| 摘要 |
<p>NEW MATERIAL:The compound of formula I [R<1> is 1-20C aliphatic acyl or (substituted) aromatic acyl; R<2> is H or OH-protecting group; R<3> is H or benzhydryl]. EXAMPLE:A carcinostatic agent having antitumor activity especially against cancer cells having Ara-C resistance. PROCESS:The compound of formula I a can be prepared, e.g. by reacting 3-deazauridine of formula II with diphenyl diazomethane in an inert solvent (e.g. hydrated acetone), reacting the obtained compound of formula III with an acid such as p-toluenesulfonic acid and ethyl orthoacetate in e.g. acetone, and acylating the resultant compound of formula IV. The obtained compound of formula I a can be converted to the compound of formula I b by removing the benzhydryl group and/or isopropylidene group therefrom.</p> |
