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1. 发明申请

WO2005095358A2 CHEMICAL PROCESS 审中-公开
标题翻译：化学工艺
公开(公告)号：WO2005095358A2
公开(公告)日：2005-10-13
申请号：PCT/GB2005/001188
申请日：2005-03-29
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , LARSSON, Ulf , RADEVIK, Kajsa
发明人： LARSSON, Ulf , RADEVIK, Kajsa
IPC分类号： C07D239/46
CPC分类号： C07D239/47
摘要： The present invention provides a process for the preparation of a compound of formula (I); wherein X is halogen; Y is ZR 1 ; Z is oxygen or sulphur; and R 1 is C 1-6 alkyl, C 1-6 haloalkyl or C 3-7 cloalkyl; the process comprising either: hydrogenating a compound of formula (II); with a suitable transition metal catalyst in a C 1-6 aliphatic alcohol, an ether, an hydrocarbon as solvent; or, b) conducting a one-pot hydrogenation of a compound of formula (III): wherein R 2 is phenyl optionally substituted by chloro,C 1-6 alkyl, C 1-6 alkoxy or (C 1-6 alkyl) 2 N; firstly at about 20 ° C to form a compound of formula (IV): and then at about 40 ° C; both steps (I) and (ii) being carried out in the presence of a suitable catalyst and in the presence of a suitable solvent.
摘要翻译：本发明提供制备式（I）化合物的方法; 其中X是卤素; Y为ZR <1>; Z是氧或硫; 且R 1为C 1-6烷基，C 1-6卤代烷基或C 3-7杂烷基; 该方法包括：将式（II）的化合物氢化; 在C 1-6脂族醇，醚，烃作溶剂中使用合适的过渡金属催化剂; 或者，b）进行式（III）化合物的一锅氢化：其中R 2是任选被氯，C 1-6烷基，C 1-6烷氧基或（C 1-6烷基）2 N取代的苯基; 首先在约20℃下形成式（IV）的化合物，然后在约40℃; 步骤（I）和（ii）都在合适的催化剂存在下和在合适的溶剂存在下进行。

2. 发明公开

EP1751117A2 PROCESS FOR THE PREPARATION OF AMINOPYRIMIDINES 有权
标题翻译：用于生产氨基嘧啶
公开(公告)号：EP1751117A2
公开(公告)日：2007-02-14
申请号：EP05729737.6
申请日：2005-03-29
申请人： AstraZeneca AB
发明人： LARSSON, Ulf , RADEVIK, Kajsa
IPC分类号： C07D239/46
CPC分类号： C07D239/47
摘要： The present invention provides a process for the preparation of a compound of formula (I); wherein X is halogen; Y is ZR1; Z is oxygen or sulphur; and R1 is C 1-6 alkyl, C1-6 haloalkyl or C3-7 cloalkyl; the process comprising either: hydrogenating a compound of formula (II); with a suitable transition metal catalyst in a C1-6 aliphatic alcohol, an ether, an hydrocarbon as solvent; or, b) conducting a one-pot hydrogenation of a compound of formula (III): wherein R2 is phenyl optionally substituted by chloro,C1-6 alkyl, C1-6 alkoxy or (C1-6 alkyl)2N; firstly at about 20°C to form a compound of formula (IV): and then at about 40°C; both steps (I) and (ii) being carried out in the presence of a suitable catalyst and in the presence of a suitable solvent.

3. 发明授权

EP1751117B1 PROCESS FOR THE PREPARATION OF AMINOPYRIMIDINES 有权
标题翻译：用于生产氨基嘧啶
公开(公告)号：EP1751117B1
公开(公告)日：2011-07-20
申请号：EP05729737.6
申请日：2005-03-29
申请人： AstraZeneca AB
发明人： LARSSON, Ulf , RADEVIK, Kajsa
IPC分类号： C07D239/46
CPC分类号： C07D239/47
摘要： The present invention provides a process for the preparation of a compound of formula (I); wherein X is halogen; Y is ZR1; Z is oxygen or sulphur; and R1 is C 1-6 alkyl, C1-6 haloalkyl or C3-7 cloalkyl; the process comprising either: hydrogenating a compound of formula (II); with a suitable transition metal catalyst in a C1-6 aliphatic alcohol, an ether, an hydrocarbon as solvent; or, b) conducting a one-pot hydrogenation of a compound of formula (III): wherein R2 is phenyl optionally substituted by chloro,C1-6 alkyl, C1-6 alkoxy or (C1-6 alkyl)2N; firstly at about 20°C to form a compound of formula (IV): and then at about 40°C; both steps (I) and (ii) being carried out in the presence of a suitable catalyst and in the presence of a suitable solvent.

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