Abstract
The synthesis of a library of 2,6-disubstituted-azaindoles relying on Sonogashira cross-coupling and intramolecular cyclization is described. Eleven examples of 6-alkynyl derivatives and three examples of 3-bromo-5-azaindoles are reported. One of the 3-bromo-5-azaindoles was also further functionalized with two different aryl trifluoroborate salts via Suzuki-Miyaura coupling reaction.
Graphical Abstract
![](/cms/asset/ff3c8738-e641-4d67-9fdd-3fbd52d27ce5/lsyc_a_1545032_uf0001_c.jpg)
Acknowledgments
We thank Professor Regina H. A. Santos from IQSC-USP for the X-ray data collection.