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铑(III)催化芳烃与甲氧基酰胺作为酰胺化试剂的C-H酰胺化反应

Rh(III)-Catalyzed C-H Amidation of Arenes with -Methoxyamide as an Amidating Reagent.

作者信息

Ju Guodong, Li Guobao, Qian Guanwen, Zhang Jingyu, Zhao Yingsheng

机构信息

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.

出版信息

Org Lett. 2019 Sep 20;21(18):7333-7336. doi: 10.1021/acs.orglett.9b02625. Epub 2019 Sep 10.

Abstract

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.

摘要

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。

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