Development of catalytic asymmetric addition reactions via direct nucleophilic activation of unactivated C-H bonds

在本研究中，我们通过亲核的C-H键激活开发了直接催化的不对称加成反应，并在质子转移条件下成功获得了手性四取代碳立体中心的α -氨基酸衍生物。反应在室温或低于室温下进行，各种酸碱敏感官能团在反应条件下是耐受的。我们还对反应进行了详细的机理分析，并分离出催化活性物质。这种活性物质可以缩短反应时间，并与其他活性较低的底物进行反应，以提供含有手性四取代碳立体中心的α -氨基酸衍生物。

Throughout this study, we developed direct catalytic asymmetric addition reactions via nucleophilic C-H bond activation, and we succeeded in obtaining alpha-amino acid derivatives containing chiral tetrasubstituted carbon stereocenters under proton-transfer conditions. The reactions proceed at or below room temperature, and various acid- and base-sensitive functionalities are tolerant under the reaction conditions.We also performed detailed mechanistic analysis of the reaction and isolated catalytically active species. This active species enabled shortening reaction time and performing reactions with other less-reactive substrates to provide alpha-amino acid derivatives containing chiral tetrasubstituted carbon stereocenters.