Construction of the 1,5-Benzodiazepine Skeleton from o-Phenylendiamine and Propargylic Alcohols via a Domino Gold-Catalyzed Hydroamination/Cyclization Process

The gold-catalyzed reaction of o-phenylenciiamine with propargylic alcohols affords 1,5-bentodiazepines bearing different substituents on the 2 and 4 positions. The method allows even for the selective preparation of 4 substituted 1,5-benzodiazepine derivatives.