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Microwave-Assisted Flexible Synthesis of 7-Azaindoles

Hartmut Schirok

*Bayer HealthCare AG, Pharma Research, D-42096 Wuppertal, Germany, Email:

H. Schirok, J. Org. Chem., 2006, 71, 5538-5545.

DOI: 10.1021/jo060512h


A robust and flexible synthesis of 1,3- and 1,3,6-substituted 7-azaindoles is presented starting from nicotinic acid derivatives or 2,6-dichloropyridine, respectively. Microwave heating dramatically accelerates the penultimate reaction step, an epoxide-opening-cyclization-dehydration sequence.

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Key Words

azaindoles, microwave synthesis, Suzuki coupling

ID: J42-Y2006-2110