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To a solution of ethyl 4-aminopyrimidine-2-carboxylate (840 mg, 5.0 mmol) in anhydrous tetrahydrofuran (50 mL) cooled at −20° C. was added a solution of methylmagnesium bromide in THF (8.5 mL, 25.0 mmol, 3.0 M) over a period of 5 minutes. The reaction mixture was stirred at 0° C. for another 2 h. It was then quenched with saturated NH4Cl (20 mL) and concentrated under reduced pressure. The residue was extracted with ethyl acetate (5×40 mL). The combined organic layer was dried over anhydrous Mg2SO4, filtered, and evaporated under reduced pressure. The residue was purified by reverse-phase Combiflash to afford 264a as yellow solid (240 mg, 32%) MS-ESI: [M+H]+ 154.1

1. customIt was then quenched with saturated NH4Cl (20 mL)
2. concentrationconcentrated under reduced pressure
3. extractionThe residue was extracted with ethyl acetate (5×40 mL)
4. dry with materialThe combined organic layer was dried over anhydrous Mg2SO4
5. filtrationfiltered
6. customevaporated under reduced pressure
7. customThe residue was purified by reverse-phase Combiflash