Yield:68210-25-3 84%

Reaction Conditions:

with potassium carbonate in ethanol at 85; for 10 h;

Steps:

i Step-i: Synthesis of 2-isopropylpyrimidin-4(3H)-one

The mixture of methyl 3-methoxyacrylate (4.0g, 34.4mmol), isobutyrimidamide hydrochloride (12.64g, 103.2 mmol) and potassium carbonate (15.2g, 110.1 mmol) in ethanol (50 mL) was stined at 85 °C for 10h. The reaction mixture was filtered through a pad of celite. The filtrate was evaporated under reduced pressure to get 2-isopropylpyrimidin-4(3H)-one (4.0g,84%). ‘H NMR (400 MHz, DMSO-d6): ? 12.37 (br s, 1H), 7.84 (d, J= 6.6 Hz, 1H), 6.14 (d, J=6.6 Hz, 1H), 2.71 - 2.83 (m, 1H), 0.97 (d, J= 6.9 Hz, 6H)); LC-MS: 138.9 [M+H].

References:

WO2016/185342,2016,A1 Location in patent:Page/Page column 44; 45