Late stage C―H activation of a privileged scaffold; synthesis of a library of benzodiazepines

A library of over twenty 5-(2-arylphenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-ones has been formed by a microwave-mediated late-stage palladium-catalysed arylation of 1,4-benzodiazepines using diaryliodonium salts. This can also be applied to nordazepam (7-chloro-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one), the active metabolite of diazepam, and subsequent N-alkylation and/or H/D exchange allows further diversification towards elaborated pharmaceuticals and their 3,3'-deuterated analogues

Four-membered ring systems

Capítulo 4, pp 85-107The search in the field of four-membered heterocycles, where a non-carbon atom is part of the ring, has been actively pursued in 2009 within Organic Chemistry, Inorganic Chemistry, Medicinal Chemistry, and Material Science. In particular, the synthesis and chemistry of oxygen- and nitrogen-containing heterocycles dominate the field in terms of the number of publications. It should be clearly stated that a comprehensive description of all the aspects of the vast research area of four-membered heterocyclic chemistry can not be fully covered in this book chapter. Instead, the present overview presents a personal selection of the topics which we believe are the more relevant.Peer reviewe