Abstract
An extensive study of the chemoselective Pd‐catalyzed inter‐ and intramolecular direct C–H arylation of N‐benzylated 5‐carboxyimidazoles with halides with and without CuI assistance in 1,4‐dioxane as a low‐polarity solvent was explored. The method was suitable for the synthesis of fused imidazole‐based tricyclic systems incorporating medium‐sized rings, including, for the first time, eight‐membered rings, which are valuable in modern drug design.
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