An asymmetric organocatalytic tandem reaction comprising cyclization/transfer hydrogenation has been established in a compatible and synergistic way, leading to the step-economical synthesis of enantioenriched tetrahydroquinoxalines and dihydroquinoxalinones from readily accessible materials in excellent enantioselectivity of up to > 99% ee. This protocol of a one-operation tandem reaction combines the merits of both tandem reactions and asymmetric organocatalysis, providing an efficient strategy for concisely and enantioselectively synthesizing nitrogen heterocycles with biological relevance.

An efficient, three-component strategy for the improved synthesis of multifunctionalized 6,7-dihydrobenzofuran-4(5H)-ones under microwave irradiation in ethyl alcohol within short periods has been established. The synthesized benzofuran-4(5H)-ones have been readily converted into polyfunctionalized cinnoline-4-carboxamides by treating with hydrazine hydratein in the same solvent through a regioselective ring-opening of the furan. Tedious workup procedures can be avoided because of the direct precipitation of products from the reaction solution by water addition, thus rendering the two-steps process ecofriendly.

A new three-component strategy for the efficient synthesis of 2,3,5-trisubstituted thiophene derivatives through a [2+2+1] heterocyclization between 3-(2-aryl-2-oxoethylidene)-2-oxindoles and α-thiocyanato ketones under microwave irradiation is described. The bond-forming efficiency, accessibility, and generality of this synthesis make it highly valuable to assemble thiophene scaffolds.

The three component reactions of 2-formylbenzoic acid, arylglyoxals, and isocyanides allow the synthesis of different substituted isocoumarins by a simple change of the solvent. -(MA, G.-H.; JIANG*, B.; TU, X.-J.; NING, Y.; TU, S.-J.; LI, G.; Org. Lett. 16 (2014) 17, 4504-4507, http://dx.doi.org/10.1021/ol502048e ; Sch. Chem. Chem. Eng., Jiangsu Norm. Univ., Jiangsu, Xuzhou 221116, Peop. Rep. China; Eng.) -Mais 10-186

BINOL--derived phosphonic acids are described as catalysts for the cyclization of phenylenediamines with substituted glyoxals followed by transfer hydrogenation with Hantzsch ester to give enantioenriched tetrahydroquinoxalines in good yields. The process can be readily extended to the synthesis of dihydroquinoxalinones from ethyl 2-oxo-2-arylacetates. -(SHI*, F.; TAN, W.; ZHANG, H.-H.; LI, M.; YE, Q.; MA, G.-H.; TU, S.-J.; LI, G.; Adv. Synth. Catal. 355 (2013) 18, 3715-3726, http://dx.doi.org/10.1002/adsc.201300576 ; Coll. Chem. Chem. Eng., Xuzhou Norm. Univ., Jiangsu, Xuzhou 221116, Peop. Rep. China; Eng.) -Mais 21-187