State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, People's Republic of China.
Chem Commun (Camb). 2019 Dec 5;55(98):14813-14816. doi: 10.1039/c9cc08056b.
Herein, we describe a protocol for alkylation reactions of C(sp3)-H bonds with diacyl peroxides by means of a process involving cross-coupling between an alkyl radical and an α-aminoalkyl radical. The mild, catalyst- and additive-free conditions make this protocol superior to previously reported C(sp3)-H alkylation strategies. The protocol was applied to 1,2,3,4-tetrahydroisoquinolines and a tetrahydro-β-carboline derivative and could be carried out on a gram scale, indicating its utility for the alkylation of late-stage synthetic intermediates.
在此，我们描述了一种通过烷基自由基与α-氨烷基自由基交叉偶联来实现二酰基过氧化物与 C(sp3)-H 键烷基化反应的方法。温和的、无催化剂和添加剂的条件使该方法优于先前报道的 C(sp3)-H 烷基化策略。该方法适用于 1,2,3,4-四氢异喹啉和四氢-β-咔啉衍生物，并可在克级规模上进行，表明其可用于后期合成中间体的烷基化。
