5-Fluorouracil → Tegafur

Participants

Reaction Steps

In 50 ml of pyridine were dissolved 2.5 g of 5-fluorouracil and 2.4 g of pyridine hydrochloride. To this solution were added 4.5 ml of 2,3-dihydrofuran in 4 portions and the mixture was reacted for 20 hours at 120° C. in an oil bath. After the reaction, a small amount of the reaction liquid was extracted and subjected to thin layer chromatography to check the state of preceeding of the reaction whereby the composition of the product was 90% of the end product, 5% of unreacted 5-fluorouracil and 5% of by-products. The reaction liquid was treated in the same manner as described in Example 7 to obtain 2.6 g of 1-(2-tetrahydrofuryl)-5-fluorouracil. The yield of the end product was 70% based on the initially used 5-fluorouracil.

Provenance & Evidence