Production of 10-hydroxycamptothecin

Abstract

Abstract PURPOSE:The treatment of 1,2,6,7-tetrahydrocamptothecin with an oxidizing agent such as lead tetra-acetate simplifies the process to give the titled compound used as an antitumor agent causing no cross resistance with existing carcinostatic agents. CONSTITUTION:1,2,6,7-Tetrahydrocamptothecin is dissolved in a solvent such as methanol and oxidized by adding an oxidizing agent thereto, such as lead tetra- acetate, celium (IV) ammonium nitrate, Fremy's salt, chromic acid, perchromate salt, potassium permanganate or ferric chloride. The reaction mixture is evaporated to dryness under reduced pressure and the residue is purified by subjecting to column chromatography to give the objective compound. 1,2,6,7-Tetrahydrocamptothecin, as a starting compound, is obtained by catalytic hydrogenation of camptothecin.

Inventors

• 👤 Sada Miyasaka
• 👤 宮坂　貞
• 👤 Seigo Sawada
• 👤 誠吾 沢田
• 👤 Kenichiro Nogata
• 👤 野方　健一郎
• 👤 Masahiko Mutai
• 👤 務台　方彦

Bibliographic Details