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11. 发明授权

US07470809B2 Process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid 有权
标题翻译：制备[2-（4-氟 - 苄基） - 苯基] - 乙酸的方法
公开(公告)号：US07470809B2
公开(公告)日：2008-12-30
申请号：US11574300
申请日：2005-08-26
申请人： Michel Joseph Maurice André Guillaume , Yolande Lydia Lang , Armin Roessler , Lars Ulmer , Stefan Marcel Herman Leurs , Dirk De Smaele
发明人： Michel Joseph Maurice André Guillaume , Yolande Lydia Lang , Armin Roessler , Lars Ulmer , Stefan Marcel Herman Leurs , Dirk De Smaele
IPC分类号： C07C51/00 , C07C55/28
CPC分类号： C07C57/58 , C07C51/08 , C07C51/373 , C07C51/377 , C07C65/34 , C07C63/72
摘要： The present invention relates to a novel process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid, a compound obtainable from phthalic anhydride. The process comprises the subsequent steps a) through e): a) reacting phthalic anhydride with fluorobenzene or a derivative thereof in appropriate reaction conditions; b) over reducing the product obtained in step a) at the ketone moiety; c) reducing the product obtained in step b) with sodium dihydro-bis(2-methoxyethoxy)aluminate (Red-Al) to the corresponding alcohol; d) chlorinating the alcohol obtained in step c); e) inserting CO into the product obtained in step d) through an appropriate Pd-containing catalytic system. In an alternative embodiment, the step e) is replaced by the steps f1) and f2): f1) reacting the product obtained in step d) with sodium cyanide; f2) hydrolysing the product obtained in step f1). The present invention provides a process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid which is suitable for industrial scale reactors (e.g. which is cleaner and more efficient). Also, [2-(4-fluoro-benzyl)-phenyl]-acetic acid is obtained as a crystalline material with a purity >95%.
摘要翻译：本发明涉及生产由邻苯二甲酸酐获得的化合物的[2-（4-氟 - 苄基） - 苯基] - 乙酸的新方法。该方法包括随后的步骤a）至e）：a）在合适的反应条件下使邻苯二甲酸酐与氟苯或其衍生物反应; b）在酮部分上还原在步骤a）中获得的产物; c）将步骤b）中得到的产物用二氢 - 双（2-甲氧基乙氧基）铝酸钠（Red-Al）还原成相应的醇; d）氯化步骤c）中得到的醇; e）通过合适的含Pd催化体系将CO插入到步骤d）中获得的产物中。在替代实施方案中，步骤e）被步骤f1）和f2）代替：f1）使步骤d）中获得的产物与氰化钠反应; f2）水解步骤f1）中获得的产物。本发明提供了适用于工业规模的反应器（例如更清洁和更有效）的[2-（4-氟 - 苄基） - 苯基] - 乙酸的生产方法。此外，得到纯度> 95％的结晶物质的2-（4-氟 - 苄基） - 苯基] - 乙酸。

12. 发明申请

US20080275270A1 Process for Preparing Quaternary Acid and Ammonium Salts 有权
标题翻译：制备季铵盐和铵盐的方法
公开(公告)号：US20080275270A1
公开(公告)日：2008-11-06
申请号：US12110667
申请日：2008-04-28
申请人： Philippe Dellis , Kamel Nasar
发明人： Philippe Dellis , Kamel Nasar
IPC分类号： C07C51/09
CPC分类号： C07C213/08 , C07C51/373 , C07C59/90 , C07C215/40
摘要： A process for preparing a quaternary ammonium salt of a fibric acid, represented by the following reaction scheme: is carried out in a single operation starting from a phenol of formula (I), an α-halogenated ester of formula (II) and a quaternary ammonium hydroxide of formula (III). This process makes it possible economically to prepare a choline salt of fenofibric acid in high purity that can be used directly as the active substance in a pharmaceutical composition intended for human consumption.
摘要翻译：由以下反应方案表示的用于制备纤维酸季铵盐的方法：以式（I）的酚，式（II）的α-卤代酯和季铵盐式（III）的氢氧化铵。该方法可以经济地制备高纯度的非诺贝酸的胆碱盐，其可以直接用作预期用于人类消费的药物组合物中的活性物质。

