8-FLUORO-3-IODOQUINOLINE synthesis

Yield: 76%

Reaction Conditions:

with N-chloro-succinimide;acetic acid;potassium iodide at 85; for 36 h;Temperature;

Steps:

5 Example 5 Preparation of 3-Iodo-8-fluoroquinoline
To a 3L reaction flask, anhydrous acetic acid (1128 g) and N-chlorosuccinimide (256 g, 1.92 mol) were added in batches. Potassium iodide (319 g, 1.92 mol) was added and after completion of the addition, stirred at 30° C. for 1 hour. 8-fluoroquinoline (141 g, 0.96 mol) was added The 8-fluoroquinoline prepared in Example 2 was heated to 85°C and stirred for 36 hours. The aqueous sodium sulfite solution quenches the reaction, After cooling to room temperature and filtering, the resulting solid was washed with water and dried in vacuo to give 3-iodo-8-fluoroquinoline (198 g).76%, gas chromatographic content >99.8%.

References:

Jinkai (Liaoning) Chemical Co., Ltd.;Li Zhenwei;Zhao Yang;Li Degang;Liu Haisheng;Wang Dong;Song Tongji;He Bingshu;Huang Fengting CN107698503, 2018, A Location in patent:Paragraph 0073-0084