Synthesis of Pyrazolofuropyrazine via One-Pot S N Ar Reaction and Intramolecular Direct C-H Arylation

Shinichiro Fuse, Megumi Inaba, Shinichi Sato, Manjusha Joshi, Hiroyuki Nakamura

研究成果: Article

2 引用 (Scopus)

抜粋

Fused-ring systems containing heterocycles are attractive templates for drug discovery. Biologically active 6-5-5+6 fused-ring systems that possess heterocycles are available, but these require a relatively large number of synthetic steps for preparation. Therefore, pyrazolofuropyrazine was designed as a 6-5-5+6 ring system template that incorporates ready accessibility for drug discovery. Pyrazolofuropyrazines were successfully constructed in only a few steps via one-pot S N Ar reaction/intramolecular C-H direct arylation. As a drug candidate, pyrazolofuropyrazine has earned a favorable LogP, although significant biological activity has yet to be established; the ready accessibility of pyrazolofuropyrazine template, however, offers an opportunity for the rapid development of promising new drug candidates.

元の言語English
記事番号ss-2017-f0762-op
ページ(範囲)1493-1498
ページ数6
ジャーナルSynthesis (Germany)
50
発行部数7
DOI
出版物ステータスPublished - 2018 4 3
外部発表Yes

ASJC Scopus subject areas

  • Catalysis
  • Organic Chemistry

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