Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Microflow Fluorinations of Benzynes: Efficient Synthesis of Fluoroaromatic Compounds
Takashi Ikawa Shigeaki MasudaShuji Akai
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2018 Volume 66 Issue 12 Pages 1153-1164

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Abstract

Fluorinated aromatic compounds are found in a variety of biologically active compounds, including clinical drugs and agrochemicals. Therefore, the synthesis of aryl fluorides is particularly important in the medicinal and process chemistry fields. In this paper, we report a method for the synthesis of aryl fluorides by benzyne fluorination under microflow conditions using the efficient Comet X-01 micromixer. In comparison to our previously reported method under ordinary batch conditions, this approach facilitates a significant reduction in reaction times, to ca. 10 s, as well as increases in the yields of fluoroarenes (by up to 51%).

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© 2018 The Pharmaceutical Society of Japan
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