应时间内产生更高的产率。相应的
铁杂环苯二氮䓬的抗疟活性在体外对抗疟原虫福32株(对
氯喹敏感)及FCB1和K1(对
氯喹耐药)株,以及加蓬临床分离株进行了评估。