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Aerobic Oxidative C–H Azolation of Indoles and One-Pot Synthesis of Azolyl Thioindoles by Flavin–Iodine-Coupled Organocatalysis

Kazumasa Tanimoto, Hayaki Okai, Marina Oka, Ryoma Ohkado, Hiroki Iida

2021Organic Letters28 citationsDOIOpen Access PDF

Abstract

The aerobic oxidative cross-coupling of indoles with azoles driven by flavin-iodine-coupled organocatalysis has been developed for the green synthesis of 2-(azol-1-yl)indoles. The coupled organocatalytic system enabled the one-pot three-component synthesis of 2-azolyl-3-thioindoles from indoles, azoles, and thiols in an atom-economical manner by utilizing molecular oxygen as the only sacrificial reagent.

Topics & Concepts

ChemistryOrganocatalysisIodineReagentFlavin groupOxidative phosphorylationCombinatorial chemistryMolecular oxygenOrganic chemistryCatalysisEnantioselective synthesisBiochemistryEnzymeCatalytic C–H Functionalization MethodsSulfur-Based Synthesis TechniquesSynthesis and Catalytic Reactions
Aerobic Oxidative C–H Azolation of Indoles and One-Pot Synthesis of Azolyl Thioindoles by Flavin–Iodine-Coupled Organocatalysis | Litcius