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Article Abstract

The structural modification of -aryl indazolols as tautomers of -aryl indazolones has been established as a hot topic in pharmaceutics and medicinal chemistry. We herein disclose the rhodium(III)-catalyzed 1,4-addition reaction of maleimides with -aryl indazol-3-ols, which provides the succinimide-bearing indazol-3-ol scaffolds with complete regioselectivity and a good functional group tolerance. Notably, the versatility of this protocol is demonstrated by the use of drug-molecule-linked and fluorescence-probe-linked maleimides.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9088931PMC
http://dx.doi.org/10.1021/acsomega.1c07363DOI Listing

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