Rh(III)-Catalyzed C−H Amidation of Arenes with N‑Methoxyamide as an Amidating Reagent
Guodong Ju†, Guobao Li†, Guanwen Qian†, 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, People’s Republic of China
‡ College of Energy, Soochow Institute for Energy and Materials Innovations, Soochow University, Suzhou 215006, People’s Republic of China
Org. Lett. 2019, 21, 7333--7336
The Rh(III)-catalyzed amidation of C(sp2)–H bonds has been reported by employing the N-methoxyamide as a novel amino source. An excellent level of functional group tolerance can be achieved when N-methoxyamide derivatives are used as the amidating reagents. Importantly, several known bioactive compounds such as Aminalon, Pregabalin, Gabapentin, and Probenecid can be transformed to effective amidating reagents, as a way to facilitate the development of new bioactive molecules.
链接:https://pubs.acs.org/doi/abs/10.1021/acs.orglett.9b02625