Synthesis of 4 H-Benzo[ e][ 1,3]oxazin-4-ones by a Carbonylation-Cyclization Domino Reaction of ortho-Halophenols and Cyanamide

Abstract

Invited for this month's cover are researchers from the Division of Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University (Sweden). The research interests in the group span areas such as enzyme inhibitors, new antibiotics, angiotensin II AT2R ligands, PET tracers, palladium catalysis, heterocycle synthesis, and the development of novel multicomponent reactions. In particular, sequential carbonylation and cyclization appeal to us as a convenient and straightforward synthetic route for the synthesis of heterocycles. The cover picture shows how carbon monoxide gas is diffused over a bridge, in the two-chamber system set-up used in this work, to take part in the catalytic cycle, and be incorporated into the heterocyclic core by a carbonylation/cyclization domino reaction to yield4H -benzo[e][1,3]oxazin-4-ones. For more details, see the full text of the Full Paper at 10.1002/open.201700130.