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1. 发明申请

US20050250959A1 Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds 有权
标题翻译：铜催化形成碳 - 杂原子和碳 - 碳键
公开(公告)号：US20050250959A1
公开(公告)日：2005-11-10
申请号：US11090951
申请日：2005-03-24
申请人： Stephen Buchwald , Artis Klapars , Fuk Kwong , Eric Streiter , Jacopo Zanon
发明人： Stephen Buchwald , Artis Klapars , Fuk Kwong , Eric Streiter , Jacopo Zanon
IPC分类号： C07D333/38 , C07B39/00 , C07B61/00 , C07C17/20 , C07C21/17 , C07C25/02 , C07C25/18 , C07C45/63 , C07C49/807 , C07C51/363 , C07C57/60 , C07C67/307 , C07C69/612 , C07C201/12 , C07C205/12 , C07C231/12 , C07C233/15 , C07C253/14 , C07C253/30 , C07C255/35 , C07C255/50 , C07C255/52 , C07C255/53 , C07C255/54 , C07C255/55 , C07C255/56 , C07C255/57 , C07C255/58 , C07C255/60 , C07C303/40 , C07C311/16 , C07C319/14 , C07C321/28 , C07C321/30 , C07C323/09 , C07C323/12 , C07C323/20 , C07C323/22 , C07C323/32 , C07C323/37 , C07C323/56 , C07C323/62 , C07D207/267 , C07D209/08 , C07D213/38 , C07D213/70 , C07D213/73 , C07D213/85 , C07D215/18 , C07D215/54 , C07D231/14 , C07D271/10 , C07D271/107 , C07D307/68 , C07D333/62 , C07D333/68 , C07C319/10
CPC分类号： C07D213/70 , C07B39/00 , C07C17/208 , C07C45/63 , C07C51/363 , C07C67/307 , C07C201/12 , C07C231/12 , C07C233/15 , C07C253/14 , C07C253/30 , C07C255/53 , C07C303/40 , C07C319/14 , C07D209/08 , C07D213/38 , C07D213/73 , C07D215/18 , C07D215/54 , C07D231/14 , C07D271/107 , C07D333/62 , C07D333/68 , C07C25/18 , C07C21/17 , C07C25/02 , C07C49/807 , C07C57/60 , C07C69/65 , C07C323/62 , C07C323/37 , C07C323/32 , C07C323/22 , C07C323/20 , C07C323/12 , C07C323/09 , C07C321/28 , C07C311/16 , C07C255/35 , C07C255/50 , C07C255/52 , C07C255/54 , C07C255/57 , C07C255/58 , C07C205/12
摘要： One aspect of the present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-sulfur bond between the sulfur atom of a thiol moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper(II)-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-carbon bond between the carbon atom of cyanide ion and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In another embodiment, the present invention relates to a copper-catalyzed method of transforming an aryl, heteroaryl, or vinyl chloride or bromide into the corresponding aryl, heteroaryl, or vinyl iodide. Yet another embodiment of the present invention relates to a tandem method, which may be practiced in a single reaction vessel, wherein the first step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl iodide from the corresponding aryl, heteroaryl, or vinyl chloride or bromide; and the second step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl nitrile, amide or sulfide from the aryl, heteroaryl, or vinyl iodide formed in the first step.
摘要翻译：本发明的一个方面涉及铜催化的碳 - 杂原子和碳 - 碳键形成方法。在某些实施方案中，本发明涉及在硫醇部分的硫原子和芳基，杂芳基或乙烯基卤化物或磺酸酯的活性炭之间形成碳 - 硫键的铜催化方法。在其它实施方案中，本发明涉及在酰胺的氮原子和芳基，杂芳基或卤化乙烯或磺酸盐的活性炭之间形成碳 - 氮键的铜（II）催化方法。在某些实施方案中，本发明涉及在氰化物离子的碳原子和芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 碳键的铜催化方法。在另一个实施方案中，本发明涉及将芳基，杂芳基或氯乙烯或溴化物转化为相应的芳基，杂芳基或碘乙烯的铜催化方法。本发明的另一个实施方案涉及可以在单个反应容器中实施的串联方法，其中该方法的第一步涉及从相应的芳基铜催化形成芳基，杂芳基或乙烯基碘，杂芳基或氯乙烯或溴化物; 并且该方法的第二步涉及在第一步中形成的芳基，杂芳基或乙烯基腈，酰胺或硫化物从芳基，杂芳基或乙烯基碘形成铜催化的形成。

