Litcius/Paper detail

Catalytic and Chemodivergent Synthesis of 1-Substituted 9<i>H</i>-Pyrrolo[1,2-<i>a</i>]indoles via Annulation of β-CF<sub>3</sub> Enones with 3-Substituted Indoles

Haritha Sindhe, Nehanaz Saiyed, Akshay Kamble, Malladi Mounika Reddy, Amardeep Singh, Satyasheel Sharma

2022The Journal of Organic Chemistry10 citationsDOI

Abstract

Chemodivergent reactions are more advantageous in organic synthesis that yield diversely functionalized scaffolds from common starting materials. Herein, we report an efficient metal-free chemodivergent protocol for the synthesis of 1-substituted 9H-pyrrolo[1,2-a]indole derivatives in the presence of catalytic amounts of Lewis acid/Brønsted acid conditions using 3-substituted indoles and β-trifluoromethyl-α,β-unsaturated ketones. Fine-tuning of the catalyst and solvent system in the reaction conditions deliver the trifluoromethyl, trifluoroethylcarboxylate, or carboxylic acid substituents on the C1-position of 9H-pyrrolo[1,2-a]indole derivatives in situ. It is postulated that the solvent and LA/BA catalyst interaction was found to be crucial for the catalytic C–F activation in these transformations.

Topics & Concepts

CatalysisIndole testAnnulationChemistryTrifluoromethylYield (engineering)Lewis acids and basesSolventBrønsted–Lowry acid–base theoryCombinatorial chemistryMedicinal chemistryLewis acid catalysisOrganic chemistryMaterials scienceAlkylMetallurgyFluorine in Organic ChemistryCatalytic C–H Functionalization MethodsCyclopropane Reaction Mechanisms