SYNTHESIS OF O~2- AND N~3-(2-PHOSPHONOMETHOXY)ETHYL DERIVATIVES OF 6-PHENYL- AND 6-PYRIDINYL-5-AZACYTOSINE

摘要

A series of hydrolytically stable O`2- and N~3-(2-phosphonomethoxy)-ethyl (PME) derivatives of 6-phenyl, pyridin-2, -3 and -4-yl-5-azacytosines was prepared by their alkylation with diisopropyl (2-chloroethoxy)methylphosphonate followed by the deprotection. No antitumor or antiviral activity was found except for 6-(pyridin-4-yl)-l,3,5-triazine-2,4-diamine (13d) which exhibited slight activity against feline herpesvirus in CrFK cell cultures with IC50 = 6.7 μg/mL.