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芳基乙酸的功能化 - 导向基团辅助远程 -C-H 活化。

Functionalization of arylacetic acids directing-group-assisted remote -C-H activation.

机构信息

Department of Chemistry, Indian Institute of Technology (IIT), Hyderabad, Kandi, Sangareddy - 502284, Telangana, India.

出版信息

Chem Commun (Camb). 2023 Jun 6;59(46):7084-7087. doi: 10.1039/d3cc01050c.

DOI:10.1039/d3cc01050c
PMID:37218426
Abstract

Herein, we report the first microwave-assisted remote-C-H functionalization aided by a simple nitrile directing template. Notably, the present protocol showed a broad substrate scope enabling -C-H arylation, acetoxylation, and cyanation. Significantly, the microwave-accelerated -C-H functionalization was effective with short reaction times without compromising yields and site selectivity. In addition, ibuprofen drug diversification was accomplished by carrying out arylation, acetoxylation, and cyanation. Importantly, -dual-hetero functionalization has been presented.

摘要

本文报道了首例通过简单腈导向模板辅助的微波辅助远程 C-H 功能化。值得注意的是,本方案具有广泛的底物范围,能够实现 -C-H 芳基化、乙酰氧基化和氰基化。显著的是,微波加速的 -C-H 功能化反应时间短,产率和位点选择性高。此外,通过进行芳基化、乙酰氧基化和氰基化,实现了布洛芬药物的多样化。重要的是,还提出了 - 双重杂芳基化。

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