Application of 4858-85-9, A common heterocyclic compound, 4858-85-9, name is 2,3-Dichloropyrazine, molecular formula is C4H2Cl2N2, its 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.
2,3-Dichloro-pyrazine (1.48 g, 0.01 mol),and Ethynyl-benzene (1.53 g, 0.015 mol) was added in a lOOmL flask which contained 30mL of Et3N with stirring, and then the catalyst of Cul(0.38 g, 0.002 mol)and Pd(PPh3) 2C12(2 g, 0.002 mol) was added into the mixture. The reaction mixture was warmed to 80C for 0.5h, lc-ms indicated 2,3-Dichloro-pyrazine was consumed. The reaction mixture was cooled to room temperature. Filtrated, the filtrate was concentrated to give the crude product, the crude product was further purified by flash chromatography to afford 2-Chloro-3-phenylethynyl-pyrazine. (1.5 g, yield: 71%). LC/MS (ESI+): 215 [M+l]+ 217 [ +3]+
The synthetic route of 4858-85-9 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; SKELTON, Nicholas; GRADL, Stefan; BLAKE, James F.; GRAHAM, James M.; GUNAWARDANA, Indrani W.; HENTEMANN, Martin; MARLOW, Allison L.; TANG, Tony P.; WO2013/78254; (2013); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem