Title:
4-DEMETHOXY4'-DEOXY-4'IODOANTHRACYCLINE GLYCOSIDE
Document Type and Number:
Japanese Patent JPH01311095
Kind Code:
A
Abstract:
NEW MATERIAL: A compound of formula I (R1 is H, hydroxy) or its salt.
EXAMPLE: 4-Demethoxy4'-deoxy-4'-iododaunorubicin.
USE: An antitumor agent.
PROCESS: First, the 4'-epi-hydroxy group of 4demethoxy-4'-epiN-trifluoroacetyl daunorubicin of formula II is converted into a 4'-epi-O-trifluoromethane sulfonyl group by being reacted with anhydrous trifluoromethane sulfonic acid preferably in anhydrous methylene dichloride in the presence of an organic base to obtain the 4'-epi-4'-O-triluoromethane sulfonate derivative of formula III. Next, the product is reacted with an iodide salt to produce 4'-demethoxy4'-deoxy-4'-iodo- Ntrifluoroacetyl-daunorubicin of formula IV, from which the N-trifluoroacetyl protective group is removed.
Inventors:
ANTONINO SUARATO
MIKERU KARUSO
SERUJIO PENKO
FUERUNANDO JIYURIANI
MIKERU KARUSO
SERUJIO PENKO
FUERUNANDO JIYURIANI
Application Number:
JP10152189A
Publication Date:
December 15, 1989
Filing Date:
April 20, 1989
Export Citation:
Assignee:
ERBA CARLO SPA
International Classes:
A61K31/70; A61K31/7028; A61K31/7034; C07H15/252; A61K31/704; A61P35/00; C07D309/14; (IPC1-7): A61K31/71; C07H15/252
Attorney, Agent or Firm:
Yoshio Kawaguchi (2 outside)
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