Institut für Organische und Biomolekulare Chemie, Georg-August-Universität Göttingen, Tammannstrasse 2, 37077, Göttingen, Germany.
Angew Chem Int Ed Engl. 2016 Feb 24;55(9):3153-7. doi: 10.1002/anie.201510743. Epub 2016 Jan 28.
The C-H alkylation of aniline derivatives with both primary and secondary alkyl halides was achieved with a versatile nickel catalyst of a vicinal diamine ligand. Step-economic access to functionalized 2-pyrimidyl anilines, key structural motifs in anticancer drugs, is thus provided. The C-H functionalization proceeded through facile C-H activation and SET-type C-X bond cleavage with the assistance of a monodentate directing group, which could be removed in a traceless fashion.
具有邻二胺配体的多功能镍催化剂实现了苯胺衍生物与伯卤代烷和仲卤代烷的 C-H 烷基化反应。因此，以经济有效的方式获得了功能化的 2-嘧啶基苯胺，这是抗癌药物中的关键结构基序。C-H 官能团化通过易发生的 C-H 活化和 SET 型 C-X 键断裂进行，其中单齿导向基团提供了协助，该导向基团可以以无痕迹的方式去除。
