Etoposide phosphate and preparative intermediates

Details Etoposide phosphate and preparative intermediates Etoposide phosphate and preparative intermediates

1995-03-27

1997-02-25

Kight, John

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

Organic compounds

Carbohydrates or derivatives

536 18, 536 182, 536 184, C07H 1524

Patent

active

056060394

ABSTRACT:
An etoposide phosphate represented by the formula (1): ##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.

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Derwent Abstract of JP Laid-Open No. Shou 63-192,793.
Ramirez et al., "Amine Catalysis in Phosphoryl Transfer From 2,4-Diniutrophenyl Phosphate in Aprotic and Protic Solvents," Tetrahedron, 35(13), 1581-1589 (1979).
Ogawa et al., "Studies on Metal-Nucleotides Complexes. IV. Studies on the Isolated Metal-Inosinic Acid (5'-IMP) Complexes by Infrared Absorption Spectra," Chem. Pharm. Bull., 19(8), 1650-1655 (1971).

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