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1. 发明授权

US09096495B2 Process for the preparation of triiodinated carboxylic aromatic derivatives 有权
标题翻译：三碘化羧酸衍生物的制备方法
公开(公告)号：US09096495B2
公开(公告)日：2015-08-04
申请号：US13143225
申请日：2010-03-12
申请人： Pier Lucio Anelli , Marino Brocchetta , Roberta Fretta , Luciano Lattuada , Armando Mortillaro
发明人： Pier Lucio Anelli , Marino Brocchetta , Roberta Fretta , Luciano Lattuada , Armando Mortillaro
IPC分类号： C07C233/06 , C07C237/46 , C07C231/02 , C07C231/10
CPC分类号： C07C237/46 , C07C231/02 , C07C231/10 , C07C235/16
摘要： The present invention relates to a process for the preparation of given carboxamido compounds, in particular of 2,4,6-triiodoisophthalic acid derivatives, as useful intermediates for the preparation of X-ray contrast media among which is iopamidol. The said process comprises reacting suitable N-sulfinyl intermediate compounds with a commercially available α-hydroxyacid or a salt thereof.
摘要翻译：本发明涉及制备给定的甲酰氨基化合物，特别是2,4,6-三碘代邻苯二甲酸衍生物的方法，作为制备X射线造影剂的有用中间体，其中碘帕醇。所述方法包括使合适的N-亚磺酰基中间体化合物与市售的α-羟基酸或其盐反应。

2. 发明申请

US20100099888A1 Process for the preparation of anticancer drugs 审中-公开
标题翻译：抗癌药物的制备工艺
公开(公告)号：US20100099888A1
公开(公告)日：2010-04-22
申请号：US12592066
申请日：2009-11-17
申请人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
发明人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： A process for preparing Anastrozole is provided. In the process the steps of a. combining 3,5-bis(2-cyanoisopropyl)toluene, a solvent selected from the group consisting of acetonitrile, dichloromethane and chlorobenzene, a brominating reagent selected from a group consisting of N-bromosuccinimide and 1,3-dibromo-5,5-dimethylhydantoin, and 2,2′-azobis(2-methylpropionitrile); b. heating; c. combining with 1,2,4-triazole, a solvent selected from a group consisting of N-methylpyrrolidine, dimethylformamide, mixtures of NMP and DMF, dimethylsulfoxide, mixtures of DMSO and toluene, acetone, ACN, and tetrahydrofuran, a base selected from a group consisting of NaOH, KOH, K2CO3, and Na2CO3, and 1,3-benzendiacetonitrile-5-(bromomethyl)-α,α,{acute over (α)},{acute over (α)}-tetramethyl, at a temperature below −20° C. are performed.
摘要翻译：提供了一种制备阿那曲唑的方法。在这个过程中，a。结合3,5-双（2-氰基异丙基）甲苯，选自乙腈，二氯甲烷和氯苯的溶剂，选自N-溴代琥珀酰亚胺和1,3-二溴-5,5-二氯苯的溴化试剂，二甲基乙内酰脲和2,2'-偶氮双（2-甲基丙腈）; b。加热; C。与1,2,4-三唑结合，选自N-甲基吡咯烷，二甲基甲酰胺，NMP和DMF的混合物，二甲基亚砜，DMSO和甲苯的混合物，丙酮，ACN和四氢呋喃的溶剂，选自由NaOH，KOH，K 2 CO 3和Na 2 CO 3组成的组，和1,3-苯撑二乙腈-5-（溴甲基）-α，α，（急性（α）}，{急（α）} - 低于-20℃。

3. 发明授权

US09238615B2 Process for the iodination of aromatic compounds 有权
标题翻译：芳香族化合物碘化方法
公开(公告)号：US09238615B2
公开(公告)日：2016-01-19
申请号：US13265165
申请日：2010-04-08
申请人： Attilio Citterio , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli , Aurelia Ferrigato , Gabriele Meli , Roberta Fretta , Roberta Mazzon
发明人： Attilio Citterio , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli , Aurelia Ferrigato , Gabriele Meli , Roberta Fretta , Roberta Mazzon
IPC分类号： C07C227/16
CPC分类号： C07C227/16 , C07C229/62
摘要： The present invention relates to a process for the preparation of iodinated anilines; in particular, it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted anilines to the corresponding 3,5-disubstituted-2,4,6-triiodoanilines, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.
摘要翻译：本发明涉及一种制备碘化苯胺的方法; 特别涉及一种方法，其包括将3,5-二取代的2,4,6-三碘苯胺与适当的活化的碘直接碘化为3,5-二取代-2,4,6-三碘苯胺，其是用于合成 x射线造影剂，以及造影剂本身的制备。

