PROCESS FOR PREPARING 2'-DEOXY-5-SUBSTITUTED URIDINE DERIVATIVES

摘要

2'-Deoxy-5-substd. uridine derivs. (I) [R1=H, benzoyl, tetrahydrofuranyl; R2=F, trifluoromethyl; R3,R4=The one is H, the other is alkyl, alkenyl or benzyl group! are prepd. for use as a medicine for a tumor. 1 g of 2'-deoxy-5-trifluoromethyl uridine is dissolved into 15 ml of 1,4-dioxane, and 2.50 g of bis-(alpha, alpha- dimethylbenzyloxy)methane and 38 mg of anhydrous toluene sulfonic acid are added into the soln.. This mixt. is stirred for 3.5 hrs. at 60≦̸C, and then distilled. The residues are seperated by silicagel column chromato graphy to give 0.40g of 2'-deoxy-5'0-(alpha, alpha- dimethylbenzyl)-5-trifluoromethyl uridine and 0.28g of 2'-deoxy-3'-0- (alpha, alpha-dimethylbenzyl)-5-trifluoromethyl uridine.