Abstract

AbstractA synthetic method was developed for the preparation of heteroaryl and diheteroaryl ketones from aldehydes and organoboronic acids through a palladium‐catalyzed 1,2‐addition and oxidation that uses an aryl iodide as the oxidant. This one‐pot process shows high tolerance for a broad range of heterocyclic substrates by using 1.0–3.0 mol‐% of the catalyst that is formed from allylpalladium chloride dimer and a thioether‐imidazolinium chloride. In addition to fine‐tuning the catalytic system, the use of a sterically hindered aryl iodide that has a substituent at the ortho position, such as 2‐iodotoluene, is important to obtain the desired ketones with heterocyclic moieties in good to excellent yields.

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