Process for producing 5-perfluoroalkyluracil derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

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C07D23902

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active

060874996

ABSTRACT:
A novel process is provided for producing a 5-perfluoroalkyl-5,6-dihydrouracil represented by General Formula (1): ##STR1## (where R.sup.1 and R.sup.2 are independently hydrogen, methyl, or ethyl, and Rf is a perfluoroalkyl of 1 to 10 carbons). The process comprises reacting .alpha.-perfluoroalkylacrylic acid represented by General Formula (2):

REFERENCES:
patent: 3502675 (1970-03-01), Duschinsky et al.
Fuchikami et al., "An Effective and Convenient Route to 5-Trifluoromethyl-5-6-dihydrouracils and Their Thio Derivatives," Synthesis, (9), 766-768 (Sep. 1984).
Tandon et al., "Detection of New Metabolites of Trifluridine (F.sub.3 TdR) Using .sup.19 F NMR Spectroscopy," Biochemical Pharmacology, 44(11), 2223-2228 (Dec. 1, 1992).
Heidelberger et al., "Syntheses of 5-Trifluoromethyluracil and 5-Trifluoromethyl-2'-deoxyuridine," J. Medicinal Chemistry, 7(1), 1-5 (Jan. 8, 1964).

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