Without employing any base and organic solvent, an economical, practical and eco-friendly protocol has been developed for the ultrasound accelerated one-pot synthesis of various functionalized 2-sulfonylquinolines from easily accessible starting materials in water under open-air conditions.

Without using any base and organic solvent, an environmentally benign methodology was developed for the aqueous synthesis of various functionalized quinolin-2(1H)ones at ambient temperature. The developed protocol has a wide substrate scope, excellent to quantitative yields, short reaction time (1−8 min), operational simplicity, reusable reaction medium and avoids further chromatographic purification. More importantly, this methodology is markedly greener than the traditional routes with an E-factor of 1.6 and eco-scale score of 89.5.

A copper-catalyzed annulation of 3-aryl-2H-azirines with 2-naphthols has been developed for the rapid assembly of C-3-naphthol-substituted benzo­[e]­indoles in one pot. This cascade reaction was realized through dearomatic nucleophilic ring opening of azirine, intramolecular cyclization, and oxidative cross-dehydrogenative coupling to furnish the important unreported π-expanded naphthol/benzo­[e]­indole biaryls.

Selectfluor, 1-chloromethyl-4-fluoro-1,4-diazoniabicyclo-[2.2.2] octane bis(tetrafluoroborate), is among the most popular fluorinating reagents owning to its commercially availability and non-hygroscopic property. The discovery and understanding of new reactivities of selectfluor are thus important for reaction design and optimization when this popular reagent is employed. It has been found that selectfluor could selectively remove Boc group from doubly protected amines in acetonitrile. This deprotection could be of interest when compared to other reported methods, not only because selectfluor is a solid and easy-to-handle, but also because the reaction is mild, operationally simple and chemoselective. The potential usefulness of this method is demonstrated by the deprotection of a series of protected amino acids and a one-step synthesis of pharmaceutically important purine derivative. The NMR experiments conducted in CD 3 CN explain why stoichiometric amount of selectfluor is needed for a successful reaction.