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

作者:Zhang Yongda*; Lu Bruce Z; Li Guisheng; Rodriguez Sonia; Tan Jonathan; Wei Han Xun; Liu Jianxiu; Roschangar Frank; Ding Fei; Zhao Wenyi; Qu Bo; Reeves Diana; Grinberg Nelu; Lee Heewon; Heckmann Golo; Niemeier Oliver; Brenner Michael; Tsantrizos Youla; Beaulieu Pierre L; Hossain Azad; Yee Nathan; Farina Vittorio; Senanayake Chris H
来源:Organic Letters, 2014, 16(17): 4558-4561.
DOI:10.1021/ol5021114

摘要

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

  • 出版日期2014-9-5