Hypervalent iodine(III) in direct oxidative amination of arenes with heteroaromatic amines

A novel, mild, and practical method of amination of simple nonfunctionalized arenes under metal free conditions has been developed. The approach allows coupling of electron-rich arenes with amino derivatives of electron-deficient heterocycles providing rapid access to scaffolds of bioactive compounds and is based on the application of the hypervalent iodine­(III) reagent as an oxidant. Regioselective functionalization of C–H bonds of arenes by the formation of C–N bonds under organocatalytic conditions was demonstrated

Synthesis and biological investigation of 1,2,4-triazolo[4,3-a]azines as potential HSF1 inductors

Derivatives of fused 1,2,4-triazines containing heterocyclic and metallocene fragments were obtained by one-pot oxidative cyclization of heterocyclic hydrazones in the presence of hypervalent iodine(III) reagents. For 1,2,4-triazolo[4,3-a]azines, the ability to activate HSF1 was investigated. The obtained compounds were shown to increase the degree of HSF1 activation. It was shown that the 1,2,4-triazines can be used to induce Hsp70 expression and decrease the extent of mutant HTT aggregate formation

Enantiomerically enriched 1,2-P,N-bidentate ferrocenyl ligands for 1,3-dipolar cycloaddition and transfer hydrogenation reactions

Novel complexes of 1,2-P,N-bidentate ferrocenyl ligands with AgOAc or with [RuCl2(PPh3)3] as catalysts have been studied in asymmetric synthesis. The catalytic activity of these systems have been studied in [3+2]-cycloaddition of azomethine ylides with olefins and the asymmetric transfer hydrogenation of ketones