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(11)    Patent No :    AP 2719   
(21)    Application No :    AP/P/2010/005226   
(22)    Filing Date :    10.10.2008   
(24)    Date of Grant &    31.07.2013   
           
(45)    Publication :

(30)  Priority Data       
(33) Country    (31) Number    (32) Date
EP    07019826.2    10.10.2007

(84)    Designated State

BW    GM    GH    KE    LS    MW  MZ   NA   SL
SD    SZ    T Z    UG    ZM    ZW

(73) Applicant(s)
CILAG AG, Hochstrasse 201, CH-8205 Schaffhausen,

Switzerland
(72) Inventors
JUNGMANN Oliver, Germany
KRAUT Norbert, Germany

(74) Representative
HONEY & BLANCKENBERG

(51)    International  Classification   C07H 19/12 (2006.01)
(54)    Title

Method of producing 2' -deoxy-5-azacytidine (Decitabine)

(57)    Abstract

Method of producing 2'-deoxy-5-azacytidine (Decitabine) by providing a compound of formula (I), wherein R is a removable substituent known per se; and R1 is a removable substituent; further providing a silylated base of formula (II), wherein R2 is a protecting group, preferably a trimethylsilyl TMS ) -residue; reacting the compound of formula (I) and the compound of formula (II) together in a suitable anhydrous solvent and in the presence of a suitable catalyst; and removing the substituents R from the compound obtained in order to obtain the compound 2'-deoxy-5-azacytidine (Decitabine), characterized in that said catalyst is selected from the group comprising a salt of an aliphatic sulphonic acid or a salt of a strong inorganic acid.

(56)    Documents Cited :    WINKLEY, MICHAEL W. et al:    LU K-C et al:    US 3 817 980 A    BEN-HATTAR, JEAN et al:

US 4 082 911 A   US 4 209 613 A

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