A Convenient Synthesis of the Orthogonally-Protected Benzodiazepine-2,5-Dione Scaffold

Abstract

We have identified the benzodiazepine-2,5-dione 4 as a convenient, orthogonally-protected template, suitable for parallel solid-phase chemistry. Scaffold 4 offers superior stability, compared to other, analogous benzodiazepine-2,5-diones, such as A. We describe a gram-scale synthesis of 4 in six steps and in 25% yield.