Efficient Pd-catalyzed domino synthesis of 1-phenyl-1H-indol-2-amine and 5-amino-indolo[1,2-a]quinazoline derivatives.

An efficient and practical one-pot domino synthesis of 1-phenyl-1H-indol-2-amine and 5-amino-indolo[1,2-a]quinazoline derivatives from readily available 2-(2-bromophenyl)acetonitriles was developed. The overall protocol involves a Buchwald-Hartwig type coupling and a base-promoted intramolecular nucleophilic reaction. The reaction scope, advantages and limitations are discussed.

An efficient and practical approach to trifluoromethylthiolation of α-haloketones/α-haloarylmethanes.

An efficient and practical approach to trifluoromethylthiolation of α-haloketones/α-haloarylmethanes was developed. The transformation employs only AgSCF3 and KI in situ generated active nucleophilic trifluoromethylthio species and cleanly occurs in up to quantitative yield at room temperature, thereby providing an unprecedentedly easy entry to various α-SCF3-substituted ketones/arylmethanes.