Development of a Process to a 4‑Arylated 2‑Methylisoquinolin-1(2H)‑one for the Treatment of Solid Tumors: Lessons in Ortho-Bromination, Selective Solubility, Pd Deactivation, and Form Control

We here present an optimized, scalable synthesis of bromodomain and extra-terminal (BET) inhibitor BMS-986378 (CC-90010). The original route and process 1A was 7 steps with 33.8% yield and featured numerous problematic solvents, process safety concerns, difficult to scale unit operations, and challe...

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Veröffentlicht in:	Organic process research & development 2022-05, Vol.26 (5), p.1458-1469
Hauptverfasser:	Primer, David N., Yong, Kelvin, Ramirez, Antonio, Kreilein, Matthew, Ferretti, Antonio C., Ruda, Antonio M., Fleary-Roberts, Nadia, Moseley, Jonathan D., Forsyth, Siân M., Evans, Graham R., Traverse, John F.
Format:	Artikel
Sprache:	eng
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