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)

1998-07-23

2000-08-15

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 5100

Patent

active

061039012

ABSTRACT:
Intermediates of Formula (III) ##STR1## wherein P.sup.1 is hydrogen or an amino-protecting group, R is lower alkyl, allyl or aralkyl, and Z is hydrogen, lower alkyl, aryl or aralkyl; and Formula (VI) ##STR2## wherein P.sup.1 is hydrogen or an amino-protecting group, P.sup.2 is an amino protecting group, and Z is hydrogen, lower alkyl, aryl or aralkyl, are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts 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), p. 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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