Synthetic Route of 418762-26-2,Some common heterocyclic compound, 418762-26-2, name is 4-Bromo-2-fluoro-5-methylaniline, molecular formula is C7H7BrFN, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
A suspension of 4-bromo-2-fluoro-5- methylaniline (15 g, 73.5 mmol) in 30 mL of concentrated HCl was added 30 mL of water and a solution of NaN02 (5.33 g, 77.2 mmol) in water (20 mL) was added over a 20 minute period at 0C. This diazonium solution was then brought to pH 6 with NaHC03. In a separate vial, a solution of CuS04 (22.9 g, 91.9 mmol) in water (100 mL) was added dropwise to a solution of KCN (23.9 mg, 368 mmol) in water (100 mL) at 0C, then toluene (100 mL) was added and the mixture was stirred and heated to 60C. The previously prepared diazonium solution was added dropwise to the brown CuCN solution at rt for 1 hour and EtOAc (100 ml) was added. The organic phase was washed with brine (200 mL) and concentrated. The crude product was purified via Prep-TLC to afford the 4-bromo-2-fluoro-5-methylbenzonitrile.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4-Bromo-2-fluoro-5-methylaniline, its application will become more common.
Reference:
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; PIO, Barbara; CHOBANIAN, Harry, R.; SHI, Zhi-Cai; DONG, Shuzhi; GUO, Yan; WALSH, Shawn, P.; GUO, Zhiqiang; FERGUSON, Ronald, D.; CATO, Brian; (114 pag.)WO2016/60941; (2016); A1;,
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