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Published on: June 23, 2019
Microwave-assisted flexible synthesis of 7-azaindoles
1Bayer HealthCare AG, Pharma Research, D-42096 Wuppertal, Germany. hartmut.schirok@bayerhealthcare.com
Abstract:
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.
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