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US 8,012,717 B2Granted
Method for the production of cladribine
AssigneeEXPLORA Laboratories S.A.
InventorsGabriele Zuffi, Simone Monciardini
Life of this patent
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Abstract
A method for producing cladribine (2-chloro-2′ deoxyadenosine) comprising the steps of: a) reaction of 2-deoxyuridine with 2-chloroadenine, in the presence of uridine phosphorylase (UPase) and purine nucleoside phosphorylase (PNPase) in an aqueous reaction medium possibly containing up to 40% v/v of an aprotic dipolar solvent, to obtain cladribine dissolved in said reaction medium; b) isolation of the cladribine by precipitation by means of concentration and alkalinisation of the reaction medium up to pH 11.5-12.5.
Claims25
A method for producing cladribine (2-chloro-2′-deoxyadenosine) comprising the steps of:
- a) reaction of 2-deoxyuridine with 2-chloroadenine, in the presence of uridine phosphorylase (UPase) and purine nucleoside phosphorylase (PNPase) in an aqueous reaction medium optionally containing up to 40% v/v of an aprotic dipolar solvent, to obtain cladribine dissolved in said reaction medium;
- b) isolation of the cladribine by precipitation by means of concentration and alkalinisation of the reaction medium to reach a pH of between 11.5-12.5.
Dependencies are inferred from the claim text.