A method for the acetylation of the exocyclic amino group of guanine d
erivatives has been developed. A series of N-2-acetylguanines was synt
hesized by reacting of N-9(7)-alkoxyalkylguanines with an excess of ac
etic anhydride in the presence of 4-dimethylaminopyridine. The method
has been used successfully also for N-2-acetylation of guanosine and i
ts 8-bromo derivative although in the latter case a partial substituti
on of bromine for a hydroxy group at the position 8 of the heterocycle
occurred.