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Understanding and Interrupting the Fischer Azaindolization Reaction
journal contribution
posted on 2017-10-12, 12:05 authored by Bryan J. Simmons, Marie Hoffmann, Pier Alexandre Champagne, Elias Picazo, Katsuya Yamakawa, Lucas A. Morrill, K. N. Houk, Neil K. GargExperimental
and computational studies pertaining to the Fischer
azaindolization reaction are reported. These studies explain why pyridylhydrazines
are poorly reactive in Fischer indolization reactions, in addition
to the origin of hydrazine substituent effects. Additionally, an interrupted
variant of Fischer azaindolization methodology is disclosed, which
provides a synthetic entryway into fused azaindoline scaffolds.