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Copper-Catalyzed Coupling between ortho-Haloanilines and Lactams/Amides: Synthesis of Benzimidazoles and Telmisartan

par Boquet, Vincent ;Sauber, Chris ;Beltran, Raphaël;Ferey, Vincent;Rodier, Fabien;Hansjacob, Pierre ;Theunissen, Cédric ;Evano, Gwilherm
Référence Journal of organic chemistry, 89, page (5469-5479)
Publication Publié, 2024-03-18

Article révisé par les pairs

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Résumé :

An efficient copper-catalyzed synthesis of (annelated) benzimidazoles is reported. This transformation is based on a simple and straightforward one-pot sequence involving a copper-catalyzed cross coupling between o-haloanilines and lactams/amides followed by a subsequent cyclization under acidic conditions. A variety of (annelated) benzimidazoles could be easily obtained in high yields from readily available starting materials and this procedure could be further applied to the synthesis of the antihypertensive blockbuster drug telmisartan.