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

作者：Su Zhaoming; Peng Lingling; Melander Christian^*

来源：Tetrahedron Letters, 2012, 53(10): 1204-1206.

DOI：10.1016/j.tetlet.2011.12.090

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

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.

• 出版日期2012-3-7