Frantz Doug E, Morency Louis, Soheili Arash, Murry Jerry A, Grabowski Edward J J, Tillyer Richard D
Department of Process Research, Merck Research Laboratories, Merck & Co., 466 Devon Park Drive, Wayne, PA 19087, USA.
Org Lett. 2004 Mar 4;6(5):843-6. doi: 10.1021/ol0498803.
A one-pot synthesis of substituted imidazoles is described. The cornerstone of this methodology involves the thiazolium-catalyzed addition of an aldehyde to an acyl imine to generate the corresponding alpha-ketoamide in situ followed by ring closure to the imidazole in a one-pot sequence. The extension of this methodology to the one-pot synthesis of substituted oxazoles and thiazoles is also described. [reaction: see text]
本文描述了一种一锅法合成取代咪唑的方法。该方法的核心是噻唑鎓催化醛与酰基亚胺加成,原位生成相应的α-酮酰胺,随后通过一锅法序列闭环生成咪唑。本文还描述了该方法扩展至一锅法合成取代恶唑和噻唑的情况。[反应:见正文]