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DOI: 10.1055/s-0036-1591885
Synthesis of Pyrazolofuropyrazine via One-Pot SNAr Reaction and Intramolecular Direct C–H Arylation
Publication History
Received: 26 November 2017
Accepted after revision: 08 December 2017
Publication Date:
11 January 2018 (online)
![](https://www.thieme-connect.de/media/synthesis/201807/lookinside/thumbnails/ss-2017-f0762-op_10-1055_s-0036-1591885-1.jpg)
Abstract
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 SNAr 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.
Supporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0036-1591885.
- Supporting Information
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