A highly efficient and mild sequential nucleophilic addition/ cyclization/copper catalyzed CÀ N coupling reaction of o-iodophenyl isothiocyanates with propargylamines has been realized, which delivers a variety of benzimidazo [2,1-b]thiazole derivatives in good yields. Moreover, this protocol could be performed at gram scale and applied to the concise synthesis of tilomisole.
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