NOVEL ANTHRACYCLIN DERIVATIVE - MICROBIAL CHEM RES FOUND

Title:

NOVEL ANTHRACYCLIN DERIVATIVE

Document Type and Number:

Japanese Patent JPS5973539

Kind Code:

A

Abstract:

NEW MATERIAL:An anthracyclin derivative shown by the formula I (R1 is H, OH, or lower alkanoyloxy).

EXAMPLE: 4-Demethoxy-11-deoxydaunomycin.

USE: An intermediate for synthesizing an antharacyclin antibiotic shown by the formula II such as 4-demethoxy-11-deoxydaunomycin (R1=H) having improved antitumor activity.

PROCESS: 5-Methoxytetralone shown by the formula III is reacted with a Grignard reagent shown by the formula (CH≡C)MgX3(X3 is halogen, especially Br) to give a compound shown by the formula IV, which is hydrolyzed to give a compound shown by the formula V. This compound is reacted with phthalic anhydride shown by the formula VI, to give a compound shown by the formula VII. This compound is selectively halogenated with N-bromosuccinic acid imide only at the 14-position, etc., it is acylated with a salt of an organic carboxylic acid, halogenated at the 7-position, and finally hydrolyzed, to give a compound shown by the formula I .

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Inventors:

UMEZAWA HAMAO
TAKEUCHI TOMIO
OSANAWA HIROSHI
TATSUTA KUNIAKI

Application Number:

JP13294583A

Publication Date:

April 25, 1984

Filing Date:

July 22, 1983

Export Citation:

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Assignee:

MICROBIAL CHEM RES FOUND

International Classes:

C07C50/38; A61K31/70; A61K31/7028; A61K31/7034; A61K31/704; A61P35/00; C07C45/00; C07C67/00; C07H15/24; C07H15/252; (IPC1-7): A61K31/71; C07C50/38; C07H15/24

Attorney, Agent or Firm:

Heiyoshi Odashima

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