YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
受賞総説
ベンザインの効率的発生法の開発
高木 晃
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ジャーナル フリー

2018 年 138 巻 1 号 p. 27-35

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 2-[(Neopentyl glycolato)boryl]phenyl triflates, readily synthesized from 2-iodophenol derivatives via halogen-magnesium exchange or Miyaura borylation, were developed as new benzyne precursors. Benzynes were generated under fluoride-ion-mediated conditions and reacted immediately with various arynophiles. Herein, we describe the generation of benzynes having reactive functional groups, such as methoxycarbonyl, acetyl, bromo, and amino groups, as well as their [4+2], (3+2), and [2+2] cycloaddition reactions which produce corresponding benzo-fused compounds.

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© 2018 The Pharmaceutical Society of Japan
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