Trimethyl phosphite → dimethyl (2-chloro-9-methyl-6-morpholino-9H-purin-8-yl)methylphosphonate

Participants

Reaction Conditions

Reaction Steps

A mixture of 8-bromomethyl-2-chloro-9-methyl-6-morpholin-4-yl-9H-purine (3.92 g, 11 3 mmol) and trimethylphosphite (20 mL, mmol) was heated to reflux (120° C.) for 2 h. The reaction mixture was concentrated in vacuo to a fluorescent green solid which was triturated with H2O. The resulting pale green solid was purified by column chromatography (Si—PCC, MeOH:EtOAc, 0-10%) affording the title compound as a green solid (3.36 g, 79%). LCMS (method A): RT 3.45 min [M+H]+ 376.1

Provenance & Evidence