Wolkenberg Scott E, Wisnoski David D, Leister William H, Wang Yi, Zhao Zhijian, Lindsley Craig W
Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck Research Laboratories, P.O. Box 4, West Point, Pennsylvania 19486, USA.
Org Lett. 2004 Apr 29;6(9):1453-6. doi: 10.1021/ol049682b.
[reaction: see text] A simple, high-yielding synthesis of 2,4,5-trisubstituted imidazoles from 1,2-diketones and aldehydes in the presence of NH(4)OAc is described. Under microwave irradiation, alkyl-, aryl-, and heteroaryl-substituted imidazoles are formed in yields ranging from 80 to 99%. Short syntheses of lepidiline B and trifenagrel illustrate the utility of this approach.
[反应：见正文] 描述了一种在醋酸铵存在下，由1,2 - 二酮和醛简单、高产率合成2,4,5 - 三取代咪唑的方法。在微波辐射下，可形成烷基、芳基和杂芳基取代的咪唑，产率在80%至99%之间。对鳞苯胺B和曲非那酯的简短合成说明了该方法的实用性。
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