5-fluoro-3,4-dihydro-2,4-dioxo-N-(3-indolyl)-1(2H)-pyrimidinecarboxamides
AssigneeChisso Corporation
InventorsRyo Yoshizawa, Masatoshi Kawashima, Hitoshi Yano
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AssigneeChisso Corporation
InventorsRyo Yoshizawa, Masatoshi Kawashima, Hitoshi Yano
Estimating the term…
5-Fluorouracil derivatives of this invention are represented by the general formula: ##STR1## wherein R indicates an alkylene group having 1-8 carbon atoms, A indicates an atomic group of --NH-- and --CO--, n is 0 or 1, and Y indicates an alkyl group having 1-10 carbon atoms, an aryl group, a heteroaryl group, a pyridinium ion having a halogen as a pair ion or an isocyanate group. These derivatives are useful as anticancer medicines and intermediates therefor. These derivatives are produced by six specified methods of this invention. A representative method is a process which comprises reacting 5-fluorouracil and an isocyanate represented by a general formula: Y--(A)n--R--NCO (VII) wherein R, A, n and Y are the same as those indicated in the formula (I).
A compound of the formula ##STR38## wherein R is a covalent bond, --CH.sub.2, --(CH.sub.2).sub.2 -- or --CH(COOC.sub.2 H.sub.5)CH.sub.2 --;
Dependencies are inferred from the claim text.
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With other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring…:…
Containing two hetero rings: linked by a chain containing hetero atoms as chain links
Containing two hetero rings: linked by a chain containing hetero atoms as chain links
Containing two hetero rings: linked by a chain containing hetero atoms as chain links
Term ended 2 Apr 2007 (estimated)
USPTO file history isn’t available for this patent, so only indexed dates are shown.
1. Fields of the Invention
This invention relates to new 5-fluorouracil derivatives useful for an anticancer medicine or intermediates thereof and processes for producing thereof.
2. Description of the Prior Art
The following examples illustrate this invention more specifically.
5-Fluoro-3,4-dihydro-2,4-dioxo-N-(2-thienyl)-1(2H-pyrimidinecarboxamide: ##STR12##
2-Thienyl isocyanate (3.09 g, 24.7 mmol) and 5-fluorouracil (3.21 g, 24.7 mmol) were added into a solvent of benzene (50 ml) and pyridine (20 ml), and stirred and refluxed at 80.degree. C. for 16 hours.