Method of synthesizing camptothecin-relating compounds

C - Chemistry – Metallurgy – 07 – C

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C07C 205/45 (2006.01) C07C 205/38 (2006.01) C07C 221/00 (2006.01)

Patent

CA 2437702

The present invention is to prepare efficiently 2'-amino-5'-hydroxypropiophenone corresponding to the AB-ring part of camptothecin (CPT) skeleton and a tricyclic ketone corresponding to the CDE-ring part in order to provide efficiently CPT by the total synthesis, which is a starting material for irinotecan hydrochloride and various kinds of camptothecin derivatives, and to provide stably CPT and its derivatives.

L'invention concerne un procédé de synthèse totale, pratiquement utilisable, de camptothécine, produit de départ de l'hydrochlorure d'irinotécan et de nombreux dérivés de camptothécine, consistant à produire de la 2'-amino-5'-hydroxypropiophénone, correspondant à l'entité cyclique AB du squelette de la camptothécine, et une cétone tricyclique, correspondant à l'entité cyclique CDE, ce qui permet de produire de la camptothécine et ses dérivés de façon régulière.

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