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.
WO/1992/009603 | POLYCYCLIC DIAMINES AND METHOD OF PREPARATION |
WO/2003/101996 | ESTERS IN POSITION 20 OF CAMPTOTHECINS |
WO/2004/029579 | FLUORESCENT LABELING REAGENTS WITH MULTIPLE DONORS AND ACCEPTORS |
SAWADA SEIGO
NOGATA KENICHIROU
MUTAI MASAHIKO
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