5-Fluorouracil → Tegafur

Participants

Reaction Steps

In 100 ml of pyridine were dissolved 13.0 g of 5-fluorouracil and 10.5 g of 2,3-dihydrofuran. To the solution were added 7.5 g of alumina and the mixture was reacted at 130° C. for 24 hours. After completion of the reaction, the reaction liquid was filtered to remove the catalyst and the solvent was distilled off. The residue was dissolved in chloroform to recover 3.04 g of insoluble unreacted 5-fluorouracil. The chloroform was distilled off from the chloroform layer and the residue was recrystallized from ethanol to give 13.52 g of 1-(2-tetrahydrofuryl)-5-fluorouracil. The yield of the end product was 88.9% based on the consumed 5-fluorouracil.

Provenance & Evidence