Abstract
AbstractA copper(I) iodide‐catalyzed, highly efficient acylation of benzothiazoles with aryl methyl ketones as carbonyl sources under a nitrogen atmosphere was developed. This is an unprecedented protocol and an extremely efficient method for the selective synthesis of 2‐acylbenzothiazoles from commercially available, cheap starting materials with excellent chemoselectivity, good functional group tolerability and high turnover numbers (up to 14,200); also scaling up to 160 mmol without loss of the efficiency is possible. A variety of 2‐acylbenzothiazoles was smoothly prepared in good to excellent yields from aryl methyl ketones and benzothiazoles by a one‐pot domino protocol of combined sp3 CH oxidation, ring opening, and condensation.magnified image
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