Regioselective C3-Formylation of 2H-Indazoles Using Selectfluor under Microwave-Assisted Conditions

Author:

Pitchai Manivel1,Vetrichelvan Muthalagu1ORCID,Kaspady Mahammed1,Indasi Gopikumar1,Krishnan Rajesh1,Maheswarappa Gururaju Sannakki1,Mathur Arvind2,Gupta Anuradha2

Affiliation:

1. Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd.

2. Small Molecule Drug Discovery, Bristol Myers Squibb Research and Early Development

Abstract

AbstractAn efficient microwave-assisted Selectfluor-mediated regioselective C3-formylation of 2H-indazoles bearing a variety of alkyl and aryl substituents using DMSO as the formylating agent has been developed. This methodology provides access to 3-formyl 2H-indazoles with moderate to excellent yields. These functionalized indazoles are potentially useful as templates for drug discovery. Control experimental results suggest that this formylation probably proceeds through a radical pathway.

Publisher

Georg Thieme Verlag KG

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