An aerobic oxidative aromatization of simple aliphatic alcohols and anilines under the Pd(OAc)₂/2,4,6-Collidine/Brønsted acid catalytic system has been established, providing a direct approach for the preparation of diverse substituted quinoline derivatives in high yields with wide functional group tolerance. Practically, the protocol can be easily scaled up to gram-scale and was utilized in the concise formal synthesis of a promising herbicide candidate.