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1. 发明申请

US20160002186A1 METHODS AND INTERMEDIATES FOR PREPARING PHARMACEUTICAL AGENTS 有权
公开(公告)号：US20160002186A1
公开(公告)日：2016-01-07
申请号：US14799090
申请日：2015-07-14
申请人： Gilead Sciences, Inc.
发明人： Richard Polniaszek , Steven Pfeiffer , Richard Yu , Aaron Cullen , Eric Dowdy , Duong Tran , Kenneth Kent , Zhongxin Zhou , Douglas Cordeau , Leah Easton-Scott
IPC分类号： C07D277/30
CPC分类号： C07D277/30 , C07C209/62 , C07C209/70 , C07C303/34 , C07C307/02 , C07C307/06 , C07D277/28 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , Y02P20/55 , C07C211/27 , C07C211/28
摘要： The invention provides methods and intermediates that are useful for preparing a compound of formula I: and salts thereof.

2. 发明申请

US20150361049A1 SYNTHESES OF N-HETEROCYCLIC CARBENES AND INTERMEDIATES THEREFOR 有权
标题翻译： N-杂环碳烯的合成及其中间体
公开(公告)号：US20150361049A1
公开(公告)日：2015-12-17
申请号：US14759595
申请日：2014-01-06
申请人： UNIVERSITY COURT OF THE UNIVERSITY OF ST ANDREWS
发明人： Steven P. Nolan , Sebastien Meiries
IPC分类号： C07D233/58 , C07C251/16 , C07C215/68 , C07C211/46
CPC分类号： C07D233/58 , B01J31/2278 , B01J2531/824 , C07C209/68 , C07C209/70 , C07C211/45 , C07C211/46 , C07C211/47 , C07C213/00 , C07C215/68 , C07C227/04 , C07C251/16 , C07D233/60 , C07D295/037 , C07D295/096 , C07F15/006
摘要： A method of preparing a 2,6 disubstituted anilines includes, reacting a 2-amino isophthalic acid diester with sufficient Grignard reagent R2CH2MgX to form the corresponding diol product, dehydrating the diol product to the corresponding dialkene; and hydrogenating the diol product to form the corresponding aniline. The 2,6 disubstituted anilines can be used to produce N-Heterocyciic Carbenes (NHCs). The NHCs can find application in various fields such as organic synthesis, catalysis and macromolecular chemistry. Palladium catalysts containing the NHCs are also described.
摘要翻译：制备2,6-二取代苯胺的方法包括：使2-氨基间苯二甲酸二酯与足够的格氏试剂R2CH2MgX反应形成相应的二醇产物，将二醇产物脱水至相应的二烯键; 并使二醇产物氢化以形成相应的苯胺。 2,6-二取代的苯胺可用于产生N-异基性碳（NHC）。 NHC可以在有机合成，催化和大分子化学等领域得到应用。还描述了含有NHC的钯催化剂。

