Pd-Catalyzed Direct C-H Activation for the C5-Olefination of Methyleneindolinones
Pd-Catalyzed Direct C-H Activation for the C5-Olefination of Methyleneindolinones
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Pd 催化直接 C-H 活化亚甲基二氢吲哚酮的 C5-烯化反应
DOI：
10.1021/acs.joc.1c00637
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发表时间：
2021
影响因子：
3.6
通讯作者：
Liu Pei-Nian
中科院分区：
文献类型：
--
作者：
Xu Xian-Kuan;Liu Jian-Wei;Li Deng-Yuan;Liu Pei-Nian
不带导向基团的C-H直接活化可以实现对位选择性，是芳烃功能化的一种有效而简洁的方法。利用这一策略，钯催化的C-H直接活化法成功地发展了亚甲基吲哚啉酮的C5-烯化反应，该反应提供了高区域选择性地快速获得5-乙烯基吲哚啉-2-酮的途径。该方法的特点是反应体系温和，避免了配体和高温。动力学同位素实验表明，C-H键断裂是反应的限速步骤。
The direct C–H activation without directing groups can realize thepara-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.