Issue 7, 2022

Remote difunctionalization of 2H-indazoles using Koser's reagents

Abstract

A new, efficient, and metal-free protocol has been developed for remote difunctionalization of unreactive C–H bonds at the benzene core of 2H-indazole by employing Koser's reagents, which act as both sulfonyloxylating and iodinating agents under ambient air. The present methodology represents facile access to C-4-sulfonyloxylated and C-7-iodinated 2H-indazole derivatives with high regioselectivity, wide functional group tolerance, and broad substrate scope in good to excellent yields. The formed 4,7 disubstituted 2H-indazoles are the precursors of various C-4,7-functionalized 2H-indazoles through simple transformations.

Graphical abstract: Remote difunctionalization of 2H-indazoles using Koser's reagents

Supplementary files

Article information

Article type
Communication
Submitted
30 Okt. 2021
Accepted
13 Dec. 2021
First published
15 Dec. 2021

Chem. Commun., 2022,58, 981-984

Remote difunctionalization of 2H-indazoles using Koser's reagents

S. Bhattacharjee, S. Laru and A. Hajra, Chem. Commun., 2022, 58, 981 DOI: 10.1039/D1CC06129A

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