Rhodium-catalyzed [2 + 2 + 2] cycloadditions, sulfonyl phthalide annulations and nitroalkene reactions have been employed for the synthesis of 56 quinone-based compounds. These were evaluated against Trypanosoma cruzi, the parasite that causes Chagas disease. The reactions described here are part of a program that aims to utilize modern, versatile and efficient synthetic methods for the one or two step preparation of trypanocidal compounds. We have identified 9 compounds with potent activity against the parasite; 3 of these were 30-fold more potent than benznidazole (Bz), a drug used for the treatment of Chagas disease. This article provides a comprehensive outline of reactions involving over 120 compounds aimed at the discovery of new quinone-based frameworks with activity against T. cruzi.

铑催化的[2 + 2 + 2]环加成反应，磺酰苯酞环化反应和硝基烯烃反应已用于合成56种基于醌的化合物。他们针对引起锥虫病的寄生虫克氏锥虫进行了评估。此处描述的反应是该计划的一部分，该计划旨在利用现代，通用和高效的合成方法来一步一步制备锥虫杀菌化合物。我们已经鉴定出9种对寄生虫具有有效活性的化合物。其中3种药物的功效比苯甲硝唑（Bz）（用于治疗南美锥虫病的药物）高30倍。本文提供了涉及120多种化合物的反应的全面概述，旨在发现新的基于醌的骨架，该骨架具有抗T. cruzi的活性。。