Method for the production of cladribine

C - Chemistry – Metallurgy – 12 – P

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Details

C12P 19/40 (2006.01) C07H 19/173 (2006.01) C12N 9/12 (2006.01) C12N 11/00 (2006.01) C12N 15/54 (2006.01)

Patent

CA 2610862

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.

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