Multikilogram Synthesis of a Potent Dual Bcl-2/Bcl‑xL Antagonist. 2. Manufacture of the 1,3-Diamine Moiety and Improvement of the Final Coupling Reaction

This paper describes the synthesis of kilogram quantities of the sulfonamide moiety 3 involved in a coupling reaction with acid moiety 2 to provide batches of drug candidate 1 for preclinical studies and first-in-human clinical trials. A first approach relying on a chiral separation furnished the de...

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Veröffentlicht in:	Organic process research & development 2020-05, Vol.24 (5), p.670-685
Hauptverfasser:	Hardouin, Christophe, Baillard, Sandrine, Barière, François, Craquelin, Anthony, Grandjean, Mathieu, Janvier, Solenn, Le Roux, Stéphane, Penloup, Christine, Russo, Olivier
Format:	Artikel
Sprache:	eng
Online-Zugang:	Volltext
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