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  Direct and Practical Synthesis of Primary Anilines through Iron-Catalyzed C–H Bond Amination

Legnani, L., Prina Cerai, G., & Morandi, B. (2016). Direct and Practical Synthesis of Primary Anilines through Iron-Catalyzed C–H Bond Amination. ACS Catalysis, 6(12), 8162-8165. doi:10.1021/acscatal.6b02576.

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 Creators:
Legnani, Luca1, Author              
Prina Cerai, Gabriele1, Author              
Morandi, Bill1, Author              
Affiliations:
1Research Group Morandi, Max-Planck-Institut für Kohlenforschung, Max Planck Society, ou_2040309              

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Free keywords: amination; aniline; C−H functionalization; iron; late-stage functionalization; PG free
 Abstract: The direct C–H amination of arenes is an important strategy to streamline the discovery and preparation of functional molecules. Herein, we report an operationally simple arene C–H amination reaction that, in contrast to most literature precedent, affords directly the synthetically versatile primary aniline products without relying on protecting group manipulations. Inexpensive Fe(II)-sulfate serves as a convenient catalyst for the transformation. The reaction tolerates a wide scope of arenes, including structurally complex drugs. Importantly, the arene substrates are used as limiting reagents in the transformation. This operationally simple transformation should considerably accelerate the discovery of medicines and functional molecules.

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Language(s): eng - English
 Dates: 2016-09-082016-10-312016-12-02
 Publication Status: Published in print
 Pages: 4
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1021/acscatal.6b02576
 Degree: -

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Title: ACS Catalysis
  Abbreviation : ACS Catal.
Source Genre: Journal
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Publ. Info: Washington, DC : ACS
Pages: - Volume / Issue: 6 (12) Sequence Number: - Start / End Page: 8162 - 8165 Identifier: ISSN: 2155-5435
CoNE: https://pure.mpg.de/cone/journals/resource/2155-5435