Concise and Efficient Access to 5,7-Disubstituted Pyrazolo[1,5-a]pyrimidines by Pd-Catalyzed Sequential Arylation, Alkynylation and SNArReaction.

Autor:	Jismy, Badr, Guillaumet, Gérald, Allouchi, Hassan, Akssira, Mohamed, Abarbri, Mohamed
Předmět:	PALLADIUM catalysts ARYLATION PYRIMIDINES INTERMEDIATES (Chemistry) ALKYNES
Zdroj:	European Journal of Organic Chemistry; 11/9/2017, Vol. 2017 Issue 41, p6168-6178, 11p
Abstrakt:	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. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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