4. 发明申请

US20120041224A1 Process For The Iodination Of Aromatic Compounds 有权
标题翻译：芳香族化合物的碘化处理
公开(公告)号：US20120041224A1
公开(公告)日：2012-02-16
申请号：US13265165
申请日：2010-04-08
申请人： Attilio Citterio , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli , Aurelia Ferrigato , Gabriele Meli , Roberta Fretta , Roberta Mazzon
发明人： Attilio Citterio , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli , Aurelia Ferrigato , Gabriele Meli , Roberta Fretta , Roberta Mazzon
IPC分类号： C07C231/02 , C07C231/12 , C07C227/16
CPC分类号： C07C227/16 , C07C229/62
摘要： The present invention relates to a process for the preparation of iodinated anilines; in particular, it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted anilines to the corresponding 3,5-disubstituted-2,4,6-triiodoanilines, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.
摘要翻译：本发明涉及一种制备碘化苯胺的方法; 特别涉及一种方法，其包括将3,5-二取代的2,4,6-三碘苯胺与适当的活化的碘直接碘化为3,5-二取代-2,4,6-三碘苯胺，其是用于合成 x射线造影剂，以及造影剂本身的制备。

5. 发明申请

US20060276657A1 Process for the preparation of anticancer drugs 失效
标题翻译：抗癌药物的制备工艺
公开(公告)号：US20060276657A1
公开(公告)日：2006-12-07
申请号：US11400639
申请日：2006-04-06
申请人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
发明人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： A process for preparing Anastrozole is provided. In the process the steps of a. combining 3,5-bis (2-cyanoisopropyl)toluene, a solvent selected from the group consisting of acetonitrile, dichloromethane and chlorobenzene, a brominating reagent selected from a group consisting of N-bromosuccinimide and 1,3-dibromo-5,5-dimethylhydantoin, and 2,2′-azobis(2-methylpropionitrile); b. heating; c. combining with 1,2,4-triazole, a solvent selected from a group consisting of N-methylpyrrolidine, dimethylformamide, mixtures of NMP and DMF, dimethylsulfoxide, mixtures of DMSO and toluene, acetone, ACN, and tetrahydrofuran, a base selected from a group consisting of NaOH, KOH, K2CO3, and Na2CO3, and 1,3-benzendiacetonitrile-5-(bromomethyl)-α,α,{acute over (α)},{acute over (α)}-tetramethyl, at a temperature below −20° C. are performed.
摘要翻译：提供了一种制备阿那曲唑的方法。在这个过程中，a。结合3,5-双（2-氰基异丙基）甲苯，选自乙腈，二氯甲烷和氯苯的溶剂，选自N-溴代琥珀酰亚胺和1,3-二溴-5,5-二氯苯的溴化试剂，二甲基乙内酰脲和2,2'-偶氮双（2-甲基丙腈）; b。加热; C。与1,2,4-三唑组合，选自N-甲基吡咯烷，二甲基甲酰胺，NMP和DMF的混合物，二甲基亚砜，DMSO和甲苯的混合物，丙酮，ACN和四氢呋喃的溶剂，选自由NaOH，KOH，K 2 CO 3 3和Na 2 CO 3 3组成的组和1,3 - 苄基乙腈-5-（溴甲基）-α，α，α，α-四甲基，在低于-20℃的温度下进行。

