Development of a general process for the synthesis of highly substituted imidazoles

Pure and Applied Chemistry - Tập 74 Số 8 - Trang 1349-1357 - 2002
Joseph Sisko1, Mark Mellinger1
1Synthetic Chemistry, GlaxoSmithKline, 709 Swedeland Road, P.O. Box 1539, UW2820, King of Prussia, PA 19406-0939, USA

Tóm tắt

Abstract Several highly substituted imidazoles have been under investigation at GlaxoSmithKline as potential therapies for the treatment of rheumatoid arthritis and have spawned the need for a general synthetic method for their preparation on a multikilogram scale. We describe herein the optimization of a general method for the preparation of aryl-substituted TosMIC reagents and the ease with which they undergo [3+2] cycloadditions with a host of imines, prepared in situ, to generate densely functionalized imidazoles with various substitution patterns in a completely regioselective manner.

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