KI-Catalyzed C(sp<sup>3</sup>)–H Amination and Acyloxylation of Indolin-3-ones Using Air as the Oxidant
Yueyue Fan, Jingwen Guo, Yuting Bao, Yuxin Yuan, Meng Hu, Xiaohui Li, Hang Yan, Yuepiao Cai, Qinqin Xia
Abstract
We have developed an efficient and green strategy for the synthesis of C2-amino indolin-3-ones and C2-acyloxy indolin-3-ones via KI-catalyzed C(sp 3 )–H amination and acyloxylation of indolin-3-ones using air as the oxidant. The reaction provides straightforward access to 2-substituted indolin-3-ones by the direct functionalization of indolin-3-ones at the C2 position under mild conditions. Moreover, the conditions enable direct functionalization of a range of complex pharmaceuticals, providing attractive products for medicinal chemistry programs.
Topics & Concepts
ChemistryAminationCatalysisSurface modificationCombinatorial chemistryOrganic chemistryPhysical chemistryCatalytic C–H Functionalization MethodsSynthesis and Catalytic ReactionsOxidative Organic Chemistry Reactions