Patent · US Active

Process for the synthesis of azacitidine and decitabine

US9266863B2 · kind B2 · utility

0Cited by

1References

17Claims

0Family size

Assignee

CHEMI S.P.A. · IT

Inventors

Lorenzo De Ferra · Patrica, IT
Maurizio Zenoni · Paullo, IT
Stefano Turchetta · Roma, IT
Mauro Anibaldi · Patrica, IT
Ettore Ammirati · Patrica, IT
Paolo Brandi · Patrica, IT
Giorgio Berardi · Patrica, IT

Key dates

Filing date	Mar 28, 2011
Grant date	Feb 23, 2016
Priority date	—
Expiry date	Jan 3, 2032

Classification

Technology area (CPC C)Chemistry; Metallurgy
CPC primaryC07H19/12
WIPO fieldOrganic fine chemistry
WIPO sectorChemistry

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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.