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US 5,580,972 AGranted
Purine nucleoside modifications by palladium catalyzed methods
AssigneeNeXstar Pharmaceuticals, Inc.
InventorsChi Tu, Bruce Eaton
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Abstract
This invention discloses an improved method for the preparation modified purine nucleosides at the 2-, 6-, or 8-position of the purine ring, using a palladium catalyst.
Claims14
A method for the preparation of a purine nucleoside modified at the 2-, 6-, or 8-positions of the purine ring comprising the steps of:
- a) reacting a purine starting material containing a halogen leaving group attached to the 2-, 6-, or 8-positions of said purine starting material with an organotin compound of the formula R.sup.2 SnR.sup.1.sub.3, wherein R.sup.2 displaces the leaving group from the purine starting material, wherein R.sup.1 is a C1 to C15 alkyl, and R.sup.2 is selected from the group consisting of a C1 to C15 alkyl and a substituted or unsubstituted C1 to C15 alkenyl or C6 to C12 aryl, in the presence of a palladium catalyst PdL.sub.3, wherein L is a ligand of palladium, and
- b) isolating and purifying said purine nucleoside.
Dependencies are inferred from the claim text.