These common heterocyclic compound, 1458-18-0, name is Methyl 3-amino-5,6-dichloropyrazine-2-carboxylate, 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. Recommanded Product: 1458-18-0
To a stirred mixture of methyl 3-amino-5, 6-dichloropyrazine-2-carboxylate (1.5 g, 6.756 nMol, 1 equiv) and (3-fluorophenyl) boronic acid (0.95 g, 6.790 nMol, 1.00 equiv) in 1, 4-dioxane (100 mL) and H 2O (5mL) were added Cs 2CO 3 (6.60 g, 0.020 nMol, 3 equiv) and Pd (dppf) Cl 2 (0.74 g, 0.001 nMol, 0.15 equiv) in portions at room temperature under nitrogen atmosphere. The resulting mixture was stirred for 3 h at 70 C under nitrogen atmosphere. The resulting mixture was filtered, the filter cake was washed with CH 2Cl 2 (1×30 mL) . The filtrate was concentrated under reduced pressure. The residue was purified by silica gel column chromatography, eluted with CH 2Cl 2 /EtOAc (4: 1) to afford methyl 3-amino-6-chloro-5- (3-fluorophenyl) pyrazine-2-carboxylate (900 mg, 47.30%) as a yellow solid. LCMS: m/z (ESI) , [M+H] + = 282.0. 1H-NMR (300 MHz, Chloroform-d) delta 4.03 (3H, s) , 7.22 (1H , m) , 7.41-7.59 (2H , m) , 7.65 (1H , ddd) .
The synthetic route of Methyl 3-amino-5,6-dichloropyrazine-2-carboxylate has been constantly updated, and we look forward to future research findings.