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)

1998-07-31

2000-03-21

Berch, Mark L.

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

Organic compounds

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

560106, 560254, C07D47318

Patent

active

060404469

ABSTRACT:
Process and novel intermediates for preparing the L-mono-valine 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 and intermediates provide for reduced impurities in the mono-valine ester end-product and lower overall production costs. The process involves the condensation of a silylated guanine compound with a substituted glycerol derivative and esterification of this product with an L-valine derivative. These mono-valine products are of value as antiviral agents with improved absorption.

REFERENCES:
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patent: 5043339 (1991-08-01), Beauchamp
patent: 5856481 (1991-01-01), Nestor
E. Jensen et al., Acta Pharm. Nord. 3(4) 243-247 (1991).
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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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