Efficient synthesis of imidazole-fused benzodiazepines using palladium-catalyzed intramolecular C-N bond formation reaction

Abstract

An efficient three-step synthetic route to imidazole-fused benzodiazepines from imidazole-2-carbaldehyde is described. Application of intramolecular Buchwald-Hartwig cycloamination reaction in the final step is shown to be a convenient method for the synthesis of fused seven-membered diazacycles. The reactions proceeded smoothly with both aliphatic and aromatic amines. © Georg Thieme Verlag Stuttgart · New York.