Title: Method for preparation of 4-demethoxy-4-amino anthrancene compounds
Application Number: 88102182 Application Date: 1988.04.20
Publication Number: 1023163 Publication Date: 1988.12.28
Approval Pub. Date: 1993.09.08 Granted Pub. Date: 1993.09.08
International Classifi-cation: A61K31/70;C07H15/252
Applicant(s) Name: Farmitalia Carlo Erba S.P.A. Address:
Inventor(s) Name: Francisco Angelucy
Attorney & Agent: TIANG YUE
Abstract:
    Anthracycline glycosides of the general formula (I): wherein R1, R2 and R3 have the meanings as the defines. These glycosides may be prepared from a daunomycinone derivative of formula (II): in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotised followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.
Time: 4