Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)

Details Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)

1996-01-26

1997-12-23

Berch, Mark L.

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

Organic compounds

Chalcogen bonded directly to ring carbon of the purine ring...

C07D47318, C07B 4306

Patent

active

057009368

ABSTRACT:
Process for preparing the L-monovaline ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process relates to an improved process whereby ganciclovir is esterified with an L-valine derivative to provide a di-valine ganciclovir intermediate. Removal of one of the valine groups with a lower alkyl amine, benzylamine or benzyl methylamine provides the mono-valine ester compound of Formula I. These products are of value as antiviral agents with improved absorption.

REFERENCES:
patent: 4355032 (1982-10-01), Verheyden et al.
patent: 5043339 (1991-08-01), Beauchamp
E. Jensen et al., Acta Pharm. Nord. 3(4) 243-247 (1991).
John C. Martin et al., J. Pharm. Sci. 76(2), pp. 180-184 (1987).
P.C. Maudgal et al., Arch. Ophthalmol. 1984; 102: 140-142.
Leon Colla et al., J. Med. Chem. 98, 3, 26, 602-604 (1983).
L. M. Beauchamp et al., Antiviral Chemistry & Chemotherapy (1992), 3 (3), 157-164.

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