Anode-induced arylthiol-amine cross-coupling: A nontraditional strategy to access sulfinamides
Pan Zhou1, Ting Zou1, Sen-Hui Wu1
1State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, Frontiers Science Center for New Organic Matter, College of Chemistry, Nankai University, Tianjin 300071, China.
Abstract:
Sulfinamides are ubiquitous structures among natural products and biologically active compounds. Generic synthetic methods for sulfinamides remain elusive because the preparation of sulfoxide precursors is notoriously difficult. Direct construction of S─N bonds represents a highly efficient economical method to access these sulfinamides. However, the most prevalent techniques for their synthesis are still the nonradical approaches of sulfoxide precursors with amines, where prepreparation of substrates, harsh reaction conditions, and restricted substrate ranges have intrinsically limited the synthetic scope. Herein, we leveraged a practical and streamlined electrocatalytic strategy to achieve sulfinamide synthesis, which involves the intermolecular oxidative cross-coupling of readily available arylthiols and aliphatic amines. Mechanistic investigations indicate that four successive oxidations at the anode play a crucial role in radical generation, S─N bond formation, and further oxidation of intermediates.
More Related Videos
08:47Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
07:30A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones
Published on: January 21, 2020
Related Concept Videos
Amines to Sulfonamides: The Hinsberg Test
Generally, a primary amine reacts with the Hinsberg reagent to produce an N-substituted benzenesulfonamide. The electron-withdrawing sulfonyl...
Preparation of 1° Amines: Azide Synthesis
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Preparation and Reactions of Sulfides
Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Amines to Amides: Acylation of Amines
Next, the second equivalent of amine serves as a Brønsted base and deprotonates the quaternary...