13. 发明申请

US20080167493A1 METHODS FOR CONVERSION OF TYROSINE TO P-HYDROXYSTYRENE AND P-HYDROXYCINNAMIC ACID 审中-公开
标题翻译：将吡啶转化为对羟基苯乙烯和对羟基杀虫酸的方法
公开(公告)号：US20080167493A1
公开(公告)日：2008-07-10
申请号：US11961072
申请日：2007-12-20
申请人： STEVEN W. SHUEY , Mukesh C. Shah
发明人： STEVEN W. SHUEY , Mukesh C. Shah
IPC分类号： C07C51/347
CPC分类号： C07C37/50 , C07C51/373 , C07C67/08 , C07C57/42 , C07C69/017 , C07C69/157 , C07C39/20
摘要： Three different reaction steps were combined to provide methods for preparing p-hydroxystyrene and p-hydroxycinnamic acid monomers from tyrosine. The three steps include reductive alkylation of tyrosine, followed by oxidation to the N-oxide, and thermal Cope elimination. During Cope elimination, either p-hydroxycinnamic acid or p-hydroxystyrene was produced depending on the absence or presence of base, respectively. Additionally, p-acetoxystyrene may be prepared by reacting the prepared p-hydroxystyrene either directly or after isolation with an acetylating agent.
摘要翻译：合并三种不同的反应步骤，提供从酪氨酸制备对羟基苯乙烯和对羟基肉桂酸单体的方法。三个步骤包括酪氨酸的还原烷基化，然后氧化成N-氧化物，并且消除热反应。在消除反应期间，根据碱的存在或不存在，分别产生对羟基肉桂酸或对羟基苯乙烯。此外，对乙酰氧基苯乙烯可以通过将制备的对羟基苯乙烯直接或分离后与乙酰化剂反应来制备。

14. 发明申请

US20060122344A1 Organometallic Fluorenyl Compounds, Preparations, and Use 失效
标题翻译：有机金属芴基化合物，制剂和用途
公开(公告)号：US20060122344A1
公开(公告)日：2006-06-08
申请号：US10260028
申请日：2002-05-10
申请人： HELMUT ALT , SYRIAC PALACKAL , KONSTANTINOS PATSIDIS , M. WELCH , ROLF GEERTS , ERIC HSIEH , MAX MCDANIEL , GIL HAWLEY , PAUL SMITH
发明人： HELMUT ALT , SYRIAC PALACKAL , KONSTANTINOS PATSIDIS , M. WELCH , ROLF GEERTS , ERIC HSIEH , MAX MCDANIEL , GIL HAWLEY , PAUL SMITH
IPC分类号： C07F17/00 , C08F4/44
CPC分类号： B01J31/143 , B01J31/2295 , B01J2531/40 , B01J2531/46 , B01J2531/48 , B01J2531/49 , B01J2531/50 , B01J2531/56 , C07C13/567 , C07C22/04 , C07C49/747 , C07C51/31 , C07C51/373 , C07C51/377 , C07C63/331 , C07C63/49 , C07C65/36 , C07C2601/10 , C07C2603/18 , C07F7/0805 , C07F7/081 , C07F17/00 , C08F4/63912 , C08F4/63922 , C08F4/65912 , C08F4/65927 , C08F10/00 , C08F110/02 , C08F110/06 , C08F210/16 , Y10S526/943 , C07C65/38 , C08F2500/12 , C08F2500/17 , C08F2500/20 , C08F2500/01 , C08F2500/08 , C08F210/14
摘要： Fluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.
摘要翻译：公开了含芴基金属茂以及制备金属茂的方法。还公开了使用金属茂作为聚合催化剂的方法。此外，公开了由这种聚合产生的聚合物。

15. 发明申请

US20060036108A1 Method for manufacturing prostaglandin analogue 有权
标题翻译：制备前列腺素类似物的方法
公开(公告)号：US20060036108A1
公开(公告)日：2006-02-16
申请号：US11193373
申请日：2005-08-01
申请人： Ryu Hirata , Tatsuya Matsukawa
发明人： Ryu Hirata , Tatsuya Matsukawa
IPC分类号： C07C61/06
CPC分类号： C07C51/373 , C07C405/00 , C07C59/353
摘要： The present invention provides a new method for manufacturing a prostaglandin analogue having one or more keto groups on the 5-membered ring and/or omega chain, which comprises the step of treating a corresponding hydroxyl group containing compound with a co-oxidizer under the presence of a tetramethylpyperidine-1-oxyl derivative to form the desired prostaglandin analogue. The method of the invention can be carried out easily under relatively mild conditions.
摘要翻译：本发明提供了一种制备在5元环和/或ω链上具有一个或多个酮基的前列腺素类似物的新方法，其包括在存在下用共氧化剂处理相应的含羟基化合物的步骤的四甲基吡啶-1-氧代衍生物形成所需的前列腺素类似物。本发明的方法可以在相对温和的条件下容易地进行。

