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- Title
Concise and Efficient Access to 5,7-Disubstituted Pyrazolo[1,5-a]pyrimidines by Pd-Catalyzed Sequential Arylation, Alkynylation and SN<sub>Ar</sub>Reaction.
- Authors
Jismy, Badr; Guillaumet, Gérald; Allouchi, Hassan; Akssira, Mohamed; Abarbri, Mohamed
- Abstract
A simple and efficient method for synthesis of 5,7- disubstituted pyrazolo[1,5-a]pyrimidines is reported. The synthetic route involved first a one-pot two-step synthesis of 7- substituted pyrazolo[1,5-a]pyrimidin-5-ones from the reaction of 3-aminopyrazole 1 with activated alkynes. These compounds were used as key intermediates to access, with excellent yields, a library of new 5,7-disubstituted pyrazolo[1,5-a]pyrimidines, which are known for their wide range of biological activities, through C-O bond activation with PyBroP (bromotripyrrolidinophosphonium hexafluorophosphate) as an activator reagent.
- Subjects
PALLADIUM catalysts; ARYLATION; PYRIMIDINES; INTERMEDIATES (Chemistry); ALKYNES
- Publication
European Journal of Organic Chemistry, 2017, Vol 2017, Issue 41, p6168
- ISSN
1434-193X
- Publication type
Article
- DOI
10.1002/ejoc.201701024