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公开(公告)号:US20130253195A1
公开(公告)日:2013-09-26
申请号:US13824620
申请日:2011-09-22
申请人: Livius Cotarca , Massimo Verzini , Elisa Melotto , Ivan Michieletto , Alfonso Melloni , Paolo Maragni , Raffaella Volpicelli , Mauro Andretto , Corrado Colli
发明人: Livius Cotarca , Massimo Verzini , Elisa Melotto , Ivan Michieletto , Alfonso Melloni , Paolo Maragni , Raffaella Volpicelli , Mauro Andretto , Corrado Colli
IPC分类号: C07D239/69 , C07C31/20
CPC分类号: C07D239/69 , C07C31/202
摘要: The present invention relates to a process for preparing Bosentan Monohydrate; in particular, the present invention provides the preparation of the novel 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-benzenesulfonamide sodium salt as an ethylene glycol solvate (Bosentan sodium salt ethylene glycol solvate), which is a useful intermediate for obtaining Bosentan Monohydrate in a pure form.
摘要翻译: 本发明涉及一种制备波生坦一水合物的方法; 特别地,本发明提供新的4-叔丁基-N- [6-(2-羟基 - 乙氧基)-5-(2-甲氧基 - 苯氧基)-2-(2-嘧啶基) - 嘧啶的制备 -4-基] - 苯磺酰胺钠盐作为乙二醇溶剂化物(波生坦钠盐乙二醇溶剂合物),其是以纯形式获得波司坦一水合物的有用中间体。
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公开(公告)号:US08933226B2
公开(公告)日:2015-01-13
申请号:US13824620
申请日:2011-09-22
申请人: Livius Cotarca , Massimo Verzini , Elisa Melotto , Ivan Michieletto , Alfonso Melloni , Paolo Maragni , Raffaella Volpicelli , Mauro Andretto , Corrado Colli
发明人: Livius Cotarca , Massimo Verzini , Elisa Melotto , Ivan Michieletto , Alfonso Melloni , Paolo Maragni , Raffaella Volpicelli , Mauro Andretto , Corrado Colli
IPC分类号: C07D403/04 , C07D239/69 , C07C31/20
CPC分类号: C07D239/69 , C07C31/202
摘要: The present invention relates to a process for preparing Bosentan Monohydrate; in particular, the present invention provides the preparation of the novel 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-benzenesulfonamide sodium salt as an ethylene glycol solvate (Bosentan sodium salt ethylene glycol solvate), which is a useful intermediate for obtaining Bosentan Monohydrate in a pure form.
摘要翻译: 本发明涉及一种制备波生坦一水合物的方法; 特别地,本发明提供新的4-叔丁基-N- [6-(2-羟基 - 乙氧基)-5-(2-甲氧基 - 苯氧基)-2-(2-嘧啶基) - 嘧啶的制备 -4-基] - 苯磺酰胺钠盐作为乙二醇溶剂合物(波生坦钠盐乙二醇溶剂合物),其是以纯形式获得波司坦一水合物的有用中间体。
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公开(公告)号:US08927740B2
公开(公告)日:2015-01-06
申请号:US14003385
申请日:2012-03-08
IPC分类号: C07D495/04
CPC分类号: C07D495/04
摘要: The present invention relates to a stereoselective reduction procedure to obtain, by means of catalytic asymmetric hydrogenation by hydrogen transfer, a compound of formula (I) in which X is S or SO2 and R4 is hydrogen or an SO2NH2 group, from the corresponding ketone precursor, said compound of formula (I) being useful as an intermediate in the preparation of dorzolamide or of the hydrochloride salt thereof.
摘要翻译: 本发明涉及通过氢转移的催化不对称氢化获得其中X为S或SO 2,R 4为氢或SO 2 NH 2基的式(I)化合物的立体选择性还原方法, 所述式(I)化合物可用作制备多佐胺或其盐酸盐的中间体。
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公开(公告)号:US20130338377A1
公开(公告)日:2013-12-19
申请号:US14003385
申请日:2012-03-08
IPC分类号: C07D495/04
CPC分类号: C07D495/04
摘要: The present invention relates to a stereoselective reduction procedure to obtain, by means of catalytic asymmetric hydrogenation by hydrogen transfer, a compound of formula (I) in which X is S or SO2 and R4 is hydrogen or an SO2NH2 group, from the corresponding ketone precursor, said compound of formula (I) being useful as an intermediate in the preparation of dorzolamide or of the hydrochloride salt thereof.
摘要翻译: 本发明涉及通过氢转移的催化不对称氢化获得其中X为S或SO 2,R 4为氢或SO 2 NH 2基的式(I)化合物的立体选择性还原方法, 所述式(I)化合物可用作制备多佐胺或其盐酸盐的中间体。
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