Antracycline glycosides, pharmaceutical compositions and method

Details Antracycline glycosides, pharmaceutical compositions and method Antracycline glycosides, pharmaceutical compositions and method

1982-10-15

1984-10-16

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,...

536 64, A61K 3170, C07H 1524

Patent

active

044774443

ABSTRACT:
Disclosed is a process for preparing the new antitumor glycosides: 4'-deoxy-3'-epi-daunorubicin and 4'-deoxy-3'-epi-doxorubicin starting from the known 3'-epi-4'-keto-N-trifluoroacetyl-daunorubicin.
Reduction of the 4'-keto group with sodium borohydride to the corresponding 4'-hydroxy group, reacting the so obtained intermediate with trifluoromethanesulphonic anhydride followed by treatment with n-tetrabutylammonium iodide, dehalogenated reductively, by treatment with tributyl tin hydride to 4'-deoxy-3'-epi-N-trifluoroacetyl-daunorubicin.
A mild alkaline hydrolysis removes the N-protecting group to give 4'-deoxy-3'-epi-daunorubicin which is successively transformed, via its 14-bromo derivative, in its doxorubicin analogue.

REFERENCES:
patent: 4067969 (1978-01-01), Penco et al.
patent: 4345068 (1982-08-01), Suarato et al.
patent: 4345070 (1982-08-01), Suarato et al.

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