2'-deoxy-5-fluorouridine derivatives

C - Chemistry – Metallurgy – 07 – H

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C07H 19/06 (2006.01) A61K 31/70 (2006.01) C07H 19/10 (2006.01)

Patent

CA 1313661

\ ABSTRACT 2'-Deoxy-5-fluorouridine derivatives of the formula Image wherein, R1 is hydrogen atom or an acyl group and R2 and R3 are respectively hydrogen atom, an acyl group or a group of the formula Image wherein X1 and X2 are respectively oxygen atom or sulfur atom; R4 is a phenyl group, a benzyl group or a naphthyl group each of which may be substituted by an alkyl group, an alkoxyl group, an alkoxycarbonyl group, an alkyl- thio group, an acyl group, a halogen atom, trifluoromethyl group, nitro group, cyano group, carboxyl group and/or methy- lenedioxy group and R5 is an alkyl group, an alkenyl group or one of the groups represented by R4 which is the same as or different from R4, at least one of R2 and R3 being a group of the formula Image , which exhibit excellent antitumour activities and have lower toxicity, methods of the production thereof and antitumour compositions containing said 2'-deoxy- 5-fluorouridine derivatives.

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