Process for the preparation of 4'-epidaunorubicin, 3',4'-diepida

Details Process for the preparation of 4'-epidaunorubicin, 3',4'-diepida Process for the preparation of 4'-epidaunorubicin, 3',4'-diepida

1980-06-30

1982-08-17

Hazel, Blondel

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

Organic compounds

Carbohydrates or derivatives

424180, C07H 1524, A61K 3171

Patent

active

043450687

ABSTRACT:
Disclosed is a process for preparing the known antitumor glycosides: 4'-epidaunorubicin, 3',4'-diepidaunorubicin, and their doxorubicin analogs by oxidizing the C-4' hydroxyl group of N-protected daunorubicin to form certain novel intermediates having a 4'-keto configuration, followed by reduction of the keto group with NaBH.sub.4 and mild alkaline hydrolysis to remove the N-protecting acyl groups.

REFERENCES:
patent: 4039663 (1977-08-01), Arcamone et al.
patent: 4112076 (1978-09-01), Arcamone et al.

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