Funai Yakuhin Kogyo Kabushiki Kaisha

Funai Kakuhin Kogyo Kabushiki Kaisha

Iwao Hashimoto

Setsuro Fujii

Masahiro Kawasaki

Bompei Yasui

Tomohisa Miyamoto

Kazuko Ando

Naoki Umeda

Mitsuo Nakamura

Mitsuru Hirohashi

Masatoshi Shiga

Yoichiro Kawai

Yuji Mino

Yoneichi Sawai

2'-Deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine derivatives possessing strong anti-tumor activity with weak toxicity and represented by the general formula: ##STR1## wherein R stands for an alkyl group, an alkoxy group or a halogen atom, m for zero or an integer of 1-3, and n for an integer of 1-14, with the proviso that when m is 2 or 3, R's may be the same or different and that when m is 2 and the adjacent two R's are alkoxy groups, the two alkyl moieties of the alkoxy groups may be combined to form together with the two adjacent oxa bridging members an alkylenedioxy group as a whole. These derivatives are prepared by acylating a 2'-deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine with corresponding benzoyl halides and are useful as active ingredients for anti-tumor agents, especially for oral administration.

2'-Deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine derivatives, a process

New ester derivatives of alkoxybenzoyldeoxyfluorouridine of the general formula ##STR1## wherein R stands for an alkoxy group having 1 to 4 carbon atoms, m for 1 or 2, and n for 3 or 4 with the proviso that when m is 2, the adjacent two R's may be combined to form an alkylenedioxy group as a whole. These derivatives are prepared by acylating a 2'-deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine with corresponding benzoyl halides and are useful as active ingredients for anti-tumor agents, especially for oral administration.

Ester derivatives of alkoxybenzoyldeoxyfluorouridine

New ester derivatives of deoxyfluorouridine of the general formula: ##STR1## wherein R and R.sup.40, may be identical or different, and may be hydrogen, halogen or methyl and n is 3 or 4. These derivatives are prepared by acylating a 2'-deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine with corresponding benzoyl halides and are useful as active ingredients for anti-tumor agents, especially for oral administeration.

Ester derivatives of deoxyfluorouridine

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Osaka, Japan

Iwao Hashimoto