16. 发明申请

US20050090685A1 Process for production of 3,3-dimethyl-2-formylcyclopropanecarboxylic acid derivatives 失效
标题翻译： 3,3-二甲基-2-甲酰基环丙烷羧酸衍生物的制备方法
公开(公告)号：US20050090685A1
公开(公告)日：2005-04-28
申请号：US10501094
申请日：2002-12-26
申请人： Kouji Yoshikawa
发明人： Kouji Yoshikawa
IPC分类号： C07C51/373 , C07C67/333 , C07C69/74
CPC分类号： C07C51/373 , C07C67/333 , C07C2601/02 , C07C62/16 , C07C69/757
摘要： A process for the production of a 3,3-dimethyl-2-formylcyclopropanecarboxylic acid derivative of formula (2): wherein R is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl, which process comprises reacting a 3,3-dimethyl-2-(2-methyl-1-propenyl)cyclopropanecarboxylic acid compound of formula (1): wherein R is as defined above, with a periodic acid compound in the presence of a ruthenium compound.
摘要翻译：制备式（2）的3,3-二甲基-2-甲酰基环丙烷羧酸衍生物的方法：其中R是氢，取代或未取代的烷基，取代或未取代的芳基或取代或未取代的芳烷基，该方法包括使在钌化合物的存在下，式（1）的3,3-二甲基-2-（2-甲基-1-丙烯基）环丙烷羧酸化合物：其中R如上定义，与高碘酸化合物反应。

17. 发明授权

US06869989B2 Method of modifying components present in cashew nut shell liquid 失效
标题翻译：修改腰果壳液中存在的成分的方法
公开(公告)号：US06869989B2
公开(公告)日：2005-03-22
申请号：US09866451
申请日：2001-05-25
申请人： Mohammed Lokman Khan , Jeremy Tomkinson , Richard James Salisbury
发明人： Mohammed Lokman Khan , Jeremy Tomkinson , Richard James Salisbury
IPC分类号： C07C45/40 , C07C51/373 , C07C65/30 , C08G8/04 , C08G8/24 , C08L61/06 , C09J161/06 , C08J5/10 , C08L99/00
CPC分类号： C09J161/06 , C07C45/40 , C07C51/373 , C07C65/30 , C08G8/04 , C08G8/24 , C08L61/06
摘要： Disclosed is a process for modifying cashew nut shell liquid (CNSL) which involves the steps of subjecting the CNSL to ozonolysis to form ozonolysis reaction products, followed by reduction of the ozonolysis reaction products to give a mixture of phenolic components and aldehydes. In a preferred embodiment, the process involves reacting CNSL with ozone to form a mixture containing ozonolysis reaction products, and then treating the mixture under reducing conditions to form a further mixture containing phenolic components with an eight carbon chain having a terminal —CHO group and alkyl components of varying lengths with either one or two terminal —CHO groups. The resulting CNSL aldehydes may be used to form adhesives for use in the manufacture of composites such as wood particle board.
摘要翻译：本发明公开了一种改性腰果壳液（CNSL）的方法，该方法涉及以下步骤：使CNSL进行臭氧分解以形成臭氧分解反应产物，然后还原臭氧分解反应产物，得到酚类组分和醛的混合物。在优选的实施方案中，该方法包括使CNSL与臭氧反应以形成含有臭氧分解反应产物的混合物，然后在还原条件下处理该混合物以形成含有具有末端-CHO基团的八个碳链的酚类组分和烷基具有一个或两个末端-CHO基团的不同长度的组分。所得到的CNSL醛可用于形成用于制造复合材料如木材刨花板的粘合剂。

18. 发明授权

US06458975B1 Production methods of citalopram and an intermediate therefor 失效
标题翻译：西酞普兰及其中间体的生产方法
公开(公告)号：US06458975B1
公开(公告)日：2002-10-01
申请号：US09996134
申请日：2001-11-28
申请人： Tetsuya Ikemoto , Wei-Guo Gao , Nobuhiro Arai , Masami Igi
发明人： Tetsuya Ikemoto , Wei-Guo Gao , Nobuhiro Arai , Masami Igi
IPC分类号： C07D30778
CPC分类号： C07D307/87 , C07C29/40 , C07C33/46 , C07C51/265 , C07C51/373 , C07C65/34
摘要： Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent.
摘要翻译：通过在N，N，N'，N'-四甲基乙二胺中的至少一种的存在下使下式[Ⅵ]化合物与3-（二甲基氨基）丙基氯反应，可以工业和经济地制备，并以高收率和1,3-二甲基-2-咪唑啉酮和缩合剂。

