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 58139-04-1 as follows. Recommanded Product: 2-Iodo-3-methoxypyrazine
Intermediate 25 (0.15 g, 0.622 mmol) was dissolved in 1,4-dioxane (6 mL). 2-Iodo-3- methoxypyrazine (0.12 g, 0.508 mmol), cesium carbonate (0.405 g, 1.244 mmol, Iota, – bis(diphenylphosphino)ferrocene (0.052 g, 0.093 mmol) and tris(dibenzylideneacetone) dipalladium(0) (0.028 g, 0.031 mmol) were added. The reaction tube was sealed and the mixture was stirred at 160 C for 1 hour under microwave irradiation. After cooling, the reaction mixture was diluted with DCM and filtered over dicalite. The filtrate was concentrated in vacuo. The crude product was purified by flash column chromatography (silica gel; eluent: 7 M solution of ammonia in methanol/DCM 0/100 to 5/95). The desired fractions were collected and concentrated. This crude was further purified by preparative HPLC on (Chiralpal Diacel AS 20x250mm). Mobile phase (C02, MeOH with 0.2% iPrNH2) to yield compound 8 (0.010 g, 5% yield).
According to the analysis of related databases, 58139-04-1, the application of this compound in the production field has become more and more popular.
Reference:
Patent; JANSSEN PHARMACEUTICA NV; GIJSEN, Henricus, Jacobus, Maria; VAN BRANDT, Sven, Franciscus, Anna; WO2013/83556; (2013); A1;,
Pyrazine – Wikipedia,
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