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A Modular Flow Design for the meta-Selective C-H Arylation of Anilines.

ABSTRACT: 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.

SUBMITTER: Gemoets HPL

PROVIDER: S-EPMC5488246 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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A Modular Flow Design for the meta-Selective C-H Arylation of Anilines.

Gemoets Hannes P L HPL Laudadio Gabriele G Verstraete Kirsten K Hessel Volker V Noël Timothy T

Angewandte Chemie (International ed. in English) 20170522 25

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 excel ...[more]

PMID: 28543979

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