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Patent Searching and Data


Title:
NOVEL 9-SUBSTITUTED CAMPTOTHECIN DERIVATIVE
Document Type and Number:
Japanese Patent JPS5951289
Kind Code:
A
Abstract:

NEW MATERIAL:The compound of formula {X is amino, alkylamino, acylamino, hydroxyl, -OR [R is acyl or lower alkyl (excluding methyl)], or halogen}.

EXAMPLE: 9-Aminocamptothecin.

USE: Carcinostatic agent having low toxicity.

PROCESS: Camptothecin is dissolved in concentrated sulfuric acid, and concentrated nitric acid is added slowly to the solution under ice cooling. The amount of nitric acid is several times equivalent based on camptothecin. The mixture is stirred and reacted at room temperature for 24W72hr. The reaction liquid is poured into water, and extracted with chloroform. The chloroform layer is dried with anhydrous magnesium sulfate, and the solvent is removed in vacuum. The residue is separated and purified by silica gel column chromatography.


Inventors:
MIYASAKA SADA
SAWADA SEIGO
NOGATA KENICHIROU
MUTAI MASAHIKO
Application Number:
JP16094582A
Publication Date:
March 24, 1984
Filing Date:
September 17, 1982
Export Citation:
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Assignee:
YAKULT HONSHA KK
International Classes:
C07D491/22; A61K31/47; A61P35/00; (IPC1-7): C07D491/22
Other References:
CHEMICAL ABSTRACTS
Attorney, Agent or Firm:
Takao Minami