7-Azaindoles are versatile building blocks, especially in medicinal chemistry, where they serve as
bioisosteres of indoles or purines. Herein, we are presenting a robust and flexible synthesis of 1,3- and
1,3,6-substituted 7-azaindoles starting from nicotinic acid derivatives or 2,6-dichloropyridine, respectively.
Microwave heating dramatically accelerates the penultimate reaction step, an epoxide-opening-cyclization-dehydration sequence. The functional group compatibility of the reaction is examined as well as the
application of the products in further functionalizations.
