Soh Chai Hoon, Chui Wai Keung, Lam Yulin
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore.
J Comb Chem. 2008 Jan-Feb;10(1):118-22. doi: 10.1021/cc700143n. Epub 2007 Dec 27.
A microwave-assisted protocol was developed for the construction of di- and monosubstituted 2-aminoimidazoles. The two-step reaction involves the synthesis of N-(1H-imidazol-2-yl)acetamides from readily available alpha-haloketones and N-acetylguanidine, followed by deacetylation. Significant rate enhancement was observed for both steps of the protocol, and the overall reaction time was shortened to 20 min compared to 48 h of the conventional procedures. A representative set of di- and monosubstituted 2-aminoimidazoles was prepared using commercially available parallel reactors.
开发了一种微波辅助方法用于构建二取代和单取代的2-氨基咪唑。该两步反应包括由易得的α-卤代酮和N-乙酰基胍合成N-(1H-咪唑-2-基)乙酰胺，然后进行脱乙酰化反应。该方法的两个步骤均观察到显著的速率提高，与传统方法的48小时相比，总反应时间缩短至20分钟。使用市售的平行反应器制备了一组具有代表性的二取代和单取代2-氨基咪唑。
