摘要 |
Uracil derivs. [I; R1 = H, III(R3 = H, alkyl, aryl; R4 = alkyl, aryl); R2 = II , having anti-cancer activity, were prepd. by reaction of 5-fluorouracil and carboxylic acid α-halogenoalkyl ester (II; X = halogen). Thus, 5-fluorouracil 6.50 g and triethylamine 15.18 g was dissolved in the dimethyl acetamide 50 ml, chloromethylpropionate 6.13 g was dropped for 30 min and then reacted for 2 hr after being left for 12 hr. The reactant was filtered, comprised dimethylacetamide was eliminated, 1-propionyloxymethyl-5-fluorouracil was separated by using silica gel packed column, and then recrystallized to give title compd. (m.p. 105-106oC) 7.93 g.
|