4.4 Article

A modular approach to the synthesis of 1,4,5-substituted-2-aminoimidazoles

Journal

TETRAHEDRON LETTERS
Volume 53, Issue 10, Pages 1204-1206

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2011.12.090

Keywords

N-H insertion; 2-Aminoimidazole; Antibiotic; Polysubstitution; Heterocycle

Funding

  1. DOD DMRDP [W81XWH-11-2-0115]

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Diversified 1,4,5-substituted-2-aminoimidazoles were rapidly assembled via sequential N-H insertion and Grignard addition to alpha-diazoesters. Lead compounds were identified as antibiotics against Gram-positive bacteria with an MIC value as low as 2 mu g/mL. (C) 2011 Elsevier Ltd. All rights reserved.

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