3. 发明申请

US20150336862A1 CATALYTIC HYDROGENATION USING COMPLEXES OF BASE METALS WITH TRIDENTATE LIGANDS 有权
标题翻译：使用三元配体的碱金属复合物进行催化氢化
公开(公告)号：US20150336862A1
公开(公告)日：2015-11-26
申请号：US13587717
申请日：2012-08-16
申请人： Kalyan V. Vasudevan , Guoqi Zhang , Susan K. Hanson
发明人： Kalyan V. Vasudevan , Guoqi Zhang , Susan K. Hanson
IPC分类号： C07C29/17 , C07F15/06 , C07F5/04 , C07C67/303 , C07C51/36 , C07D211/46 , C07C41/20 , C07C41/18 , C07C29/145 , C07C41/01 , C07C17/354 , C07C45/62 , C07C209/52 , C07C5/03 , C07C5/05 , B01J31/24 , C07F15/04
CPC分类号： B01J31/2295 , B01J31/189 , B01J31/2476 , B01J2231/643 , B01J2231/645 , B01J2231/646 , B01J2531/0244 , B01J2531/845 , B01J2531/847 , C07C5/03 , C07C5/05 , C07C17/354 , C07C29/141 , C07C29/145 , C07C29/172 , C07C29/175 , C07C41/01 , C07C41/18 , C07C41/20 , C07C41/26 , C07C45/62 , C07C51/36 , C07C67/303 , C07C209/52 , C07C209/70 , C07C2531/14 , C07C2531/22 , C07C2531/28 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/08 , C07C2602/42 , C07C2603/12 , C07C2603/18 , C07D211/02 , C07D211/46 , C07F5/04 , C07F15/04 , C07F15/045 , C07F15/06 , C07F15/065 , Y02P20/52 , C07C43/23 , C07C33/20 , C07C33/22 , C07C33/24 , C07C35/38 , C07C69/24 , C07C53/126 , C07C31/125 , C07C33/46 , C07C43/04 , C07C35/32 , C07C43/205 , C07C49/403 , C07C211/27 , C07C211/48 , C07C25/13 , C07C15/073 , C07C15/02 , C07C15/085 , C07C11/02 , C07C13/26 , C07C13/64 , C07C13/20
摘要： Complexes of cobalt and nickel with tridentate ligand PNHPR are effective for hydrogenation of unsaturated compounds. Cobalt complex [(PNHPCy)Co(CH2SiMe3)]BArF4 (PNHPCy=bis[2-(dicyclohexylphosphino)ethyl]amine, BArF4=B(3,5-(CF3)2C6H3)4)) was prepared and used with hydrogen for hydrogenation of alkenes, aldehydes, ketones, and imines under mild conditions (25-60° C., 1-4 atm H2). Nickel complex [(PNHPCy)Ni(H)]BPh4 was used for hydrogenation of styrene and 1-octene under mild conditions. (PNPCy)Ni(H) was used for hydrogenating alkenes.
摘要翻译：钴和镍与三齿配体PNHPR的配合物对于不饱和化合物的氢化是有效的。钴配合物[（PNHPCy）Co（CH2SiMe3）] BArF4（PNHPCy =双[2-（二环己基膦基）乙基]胺，BArF 4 = B（3,5-（CF 3）2 C 6 H 3）4）的烯烃，醛，酮和亚胺在温和条件下（25-60℃，1-4atm H 2）。镍络合物[（PNHPCy）Ni（H）] BPh4用于在温和条件下苯乙烯和1-辛烯的氢化。（PNPCy）Ni（H）用于氢化烯烃。

4. 发明授权

US08877978B2 Method for producing tertiary amine 有权
标题翻译：叔胺的制备方法
公开(公告)号：US08877978B2
公开(公告)日：2014-11-04
申请号：US13996311
申请日：2011-12-19
申请人： Yasumitsu Sakuma , Wataru Nomura , Goshi Yamamoto , Takeshi Narushima
发明人： Yasumitsu Sakuma , Wataru Nomura , Goshi Yamamoto , Takeshi Narushima
IPC分类号： C07C209/16 , B01J23/72 , B01J35/04 , B01J29/068 , B01J29/072
CPC分类号： C07C209/22 , B01J23/72 , B01J29/068 , B01J29/072 , B01J35/04 , B01J2229/186 , B01J2229/38 , B01J2229/42 , C07C209/16 , C07C209/70 , C07C211/08
摘要： The present invention discloses the method for producing a tertiary amine, using the column reactor packed with catalyst layers, containing supplying a liquid and a gaseous raw materials from the bottom of the column, reacting these raw materials in the column, and discharging the product from the top of the column, wherein the column reactor includes two or more honeycomb catalyst layers as the catalyst layers, one or more spaces between each honeycomb catalyst layer, and one or more rectifying sections that prevents a partial or whole back flow of the raw materials, arranged in each space without contacting with the honeycomb catalyst layer.
摘要翻译：本发明公开了使用填充有催化剂层的柱反应器的叔胺的制造方法，其包含从塔底供给液体和气态原料，使塔中的这些原料反应，并将产物从塔的顶部，其中塔反应器包括作为催化剂层的两个或更多个蜂窝催化剂层，每个蜂窝催化剂层与一个或多个防止原料的部分或整个反向流动的整流部分之间的一个或多个空间布置在每个空间中，而不与蜂窝催化剂层接触。

5. 发明申请

US20140323764A1 METHOD FOR PRODUCING TERTIARY AMINE 审中-公开
标题翻译：生产亚胺的方法
公开(公告)号：US20140323764A1
公开(公告)日：2014-10-30
申请号：US14327936
申请日：2014-07-10
申请人： KAO CORPORATION
发明人： Yasumitsu SAKUMA , Wataru NOMURA , Goshi YAMAMOTO , Takeshi NARUSHIMA
IPC分类号： C07C209/22 , C07C209/70
CPC分类号： C07C209/22 , B01J23/72 , B01J29/068 , B01J29/072 , B01J35/04 , B01J2229/186 , B01J2229/38 , B01J2229/42 , C07C209/16 , C07C209/70 , C07C211/08
摘要： The present invention discloses the method for producing a tertiary amine, using the column reactor packed with catalyst layers, containing supplying a liquid and a gaseous raw materials from the bottom of the column, reacting these raw materials in the column, and discharging the product from the top of the column, wherein the column reactor includes two or more honeycomb catalyst layers as the catalyst layers, one or more spaces between each honeycomb catalyst layer, and one or more rectifying sections that prevents a partial or whole back flow of the raw materials, arranged in each space without contacting with the honeycomb catalyst layer.
摘要翻译：本发明公开了使用填充有催化剂层的柱反应器的叔胺的制造方法，其包含从塔底供给液体和气态原料，使塔中的这些原料反应，并将产物从塔的顶部，其中塔反应器包括作为催化剂层的两个或更多个蜂窝催化剂层，每个蜂窝催化剂层与一个或多个防止原料的部分或整个反向流动的整流部分之间的一个或多个空间布置在每个空间中，而不与蜂窝催化剂层接触。

