tert-butyl (pyrazin-2-yl)methylcarbamate synthesis

Yield:1026790-47-5 100%

Reaction Conditions:

in isopropyl alcohol at 20; for 2 h;

Steps:

20 Synthesis of pyrazin-2-ylmethyl-carbamic acid tert-butyl ester (Compound AA)

To a solution of 2-aminomethyl-pyrazine (5.0 g, 45.87 mmol) in isopropanol (50 ml) was added di-tert-butyl-pyrocarbonate (12.0 g, 55.84 mmol); the mixture was stirred at ambient temperature for 2 h. Next, the solvent was evaporatedand the residue was dissolved in DCM (30 ml), and subjected to silica gel purification (chloroformlmethanol gradient 0-30% in 100 mm.). Fractions containing desired product were combined and evaporated. Residue was dried under vacuum to provide Compound AA in quantitative yield(10.22 g, 99% purity) as amorphous solid. LC-MS: (mlz) observed (M+H) 210.5 (C10H15N302+H calc: 210.3)

References:

US9139612,2015,B2 Location in patent:Page/Page column 151