Title:
TRIFLUOROTHYMIDINE DERIVATIVE, ITS PR0DUCTI0N AND ANTITUMOR AGENT CONTAINING THE SAME DERIVATIVE
Document Type and Number:
Japanese Patent JP3040200
Kind Code:
B2
Abstract:
PURPOSE: To obtain the subject new derivative useful as an antitumor agent, having low toxicity and strong antitumor activity, industrially and advantageously by reacting a specific trifluorothymidine derivative with an aldose derivative.
CONSTITUTION: α, α, α-Trifluorothymidine shown by formula I is made to react with chloro-t-butyldimethylsilane, etc., in the presence of imidazole in dimethylformamide to give an α, α, α-trifluorothymidine derivative shown by formula II [R1 is substituted silyl or (substituted)trityl], which is reacted with an aldose derivative shown by the formula R2-Y [R2 is (substituted)aldose residue, lower acyl, (substituted)benzoyl or phthaloylamino group-substituted deoxyaldose residue] or formula III to give the objective derivative [3'-O-(2,3,4,6- tetra-O-benzyl-β-D-glucopyranosyl)-@α, α, α-trifluorothymidine] shown by formula IV.
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Inventors:
Fukazawa, Nobuyuki
Komatsu, Hironori
Kawauchi, Keiya
Iwata, Daiji
Nakanishi, Osamu
Yano, Osamu
Komatsu, Hironori
Kawauchi, Keiya
Iwata, Daiji
Nakanishi, Osamu
Yano, Osamu
Application Number:
JP16298291A
Publication Date:
May 08, 2000
Filing Date:
July 03, 1991
Export Citation:
Assignee:
MITSUI TOATSU CHEM INC
International Classes:
A61K31/70; A61K31/7042; A61K31/7052; A61K31/7064; A61K31/7072; A61P35/00; C07H19/073; (IPC1-7): C07H19/073; A61K31/7072; A61P35/00