19. 发明授权

US06440056B1 Diacetylenics containing adjacent triple bonds 失效
标题翻译：含有相邻三键的二乙酰基
公开(公告)号：US06440056B1
公开(公告)日：2002-08-27
申请号：US09845106
申请日：2001-04-27
申请人： Alok Singh , Paul Schoen , Dan Zabetakis , Joel M. Schnur
发明人： Alok Singh , Paul Schoen , Dan Zabetakis , Joel M. Schnur
IPC分类号： C11B300
CPC分类号： C07C51/373 , C07C51/353 , C07C57/24 , C07C59/76 , C07C59/84
摘要： This invention pertains to a process for preparing diacetylenics, to diacetylenic compounds and to reduced diacetylenic compounds. The process includes the steps of reacting coupling an acetylenic acid in presence of cupric chloride in Ethylamine and hydroxylamine hydrochloride to form a diacetylenic diacid; reacting the diacetylenic diacid with a lithium compound, trimethylsilyl chloride and hydrochloric acid to form a diacetylenic compound; and reducing the diacetylenic compound to a reduced diacetylenic compound. The diacetylenic compounds have the formula COOH—(CH2)m—C≡C—C≡C—(CH2)m—C(═O)—R or R—C(═O)—(CH2)m—C≡C—C≡C—(CH2)m—C(═O)—R and the reduced cyclic diacetylenic compounds have the formula COOH—(CH2)m—C≡C—C≡C—(CH2)m—CH2—R or R—CH2—(CH2)m—C≡C—C≡C—(CH2)m—CH2—R, where m is 1-18 and R is selected from alkyl groups of 1-10 and cyclic groups containing 6-35 carbon atoms and aryl moieties
摘要翻译：本发明涉及制备二乙炔基化合物，二乙炔化合物和还原二炔化合物的方法。该方法包括使乙酸氯化物在乙胺和盐酸羟胺存在下偶联乙酸以形成二乙炔二酸的步骤; 使二乙炔二酸与锂化合物，三甲基甲硅烷基氯和盐酸反应，形成二乙炔化合物; 并将二乙炔化合物还原成还原的二乙炔化合物。二乙炔化合物具有式COOH-（CH2）mC = CC = C-（CH2）mC（= O）-R或RC（= O） - （CH2）mC = CC = C-（CH2）mC（= O ）-R并且还原的环状二炔化合物具有式COOH-（CH 2）m C = CC = C-（CH 2）m -CH 2 -R或R-CH 2 - （CH 2）m C = CC = C-（CH 2）m - CH2-R，其中m为1-18，R选自1-10的烷基和含有6-35个碳原子的环状基团和芳基部分

20. 发明授权

US06433196B1 Production method of citalopram, intermediate therefor and production method of the intermediate 失效
标题翻译：西酞普兰的生产方法，中间体和中间体的生产方法
公开(公告)号：US06433196B1
公开(公告)日：2002-08-13
申请号：US09654768
申请日：2000-09-05
申请人： Tetsuya Ikemoto , Wei-Guo Gao , Nobuhiro Arai , Masami Igi
发明人： Tetsuya Ikemoto , Wei-Guo Gao , Nobuhiro Arai , Masami Igi
IPC分类号： C07D30778
CPC分类号： C07D307/87 , C07C29/40 , C07C33/46 , C07C51/265 , C07C51/373 , C07C65/34
摘要： Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent. The compound of the following formula [III], which is a key compound for the production of citalopram, can be easily produced by subjecting the compound of the following formula [II] to reduction and cyclization.
摘要翻译：通过在N，N，N'，N'-四甲基乙二胺中的至少一种的存在下使下式[Ⅵ]化合物与3-（二甲基氨基）丙基氯反应，可以工业和经济地制备，并以高收率和1,3-二甲基-2-咪唑啉酮和缩合剂。通过使下式[Ⅱ]的化合物还原和环化，可以容易地制备作为西酞普兰生产的关键化合物的下式[III]的化合物。

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