Formal [1 + 2 + 3] Annulation of Anilines and CF₃‑Containing Ynones via 6π-Electrocyclization.

ABSTRACT: Six-membered N-heterocycles, such as 2-pyridones, are crucial in bioactive compounds and prevalent in natural products and pharmaceuticals, necessitating innovative synthesis approaches. Traditional methods, typically reliant on the transition-metal-catalyzed direct cyclization of alkynes, face limitations in product complexity. This study introduces a [1 + 2 + 3] annulation strategy for synthesizing 2-pyridones, employing anilines and CF₃-ynones through a base-promoted metal-free catalytic system. This method offers a more streamlined approach to generating polysubstituted 2-pyridones, demonstrating enhanced functional group compatibility across substrates compared with existing transformations. The anilines' adjacent dialkyl amino groups significantly contribute to the

SUBMITTER: Feng L 

PROVIDER: S-EPMC12308597 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature