Shanghai Key Laboratory of Functional Materials Chemistry, Key Laboratory for Advanced Materials and School of Chemistry and Molecular Engineering, East China University of Science and Technology, Meilong Road 130, Shanghai 200237, China.
J Org Chem. 2021 May 21;86(10):7288-7295. doi: 10.1021/acs.joc.1c00637. Epub 2021 May 6.
The direct C-H activation without directing groups can realize the -selectivity, which is a powerful and concise approach for functionalization of arenes. Utilizing the strategy, a C5-olefination of methyleneindolinones has been successfully developed by palladium-catalyzed direct C-H activation, which provides an expeditious access to 5-vinylindolin-2-ones with high regioselectivity. The protocol is distinguished by a mild reaction system avoiding ligand and high temperature. The kinetic isotope experiments indicate that the C-H bond cleavage is the rate-limiting step.
无需导向基团的直接 C-H 活化可以实现选择性，这是芳基功能化的一种强大而简洁的方法。利用该策略，通过钯催化的直接 C-H 活化成功开发了亚甲基吲哚啉酮的 C5-烯丙基化反应，为高区域选择性的 5-乙烯基吲哚啉-2-酮提供了一种快捷的途径。该方案的特点是反应体系温和，无需配体和高温。动力学同位素实验表明，C-H 键的断裂是速率限制步骤。
