Microwave-Assisted Ru(II)-Catalyzed Regioselective Methyl Acylation of 2-Arylbenzoazoles: Synthesis of Benzofuran Conjugates via C-H Activation/Annulation.

An efficient Ru(II)-catalyzed C-H functionalization protocol for 2-arylbenzoazoles as the directing group and sulfoxonium ylide has been developed. Gratifyingly, concomitant annulation was observed when 3-(benzo[]azol-2-yl) phenol was used, enabling the construction of benzofuran conjugates. Notably, the utilization of water as the solvent and an energy efficient approach makes the reaction greener, contributing to overall sustainability.

Exploration of cytotoxic potential and tubulin polymerization inhibition activity of -stilbene-1,2,3-triazole congeners.

To scrutinize -stilbene based molecules with potential anticancer and tubulin polymerization inhibition activity, a new series of -stilbene-1,2,3-triazole congeners was designed and synthesized a click chemistry protocol. The cytotoxicity of these compounds 9a-j and 10a-j was screened against lung, breast, skin and colorectal cancer cell lines. Based on the results of MTT assay, we further evaluated the selectivity index of the most active compound 9j (IC 3.

Ru(II)-Catalyzed regioselective carbene insertion into β-carbolines and isoquinolines.

A protocol for carbene insertion into the inert C(sp)-H bond has been established wherein β-carbolines and isoquinolines are explored as intrinsic directing groups. The Ru(II)-catalyzed strategy employing sulfoxonium ylides as the carbene precursor offers an effective and atom-economical functionalization of substrates of biological interest with only DMSO as the sole by-product. The strategy is scalable to gram scale, and it also showcases a wide range of functional group tolerance.

Ru(II)-Catalyzed Regioselective C-N Bond Formation on Benzothiazoles Employing Acyl Azide as an Amidating Agent.

A Ru(II)-catalyzed regioselective direct -amidation of 2-aryl benzo[]thiazoles employing acyl azides as a nitrogen source has been accomplished. This approach utilizes the efficiency of benzothiazole as a directing group and the role of acyl azide as an effective amidating agent toward C-N bond formation, thereby evading the general Curtius rearrangement. The protocol highlights significant functional group tolerance, single-step, and external oxidant-free conditions, with the release of only innocuous molecular nitrogen as the byproduct.

Microwave-assisted multicomponent reactions in heterocyclic chemistry and mechanistic aspects.

Microwave-assisted (MWA) multicomponent reactions (MCRs) have successfully emerged as one of the useful tools in the synthesis of biologically relevant heterocycles. These reactions are strategically employed for the generation of a variety of heterocycles along with multiple point diversifications. Over the last few decades classical MCRs such as Ugi, Biginelli, etc.

Development of β-carboline-benzothiazole hybrids via carboxamide formation as cytotoxic agents: DNA intercalative topoisomerase IIα inhibition and apoptosis induction.

In quest of promising anticancer agents, the pharmacophores of natural (β-carboline) and synthetic origin (benzothiazole) were adjoined by a carboxamide bridge and three-point diversification was accomplished. The in vitro cytotoxic ability of the compounds was established on adherent and suspension human cancer cell lines and compounds 8u and 8f advanced as pre-eminent molecules with IC values of 1.46 and 1.

β-Carboline directed regioselective hydroxylation by employing Cu(OAc) and mechanistic investigation by ESI-MS.

A β-carboline directed regioselective C-H activation protocol for hydroxylation has been developed by employing Cu(OAc)2, a cost-effective 3d metal. This fastidious reaction proceeds under microwave irradiation and furnishes exclusively ortho-hydroxylated products with moderate to good yields under greener reaction conditions. Gratifyingly, this approach retains considerable functional group tolerance and is feasible on both electron-rich and electron-deficient substrates.