6. 发明申请

US20120232151A1 Process for the Preparation of Gadobenate Dimeglumine Complex in a Solid Form 审中-公开
标题翻译：以固体形式制备钆酸二甲酚复合物的方法
公开(公告)号：US20120232151A1
公开(公告)日：2012-09-13
申请号：US13510409
申请日：2010-11-23
申请人： Pier Lucio Anelli , Pierfrancesco Morisini , Silvia Ceragioli , Fulvio Uggeri , Luciano Lattuada , Roberta Fretta , Aurelia Ferrigato
发明人： Pier Lucio Anelli , Pierfrancesco Morisini , Silvia Ceragioli , Fulvio Uggeri , Luciano Lattuada , Roberta Fretta , Aurelia Ferrigato
IPC分类号： C07C227/00 , A61K31/197 , C07C229/36
CPC分类号： A61K49/1887 , A61K9/0019 , B29C67/24 , C07C213/10 , C07C227/38 , C07C227/40 , Y10T428/2982 , C07C229/22
摘要： The present invention discloses a process for the preparation of gadobenate dimeglumine complex in a solid form. In particular, said solid form is conveniently obtained by spray-drying a corresponding liquid suspension at a given temperature and concentration. The present invention is particularly advantageous for the industrial scale as the solid form may be obtained by employing water as a solvent, which is a non-toxic solvent, easy to handle and basically not requiring troublesome health or safety precautions.
摘要翻译：本发明公开了一种以固体形式制备钆酸二甲酚络合物的方法。特别地，所述固体形式通过在给定温度和浓度下喷雾干燥相应的液体悬浮液而方便地得到。本发明对于工业规模是特别有利的，因为固体形式可以通过使用水作为溶剂，其是无毒溶剂，易于处理并且基本上不需要麻烦的健康或安全预防措施来获得。

7. 发明授权

US07692025B2 Process for the preparation of anticancer drugs 失效
标题翻译：抗癌药物的制备工艺
公开(公告)号：US07692025B2
公开(公告)日：2010-04-06
申请号：US11400639
申请日：2006-04-06
申请人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
发明人： Marco Villa , Roberta Fretta , Nicola Diulgheroff , Alessandro Pontiroli
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： A process for preparing Anastrozole is provided. In the process the steps of a. combining 3,5-bis(2-cyanoisopropyl)toluene, a solvent selected from the group consisting of acetonitrile, dichloromethane and chlorobenzene, a brominating reagent selected from a group consisting of N-bromosuccinimide and 1,3-dibromo-5,5-dimethylhydantoin, and 2,2′-azobis(2-methylpropionitrile); b. heating; c. combining with 1,2,4-triazole, a solvent selected from a group consisting of N-methylpyrrolidinone, dimethylformamide, mixtures of NMP and DMF, dimethylsulfoxide, mixtures of DMSO and toluene, acetone, ACN, and tetrahydrofuran, a base selected from a group consisting of NaOH, KOH, K2CO3, and Na2CO3, and 1,3-benzendiacetonitrile-5-(bromomethyl)-α,α,{acute over (α)},{acute over (α)}-tetramethyl, at a temperature below −20° C. are performed.
摘要翻译：提供了制备阿那曲唑的方法。在这个过程中，a。结合3,5-双（2-氰基异丙基）甲苯，选自乙腈，二氯甲烷和氯苯的溶剂，选自N-溴代琥珀酰亚胺和1,3-二溴-5,5-二氯苯的溴化试剂，二甲基乙内酰脲和2,2'-偶氮双（2-甲基丙腈）; b。加热; C。与1,2,4-三唑组合，选自N-甲基吡咯烷酮，二甲基甲酰胺，NMP和DMF的混合物，二甲基亚砜，DMSO和甲苯的混合物，丙酮，ACN和四氢呋喃的溶剂，选自由NaOH，KOH，K 2 CO 3和Na 2 CO 3组成的组，和1,3-苯撑二乙腈-5-（溴甲基）-α，α，（急性（α）}，{急（α）} - 低于-20℃。

8. 发明申请

US20060047108A1 Synthesis of idarubicin aglycone 审中-公开
标题翻译：伊达比星糖苷配基的合成
公开(公告)号：US20060047108A1
公开(公告)日：2006-03-02
申请号：US11210605
申请日：2005-08-23
申请人： Marco Villa , Roberto Arosio , Roberta Fretta , Nicola Diulgheroff
发明人： Marco Villa , Roberto Arosio , Roberta Fretta , Nicola Diulgheroff
IPC分类号： C07H15/24 , C07C46/00
CPC分类号： C07C50/38 , C07C46/00 , C07C2603/44
摘要： The present invention provides a new method of producing high quality idarubicin aglycone from 4-protected demethoxydaunomycinones such as 4-demethoxydaunomycinone-4-triflate.
摘要翻译：本发明提供了一种从4-保护的脱甲氧基多霉素酮如4-脱氧山梨醇酮-4-三氟甲磺酸盐生产高品质伊达比星苷元的新方法。

