Electric Literature of 77992-44-0, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 77992-44-0 as follows.
INTERMEDIATE 1N-(5-Bromopyridin-2-yl)-2-[2-(difluoromethoxy)phenyllacetohydrazideTo a stirred solution of 2-(difluoromethoxy)phenylacetic acid (3.0 g, 14.85 mmol) in DCM (10 mL) at 0C was added triethylamine (4.4 g, 44.5 mmol), followed by EDCI (3.4 g, 21.90 mmol). The reaction mixture was stirred at 0C for 30 minutes. 5-Bromo-2- hydrazinopyridine (3.07 g, 16.4 mmol) was added and the reaction mixture was stirred at room temperature for 12 h, then diluted with DCM. The organic layer was washed with H20 and brine, then concentrated in vacuo. The crude material obtained was triturated with pentane and Et20 to give the title compound (3.90 g, 70%), which was used for the next reaction without any further purification. deltaEta (400 MHz, DMSO-d6) 10.09-9.90 (m, 1H), 8.67-8.44 (m, 1H), 8.12 (d, 1H, J2.4 Hz), 7.66 (dd, 1H, J 9.0, 2.4 Hz), 7.41 (dd, 1H, J7.6, 1.8 Hz), 7.37-7.26 (m, 1H), 7.26-7.09 (m, 3H), 6.58 (d, 1H, J 8.9 Hz), 3.58 (s, 2H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,77992-44-0, its application will become more common.
Reference:
Patent; UCB BIOPHARMA SPRL; BROOKINGS, Daniel Christopher; JACKSON, Victoria Elizabeth; WO2015/86496; (2015); A1;,
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