Process for the preparation of etoposide phosphate and intermedi

Details Process for the preparation of etoposide phosphate and intermedi Process for the preparation of etoposide phosphate and intermedi

1995-06-07

1997-06-10

Kight, John

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

Organic compounds

Carbohydrates or derivatives

536 41, 536 171, 536 185, A61K 3170

Patent

active

056376804

ABSTRACT:
An etoposide phosphate represented by the formula ##STR1## is prepared by blocking the hydroxyl groups of the saccharide moiety of etoposide with halogenoacetyl groups, thereafter phosphorylating the 4'-position, and removing the halogenoacetyl groups from the obtained phosphate in the presence of an amine. This process can give the objective etoposide phosphate in a higher yield than that of the prior art to enable the industrial mass-production thereof.

REFERENCES:
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patent: 4904768 (1990-02-01), Saulnier et al.
patent: 5036055 (1991-07-01), Ohnuma et al.
patent: 5041424 (1991-08-01), Saulnier et al.
patent: 5081234 (1992-01-01), Ohnuma et al.
patent: 5206350 (1993-04-01), Wang et al.
Perich et al. J. Org. Chem., vol. 54(7):1750-1752, (1989). Abstract only.
Derwent Abstract of JP Laid-Open No. Shou 63-192.793 (Aug. 10, 1988).

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