从 α-羟基酮、3-氧代丁腈和苯胺出发简明合成吡咯类药物候选物。
A Concise Synthesis of Pyrrole-Based Drug Candidates from α-Hydroxyketones, 3-Oxobutanenitrile, and Anilines.
机构信息
School of Chemistry, Chemical Engineering and Biotechnology, Nanyang Technological University, 62 Nanyang Drive, N1.2-B1-14, Singapore 637459, Singapore.
Department of Chemistry, Faculty of Science, Institut Teknologi Sepuluh Nopember, Sukolilo, Surabaya 60111, Indonesia.
出版信息
Molecules. 2023 Jan 28;28(3):1265. doi: 10.3390/molecules28031265.
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.
从α-羟基酮、氧代乙腈和苯胺之间的反应出发，开发了一种简单而简洁的三组分合成关键吡咯骨架的方法。该合成方法用于获得几种基于吡咯的药物候选物，包括 COX-2 选择性 NSAID、抗结核先导候选物 BM212、BM521 和 BM533 以及几种类似物。这条路线有可能以简洁的方式获得这些吡咯候选物的各种文库，从而开发出最佳的先导化合物。
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