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

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)


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.

Original languageEnglish
Article numberss-2017-f0762-op
Pages (from-to)1493-1498
Number of pages6
JournalSynthesis (Germany)
Issue number7
Publication statusPublished - 2018 Apr 3


  • C-H activation
  • antitumor agents
  • cyclization
  • fused-ring systems
  • heterocycles

ASJC Scopus subject areas

  • Catalysis
  • Organic Chemistry

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