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1. 发明申请

WO2011113476A3 METHOD FOR PRODUCING 2'-DEOXYADENOSINE COMPOUNDS 审中-公开
公开(公告)号：WO2011113476A3
公开(公告)日：2011-09-22
申请号：PCT/EP2010/053352
申请日：2010-03-16
申请人： CILAG AG , JUNGMANN, Oliver , THALER, Adrian , HÄNSELER, Rolf
发明人： JUNGMANN, Oliver , THALER, Adrian , HÄNSELER, Rolf
IPC分类号： C07H19/173
摘要： (A) reacting the alkali metal salt of 2, 6-dichlorpurine with a 2-desoxy-3, 5 -di-O-p-toluoyl-alpha-D-erythro-pentofuranose or a derivative thereof, in a suitable organic solvent, said reaction optionally being carried out in the presence of a Lewis-acid, whereby a mixture comprising the intermediate N (9) -beta-compound, the N (7) -beta-regio- isomer, and the N (9) -alpha-stereoisomer is formed; (B) isolating from said reaction mixture formed the crude reaction product comprising the intermediate N (9) -beta- compound by a purification method, preferably by precipitation or crystallization, using a suitable organic solvent or a mixture of such organic solvents or a mixture of one or more of such organic solvents with water, without using a chromatographic purification method, and (C) subjecting the isolated intermediate N (9 ) -beta-compound to ammonolysis, where upon the 2 '-deoxyadenosine compound is formed, and (D) precipitating or crystallizing the 2 '-deoxyadenosine compound as formed in step (C) from a suitable organic solvent.

2. 发明申请

WO2005063696A3 NEUE KRISTALLINE FORMEN VON ENTACAPONE UND DEREN HERSTELLUNG 审中-公开
公开(公告)号：WO2005063696A3
公开(公告)日：2005-07-14
申请号：PCT/CH2004/000754
申请日：2004-12-27
申请人： CILAG AG , BADER, Thomas , FUREGATI, Markus , JUNGMANN, Oliver
发明人： BADER, Thomas , FUREGATI, Markus , JUNGMANN, Oliver
IPC分类号： C07C255/41
摘要： Beschrieben werden drei neue kristalline Formen von Entacapone. Diese sind periphere und selektive COMT-Inhibitoren, welche - in Kombination mit Levodopa und einem Decarboxylasehemmer - zur Behandlung des Parkinson-Syndroms verwendet werden können. Diese neuen Formen entstehen durch Kristallisation von Entacapone unter jeweils bestimmten Bedingungen. In gewissen Fällen kann dabei das Entacapone als Rohprodukt eingesetzt werden, in einem speziellen Fall sogar in stitu als Produkt einer Knoevenagel-Kondensation von 3,4-Dihydroxy-5-nitro-benzaldehyd und N,N-Diethyl-2-cyano-acetamid. Beschrieben werden weiterhin Verbesserungen dieser Kondensation bezüglich des Katalysators und der Herstellung ihrer beiden Komponenten.

3. 发明申请

WO2009047314A3 METHOD OF PRODUCING NUCLEOSIDES 审中-公开
公开(公告)号：WO2009047314A3
公开(公告)日：2009-04-16
申请号：PCT/EP2008/063582
申请日：2008-10-10
申请人： Cilag AG , JUNGMANN, Oliver , KRAUT, Norbert
发明人： JUNGMANN, Oliver , KRAUT, Norbert
IPC分类号： C07H19/00 , C07H19/06 , C07H19/12 , C07H19/16
摘要： Method of producing a free nucleoside compound, the compound 2'- deoxy-5-azacytidine (Decitabine) being excluded, by reacting a glycoside donor preferably a 1-halogen derivative, or 1-0-acyl, 1-0-alkyl, or an imidate preferably a trichloromethyl derivative, or a thio-alkyl derivative of a blocked monosaccharide or oligosaccharide preferably ribose and 2-desoxyribose derivatives with a protected nucleoside base, in a suitable anhydrous solvent and in the presence of a catalyst, and removing the protecting groups from said blocked nucleoside compound, wherein said catalyst is selected from the group comprising salts of an aliphatic sulphonic acid and/or salts a strong inorganic acid containing a non-nucleophilic anion.

4. 发明申请

WO2009047313A2 METHOD OF PRODUCING 2' -DEOXY-5-AZACYTIDINE (DECITABINE) 审中-公开
标题翻译： 2'-氧代-5-氮杂环丁烷的生产方法（DECATABINE）
公开(公告)号：WO2009047313A2
公开(公告)日：2009-04-16
申请号：PCT/EP2008/063581
申请日：2008-10-10
申请人： Cilag AG , JUNGMANN, Oliver , KRAUT, Norbert
发明人： JUNGMANN, Oliver , KRAUT, Norbert
IPC分类号： C07H19/12
CPC分类号： C07H19/12 , Y02P20/55
摘要： 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 R 1 is a removable substituent; further providing a silylated base of formula (II), wherein R 2 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.
摘要翻译：通过提供式（I）化合物制备2'-脱氧-5-氮杂胞苷（地西他滨）的方法，其中R是本身已知的可除去的取代基; R1是可取代的取代基; 进一步提供式（II）的甲硅烷基化碱，其中R 2是保护基，优选三甲基甲硅烷基TMS） - 残基; 使式（I）化合物和式（II）化合物在合适的无水溶剂中和在合适的催化剂存在下反应; 并从得到的化合物中除去取代基R，得到化合物2'-脱氧-5-氮杂胞苷（地西他滨），其特征在于所述催化剂选自脂肪族磺酸盐或其盐强无机酸。

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