Synthesis and biological activity of 1-(2-deoxy-2-C-fluoromethyl- and 2-C-hydroxymethylarabinofuranosyl)-cytosines.
We newly synthesized 1-(2-deoxy-2-C-fluoromethyl- and 2-C-hydroxymethyl-arabinofuranosyl)cytosines and evaluated their biological activities. The syntheses of these compounds were achieved by radical deoxygenation of tert-alcohol of 2'-position of the corresponding fluorohydrine and acetoxymethyl derivative. 1-(2-Deoxy-2-C-fluoromethylarabinofuranosyl)cytosine (5) showed potent antileukemic and anticytomegalovirus activities.