2. 发明授权

US06888032B2 Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds 有权
标题翻译：铜催化形成碳 - 杂原子和碳 - 碳键
公开(公告)号：US06888032B2
公开(公告)日：2005-05-03
申请号：US10631480
申请日：2003-07-31
申请人： Stephen L. Buchwald , Artis Klapars , Fuk Y. Kwong , Eric R. Streiter , Jacopo Zanon
发明人： Stephen L. Buchwald , Artis Klapars , Fuk Y. Kwong , Eric R. Streiter , Jacopo Zanon
IPC分类号： C07D333/38 , C07B39/00 , C07B61/00 , C07C17/20 , C07C21/17 , C07C25/02 , C07C25/18 , C07C45/63 , C07C49/807 , C07C51/363 , C07C57/60 , C07C67/307 , C07C69/612 , C07C201/12 , C07C205/12 , C07C231/12 , C07C233/15 , C07C253/14 , C07C253/30 , C07C255/35 , C07C255/50 , C07C255/52 , C07C255/53 , C07C255/54 , C07C255/55 , C07C255/56 , C07C255/57 , C07C255/58 , C07C255/60 , C07C303/40 , C07C311/16 , C07C319/14 , C07C321/28 , C07C321/30 , C07C323/09 , C07C323/12 , C07C323/20 , C07C323/22 , C07C323/32 , C07C323/37 , C07C323/56 , C07C323/62 , C07D207/267 , C07D209/08 , C07D213/38 , C07D213/70 , C07D213/73 , C07D213/85 , C07D215/18 , C07D215/54 , C07D231/14 , C07D271/10 , C07D271/107 , C07D307/68 , C07D333/62 , C07D333/68 , C07C319/04
CPC分类号： C07D213/70 , C07B39/00 , C07C17/208 , C07C45/63 , C07C51/363 , C07C67/307 , C07C201/12 , C07C231/12 , C07C233/15 , C07C253/14 , C07C253/30 , C07C255/53 , C07C303/40 , C07C319/14 , C07D209/08 , C07D213/38 , C07D213/73 , C07D215/18 , C07D215/54 , C07D231/14 , C07D271/107 , C07D333/62 , C07D333/68 , C07C25/18 , C07C21/17 , C07C25/02 , C07C49/807 , C07C57/60 , C07C69/65 , C07C323/62 , C07C323/37 , C07C323/32 , C07C323/22 , C07C323/20 , C07C323/12 , C07C323/09 , C07C321/28 , C07C311/16 , C07C255/35 , C07C255/50 , C07C255/52 , C07C255/54 , C07C255/57 , C07C255/58 , C07C205/12
摘要： One aspect of the present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-sulfur bond between the sulfur atom of a thiol moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper(II)-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-carbon bond between the carbon atom of cyanide ion and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In another embodiment, the present invention relates to a copper-catalyzed method of transforming an aryl, heteroaryl, or vinyl chloride or bromide into the corresponding aryl, heteroaryl, or vinyl iodide. Yet another embodient of the present invention relates to a tandem method, which may be practiced in a single reaction vessel, wherein the first step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl iodide from the corresponding aryl, heteroaryl, or vinyl chloride or bromide; and the second step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl nitrile, amide or sulfide from the aryl, heteroaryl, or vinyl iodide formed in the first step.
摘要翻译：本发明的一个方面涉及铜催化的碳 - 杂原子和碳 - 碳键形成方法。在某些实施方案中，本发明涉及在硫醇部分的硫原子和芳基，杂芳基或乙烯基卤化物或磺酸酯的活性炭之间形成碳 - 硫键的铜催化方法。在其它实施方案中，本发明涉及在酰胺的氮原子和芳基，杂芳基或卤化乙烯或磺酸盐的活性炭之间形成碳 - 氮键的铜（II）催化方法。在某些实施方案中，本发明涉及在氰化物离子的碳原子和芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 碳键的铜催化方法。在另一个实施方案中，本发明涉及将芳基，杂芳基或氯乙烯或溴化物转化为相应的芳基，杂芳基或碘乙烯的铜催化方法。本发明的另一个实施方案涉及串联方法，其可以在单个反应容器中实施，其中该方法的第一步骤涉及从相应的芳基铜催化形成芳基，杂芳基或乙烯基碘，杂芳基或氯乙烯或溴化物; 并且该方法的第二步涉及在第一步中形成的芳基，杂芳基或乙烯基腈，酰胺或硫化物从芳基，杂芳基或乙烯基碘形成铜催化的形成。

