A short synthesis of Dronedarone

A short synthesis of Dronedarone

[Display omitted] A modification of the Nenitzescu reaction was used to obtain Dronedarone from quinonimine 20 and 1,3-diketone 14 (R = CH2CH2CH2NBu2) in a two-stage process in almost 55% overall yield. Our results represent significant improvement over other state-of-the-art methods as no extra ste...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2018-08, Vol.26 (14), p.4330-4335
Hauptverfasser: Piotrkowska, Barbara, Nerdinger, Sven, Schreiner, Erwin, Selič, Lovro, Graczyk, Piotr P.
Format: Artikel
Sprache:eng
Schlagworte:
Dronedarone
Nenitzescu
Optimization
Quinonimine
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Zusammenfassung:[Display omitted] A modification of the Nenitzescu reaction was used to obtain Dronedarone from quinonimine 20 and 1,3-diketone 14 (R = CH2CH2CH2NBu2) in a two-stage process in almost 55% overall yield. Our results represent significant improvement over other state-of-the-art methods as no extra steps for the decoration of the benzofuran core are required.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2018.03.041