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US 6,646,125 B1Granted
Process for the synthesis of chloropurine intermediates
AssigneeSmithKline Beecham Corporation
InventorsMartin Francis Jones, Christopher John Wallis
Life of this patent
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Abstract
The present invention relates to a process for the preparation of a carbocyclic purine nucleoside analogue of formula (I), its salts and pharmaceutically acceptable derivatives thereof which comprises hydrolysing a compound of formula (IV) wherein P is a protecting group, in the presence of an acid, condensing the product of formula (V) formed in situ in the presence of a base with a compound of formula (VI) followed by in situ ring closure of the resulting intermediate.
Claims13
A process for the preparation of a compound of formula (1),
- optionally in the form of its salt complex comprising, hydrolyzing a compound of formula (IV)
- wherein P is a protecting group,in the presence of an acid, condensing the product of formula (V)
- formed in situ in the presence of a base with a compound of formula (VI)
- in which R represents CHO or H, followed by ring closure in situ of the resulting intermediate of formula (VII)
- in which R represents CHO or H, with a trialkylorthofornate, in the presence of a mineral acid, to produce a compound of formula (1), which can then be optionally reacted with an acid to form its salt.
2 more elements
Dependencies are inferred from the claim text.