3. 发明授权

US07323608B2 Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds 有权
标题翻译：铜催化形成碳 - 杂原子和碳 - 碳键
公开(公告)号：US07323608B2
公开(公告)日：2008-01-29
申请号：US11090951
申请日：2005-03-24
申请人： Stephen L. Buchwald , Artis Klapars , Fuk Y. Kwong , Eric R. Streiter , Jacopo Zanon
发明人： Stephen L. Buchwald , Artis Klapars , Fuk Y. Kwong , Eric R. Streiter , Jacopo Zanon
IPC分类号： C07C17/20
CPC分类号： C07D213/70 , C07B39/00 , C07C17/208 , C07C45/63 , C07C51/363 , C07C67/307 , C07C201/12 , C07C231/12 , C07C233/15 , C07C253/14 , C07C253/30 , C07C255/53 , C07C303/40 , C07C319/14 , C07D209/08 , C07D213/38 , C07D213/73 , C07D215/18 , C07D215/54 , C07D231/14 , C07D271/107 , C07D333/62 , C07D333/68 , C07C25/18 , C07C21/17 , C07C25/02 , C07C49/807 , C07C57/60 , C07C69/65 , C07C323/62 , C07C323/37 , C07C323/32 , C07C323/22 , C07C323/20 , C07C323/12 , C07C323/09 , C07C321/28 , C07C311/16 , C07C255/35 , C07C255/50 , C07C255/52 , C07C255/54 , C07C255/57 , C07C255/58 , C07C205/12
摘要： One aspect of the present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-sulfur bond between the sulfur atom of a thiol moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper(II)-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-carbon bond between the carbon atom of cyanide ion and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In another embodiment, the present invention relates to a copper-catalyzed method of transforming an aryl, heteroaryl, or vinyl chloride or bromide into the corresponding aryl, heteroaryl, or vinyl iodide. Yet another embodiment of the present invention relates to a tandem method, which may be practiced in a single reaction vessel, wherein the first step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl iodide from the corresponding aryl, heteroaryl, or vinyl chloride or bromide; and the second step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl nitrile, amide or sulfide from the aryl, heteroaryl, or vinyl iodide formed in the first step.
摘要翻译：本发明的一个方面涉及铜催化的碳 - 杂原子和碳 - 碳键形成方法。在某些实施方案中，本发明涉及在硫醇部分的硫原子和芳基，杂芳基或乙烯基卤化物或磺酸酯的活性炭之间形成碳 - 硫键的铜催化方法。在其它实施方案中，本发明涉及在酰胺的氮原子和芳基，杂芳基或卤化乙烯或磺酸盐的活性炭之间形成碳 - 氮键的铜（II）催化方法。在某些实施方案中，本发明涉及在氰化物离子的碳原子和芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 碳键的铜催化方法。在另一个实施方案中，本发明涉及将芳基，杂芳基或氯乙烯或溴化物转化为相应的芳基，杂芳基或碘乙烯的铜催化方法。本发明的另一个实施方案涉及可以在单个反应容器中实施的串联方法，其中该方法的第一步涉及从相应的芳基铜催化形成芳基，杂芳基或乙烯基碘，杂芳基或氯乙烯或溴化物; 并且该方法的第二步涉及在第一步中形成的芳基，杂芳基或乙烯基腈，酰胺或硫化物从芳基，杂芳基或乙烯基碘形成铜催化的形成。

