Farmabios S.p.a.

Industriale Chimica S.r.l.

Lorenzo Menna

Roberto Lenna

Claudio Gianluca Pozzoli

Marco Brusasca

Matteo Curti

Valentina Canevari

Silvio Pirovano

A process for the preparation of nucleosides, derivatives and analogues thereof by coupling reaction of a protected suitable nitrogeneous purine or pyrimidine base, a derivative or analogue thereof and a protected suitable sugar in the presence of SnClcomprising the removal of SnCl4 by adding DMSO directly into the reaction mixture is described. Preferably said process is used for the preparation of antiviral and antitumor agents having a nucleoside or nucleoside-like structure, still more preferably for the preparation of azacytidine, decitabine, chlorfarabine, cladribine, mizoribine. A residual tin content lower than 300 ppm is obtained with said process.

Synthesis of nucleosides

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Milan, Italy

Lorenzo Menna