(S)-2-((2,6-dichloropyrimidin-4-yl)amino)propan-1-ol synthesis

Yield:-

Reaction Conditions:

with triethylamine in acetonitrile at 0 - 20; for 12 h;

Steps:

(S)-2-((2,6-dichloropyrimidin-4-yl)amino)propan-l-ol

(S)-2-((2,6-dichloropyrimidin-4-yl)amino)propan-l-ol To a solution of 2,4,6-trichloropyrimidine (4.70 g, 25.6 mmol) and triethylamine (7.78 g, 77.0 mmol) in acetonitrile (150 mL) was added a solution of (S)-2-aminopropan-l -ol (2.31 g, 30.7 mmol) in acetonitrile (150 mL) at 0 °C. The reaction mixture was allowed to room temperature and stirred for 12 h, then filtered and concentrated. Purification via column chromatography (elutriant: petroleum ether/ethyl acetate = 4/1) afforded the title product. LC-MS (ESI): m/z 222 [M + H]⁺; 0.86 min (ret time).

References:

WO2014/114694,2014,A1 Location in patent:Page/Page column 29