We describe the synthesis of new diaryl substituted diazabicyclo[3.2.1]octanes from diazepanes which were prepared by the reduction of diazepanones. The formation of the bicyclic system was optimized by microwave irradiation and the structures of the new compounds were established by single crystal structure analysis and NMR spectroscopy. All new compounds were tested for their potencies against Plasmodium falciparum K1 and Trypanosoma b. rhodesiense, the causative organisms of malaria tropica and the East African form of sleeping sickness.
我们描述了从二氮杂环庚烷合成新的二芳基取代的二氮杂双环[3.2.1]辛烷的过程,这些辛烷是通过还原二氮杂环庚酮制备的。通过微波辐照优化了双环体系的形成,并通过单晶结构分析和核磁共振光谱确定了新化合物的结构。测试了所有新化合物对恶性疟原虫 K1 和罗得西亚锥虫的药效,恶性疟原虫 K1 和罗得西亚锥虫是热带疟疾和东非昏睡病的病原体。