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An efficient and practical synthetic approach to access to 2H-pyrrolo[3,4-c]quinolin-4(5H)-one/2H-pyrrolo[3,4-c]quinoline derivatives by the reaction of 2-aminoarylacrylates/2-aminochalcones and tosylmethyl isocyanide (TosMIC) via a one pot van Leusen reaction and cyclization under basic conditions has been reported. The desired products could be obtained(More)
A novel CuI/BF(3)·Et(2)O/O(2)-mediated reaction utilizing ketones and benzylamines for the construction of substituted imidazoles in one step under mild conditions has been demonstrated. This protocol involved the removal of eight hydrogen atoms, the functionalization of four C(sp(3))-H bonds and three new C-N bond formations.
A novel silver-catalyzed fluorination reaction of carbonyl directed alkynes in the presence of N-fluorobenzenesulfonimide and water with high regioselectivities has been developed. The established protocol provides an alternative method for rapid assembly of α-fluoroketone derivatives under simple and mild reaction conditions. The reaction pathway involves(More)
A novel synthetic approach toward 1,4-disubstituted 1,2,3-triazoles and 1,5-disubstituted 1,2,3-triazoles by aerobic oxidative cycloaddition of α-chlorotosylhydrazone with primary aryl amine has been developed. Significantly, the reaction proceeds smoothly to afford 1,4-disubstituted 1,2,3-triazoles and 1,5-disubstituted 1,2,3-triazoles under catalyst-free,(More)
A Pd-catalyzed highly regioselective 6-exo-dig cyclization/alkenylation reaction of ortho-ethynylanilides has been developed. This tandem cross-coupling protocol represents a simple, efficient, step- and atom-economic approach for the construction of scarcely known polyene-substituted benzo[d][1,3]oxazines in moderate to excellent yields with a broad(More)
An efficient I2 (20 mol %)/TBPB mediated oxidative formal [4 + 1] cycloaddition of N-tosylhydrazones with anilines via C-N/N-N bond formation and S-N cleavage has been developed. This protocol represents a simple, general, and efficient approach for the construction of 1,2,3-triazoles under metal-free and azide-free conditions by utilizing a catalytic(More)
A novel I2/TBHP-mediated direct oxidative diamination reaction of indoles with anilines was developed. The reaction proceeded smoothly under aqueous and open air reaction conditions. This protocol provides a practical synthetic method for the synthesis of Tryptanthrin and the construction of N-C3 linked pyrrolidinoindolines which is the core structure of(More)