4-(aminomethyl)pyrimidin-2-amine hydrochloride synthesis

Yield:929973-95-5 92%

Reaction Conditions:

with ammonia;hydrogen in methanol at 20; under 24377.4 Torr; for 22 h;

Steps:

223 Intermediate 1-11-4

Intermediate 1-11-4
To a solution of 2-aminopyrimidine-4-carbonitrile (1 g, 8.3 mmol) in 7M NH3 in MeOH (25.5 mL) was added Raney-Nickel (50% wet, 1.955 g, 33 mmol) and stirred at RT under an H2 atmosphere (32.5 bar) for 22h. The reaction was filtered and concentrated to give the intermediate 1-11-4 (954 mg, 92%) which was used without further purification.1H-NMR (400 MHz ,DMSO-d6), Shift [ppm]= 3.55 (2H), 6.34-6.54 (2H), 6.63 (1H), 8.09- 8.21 (1H).

References:

WO2015/193339,2015,A1 Location in patent:Page/Page column 321; 322