An efficient base-catalyzed protocol for the synthesis of benzothiophene is described. The reaction proceeds via base-promoted propargyl-allenyl rearrangement followed by cyclization and allyl migration. Phosphine-substituted indoles can be synthesized by a similar strategy.

Intramolecular tin and sulfur mediated free-radical cyclizations between an aryl isonitfile and a pendant TMSsubstituted alkyne give 2,3-disubstituted indoles from 5-exo-dig cyclization and nucleophilic trapping of the resulting indolenine intermediate. © 1999 Elsevier Science Ltd. All fights reserved. In spite of the fact that Fischer first described their synthesis some 115 years ago, 1 the g...

In search for new leads towards potent anti-inflammatory agents, an array of 5-methoxy-3-(3’-chloro-2’oxo-4-substitutedaryl-1’-azetidinyl)indoles (4a-4e) and 5-methoxy-3-(2’-substitutedaryl-4’-oxo-1’,3’-thiazolidin-3’-yl)indoles (5a-5e) have been synthesized form 5-methoxy-3-substitutedbenzylidenlaminoindoles (3a-3e). Structure of all the synthesized compounds has been analyzed using elemental ...

The indoles plant growth hormones have exhibited potentially antitumor activities. However, the targets of these indoles have not been clearly elucidated. By introduction of hydroxamic acid group to the structure of indolebutyric acid, the derived molecule (IBHA) exhibited potent HDAC2 (IC50 value of 0.32 ± 0.02 µM) and HDAC3 (IC50 value of 0.14 ± 0.01 µM) inhibitory activities compared with SA...

We report an enantioselective coupling between alkynes and indoles. A Rh-hydride catalyst isomerizes alkynes to generate a metal-allyl species that can be trapped with both aromatic and heteroaromatic nucleophiles.

Synthesis of various potential biologically active compounds from the reaction of quinoline and vanillin based aldehydes and ethereal dialdehydes with indoles in the presence of RuCl3.nH2O as a homogeneous catalyst at room temperature is described.

The coupling of rhodium carbenoids from vinyl diazoacetates with 2-thio-3-alkyl indoles was found to generate C(3) quaternary substituted indolines via a thionium ylide-initiated [3,3]-sigmatropic rearrangement.

Using copper complexes with an axially chiral bipyridine ligand C4-ACBP as the catalyst, an enantioselective functionalization of indoles with diazo compounds was developed with up to 95% ee. This protocol paves the way for further applications of these ligands.

N-Indolyl or N-benzofuranyl indoles and benzimidazoles were prepared through metal-catalyzed tandem reactions between 2-alkynyl cyclohexadienimines or cyclohexadienones and 2-alkynylanilines or N(1)-benzylbenzene-1,2-diamine.

Ru(III)-exchanged FAU-Y zeolite was used as an efficient reusable heterogeneous catalyst for preparation of oxindoles from condensation reaction of indoles with isatins under very mild reaction conditions.