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公开(公告)号：US08445716B2
公开(公告)日：2013-05-21
申请号：US12779268
申请日：2010-05-13
IPC分类号： C07C67/14
CPC分类号： C07C219/28
摘要： A process is described for preparing fesoterodine and/or fesoterodine fumarate comprising the esterification of (R)-feso deacyl with isobutyric acid or a precursor thereof, such as an isobutyryl halide or the isobutyric acid anhydride to give fesoterodine, in a mixture of water at alkaline pH and/or at least one organic solvent. This process allows obtaining products with high yields and purities, and in particular a product having a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-isobutyroyloxymethyl-phenyl isobutyrate less than 1% by mole and a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol less than 0.05% by mole.
摘要翻译： 描述了一种制备费索托定和/或富马酸菲索特罗的方法，其包括（R） - 异丙酰基与异丁酸或其前体如异丁酰卤或异丁酸酐的酯化反应，得到非索特罗定，在水的混合物中 碱性pH和/或至少一种有机溶剂。 该方法允许获得具有高产率和纯度的产物，特别是具有小于1摩尔％的（R）-2- [3-（二异丙基氨基）-1-苯基丙基] -4-异丁酰氧基甲基 - 苯基异丁酸酯含量的产物 和（R）-2- [3-（二异丙基氨基）-1-苯基丙基] -4-（羟甲基）苯酚的含量小于0.05摩尔％。
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公开(公告)号：US20100292503A1
公开(公告)日：2010-11-18
申请号：US12779268
申请日：2010-05-13
IPC分类号： C07C67/08
CPC分类号： C07C219/28
摘要： A process is described for preparing fesoterodine and/or fesoterodine fumarate comprising the esterification of (R)-feso deacyl with isobutyric acid or a precursor thereof, such as an isobutyryl halide or the isobutyric acid anhydride to give fesoterodine, in a mixture of water at alkaline pH and/or at least one organic solvent. This process allows obtaining products with high yields and purities, and in particular a product having a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-isobutyroyloxymethyl-phenyl isobutyrate less than 1% by mole and a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol less than 0.05% by mole.
摘要翻译： 描述了一种制备费索托定和/或富马酸菲索特罗的方法，其包括（R） - 异丙酰基与异丁酸或其前体如异丁酰卤或异丁酸酐的酯化反应，得到非索特罗定，在水的混合物中 碱性pH和/或至少一种有机溶剂。 该方法允许获得具有高产率和纯度的产物，特别是具有小于1摩尔％的（R）-2- [3-（二异丙基氨基）-1-苯基丙基] -4-异丁酰氧基甲基 - 苯基异丁酸酯含量的产物 和（R）-2- [3-（二异丙基氨基）-1-苯基丙基] -4-（羟甲基）苯酚的含量小于0.05摩尔％。
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公开(公告)号：US20100292502A1
公开(公告)日：2010-11-18
申请号：US12779216
申请日：2010-05-13
IPC分类号： C07C69/017
CPC分类号： C07C227/16 , C07C59/40 , C07C219/28
摘要： A process is described for preparing fesoterodine fumarate comprising the salification reaction of fesoterodine with fumaric acid in an organic solvent, preferably a ketone, at a temperature not greater than 45° C. Such process allows obtaining products with high yields and purities, and in particular a product having a content of (2E)-4-[(3-(3-diisopropylamino-1-phenylpropyl)-4-(2-isobutyroyloxyphenyl)methoxy]-4-oxobut-2-enoic acid less than or equal to 0.15% by mole.
