Experimental study demonstrates efficient C2-arylacylation of 2H-benzothiazoles via synergistic PIFA/KOH promotion, highlighting a robust pathway to synthesize potential drug scaffolds.
To discover an efficient and convenient method to synthesize C2-arylacylated benzothiazoles as potential drug scaffolds, a novel [bis(trifluoroacetoxy)iodo]benzene(PIFA)/KOH synergistically promoted direct ring-opening C2-arylacylation reaction of 2H-benzothiazoles with aryl methyl ketones has been developed. Various substrates were tolerated under optimized conditions affording the C2-arylacylation products in 70–95% yields for 38 examples. A plausible mechanism was also proposed based on a series of controlled experiments.
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Sun et al. (2022) studied this question.
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