Palladium-catalyzed aerobic oxidative cross-couplings of indoles and benzene have been achieved by using 4,5-diazafluorene derivatives as ancillary ligands. Proper choice of the neutral and anionic ligands enables control over the reaction regioselectivity.

A FeCl3-catalyzed highly regioselective 1,2-addition/substitution sequence of 3-acetylcoumarins and indoles has been developed to afford highly hindered tetrasubstituted bis(indolyl)methanes bearing a biologically useful coumarin motif in 56-99% yields.

The tandem Michael addition/decarboxylation of (thio)coumarin-3-carboxylic acids with indoles has been developed and the biologically important indole-3-substituted dihydrocoumarins were obtained in good to excellent yields under catalyst-free conditions.

Iodine-catalyzed reaction of indoles with α,α'-bis(arylmethylene)cyclopentanones afforded one diastereomer of the corresponding Michael adducts, namely, E-2-(3-indolylphenylmethyl)-5-phenylmethylenecyclopentanones, in a good yield. The products form a new group of indole derivatives.

A direct coupling of unprotected indoles and α-halo ketones via in situ generated oxyallyl cation intermediates is described. The reactions efficiently afford α-indole carbonyl compounds with good to quantitative yields.

Organocatalytic direct C3 alkenylation of indoles has been developed. Simple and readily available morpholine trifluoroacetic acid salt is employed as an efficient catalyst in this oxidative dehydrogenative reaction. Simplicity and practicality constitute the most attractive advantages of this reaction.

Versatile nickel catalysts enabled the step-economical synthesis of decorated indoles through alkyne annulations with anilines bearing removable directing groups. The C-H/N-H activation strategy efficiently occurred in the absence of any metal oxidants and with excellent selectivities.

Cancer is a disease with fatal consequences; thus, searching for innovative compounds anticancer properties remains an active pursuit. One of the highly promising candidates compound derived from 3-thiocyanato-1H-indoles. However, number derivative currently limited. A quantitative structure and activity relationship (QSAR) study was conducted on derivate 3-thiocyanato-1H-indoles to establish e...

A rhodium-catalyzed oxidative C2-acylation of indoles with aryl and alkyl aldehydes via C-H bond activation is described. The reaction is highly atom-economic and provides easy access to a wide variety of 2-aroylindoles.