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A highly efficient approach to polysubstituted 2-amino­pyrroles containing a coumarin derivative unit at the 5-position of the pyrrole ring was developed via a novel multicomponent domino reaction of glyoxal monohydrate derivatives, anilines, coumarin derivatives, and malononitrile. This transformation proceeded via an α-amino­ketone as the key intermediate. [ABSTRACT FROM AUTHOR]

A divergentcascade annulation has been developed using readilyavailable vinyl azides and carbazates with a wide range of substituents.Vinyl azides were successfully applied as bifunctional partners toprepare aza-pyrimidinones via 6-ring closure with carbazates as wellas to construct polyfunctionalized imidazoles via 5-ring closure with N-substituted carbazates. The aza-heterocycles were obtainedwith high levels of chemoselectivity and excellent yields. [ABSTRACT FROM AUTHOR]

A tandem reaction of heterocyclic ketene aminals and 1,2-diaza-1,3-dienes was developed for the expedient synthesis of pyrimidopyrrolopyridazine derivatives. This process involved an intramolecular conjugate addition followed by CuCl2-catalyzed hydrazone formation. [ABSTRACT FROM AUTHOR]

A novel sequential [3+2] annulation reaction has been developed using prop-2-ynylsulfonium salts and hydrazonyl chlorides, affording a series of pyrazoles with functional motifs that can be post modified in the preparation of various drugs or drug candidates. Further transformation and gram-scale operations could also be achieved efficiently. [ABSTRACT FROM AUTHOR]