6"-Deoxydibekacin, 4",6"-dideoxydibekacin and 1-N-aminoacyl deri

Details 6"-Deoxydibekacin, 4",6"-dideoxydibekacin and 1-N-aminoacyl deri 6"-Deoxydibekacin, 4",6"-dideoxydibekacin and 1-N-aminoacyl deri

1980-08-01

1982-06-01

Brown, Johnnie R.

Drug, bio-affecting and body treating compositions

Conjugate or complex of monoclonal or polyclonal antibody,...

Conjugated via claimed linking group, bond, chelating agent,...

424181, 536 137, 536 138, A61K 3171, C07H 1522

Patent

active

043327940

ABSTRACT:
New compounds, 6"-deoxydibekacin, 4", 6"-dideoxydibekacin, 1-N-(L-4-amino-2-hydroxybutyryl)-6"-deoxydibekacin and 1-N-(L-4-amino-2-hydroxybutyryl)-4",6"-dideoxydibekacin are now produced semi-synthetically from dibekacin, i.e. 3',4'-dideoxykanamycin B. These four new compounds are each useful as an antibacterial agent. Production of 6"-deoxydibekacin or 4",6"-dideoxydibekacin is made by removal of the 6"-hydroxyl group or by removal of the 4"- and 6"-hydroxyl groups from an amino-protected and hydroxyl-protected derivative of dibekacin. Production of 1-N-(L-4-amino-2-hydroxybutyryl)-6"-deoxydibekacin or -4",6"-dideoxydibekacin is made by acylating the 1-amino group of 6"-deoxydibekacin or 4",6"-dideoxydibekacin with the L-4-amino-2-hydroxybutyryl group, or alternatively by removal of the 6"-hydroxyl group or the 4"- and 6"-hydroxyl groups from a known compound, 1-N-(L-4-amino-2-hydroxybutyryl)-dibekacin.

REFERENCES:
patent: 3929762 (1975-12-01), Umezawa et al.
patent: 4020269 (1977-04-01), Hiraga et al.
patent: 4029883 (1977-06-01), Hiraga et al.
patent: 4051315 (1977-09-01), Godfrey et al.
patent: 4156078 (1979-05-01), Umezawa et al.

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