Yin Xianglin, Mohammad Haroon, Eldesouky Hassan E, Abdelkhalek Ahmed, Seleem Mohamed N, Dai Mingji
Department of Chemistry and Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, USA.
Chem Commun (Camb). 2017 Jun 29;53(53):7238-7241. doi: 10.1039/c7cc02494k.
A novel and efficient palladium-catalyzed aminocarbonylative lactonization of amino propargylic alcohols has been developed to provide rapid access to various bicyclic lactones especially dihydropyrrole-fused furanones, which are novel structures and have not been explored in biological and medicinal settings. This method can also be used to access β-lactone products such as 16. Preliminary biological evaluations revealed that compounds 13h and 13s demonstrated promising activity against Clostridium difficile and compounds 13h, 13k, 13s, and 16b showed activity against several important fungal pathogens.
已开发出一种新颖且高效的钯催化氨基炔丙醇的氨羰基化内酯化反应，可快速合成各种双环内酯，特别是二氢吡咯并稠合呋喃酮，这些都是新颖的结构，尚未在生物学和医学领域得到探索。该方法还可用于制备β-内酯产物，如16。初步生物学评估显示，化合物13h和13s对艰难梭菌表现出有前景的活性，化合物13h、13k、13s和16b对几种重要的真菌病原体具有活性。
