The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 23, 2016

Filed:

Mar. 28, 2011
Applicants:

Lorenzo DE Ferra, Patrica, IT;

Maurizio Zenoni, Patrica, IT;

Stefano Turchetta, Patrica, IT;

Mauro Anibaldi, Patrica, IT;

Ettore Ammirati, Patrica, IT;

Paolo Brandi, Patrica, IT;

Giorgio Berardi, Patrica, IT;

Inventors:

Lorenzo De Ferra, Patrica, IT;

Maurizio Zenoni, Patrica, IT;

Stefano Turchetta, Patrica, IT;

Mauro Anibaldi, Patrica, IT;

Ettore Ammirati, Patrica, IT;

Paolo Brandi, Patrica, IT;

Giorgio Berardi, Patrica, IT;

Assignee:

CHEMI SPA, Cinisello Balsamo (MI), IT;

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07H 19/12 (2006.01); C07H 1/00 (2006.01); C07D 405/04 (2006.01);
U.S. Cl.
CPC ...
C07D 405/04 (2013.01); C07H 1/00 (2013.01); C07H 19/12 (2013.01);
Abstract

Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.


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