Palladium-Catalyzed [5 + 2] Rollover Annulation of 1-Benzylpyrazoles with Alkynes: A Direct Entry to Tricyclic 2-Benzazepines

Org. Lett.

8 de maio de 2023 LAbI UFSCar Artigo 0

Palladium-Catalyzed [5 + 2] Rollover Annulation of 1-Benzylpyrazoles with Alkynes: A Direct Entry to Tricyclic 2-Benzazepines

Abstract: The first Pd-catalyzed [5 + 2] rollover annulation of 1-benzylpyrazoles with alkynes to assemble 10H-benzo[e]pyrazolo[1,5-a]azepines (tricyclic 2-benzazepines) has been developed. The rollover annulation implies a twofold C–H activation of aryl and heteroaryl Csp2–H bonds (C–H/C–H) of 1-benzylpyrazoles (five-atom partners) and alkynes to give the [5 + 2] annulated compounds.

Author(s): Suarez-Lustres, A.; Martinez-Yanez, N.; Velasco-Rubio, A.; Varela, J. A.; Saa, C.

Org. Lett.

Published: January 31, 2023

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DOI: https://doi.org/10.1021/acs.orglett.2c04300

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