6. 发明授权

US08853210B2 Methods and intermediates for preparing pharmaceutical agents 有权
标题翻译：制备药剂的方法和中间体
公开(公告)号：US08853210B2
公开(公告)日：2014-10-07
申请号：US13925302
申请日：2013-06-24
申请人： Gilead Sciences, Inc.
发明人： Richard Polniaszek , Steven Pfeiffer , Richard Yu , Aaron Cullen , Eric Dowdy , Duong Tran , Kenneth Kent , Zhongxin Zhou , Doug Cordeau , Leah Easton-Scott
IPC分类号： A61K31/5377 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07C209/62 , C07C307/06 , C07D277/28 , C07D277/30 , C07C209/70
CPC分类号： C07D277/30 , C07C209/62 , C07C209/70 , C07C303/34 , C07C307/02 , C07C307/06 , C07D277/28 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , Y02P20/55 , C07C211/27 , C07C211/28
摘要： The invention provides methods and intermediates that are useful for preparing a compound of formula I: and salts thereof.
摘要翻译：本发明提供了可用于制备式I化合物及其盐的方法和中间体。

7. 发明授权

US08497396B2 Methods and intermediates for preparing pharmaceutical agents 有权
公开(公告)号：US08497396B2
公开(公告)日：2013-07-30
申请号：US12752639
申请日：2010-04-01
申请人： Richard Polniaszek , Steven Pfeiffer , Richard Yu , Aaron Cullen , Eric Dowdy , Duong Tran , Kenneth Kent , Zhongxin Zhou , Doug Cordeau , Leah Easton
发明人： Richard Polniaszek , Steven Pfeiffer , Richard Yu , Aaron Cullen , Eric Dowdy , Duong Tran , Kenneth Kent , Zhongxin Zhou , Doug Cordeau , Leah Easton
IPC分类号： C07C307/06 , C07D413/14
CPC分类号： C07D277/30 , C07C209/62 , C07C209/70 , C07C303/34 , C07C307/02 , C07C307/06 , C07D277/28 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , Y02P20/55 , C07C211/27 , C07C211/28
摘要： The invention provides methods and intermediates that are useful for preparing a compound of formula I: and salts thereof.

8. 发明申请

US20130178654A1 PROCESS FOR CINACALCET HYDROCHLORIDE 有权
标题翻译： CINACALCET HYDROCHLORIDE的方法
公开(公告)号：US20130178654A1
公开(公告)日：2013-07-11
申请号：US13810319
申请日：2010-07-16
申请人： Bandi Parthasaradhi Reddy , Kura Rathnakar Reddy , Dasari Muralidhara Reddy , Rapolu Raji Reddy , Jambula Mukunda Reddy , Bandi Vamsi Krishna
发明人： Bandi Parthasaradhi Reddy , Kura Rathnakar Reddy , Dasari Muralidhara Reddy , Rapolu Raji Reddy , Jambula Mukunda Reddy , Bandi Vamsi Krishna
IPC分类号： C07C45/41 , C07C209/84 , C07C209/70
CPC分类号： C07C45/41 , C07C209/28 , C07C209/70 , C07C209/84 , C07C211/30
摘要： 3-[3-(Trifluoromethyl)phenyl]propionaldehyde is a key intermediate for the preparation of cinacalcet hydrochloride. The present invention provides a novel process for the preparation of 3-[3-(trifluoromethyl)phenyl]propionaldehyde. The present invention also provides an improved process for preparation of cinacalcet hydrochloride in high yields. The present invention further provides a process for purification of cinacalcet hydrochloride.
摘要翻译： 3- [3-（三氟甲基）苯基]丙醛是制备西那卡塞盐酸盐的关键中间体。本发明提供了制备3- [3-（三氟甲基）苯基]丙醛的新方法。本发明还提供了以高产率制备盐酸西那卡塞的改进方法。本发明还提供了盐酸西那卡塞的纯化方法。