9. 发明申请

US20110275850A1 Process For The Preparation Of Triiodinated Carboxylic Aromatic Derivatives 有权
标题翻译：三碘化羧基芳族衍生物的制备方法
公开(公告)号：US20110275850A1
公开(公告)日：2011-11-10
申请号：US13143225
申请日：2010-03-12
申请人： Pier Lucio Anelli , Marino Brocchetta , Roberta Fretta , Luciano Lattuada , Armando Mortillaro
发明人： Pier Lucio Anelli , Marino Brocchetta , Roberta Fretta , Luciano Lattuada , Armando Mortillaro
IPC分类号： C07C231/10 , C07C231/02
CPC分类号： C07C237/46 , C07C231/02 , C07C231/10 , C07C235/16
摘要： The present invention relates to a process for the preparation of given carboxamido compounds, in particular of 2,4,6-triiodoisophthalic acid derivatives, as useful intermediates for the preparation of X-ray contrast media among which is iopamidol. The said process comprises reacting suitable N-sulfinyl intermediate compounds with a commercially available α-hydroxyacid or a salt thereof.
摘要翻译：本发明涉及制备给定的甲酰氨基化合物，特别是2,4,6-三碘代邻苯二甲酸衍生物的方法，作为制备X射线造影剂的有用中间体，其中碘帕醇。所述方法包括使合适的N-亚磺酰基中间体化合物与市售的α-羟基酸或其盐反应。

10. 发明申请

US20060035872A1 Process for the preparation of 3-oximino steroids 审中-公开
标题翻译： 3-肟基类固醇的制备方法
公开(公告)号：US20060035872A1
公开(公告)日：2006-02-16
申请号：US11202191
申请日：2005-08-12
申请人： Marco Villa , Roberta Fretta , Nicola Diulgheroff
发明人： Marco Villa , Roberta Fretta , Nicola Diulgheroff
IPC分类号： A61K31/56 , C07J41/00
CPC分类号： C07J41/00 , C07J41/0016
摘要： The present invention provides a method of preparing norelgestromin or norgestimate by reacting the corresponding 3-oxosteroid precursor with hydroxylamine HCl and a base to obtain a reaction mixture forming norelgestromin or norgestimate; monitoring the anti/syn ratio of the norelgestromin or norgestimate produced in the reaction mixture; adding a base to the reaction mixture to neutralize acidity in the reaction mixture when a desired anti/syn ratio is detected; and isolating the norelgestromin or norgestimate. The present invention also provides a process allowing a control of the formation of the anti isomer and syn isomer of norelgestromin or norgestimate by reacting the corresponding 3-oxosteroid precursor with hydroxylamine HCl and a base to obtain a reaction mixture forming norelgestromin or norgestimate; regulating the acidity of the reaction mixture to adjust the anti/syn ratio of the norelgestromin or norgestimate produced in the reaction mixture; adding a base to the reaction mixture to neutralize acidity in the reaction mixture when a desired anti/syn ratio is detected; and isolating the norelgestromin or norgestimate.
摘要翻译：本发明提供了通过使相应的3-氧代甾体前体与羟胺HCl和碱反应来制备诺美孕酮或诺孕酯的方法，以获得形成诺美孕酮或诺孕酯的反应混合物; 监测反应混合物中产生的去甲孕酮或诺孕酯的抗/顺应比; 当检测到所需的抗/顺式比时，向反应混合物中加入碱以中和反应混合物中的酸度; 并分离去甲孕酮或诺孕酯。本发明还提供一种方法，其通过使相应的3-氧代甾体前体与羟胺HCl和碱反应以获得形成去甲孕激素或诺孕酯的反应混合物，从而控制去甲孕酮或诺孕酯的抗异构体和顺式异构体的形成; 调节反应混合物的酸度以调节反应混合物中产生的诺美辛溴或诺孕酯的抗/顺比; 当检测到所需的抗/顺式比时，向反应混合物中加入碱以中和反应混合物中的酸度; 并分离去甲孕酮或诺孕酯。

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