A Novel Strategy for the Construction of Functionalized 1,5-Benzodiazepines via a Tandem Conjugated Addition/Cyclization Process.

A novel approach for the synthesis of functionalized 1,5-benzodiazepine is described. The protocol is triggered by a tandem conjugated addition/cyclization process from the readily available starting materials 1,2-phenylenediamine and ethyl propiolate. The products have secondary amino and ester groups, and a β-enamino ester, which can serve in further functionalizations to produce molecular diversity.