摘要翻译： 描述了在不高于45℃的温度下，在有机溶剂（优选酮）中制备非索特罗定富马酸与富马酸的成盐反应的方法，该方法允许获得高产率和纯度的产物，特别是 具有（2E）-4 - [（3-（3-二异丙基氨基-1-苯基丙基）-4-（2-异丁酰氧基苯基）甲氧基] -4-氧代丁-2-烯酸含量小于或等于0.15的产物 ％摩尔。
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公开(公告)号：US20100152483A1
公开(公告)日：2010-06-17
申请号：US12654123
申请日：2009-12-10
IPC分类号： C07C69/02
CPC分类号： C07C219/28 , C07C57/15
摘要： New solid forms of fesoterodine fumarate are described. In particular, amorphous fesoterodine fumarate, characterised by a powder X-ray diffraction spectrum as shown in FIG. 1 and by an IR spectrum as shown in FIG. 2 is described. Also fesoterodine fumarate in crystalline form I, characterised by a powder X-ray diffraction spectrum as shown in FIG. 3, by a DSC profile as shown in FIG. 4, by an IR spectrum as shown in FIG. 5, by a solid state 13C-NMR spectrum as shown in FIG. 6 and by a Raman spectrum as shown in FIGS. 7, 8 and 9 is described.
摘要翻译： 描述富马酸非索罗定的新固体形式。 特别是富马酸非索非罗丹，其特征在于如图1所示的粉末X射线衍射光谱。 1和IR光谱如图1所示。 描述图2。 还有结晶形式I的富马酸菲索特罗，其特征在于如图1所示的粉末X射线衍射光谱。 如图3所示，通过如图3所示的DSC轮廓。 如图4所示，通过如图4所示的IR光谱。 如图5所示，通过图13所示的固态13 C-NMR光谱。 如图6所示，通过拉曼光谱。 描述图7,8和9。
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公开(公告)号：US09096491B2
公开(公告)日：2015-08-04
申请号：US14232020
申请日：2012-07-09
申请人： Maurizio Zenoni , Umberto Ciambecchini , Lorenzo De Ferra , Stefano Turchetta , Vincenzo De Sio
发明人： Maurizio Zenoni , Umberto Ciambecchini , Lorenzo De Ferra , Stefano Turchetta , Vincenzo De Sio
IPC分类号： C07C227/04 , C07C229/64 , C07C229/42
CPC分类号： C07C227/04 , C07C229/42 , C07C229/64
摘要： A process for the preparation of a prodrug of 5-aminosalicylic acid, namely 2-butanoyloxy-5-amino-benzoic acid, and solid forms of such compound are described.
摘要翻译： 描述了制备5-氨基水杨酸的前药的方法，即2-丁酰氧基-5-氨基 - 苯甲酸，以及这种化合物的固体形式。
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6.发明申请PROCESS FOR THE PREPARATION OF 2-HYDROXY-4-PHENYL-3,4-DIHYDRO-2H-CHROMEN-6-YL-METHANOL AND (R)-FESO-DEACYL 有权制备2-羟基-4-苯基-3,4-二氢-2H-吡喃-6-基甲醇和（R） - 脱乙酰基的方法公开(公告)号：US20130079532A1
公开(公告)日：2013-03-28
申请号：US13702403
申请日：2011-04-29
IPC分类号： C07D311/20 , C07C213/10 , C07C213/00 , C07C213/02 , C07C215/54
CPC分类号： C07D311/20 , C07C213/00 , C07C213/02 , C07C213/10 , C07C215/54
摘要： The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called “feso chromenyl” and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called “(R)-feso deacyl”, which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate “(R)-feso deacyl”, called form B.
摘要翻译： 本发明涉及一种改进和工业上有利的制备2-羟基-4-苯基-3,4-二氢-2H-色烯-6-基 - 甲醇中间体的方法，也称为feso色烯基和（R）-2 - [3-（二异丙基氨基）-1-苯基丙基] -4-（羟甲基）苯酚，也称为（R） - 非索酰基，它们又用于合成西索罗定，特别是富马酸非索罗定。 该方法利用在工业水平上无毒且易于处理的试剂，能够获得称为B型关键中间体（R） - 二甲酰基的新的稳定和非吸湿结晶形式。
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7.发明授权Process for the preparation of 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol and (R)-feso-deacyl 有权制备2-羟基-4-苯基-3,4-二氢-2H-色烯-6-基 - 甲醇和（R） - 壬酰基公开(公告)号：US08946456B2
公开(公告)日：2015-02-03
申请号：US13702403
申请日：2011-04-29
IPC分类号： C07D311/20 , C07C213/10 , C07C213/00 , C07C213/02 , C07C215/54
CPC分类号： C07D311/20 , C07C213/00 , C07C213/02 , C07C213/10 , C07C215/54
摘要： The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called “feso chromenyl” and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called “(R)-feso deacyl”, which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate “(R)-feso deacyl”, called form B.