9. 发明申请

US20090221856A1 PROCESS FOR THE PREPARATION OF AMINES 有权
标题翻译：制备氨基酸的方法
公开(公告)号：US20090221856A1
公开(公告)日：2009-09-03
申请号：US12096796
申请日：2006-12-11
申请人： Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
发明人： Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
IPC分类号： C07C211/31
CPC分类号： C07C209/62 , C07B2200/09 , C07C17/23 , C07C17/30 , C07C17/354 , C07C25/22 , C07C25/24 , C07C209/10 , C07C209/70 , C07C211/61 , C07C2603/66 , C07C23/10
摘要： The present invention relates to a novel a process for the preparation of the compound of the general formula (I), wherein R1 and R2 are independently H or C1-6 alkyl, which comprises treating with a reducing agent either a compound of the general formula (II), wherein R1 and R2 have the meanings given for the compound of the formula (I), R3 is H or C1-4alkyl and Ph is phenyl, or a compound of the general formula (III), wherein R1, R2, R3 and Ph have the meanings given for the compound of the formula (II), the reducing agent being effective to cleave the benzyl moiety Ph-CH(R3)— from the benzylamino moiety PhCH(R3)NH— in the compound of the formula (II) or in the compound of the formula (III) to leave an amino group and, in addition, in the case of the compound of the formula (III), to reduce both the 2,3-double bond and the double bond joining the R1R2C— moiety to the 9-position of the benzonorbornene ring to single bonds. It also relates to processes for the preparation of the compounds (II) and (III) and their precursors and to the compounds (II) and (III) themselves and certain of their precursors, which are novel compounds. The compounds (I) are useful for the preparation of various fungicidal heterocyclyl-carboxylic acid benzonorbornen-5-yl-amides.
摘要翻译：本发明涉及一种制备通式（I）化合物的方法，其中R 1和R 2独立地为H或C 1-6烷基，其包括用还原剂处理通式（II）化合物，其中R1和R2具有式（I）化合物所给出的含义，R 3是H或C 1-4烷基，Ph是苯基，或通式（III）的化合物，其中R1，R2， R3和Ph具有式（II）化合物所给出的含义，还原剂有效地从式（II）化合物中的苄基氨基部分PhCH（R3）NH-切割苄基部分Ph-CH（R3）（II）化合物或式（III）化合物中，以留下氨基，另外，在式（III）化合物的情况下，为了还原2,3-双键和双键将R1R2C-部分连接到苯并降冰片烯环的9位到单键。它还涉及制备化合物（II）和（III）及其前体以及化合物（II）和（III）本身及其某些新型化合物的前体的方法。化合物（I）可用于制备各种杀真菌性杂环基 - 羧酸苯并降冰片烯-5-基 - 酰胺。

10. 发明申请

US20090163569A1 PROCESS FOR THE PRODUCTION OF AMIDES 有权
标题翻译：生产助剂的方法
公开(公告)号：US20090163569A1
公开(公告)日：2009-06-25
申请号：US12066683
申请日：2006-09-14
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
IPC分类号： A01N43/56 , C07D231/14 , C07C211/45 , C07C205/11 , C07D403/12 , A01P7/00
CPC分类号： C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要： The present invention relates to a process for the preparation of compounds of formula (I) wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula (II) wherein R1 and R2 are as defined for formula (I), with at least one reducing agent to form a compound of formula (III) wherein R1 and R2 are as defined for formula (I), and b) reaction of that compound with at least one reducing agent to form a compound of formula (IV) wherein R1 and R2 are as defined for formula (I), and (c) reaction of that compound with a compound of formula (V) wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula (I), to form the compound of formula (I); and to novel intermediates for use in that process.
摘要翻译：本发明涉及制备式（I）化合物的方法，其中R 1和R 2各自独立地为氢或C 1 -C 5烷基，R 3为CF 3或CF 2 H，通过a）式（Ⅱ）化合物）其中R1和R2如式（I）所定义，与至少一种还原剂形成式（III）化合物，其中R 1和R 2如式（I）所定义，和b）该化合物与至少一种还原剂形成式（Ⅳ）化合物，其中R1和R2如式（Ⅰ）所定义，和（c）该化合物与式（Ⅴ）化合物的反应其中Q是氯，氟，溴，碘，羟基或C 1 -C 6烷氧基，R 3如式（I）所定义，形成式（I）化合物; 以及用于该过程的新型中间体。

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