Synthesis of Tegafur by the Alkylation of 5-Fluorouracil under the Lewis Acid and Metal Salt-Free Conditions

DOI: 10.1021/acs.oprd.7b00103

Source and publish data:

Organic Process Research and Development p. 885 - 889 (2017)

Update date:2022-08-24

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Authors:

Zasada, Aleksandra

Mironiuk-Puchalska, Ewa

Koszytkowska-Stawińska, Mariola

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Article abstract of DOI:10.1021/acs.oprd.7b00103

A novel protocol for preparation of tegafur (a prodrug of 5-fluorouracil) is reported. The process involves the 1,8-diazabicycloundec-7-ene-mediated alkylation of 5-fluorouracil with 2-acetoxytetrahydrofuran at 90 °C, followed by treatment of the prepurified mixture of the alkylation products with aqueous ethanol at 70 °C. The yield of the two-step process is 72%.

Full text of DOI:10.1021/acs.oprd.7b00103

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