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Download fileNi-Catalyzed C–H Functionalization in the Formation of a Complex Heterocycle: Synthesis of the Potent JAK2 Inhibitor BMS-911543
journal contribution
posted on 2015-06-19, 00:00 authored by Monica
A Fitzgerald, Omid Soltani, Carolyn Wei, Dimitri Skliar, Bin Zheng, Jun Li, Jacob Albrecht, Michael Schmidt, Michelle Mahoney, Richard J. Fox, Kristy Tran, Keming Zhu, Martin D. EastgateBMS-911543
is a complex pyrrolopyridine investigated as a potential
treatment for myeloproliferative disorders. The development of a short
and efficient synthesis of this molecule is described. During the
course of our studies, a Ni-mediated C–N bond formation was
invented, which enabled the rapid construction of the highly substituted
2-aminopyridine core. The synthesis of this complex, nitrogen-rich
heterocycle was accomplished in only eight steps starting from readily
available materials.