4. 发明授权

US07608711B2 Process for the preparation of ziprasidone 失效
标题翻译：齐拉西酮制备方法
公开(公告)号：US07608711B2
公开(公告)日：2009-10-27
申请号：US11595861
申请日：2006-11-13
申请人： Jacopo Zanon , Oscar Martini , Francesco Ciardella , Luca Gregori , Federico Sbrogio , Andrea Castellin
发明人： Jacopo Zanon , Oscar Martini , Francesco Ciardella , Luca Gregori , Federico Sbrogio , Andrea Castellin
IPC分类号： C07D417/12 , C07D209/34
CPC分类号： C07D417/12 , C07D209/34
摘要： A process for the preparation of ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the desired compound.
摘要翻译：一种制备齐拉西酮和一种可用于其制备的新型中间体的方法。该方法包括还原化合物（III）以得到化合物（V），然后将其还原成化合物（II）。使其与化合物（IV）反应，得到所需化合物。

5. 发明申请

US20110028726A1 METHOD FOR PREPARING ARGATROBAN MONOHYDRATE AND A PROCESS FOR ITS SYNTHESIS 有权
标题翻译：制备阿糖胞苷单硬脂酸酯的方法及其合成方法
公开(公告)号：US20110028726A1
公开(公告)日：2011-02-03
申请号：US12935512
申请日：2009-04-06
申请人： Jacopo Zanon , Giovanna Libralon , Andrea Nicole
发明人： Jacopo Zanon , Giovanna Libralon , Andrea Nicole
IPC分类号： C07D215/36
CPC分类号： C07D401/12
摘要： A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[NG-nitro-N2-(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2-piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico-chemical characteristics.The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.
摘要翻译：描述了从（2R，4R）-1- [NG-硝基-N 2 - （3-甲基-8-喹啉磺酰基）-L-精氨酰基] -4-甲基-2-哌啶羧酸得到的制备阿格曲班一水合物的方法，适当处理粗制阿加曲班。该方法包括在连续步骤中制备阿加曲班一水合物或分离纯化的阿加曲班的中间步骤。也可从阿加曲班一水合物获得的是无水阿加曲班，显示具有新的物理化学特性。所述的阿加曲班合成和纯化方法因此能够获得三种不同形式的阿加曲班，没有以前描述，其具有独特的物理化学特性，特别是能够以高产率和高纯度获得阿格曲班一水合物，因此是适用于专利药物活性成分的产品。

6. 发明申请

US20130123539A1 METHODS FOR PREPARING RITODRINE HYDROCHLORIDE 有权
标题翻译：制备雷托品氯化氢的方法
公开(公告)号：US20130123539A1
公开(公告)日：2013-05-16
申请号：US13643101
申请日：2011-03-24
申请人： Jacopo Zanon
发明人： Jacopo Zanon
IPC分类号： C07C215/60 , C07C213/08
CPC分类号： C07C215/60 , C07C213/08 , C07C213/10
摘要： Methods for preparing Ritodrine hydrochloride are provided. Also provided is non-hygroscopic, crystalline, polymorphic Ritodrine hydrochloride of Form I.
摘要翻译：提供盐酸利托君的制备方法。还提供了形式I的非吸湿性，结晶性，多晶型盐酸利托君。

7. 发明授权

US08378106B2 Method for preparing argatroban monohydrate and a process for its synthesis 有权
标题翻译：制备阿加曲班一水合物的方法及其合成方法
公开(公告)号：US08378106B2
公开(公告)日：2013-02-19
申请号：US12935512
申请日：2009-04-06
申请人： Jacopo Zanon , Giovanna Libralon , Andrea Nicole′
发明人： Jacopo Zanon , Giovanna Libralon , Andrea Nicole′
IPC分类号： C07D215/38
CPC分类号： C07D401/12
摘要： A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[NG-nitro-N2-(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2-piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico-chemical characteristics.The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.
摘要翻译：描述了从（2R，4R）-1- [NG-硝基-N 2 - （3-甲基-8-喹啉磺酰基）-L-精氨酰基] -4-甲基-2-哌啶羧酸得到的制备阿格曲班一水合物的方法，适当处理粗制阿加曲班。该方法包括在连续步骤中制备阿加曲班一水合物或分离纯化的阿加曲班的中间步骤。也可从阿加曲班一水合物获得的是无水阿加曲班，显示具有新的物理化学特性。所述的阿加曲班合成和纯化方法因此能够获得三种不同形式的阿加曲班，没有以前描述，其具有独特的物理化学特性，特别是能够以高产率和高纯度获得阿格曲班一水合物，因此是适用于专利药物活性成分的产品。

