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Synthesis of Azacarbolines via PhIO2-Promoted Intramolecular Oxidative Cyclization of α-Indolylhydrazones

Journal of Organic Chemistry (2021) 86(24) 17918-17929
DOI: 10.1021/acs.joc.1c02217
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Abstract

An unprecedented synthesis of polysubstituted indole-fused pyridazines (azacarbolines) from α-indolylhydrazones under oxidative conditions using a combination of iodylbenzene (PhIO2) and trifluoroacetic acid (TFA) has been developed. This transformation is conducted without the need for transition metals, harsh conditions, or an inert atmosphere.

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Corrieri, M., De Crescentini, L., Mantellini, F., Mari, G., Santeusanio, S., & Favi, G. (2021). Synthesis of Azacarbolines via PhIO2-Promoted Intramolecular Oxidative Cyclization of α-Indolylhydrazones. Journal of Organic Chemistry, 86(24), 17918–17929. https://doi.org/10.1021/acs.joc.1c02217

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