4-demethoxy-4-amino-anthracyclines

Details 4-demethoxy-4-amino-anthracyclines 4-demethoxy-4-amino-anthracyclines

1988-04-14

1990-03-06

Griffin, Ronald W.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

C07H 1524

Patent

active

049067435

ABSTRACT:
Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## 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 diazotized 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.

REFERENCES:
patent: 4166848 (1979-09-01), Bernardi
patent: 4366149 (1982-12-01), Bargiotti
patent: 4413120 (1983-04-01), Whistler
patent: 4563444 (1986-01-01), Angelucci
patent: 4591637 (1988-05-01), Acton
patent: 4749693 (1988-06-01), Angelucci et al.
Tumori, (1980), vol. 66, pp. 549-555, "Antileukemic Activity of 4-Demethoxydaunorubicin in Mice", Casazza et al.

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