Direct nitration of the corresponding N-oxide of 7-azaindole (2 ) always provides 3- and 4-position regioisomers. Purification of the desired 4-position isomer requires tedious separation which results in a very low yield process. Herein we would like to report a new process toward the synthesis of 4-nitro-7-azaindole (1 ).Starting from 7-azaindole (2 ), > 1 kg of compound 1  can be obtained in a single batch after a five-step sequence, with a total yield of 45-50%.

Improved process for synthesis of 4-nitro-7-azaindole

248th National Meeting (2014)

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