Ammonia → 4-Amino-5-bromo-2-chloropyrimidine

Participants

Reaction Steps

2,4-Dichloro-5-bromopyrimidine (200 g, 0.88 mol) is added slowly to NH3 (1000 ml, 7 M in MeOH) while the reaction mixture is kept below 10° C. The reaction mixture is stirred at rt for 2 h, heated to 60° C. for 2 h, and then cooled again to rt and stirred for 55 h. It is concentrated under reduced pressure, and the residue is suspended in H2O (500 ml). The aqueous layer is extracted with EtOAc (3×) and the combined organic layers are dried over MgSO4, filtered, and concentrated under reduced pressure to yield the title compound as a white solid.

Provenance & Evidence