Alkylation of N-2-acetyl-8-bromoguanine with alpha-chloroethers has be
en studied in DMF at room temperature in the presence of K2CO3 or with
out a catalyst. It has been found that N-2-acetyl-8-bromoguanine is mo
re reactive under these conditions than N-2-acetylguanine. In the pres
ence of K2CO3N9- and N-7-alkylated compounds have been obtained. in a
high yield. The substitution of bromine for chlorine in the position 8
of guanine has been observed without the alkaline catalyst. Compounds
synthesized were found to inhibit purine nucleoside phosphorylase (PN
P) from rabbit kidney.