Clariant Finance (Bvi) Limited

Explora Laboratories S.a.

Simone Monciardini

Giovanni Cotticelli

Giuseppe De Meglio

Gabriele Zuffi

Giancarlo Ordanini

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.

Method for the production of cladribine

A process for the preparation of 5&prime;-deoxy-5-fluorouridine, which comprises the transformation of 2&prime;,3&prime;-O-isopropylidene-5-fluorouridine in the corresponding 5&prime;-O-sulfonyl derivative, subsequent reaction with alkaline or earth-alkaline iodides and, after hydrolysis of the isopropylidene group, reduction of the 5&prime;-deoxy-5&prime;-iodo-5-fluorouridine thus obtained, is described.

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Varese, Italy

Simone Monciardini