Single‐Step Synthesis of 3‐Iodoquinolines from 2‐Aminophenyl Ketones through a Regioselective (6‐endo‐dig) Electrophilic Cyclization

다국어 초록 (Multilingual Abstract)

A highly facile single‐step synthetic approach to 3‐iodoquinolines has been developed for the first time from readily available 2‐aminobenzophenones and terminal alkynes. The reaction involves the nucleophilic addition of terminal alkynes to 2‐aminobenzophenones followed by a regioselective iodocyclization (6‐endo‐dig) to furnish 2,4‐disubstituted 3‐iodoquinolines in high yields. In general, 2,4‐diaryl‐substituted products were isolated without the need for column chromatography.
A single‐step approach to the synthesis of 3‐iodoquinolines has been achieved through a regioselective iodocyclization. The synthesis began from readily available materials in an aqueous ethyl acetate medium and was promoted by KOtBu and I2 at room temperature. Various cross‐coupling reactions were used to demonstrate the synthetic utility of the products.