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Title:
FLUORO-NAPHTHACENEDIONE, ITS GLYCOSILATED DERIVATIVE AND ITS MANUFACTURE PROCEDURE
Document Type and Number:
Japanese Patent JPH03209343
Kind Code:
A
Abstract:

NEW MATERIAL: A compd. of formula I (X is H, OH; one of R, R1 is H and the other is F; R2 is H, OH, alkoxy).

EXAMPLE: 2β-acetyl2α,4α,5,12tetrahydroxy3β-fluoro1,2,3,4tetrahydro6,11 nephthacenedione.

USE: A intermediates for novel anthracycline derivatives useful for antitumor and antivirus drugs.

PROCESS: A compd. of formula I (R=H; R1=F) is obtained by a manufacturing procedure comprising cyclizing optionally substd. 1,4-dimethoxy2,3-bis(bromomethyl) anthraquinone with 3-butyn2-one, epoxidation, ring opening of an oxylan ring by a nucleophilic fluorine, demethylation and protection of an acetyl chain, bromontion of 4-position, introduction of OH and deprotection. The compd. of formula I is useful for an intermediate of a new drug of formula III (R3 is glycoside residue).


Inventors:
JIORITSUTEI ARESANDORO
GUIDEI ANTONIO
PASUKUI FURANKO
PESUTERINI BUITSUTORIO
ARUKAMONE FUEDEERIKO
Application Number:
JP30417590A
Publication Date:
September 12, 1991
Filing Date:
November 13, 1990
Export Citation:
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Assignee:
MENARINI SAS
International Classes:
A61K31/122; A61K31/70; A61P31/12; A61P35/00; A61K31/12; C07C46/00; C07C49/703; C07C49/747; C07C49/753; C07C49/825; C07C50/22; C07C50/36; C07C50/38; C07D303/10; C07D317/26; C07H15/24; C07H15/252; (IPC1-7): A61K31/12; C07C46/00; C07C50/38
Attorney, Agent or Firm:
Shigeru Yagita (2 outside)