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Fox, Richard J; Cuniere, Nicolas L; Bakrania, Lopa; Wei, Carolyn; Strotman, Neil A; Hay, Michael; Fanfair, Dayne; Regens, Christopher; Beutner, Gregory L; Lawler, Michael; Lobben, Paul; Soumeillant, Maxime C; Cohen, Benjamin; Zhu, Keming; Skliar, Dimitri; Rosner, Thorsten; Markwalter, Chester E; Hsiao, Yi; Tran, Kristy; Eastgate, Martin D
Journal of organic chemistry, 04/2019, Letnik: 84, Številka: 8Journal Article
The development of an improved short and efficient commercial synthesis of the JAK2 inhibitor, a complex pyrrolopyridine, BMS-911543, is described. During the discovery and development of this synthesis, a Pd-catalyzed C–H functionalization was invented which enabled the rapid union of the key pyrrole and imidazole fragments. The synthesis of this complex, nitrogen-rich heterocycle was accomplished in only six steps (longest linear sequence) from readily available materials.
