1978 年 26 巻 3 号 p. 981-984
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.