No abstract

An efficient and convenient Rh(III)-catalyzed double aryl C(sp2)−H bond and N−H activation and annulation reaction is reported for the synthesis of indolo[2,1-a]isoquinolines in the presence of the Cu(OAc) 2 oxidant under heating conditions. Distinct from previous works with other arylamine donors, one molecule of 1,3-diarylurea can serve as a precursor of two molecules of arylamine in the reaction with diaryl-substituted alkynes.

Nonsymmetrical malonamides are often found in pharmacologically relevant molecules. A flexible and atom-economical method is developed for efficient preparation of nonsymmetrical malonamides from commercial or readily available isocyanates and β-ketoamides....