A metal-free synthesis of bifunctionalized indole derivatives was developed through a novel TBHP/TBAI-mediated oxidative coupling of C2,C3-unsubstituted indoles with arylsulfonyl hydrazide. Under the same conditions C3-methyl substituted indoles underwent a diazotization process, affording 2-sulfonyldiazenyl-1H-indoles. The former reaction simultaneously established C-S and C-N bonds through se...

The title compound, C(15)H(12)N(4)O(2), contains two substituted benzohydrazide and indole rings linked via a C=N double bond. The dihedral angle between the benzene ring and the indole ring system is 11.38 (10)°. The mol-ecular structure is stabilized by an intra-molecular N-H⋯O hydrogen bond, forming a six-membered ring. The crystal structure is consolidated by inter-molecular N-H⋯O and C-H⋯O...

A series of N-(aminoiminomethyl)-1H-indole carboxamide derivatives were synthesized and their inhibitory potencies against the Na+/H+ exchanger were measured. Variation of the carbonylguanidine group at the 2- to 7-position of the indole ring system showed that a substitution at the 2-position improved the Na+/H+ exchanger inhibitory activity the most in vitro. This led to the synthesis and eva...

Novel azepino[3,4-b]indol-1-ones were synthesized from alkyne-substituted indole-2-carboxamides by catalytic intramolecular cyclization in the presence of PtCl(2). The scope and limitations of this straightforward protocol are reported.

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.

CuCl2-mediated intramolecular C-H/C-H cross-dehydrogenative coupling (CDC) of thioalkyl-substituted α-acetyl or α-aroyl ketene N,S-acetals afforded 2-thioalkyl indoles. Tunable C-S bond transformations of the resultant indoles led to highly functionalized N-heterocyclic compounds. A β-thioalkyl is necessary to activate the N,S-acetal substrate and enable the CDC reaction to occur, and the relev...

3-Methyleneoxindole is a cytotoxic metabolite of indole-3-acetic acid with potential for use in cancer therapy. This species and ring-substituted analogues are conveniently synthesised from the corresponding isatins via a Peterson olefination.

<p>In this research, we have described a facile and user-friendly protocol for the formation of 2((1H-Indole-3yl)(Phenyl)methyl)malononitrile derivatives using recoverable efficient TiO2 nanocatalyst. This is simple incredibly synthesis novel derivatives. Nanoscale used as catalyst. Since TiO<sub>2 </sub>has more surface area easily binds with active site reactive molecule ini...

A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet a...

A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet a...