A Direct Approach to Decoration of Bioactive Compounds via C−H Amination Reaction

Guodong Ju^†, Chunchen Yuan^†, Dongjie Wang^†, Jingyu Zhang^*,‡（张静宇）and Yingsheng Zhao^*,†（赵应声）

^†Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science Soochow University, Suzhou 215123, P. R. China

^‡College of Energy, Soochow Institute for Energy and Materials Innovations, Soochow University, Suzhou 215006, P. R. China

Org. Lett.2019,21, 9852--9855

The development of new methods to achieve the direct synthesis of bioactive organic molecules is always an important topic in organic synthesis. We hereby demonstrate that N-methoxyamide is an excellent amino source in the iridium-catalyzed intermolecular C–H amination reaction. The linkage of two bioactive organic molecules can be well achieved with this new protocol. More than 20 examples of decorated bioactive compounds were reported, which can facilitate the discovery of new bioactive molecules.

链接：https://pubs.acs.org/doi/10.1021/acs.orglett.9b03717