Synthesis of substituted imidazoles via organocatalysis |
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| Authors: | Frantz Doug E Morency Louis Soheili Arash Murry Jerry A Grabowski Edward J J Tillyer Richard D |
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| Affiliation: | Department of Process Research, Merck Research Laboratories, Merck & Co., 466 Devon Park Drive, Wayne, PA 19087, USA. |
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| Abstract: | 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] |
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