Key Laboratory of Green Chemistry and Technology of Ministry of Education, College of Chemistry, Sichuan University , 29 Wangjiang Road, Chengdu 610064, P.R. China.
Org Lett. 2017 Sep 15;19(18):4782-4785. doi: 10.1021/acs.orglett.7b02167. Epub 2017 Aug 30.
The development of the oxidative cross-coupling of unreactive C(sp)-H bonds with (hetero)arene C(sp)-H bonds is considerably appealing, yet conceptually and practically challenging. Here, we disclose the rhodium-catalyzed oxidative heteroarylation of unactivated C(sp)-H bonds with heteroarene C(sp)-H bonds. This method provides a step-economic route to β-heteroarylated 2-ethylpyridine derivatives, which exhibits relatively broad substrate scope, high tolerance level of sensitive functional groups, and high selectivity. The protocol can also be extended to the coupling reaction between 8-methylquinoline derivatives and heteroarenes.
发展惰性 C(sp)-H 键与（杂）芳环 C(sp)-H 键的氧化交叉偶联反应具有相当大的吸引力，但在概念和实践上具有挑战性。在这里，我们公开了铑催化的未活化 C(sp)-H 键与杂芳环 C(sp)-H 键的氧化杂芳基化反应。该方法提供了一条具有经济性的β-杂芳基化 2-乙基吡啶衍生物的途径，具有较宽的底物范围、对敏感官能团的高容忍度和高选择性。该方案还可以扩展到 8-甲基喹啉衍生物与杂芳烃之间的偶联反应。
