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Synthesis of 2‑(1H‑Indol-2-yl)acetamides via Brønsted Acid-Assisted Cyclization Cascade

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journal contribution
posted on 16.09.2020, 21:31 by Nicolai A. Aksenov, Dmitrii A. Aksenov, Anton A. Skomorokhov, Lidiya A. Prityko, Alexander V. Aksenov, Georgii D. Griaznov, Michael Rubin
An efficient and straightforward Brønsted-acid mediated cascade process was developed, involving cyclization of readily available β-ketonitriles into 2-aminofurans, and their subsequent recyclization into 2-(1H-indol-2-yl)­acetamides is developed. This synthetic route opens a new avenue for an expeditious assembly of various isotryptamine derivatives for medicinal chemistry.