Regioselective Conversion of Arenes to N‐aryl‐1,2,3‐triazoles Using CH Borylation |
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| Authors: | Dr. Rajavel Srinivasan Dr. Anthony G. Coyne Prof. Dr. Chris Abell |
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| Affiliation: | Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW (UK) |
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| Abstract: | A one‐pot protocol for the synthesis of N‐aryl 1,2,3‐triazoles from arenes by an iridium‐catalyzed C?H borylation/copper catalyzed azidation/click sequence is described. 1 mol % of Cu(OTf)2 was found to efficiently catalyze both the azidation and the click reaction. The applicability of this method is demonstrated by the late‐stage chemoselective installation of 1,2,3‐triazole moiety into unactivated molecules of pharmaceutical importance. |
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| Keywords: | azidation C H borylation click chemistry synthetic methods |
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