One-Pot Modified Madelung Synthesis of 3-Tosyl- and 3-Cyano-1,2-disubstituted Indoles

Grigorii K Sterligov; Alexandra A Ageshina; Sergey A Rzhevskiy; Olga V Shurupova; Maxim A Topchiy; Lidiya I Minaeva; Andrey F Asachenko

doi:10.1021/acsomega.2c03754

One-Pot Modified Madelung Synthesis of 3-Tosyl- and 3-Cyano-1,2-disubstituted Indoles

ACS Omega. 2022 Oct 19;7(43):38505-38511. doi: 10.1021/acsomega.2c03754. eCollection 2022 Nov 1.

Authors

Grigorii K Sterligov¹, Alexandra A Ageshina¹, Sergey A Rzhevskiy¹, Olga V Shurupova¹, Maxim A Topchiy¹, Lidiya I Minaeva¹, Andrey F Asachenko¹

Affiliation

¹ A. V. Topchiev Institute of Petrochemical Synthesis, Russian Academy of Sciences, Leninskiy Prospect 29, 119991 Moscow, Russia.

Abstract

A One-pot, two-step procedure for the synthesis of 1,2-disubstituted-3-tosyl and 1,2-disubstituted-3-cyanoindoles from the corresponding N-(o-tolyl)benzamides is reported. The developed procedure is operationally simple, does not utilize any transition metals, and provides variably substituted indoles in good yields from readily available starting materials.