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US 2002/0173649 A1Published application
Chloropvrimidine intermediates
AssigneeSmithKline Beecham Corporation
InventorsSusan Mary Daluge, Michelle Joanne Fugett, Michael Tolar Martin
Life of this patent
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Abstract
The present invention relates to certain novel pyrimidine intermediates and their salts, processes for their preparation and processes for their conversion to 9-substituted-2-aminopurines which are useful in medical therapy.
Claims2
A compound of formula (VI)
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- wherein R3 is hydrogen;
- hydroxyl or a protected hydroxyl;
- a C3-7 carbocyclic group optionally substituted with one or more groups selected from C1-4 alkyl, C1-4 alkoxy, hydroxyl or protected hydroxyl, azido, phosphonyl, or halogen;
- a C2-8 hydrocarbyl group, wherein carbon atoms may be substituted by one or more heteroatoms selected from N, O or S, and wherein such C2-8 hydrocarbyl group may be optionally substituted with one or more groups selected from C1-4 alkyl, C1-4 alkoxy, hydroxyl or protected hydroxyl, azido, phosphonyl, or halogen;
- or a C4-7 heterocyclic group, wherein one or more carbon atom is replaced by a N, O, or S atom and wherein such C4-7 heterocyclic group may be optionally substituted with one or more groups selected from C1-4 alkyl, C1-4 alkoxy, hydroxyl or protected hydroxyl, azido, phosphonyl, or halogen;
- provided that such groups are not attached by a glycosidic bond.
4 more elements
A process for the preparation of a compound of formula (VI):
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- wherein R3 is hydrogen;
- hydroxyl or a protected hydroxyl;
- a C3-7 carbocyclic group optionally substituted with one or more groups selected from C1-4 alkyl, C1-4 alkoxy, hydroxyl or protected hydroxyl, azido, phosphonyl, or halogen;
- a C2-8 hydrocarbyl group, wherein carbon atoms may be substituted by one or more heteroatoms selected from N, O or S and wherein such C2-8 hydrocarbyl group may be optionally substituted with one or more groups selected from C1-4 alkyl, C1-4 alkoxy, hydroxyl or protected hydroxyl, azido, phosphonyl, or halogen;
- or a C4-7 heterocyclic group, wherein one or more carbon atom is replaced by a N, O, or S atom and wherein such C4-7 heterocyclic group may be optionally substituted with one or more groups selected from C1-4 alkyl, C1-4 alkoxy, hydroxyl or protected hydroxyl, azido, phosphonyl, or halogen;
- provided that such groups are not attached by a glycosidic bond, comprising:
- reacting a compound of formula (III):
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- with an amine of formula R3 NH2 in the presence of a base.
7 more elements
Dependencies are inferred from the claim text.