945983-70-0Relevant articles and documents
Synthesis of Pyrazolofuropyrazine via One-Pot S N Ar Reaction and Intramolecular Direct C-H Arylation
Fuse, Shinichiro,Inaba, Megumi,Sato, Shinichi,Joshi, Manjusha,Nakamura, Hiroyuki
, p. 1493 - 1498 (2018/01/17)
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.