Manufacture of the PI3K β‑Sparing Inhibitor Taselisib. Part 1: Early-Stage Development Routes to the Bromobenzoxazepine Core

Two convergent regioselective routes for the synthesis of the tetracyclic imidazobenzoxazepine triazole 1, a key intermediate toward the synthesis of taselisib, are described. In the first-generation route, a chemoselective Negishi cross-coupling reaction was developed between iodoimidazole 3 and tr...

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Veröffentlicht in:	Organic process research & development 2019-05, Vol.23 (5), p.775-782
Hauptverfasser:	Remarchuk, Travis, Angelaud, Rémy, Askin, David, Kumar, Archana, Thompson, Andrew S, Cheng, Hua, Reichwein, John F, Chen, Yanping, St-Jean, Frédéric
Format:	Artikel
Sprache:	eng
Online-Zugang:	Volltext
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