Application of 912773-21-8, 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 912773-21-8 as follows.
A mixture of 2-bromo-5-chloro-pyrazine (1 g, 5.17 mmol), 3-fluoro-5-(4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2-yl)-2-[(lS)-2,2,2-trifluoro-l- methyl -ethoxy ] pyridine (1.73 g, 5.17 mmol), CS2CO3 (3.37 g, 10.34 mmol) and Pd(dppf)Cl2 (567.41 mg, 0.78 mmol) in l,4-Dioxane (100 mL) and Water (10 mL) was stirred at 55 C under N2 for 5 hours. From LCMS, desired MS was observed and no starting material was remained. The solution was cooled to room temperature and concentrated to give a residue. To the residue was added water (50 mL), extracted with EtOAc (50 mL x 2). The combined organic phase was washed with water (50 mL), brine (50 mL x 2), dried over anhydrous Na2S04, filtered and concentrated to give the crude product. The crude product was purified by flash chromatography column on silica gel (EtOAc in PE = 0% to 5%) to give the product (1.4 g,4.35 mmol, 84% yield) as a solid. ‘H NMR (DMSO-c, 400MHz) 5H= 9.18 (s, 1H), 8.91 – 8.74 (m, 2H), 8.46 (dd, 1H), 6.05 – 5.99 (m, 1H), 1.53 (d, 3H).
According to the analysis of related databases, 912773-21-8, the application of this compound in the production field has become more and more popular.
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