Department of Chemical Engineering and Chemistry, Micro Flow Chemistry & Process Technology, Eindhoven University of Technology, Den Dolech 2, 5612, AZ, Eindhoven, The Netherlands.
Angew Chem Int Ed Engl. 2017 Jun 12;56(25):7161-7165. doi: 10.1002/anie.201703369. Epub 2017 May 22.
Described herein is an effective and practical modular flow design for the meta-selective C-H arylation of anilines. The design consists of four continuous-flow modules (i.e., diaryliodonium salt synthesis, meta-selective C-H arylation, inline copper extraction, and aniline deprotection) which can be operated either individually or consecutively to provide direct access to meta-arylated anilines. With a total residence time of 1 hour, the desired product could be obtained in high yield and excellent purity without the need for column chromatography, and the residual copper content meets the standards for parenterally administered pharmaceutical substances.
本文介绍了一种有效且实用的模块化流动设计，用于苯胺的元选择性 C-H 芳基化反应。该设计由四个连续流动模块（即二芳基碘鎓盐合成、元选择性 C-H 芳基化、在线铜萃取和苯胺脱保护）组成，可以单独或连续操作，从而直接得到间位芳基化的苯胺。在 1 小时的总停留时间内，无需柱层析即可获得高产率和高纯度的目标产物，并且残留的铜含量符合注射用药物物质的标准。