摘要翻译： 本发明涉及一种改进的和工业上有利的制备2-羟基-4-苯基-3,4-二氢-2H-色烯-6-基 - 甲醇中间体的方法，也称为“feso chromenyl”和（R） -2- [3-（二异丙基氨基）-1-苯基丙基] -4-（羟甲基）苯酚，也称为“（R） - 非索酰基”，它们又用于合成西索罗定，特别是富马酸非索罗定。 该方法利用在工业水平上无毒且易于管理的试剂，能够获得称为B型关键中间体“（R） - feso deacyl”的新型稳定和非吸湿结晶形式。
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公开(公告)号：US20140163251A1
公开(公告)日：2014-06-12
申请号：US14232020
申请日：2012-07-09
申请人： Maurizio Zenoni , Umberto Ciambecchini , Lorenzo De Ferra , Stefano Turchetta , Vincenzo De Sio
发明人： Maurizio Zenoni , Umberto Ciambecchini , Lorenzo De Ferra , Stefano Turchetta , Vincenzo De Sio
IPC分类号： C07C227/04 , C07C229/42
CPC分类号： C07C227/04 , C07C229/42 , C07C229/64
摘要： A process for the preparation of a prodrug of 5-aminosalicylic acid, namely 2-butanoyloxy-5-amino-benzoic acid,and solid forms of such compound are described.
摘要翻译： 描述了制备5-氨基水杨酸的前药的方法，即2-丁酰氧基-5-氨基 - 苯甲酸，以及这种化合物的固体形式。
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公开(公告)号：US08981090B2
公开(公告)日：2015-03-17
申请号：US13176199
申请日：2011-07-05
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to a novel process for the preparation of pemetrexed diethyl ester 2 by purifying the mixture obtainable by reacting compounds 1 and 1a in the presence of a chemical agent capable of promoting the formation of a peptide bond in an aprotic organic solvent characterized in that the mixture is subjected to the following steps: a) washing with a basic aqueous solution; b) concentration of the organic phase; c) addition of a polar organic solvent and/or a mixture of polar organic solvents; d) precipitation of the pemetrexed diethyl ester 2.
摘要翻译： 本发明涉及一种制备培美曲塞二乙酯2的新方法，该方法是通过使化合物1和1a在能够促进肽键形成的化学试剂存在下纯化得到的混合物，其特征在于： 对混合物进行以下步骤：a）用碱性水溶液洗涤; b）有机相的浓度; c）加入极性有机溶剂和/或极性有机溶剂的混合物; d）培美曲塞二乙酯沉淀2。
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公开(公告)号：US08049031B2
公开(公告)日：2011-11-01
申请号：US12654123
申请日：2009-12-10
IPC分类号： C07C67/02
CPC分类号： C07C219/28 , C07C57/15
摘要： New solid forms of fesoterodine fumarate are described. In particular, amorphous fesoterodine fumarate, characterized by a powder X-ray diffraction spectrum as shown in FIG. 1 and by an IR spectrum as shown in FIG. 2 is described. Also fesoterodine fumarate in crystalline form I, characterized by a powder X-ray diffraction spectrum as shown in FIG. 3, by a DSC profile as shown in FIG. 4, by an IR spectrum as shown in FIG. 5, by a solid state 13C-NMR spectrum as shown in FIG. 6 and by a Raman spectrum as shown in FIGS. 7, 8 and 9 is described.
摘要翻译： 描述富马酸非索罗定的新固体形式。 特别是富马酸非索非罗丹，其特征在于如图1所示的粉末X射线衍射光谱。 1和IR光谱如图1所示。 描述图2。 还有结晶形式I的富马酸菲索特罗，其特征在于如图1所示的粉末X射线衍射光谱。 如图3所示，通过如图3所示的DSC轮廓。 如图4所示，通过如图4所示的IR光谱。 如图5所示，通过图13所示的固态13 C-NMR光谱。 如图6所示，通过拉曼光谱。 描述图7,8和9。
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