Application of 912773-21-8, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 912773-21-8 name is 2-Bromo-5-chloropyrazine, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.
A mixture of 5-(4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2- yl)-2-[(lS)-2,2,2-trifluoro-l-methyl-ethoxy]pyridine (600 mg, 1.89 mmol), 2-bromo-5- chloro-pyrazine (329.39 mg, 1.7 mmol), Pd(dppf)Cl2 (207.67 mg, 0.28 mmol) and CS2CO3 (1232.88 mg, 3.78 mmol) in l,4-Dioxane (15 mL) and Water (1.5 mL) was stirred at 60 C for 5 hours under N2. After cooling to room temperature, the mixture was concentrated to give the residue. The residue was diluted with FLO (20 mL), and the mixture was extracted with EtOAc (30 mL x 2). The combined organic phase was washed with water (20 mL) and brine (20 mL), dried over Na2S04,filtered and concentrated to give the crude product. The crude product was purified by flash chromatography on silica gel (EtOAc in PE = 0% to 3%) to give the product (350 mg, 1.15 mmol, 61% yield) as an oil. LCMS Rt= 0.95 min in 1.5 min chromatography, 5-95 AB, MS ESI calcd. for C i HioCIFiN iO [M+H]+304.0, found 304.1.
At the same time, in my other blogs, there are other synthetic methods of this type of compound, 2-Bromo-5-chloropyrazine, and friends who are interested can also refer to it.
Reference:
Patent; PRAXIS PRECISION MEDICINES, INC.; GRIFFIN, Andrew, Mark; MARRON, Brian, Edward; MARTINEZ BOTELLA, Gabriel; REDDY, Kiran; WITTMANN, Marion; (0 pag.)WO2019/232209; (2019); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem