4.7 Article

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

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CHEMICAL COMMUNICATIONS
卷 59, 期 46, 页码 7084-7087

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ROYAL SOC CHEMISTRY
DOI: 10.1039/d3cc01050c

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In this study, the first microwave-assisted remote-C-H functionalization was achieved with the help of a simple nitrile directing template. This method exhibited a wide range of substrate scope by enabling meta-C-H arylation, acetoxylation, and cyanation. Moreover, the microwave-accelerated meta-C-H functionalization was highly efficient with short reaction times and preserved the yield and site selectivity. Additionally, the diversification of the ibuprofen drug was successfully achieved through arylation, acetoxylation, and cyanation. Importantly, the study presented a new method for meta-dual-hetero functionalization.
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 via enabling meta-C-H arylation, acetoxylation, and cyanation. Significantly, the microwave-accelerated meta-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, meta-dual-hetero functionalization has been presented.

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