Tetrahedron template

Benzodiazepines are very useful scaffolds in medicinal chemistry and they have been successfully exploited in the discovery and optimization of several bioactive compounds. 2 With their good druglike properties and ability to provide potent and selective ligands for different biological targets, benzodiazepines are considered privileged structures. In addition to their well known anxiolytic, sedative and anticonvulsant activities, 1,4-benzodiazepine scaffolds can be found in a wide variety of bioactive molecules such as antitumor, antithrombotic, 13 anti-HIV, 15 and antimalarial agents. 17 The capacity of 1,4-benzodiazepinones to mimic different peptide secondary structures such as βand γ-turns offers attractive opportunities for the development of small molecule protein-ligands and protein-protein interaction inhibitors. 16, 18-24 For this reason, the development of new synthetic methodologies to access highly diversified benzodiazepinones and prepare libraries is of continuous interest.