Ni-Catalyzed C鈥揌 Functionalization in the Formation of a Complex Heterocycle: Synthesis of the Potent JAK2 Inhibitor BMS-911543
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- 作者：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. Eastgate
- 刊名：Journal of Organic Chemistry
- 出版年：2015
- 出版时间：June 19, 2015
- 年：2015
- 卷：80
- 期：12
- 页码：6001-6011
- 全文大小：559K
- ISSN：1520-6904
文摘
BMS-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鈥揘 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.