2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative
AssigneeSyntex (U.S.A.) Inc.
InventorsJohn Joseph Nestor, Hans Maag
Life of this patent
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Abstract
The L-monovaline ester derived from 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
Claims20
A process for preparing the compound 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-3-hydroxy-1-propanyl-L-val inate or a pharmaceutically acceptable salt thereof, comprising:
- (a) removal of the amino- and hydroxy-protecting groups from a compound of the formula ##STR15## where:
- P.sup.1 is hydrogen or a hydroxy-protecting group,
- P.sup.2 is an amino-protecting group,
- P.sup.3 is hydrogen or P.sup.2, and
- the asterisk denotes an asymmetric carbon atom;
- to afford the compound 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-methoxy-3-hydroxy-1-propanyl-L-va linate;
- optionally followed by
- (b) conversion of the 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-methoxy-3-hydroxy-1-propanyl-L-va linate into a pharmaceutically acceptable salt thereof.
A process for preparing the compound 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-3-hydroxy-1-propanyl-L-val inate or a pharmaceutically acceptable salt thereof, comprising:
- (a) removal of the amino- and hydroxy-protecting groups from a compound of the formula ##STR16## where:
- P.sup.1 is a hydroxy-protecting group,
- P.sup.2 is an amino-protecting group,
- P.sup.3 is hydrogen or P.sup.2, and
- the asterisk denotes an asymmetric carbon atom;
- to afford the compound 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-methoxy-3-hydroxy-1-propanyl-L-va linate;
- optionally followed by
- (b) conversion of the 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-methoxy-3-hydroxy-1-propanyl-L-va linate into a pharmaceutically acceptable salt thereof.
A process for preparing the compound 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-3-hydroxy-1-propanyl-L-val inate or a pharmaceutically acceptable salt thereof, comprising:
- (a) removal of the amino- and hydroxy-protecting groups from a compound of the formula ##STR17## where:
- P.sup.1 is a hydroxy-protecting group removable under acidic conditions or by hydrogenolysis,
- P.sup.2 is an amino-protecting group,
- P.sup.3 is hydrogen or P.sup.2, and
- the asterisk denotes an asymmetric carbon atom;
- to afford the compound 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-methoxy-3-hydroxy-1-propanyl-L-va linate;
- optionally followed by
- (b) conversion of the 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-methoxy-3-hydroxy-1-propanyl-L-va linate into a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.