Synthesis
DOI: 10.1055/a-2464-7068
paper

Synthesis the C1–C15 Fragment of Incednine

Damien Cordeau
a   CiTCoM, UMR 8038, CNRS - Université Paris Cité, Faculté de Pharmacie, 4, avenue de l’Observatoire, 75006, Paris, France
,
Stéphanie Norsikian
b   Université Paris-Saclay, CNRS, Institut de Chimie des Substances Naturelles, UPR 2301 1, Avenue de la Terrasse, 91198, Gif-sur-Yvette, France
,
Grégory Genta-Jouve
c   UAR 3456 CNRS LEEISA, Centre de Recherche de Montabo, IRD, 275 Route de Montabo, CEDEX BP 70620, 97334, Cayenne, France
,
Emmanuel Roulland
a   CiTCoM, UMR 8038, CNRS - Université Paris Cité, Faculté de Pharmacie, 4, avenue de l’Observatoire, 75006, Paris, France
› Author Affiliations
This work has been funded by the Agence Nationale de la Recherche (ANR) (SynTense ANR-21-CE07-0041-02), the Centre National de la Recherche Scientifique (CNRS), and the Université Paris Cité.


Abstract

We report on our progress towards the synthesis of the exotic, delicate, and tense polyketidic macrolactam of incednine. This work constitutes a significant advancement towards the total synthesis of a family of molecules of biological and medicinal interest. Some of the key features of this synthesis required evolutions from the initially designed strategy, leading to the use of a Horner–Wadsworth–Emmons olefination to build the C2–C9 tetraene. For this purpose, a polyfunctionalized phosphonate was used that was obtained through an unprecedented Pd-catalyzed cross-coupling involving the zinc salt of diethyl methylphosphonate. The resulting desired C1–C15 fragment displays a carboxylic acid ester at C1 and a vinyl iodide at C15, both functions being ready for subsequent amide coupling with the C16–C23 fragment and final Suzuki cyclization, respectively.

Supporting Information



Publication History

Received: 11 October 2024

Accepted after revision: 08 November 2024

Accepted Manuscript online:
08 November 2024

Article published online:
17 December 2024

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