The Synthesis of new Derivatives of 1-β-D-Arabinofuranosylcytosine

Abstract

In order to obtain 1-β-D-arabinofuranosylcytosine derivatives with better antitumor effect, 12 kinds of saturated fatty acyl groups were introduced at the N⁴-position of 1-β-D-arabinofuranosylcytosine. The presence of a great excess of water and about two-fold equivalents of carboxylic anhydride was found to be most desirable for selective N⁴-acylation. This simple method of one-step N⁴-acylation should be generally applicable to cytosine nucleosides and a variety of carboxylic anhydrides.