Electric Literature of 5521-55-1, These common heterocyclic compound, 5521-55-1, name is 5-Methylpyrazine-2-carboxylic acid, 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.
Example B5Preparation of compound 6: rac-5-methyl-pyrazine-2-carboxylic acid [3-(6-amino-2,4- dimethy 1-3 -oxo -2,3,4,5 -tetrahydro -pyrazin-2-y l)-pheny 1] -amide5-Methylpyrazine-2-carboxylic acid (0.014 g, 0.104 mmol) was added to a suspension of intermediate 18 (0.021 g, 0.09 mmol) in DCM (1.5 mL) at room temperature. Then, pyridine (0.01 mL, 0.118 mmol) was added and after stirring at room temperature for 5 minutes HATU (0.038 g, 0.099 mmol) was added. The mixture was stirred at room temperature for 16 hours. The mixture was diluted with water and extracted with DCM. The organic layer was separated, dried (Na2S04), filtered and the solvents evaporated in vacuo. The crude product was purified by flash column chromatography (silica gel; MeOH in DCM 0/100 to 10/90). The desired fractions were collected and concentrated in vacuo. The residue was purified again by flash column chromatography (silica gel; solid injection; 7 M solution of ammonia in methanol in DCM 0/100 to 2/98). The desired fractions were collected and concentrated in vacuo to yield compound 6(0.009 g, 28% yield).
The synthetic route of 5521-55-1 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; JANSSEN PHARMACEUTICA NV; TRABANCO-SUAREZ, Andres, Avelino; TRESADERN, Gary, John; MACDONALD, Gregor, James; VEGA RAMIRO, Juan, Antonio; WO2011/154374; (2011); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem