1,1-dibromo-1-alkenes as valuable partners in the copper-catalyzed direct alkynylation of azoles
The copper-catalyzed direct alkynylation of azoles with 1,1-dibromo-1-alkenes as electrophiles is described. These easily accessible substrates are a useful addition to the field of direct alkynylations in an efficient and functional group tolerant reaction to provide a straightforward entry to diverse alkynyl heterocycles.
Copper as a powerful catalyst in the direct alkynylation of azoles
[Chemical equation presented] Copper-bottomed catalysis! The direct alkynylation of azoles through a copper-based C - H bond activation, using alkynylbromides as the coupling partner, has been developed (see scheme). The method is very rapid, is functional-group tolerant, and provides a straightforward entry to diverse alkynyl heterocycles that is complementry to the Sonogashira reaction.
Besselievre, Francois,Piguel, Sandrine
experimental part
p. 9553 - 9556
(2010/03/25)
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