2-((2-Amino-5-nitropyrimidin-4-yl)amino)ethan-1-ol → 2,5-Diamino-4-(2-hydroxyethylamino)pyrimidine

Participants

Reaction Steps

As shown in reaction scheme (7) below, 2-amino-4-(2-hydroxyethylamino)-5-nitropyrimidine is reacted with a reducing agent, such as Raney-nickel or iron powder, in a polar organic solvent at a temperature of about 0-100° C., and preferably about 30-50° C., for about 1-10 hours, and preferably about 2-5 hours, to give 2,5-diamino-4-(2-hydroxyethylamino)pyrimidine of formula (XXV). Then, the compound of formula (XXV) is allowed to react immediately without separation, in triethylorthoformate of formula (XVIII) at a temperature of about 50-150° C., and preferably about 70-90° C., for about 5-15 hours, and preferably about 8-10 hours, to give 2-amino-9-(2-hydroxyethyl)purine.

Provenance & Evidence