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An efficient one-pot reaction of propargylamides, isocyanides, and water catalyzed by zinc was developed for the rapid construction of 2-oxazolines with a wide functional group tolerance. The methylene-3-oxazoline was proven to play a vitally important role to start the tandem cascade transformation through unfunctionalized alkynes with sequential nucleophilic addition approaches of isocyanide and water. Notably, with a slight alteration of the reaction temperature and the addition of one molecule of water, various β-amino amide derivatives were synthesized in good to excellent yields.

Reported herein is a unified strategy to generate difluoroalkyl radicals from readily prepared α-difluorinated gem-diols by single electron oxidation. Under microwave irradiation, a catalytic amoun...

Structurally unique 2,2-disubstituted indolin-3-ones with a quaternary carbon center have been constructed through a novel C-C bond formation at the C3 position of Ugi

Reported herein is a unified strategy to generate difluoroalkyl radicals from readily prepared α-difluorinated

Understanding the mechanism of the catalytic reaction is an effective way to design new high-performance catalysts. The mechanisms of alkyne/olefin hydrogenations catalyzed by a nonclassical Co–N2 ...

An N-heterocyclic carbene-catalyzed asymmetric [3 + 3] spiroannulation of β-ketothioamide was successfully developed. β-Ketothioamides exhibit an unusual reactivity to undergo a previously challenging lactamization reaction, and the desired spiro-piperidinone derivatives containing two vicinal stereogenic centers were synthesized in good to high yields with high stereoselectivities, whose structure can be converted to the corresponding imide and δ-lactam derivatives smoothly.

The total synthesis of a natural atropisomer, 4‘,4‘‘‘,7,7‘‘-tetra-O-methylcupressuflavone (1), has been achieved. The key intermediate, 3,3‘-diacetyl-4,4‘,6,6‘-tetramethoxy-2,2‘-biphenyldiol (5), was synthesized by the solid state phenol coupling reaction, and the racemate 5 was enantioresolved as bis(camphanate) esters. The absolute configuration of bis(camphanate) ester (−)-8b was determined to be (aR) by X-ray analysis. The ester (aR)-(−)-8b was converted to the natural biflavone [CD(+)362.0]-(−)-1, leading to the (aR) absolute configuration of 1. This conclusion is consistent with our previous theoretical determination of the absolute stereochemistry of biflavone 1 by the molecular orbital calculation of CD spectra.