A concise synthesis of pyrrole-based drug candidates from α-hydroxyketones, 3-oxobutanenitrile, and anilines

A simple and concise three-component synthesis of a key pyrrole framework was developed from the reaction between α-hydroxyketones, oxoacetonitriles, and anilines. The synthesis was used to obtain several pyrrole-based drug candidates, including COX-2 selective NSAID, antituberculosis lead candidates BM212, BM521, and BM533, as well as several analogues. This route has potential to obtain diverse libraries of these pyrrole candidates in a concise manner to develop optimum lead compounds.Nanyang Technological UniversityPublished versionThis research was funded by the College of Engineering (Startup Grant), Nanyang Technological University, Singapore, and by the United Arab Emirates University (UAEU), Al-Ain (Grant no.G00003918)