A Highly Concise and Convergent Synthesis of HCV Polymerase Inhibitor Deleobuvir (BI 207127): Application of a One-Pot Borylation鈥揝uzuki Coupling Reaction

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• 作者：Yongda Zhang ; Bruce Z. Lu ; Guisheng Li ; Sonia Rodriguez ; Jonathan Tan ; Han-Xun Wei ; Jianxiu Liu ; Frank Roschangar ; Fei Ding ; Wenyi Zhao ; Bo Qu ; Diana Reeves ; Nelu Grinberg ; Heewon Lee ; Golo Heckmann ; Oliver Niemeier ; Michael Brenner ; Youla Tsantrizos ; Pierre L. Beaulieu ; Azad Hossain ; Nathan Yee ; Vittorio Farina ; Chris H. Senanayake
• 刊名：Organic Letters
• 出版年：2014
• 出版时间：September 5, 2014
• 年：2014
• 卷：16
• 期：17
• 页码：4558-4561
• 全文大小：335K
• ISSN：1523-7052

文摘

A highly concise and convergent synthesis of HCV polymerase inhibitor Deleobuvir (BI 207127, 1) was achieved, featuring efficient Pd-catalyzed one-pot borylation鈥揝uzuki coupling where TFP was identified as the unique ligand effective for these transformations.