8. 发明授权

US08912360B2 Methods for preparing ritodrine hydrochloride 有权
标题翻译：盐酸利托君的制备方法
公开(公告)号：US08912360B2
公开(公告)日：2014-12-16
申请号：US13643101
申请日：2011-03-24
申请人： Jacopo Zanon , Giovanna Libralon , Carla De Faveri , Florian Anton Martin Huber
发明人： Jacopo Zanon , Giovanna Libralon , Carla De Faveri , Florian Anton Martin Huber
IPC分类号： C07C213/00 , C07C209/00 , C07C217/00 , C07C215/60 , C07C213/08 , C07C213/10
CPC分类号： C07C215/60 , C07C213/08 , C07C213/10
摘要： Methods for preparing Ritodrine hydrochloride are provided. Also provided is non-hygroscopic, crystalline, polymorphic Ritodrine hydrochloride of Form I.
摘要翻译：提供盐酸利托君的制备方法。还提供了形式I的非吸湿性，结晶性，多晶型盐酸利托君。

9. 发明申请

US20090264656A1 METHOD FOR MANUFACTURE OF SERTINDOLE 审中-公开
标题翻译：方法制造系列
公开(公告)号：US20090264656A1
公开(公告)日：2009-10-22
申请号：US12360338
申请日：2009-01-27
申请人： Jacopo Zanon , Marco Villa , Francesco Ciardella
发明人： Jacopo Zanon , Marco Villa , Francesco Ciardella
IPC分类号： C07D401/04
CPC分类号： C07D401/14 , C07D209/08
摘要： The present invention relates to a novel method for manufacture of sertindole comprising manufacturing 5-chloro-1-(4-fluorophenyl)-indole and converting it to sertindole wherein the method for manufacture of 5-chloro-1-(4-fluorophenyl)-indole comprises reacting 5-chloro-indole with a 4-fluorophenylhalide in the presence of a base, a chelating ligand and catalytic amounts or a copper salt comprising copper(I) or copper(II) and an anion which does not interfere in an unfavourable way with the reaction.
摘要翻译：本发明涉及一种制造塞丁醇的新方法，其包括制备5-氯-1-（4-氟苯基） - 吲哚并将其转化为三氢吲哚，其中制备5-氯-1-（4-氟苯基） - 吲哚的方法，吲哚包括在碱，螯合配体和催化量存在下使5-氯 - 吲哚与4-氟苯基卤反应，或包含铜（I）或铜（II）的铜盐和不干扰不利的阴离子方式与反应。

10. 发明申请

US20070117810A1 Process for the preparation of ziprasidone 失效
标题翻译：齐拉西酮制备方法
公开(公告)号：US20070117810A1
公开(公告)日：2007-05-24
申请号：US11595861
申请日：2006-11-13
申请人： Jacopo Zanon , Oscar Martini , Francesco Ciardella , Luca Gregori , Federico Sbrogio , Andrea Castellin
发明人： Jacopo Zanon , Oscar Martini , Francesco Ciardella , Luca Gregori , Federico Sbrogio , Andrea Castellin
IPC分类号： A61K31/496 , C07D417/14
CPC分类号： C07D417/12 , C07D209/34
摘要： A process for the preparation of ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the desired compound.
摘要翻译：一种制备齐拉西酮和一种可用于其制备的新型中间体的方法。该方法包括还原化合物（III）以得到化合物（V），然后将其还原成化合物（II）。使其与化合物（IV）反应，得到所需化合物。

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