Organic chemistry

Combinatorial chemistry

Catalysis

Medicinal chemistry

Chemistry

Aldehyde

Annulation

European Journal of Organic Chemistry

A Cu 0 ‐catalyzed protocol is proposed for the synthesis of 8‐acylquinolines through a [3+2+1] annulation starting from anthranils and phenylacetaldehydes. This protocol is of particular interest in preparing 8‐aldehyde quinolines, which have been hard to access so far. Both AgOTf and dioxygen played an important role in the reaction. C3‐heterocycle or phenylethylene substituted anthranils could also be employed in the reaction. An interesting esterification of aldehyde was observed.

Copper‐catalyzed [3+2+1] Annulation of Anthranils with Phenylacetaldehydes: Synthesis of 8‐Acylquinolines