Abstract
AbstractA metal‐free approach for the synthesis of 5‐trifluoromethyl‐1,2,4‐triazoles via I2‐mediated [4+1] annulation of readily available trifluoroacetimidohydrazides and methyl ketones has been achieved. The transformation involves iodination/Kornblum oxidation, intermolecular dehydration condensation and an iodine‐mediated intramolecular cyclization/aromatization sequence. The developed protocol can be easily scaled up to 3 mmol scale without obvious efficiency decrease and be implemented by a consecutive one‐pot manner.magnified image
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