College of Chemistry, Beijing Normal University, Beijing 100875, China.
J Org Chem. 2013 Mar 15;78(6):2720-5. doi: 10.1021/jo302511s. Epub 2013 Feb 14.
A facile arylation, alkenylation, and alkylation of functionalized 2-halopyridine N-oxides with various Grignard reagents was developed. It represented a highly efficient and selective C-H bond functionalization of pyridine derivatives in the presence of reactive C-Cl or C-Br bonds. Using Cl or Br as a blocking group, C2/C6 site-controllable functionalization of pyridine derivatives has been achieved. Various pyridine compounds can be prepared as illustrated in the total syntheses of Onychine, dielsine, and PARP-1 inhibitor GPI 16539.
发展了一种功能化 2-卤代吡啶 N-氧化物与各种格氏试剂的简便芳基化、烯基化和烷基化反应。它代表了在活性 C-Cl 或 C-Br 键存在下吡啶衍生物中 C-H 键的高效和选择性功能化。使用 Cl 或 Br 作为封锁基团，可以实现吡啶衍生物的 C2/C6 位可控功能化。各种吡啶化合物可以通过总合成如onychine、dielsine 和 PARP-1 抑制剂 GPI 16539 来制备。
