Ju Guodong, Li Guobao, Qian Guanwen, Zhang Jingyu, Zhao Yingsheng
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 Sep 20;21(18):7333-7336. doi: 10.1021/acs.orglett.9b02625. Epub 2019 Sep 10.
The Rh(III)-catalyzed amidation of C(sp)-H bonds has been reported by employing the -methoxyamide as a novel amino source. An excellent level of functional group tolerance can be achieved when -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.
通过使用甲氧基酰胺作为新型氨基源,已报道了铑(III)催化的C(sp)-H键酰胺化反应。当使用甲氧基酰胺衍生物作为酰胺化试剂时,可以实现优异的官能团耐受性。重要的是,几种已知的生物活性化合物,如氨基丙二酸、普瑞巴林、加巴喷丁和丙磺舒,可以转化为有效的酰胺化试剂,以此促进新生物活性分子的开发。