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1. 发明授权

US11578025B2 Processes for the preparation of zuclomiphene intermediates 有权
公开(公告)号：US11578025B2
公开(公告)日：2023-02-14
申请号：US17503727
申请日：2021-10-18
申请人： Apotex Inc.
发明人： Dineshkumar Patel , Avedis Karadeolian , Fabio E. S. Souza , Allan W. Rey
IPC分类号： C07C37/62 , B01J23/755 , C07C17/263 , C07C37/14
摘要： The present invention provides continuous flow processes for the preparation of the compound of Formula (2-A), an intermediate used in the preparation of zuclomiphene or a salt thereof.

2. 发明授权

US11111207B2 One pot, one step process for the halogenation of aromatics using solid acid catalysts 有权
公开(公告)号：US11111207B2
公开(公告)日：2021-09-07
申请号：US16086831
申请日：2017-03-17
申请人： COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
发明人： Shubhangi Bhalchandra Umbarkar , Atul Balasaheb Kulal , Amar Jaywant Deshmukh
IPC分类号： C07C209/74 , C07C37/62 , C07C45/63 , B01J21/06 , B01J21/08 , B01J21/12 , B01J23/28 , B01J23/30 , C07C231/12 , C07C39/27 , C07C47/55 , C07C211/52 , C07C237/30
摘要： The present invention disclosed an improved one pot, one step process for halogenation of compound of formula (II) to afford corresponding halogenated compound of formula (I) having improved yield and increased selectivity under very mild conditions.

3. 发明授权

US10287220B2 Fluorination method 有权
公开(公告)号：US10287220B2
公开(公告)日：2019-05-14
申请号：US15127599
申请日：2015-03-20
申请人： Oxford University Innovation Limited
发明人： Veronique Gouverneur , Matthew Tredwell , Sean Preshlock
IPC分类号： C07D295/16 , C07B59/00 , C07F5/04 , C07C17/361 , C07C37/62 , C07C41/22 , C07C45/65 , C07C67/317 , C07C201/12 , C07C209/74 , C07C231/12 , C07C253/30 , C07C303/40 , C07D209/08 , C07D215/18 , C07D277/30 , C07D295/073 , C07F5/02
摘要： The present invention relates to a process for producing an organic compound comprising an 18F atom. The compounds comprising an 18F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridized carbon atom, with (i) 18F— and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridized carbon atom, in a process for producing an organic compound comprising an 18F atom, which process comprises treating the organoboron compound with (i)18F— and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PGA is independently H or an alcohol protecting group; PGB is H or a carboxylic acid protecting group; each PGC is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4.

4. 再颁专利

USRE46151E1 Method for the production of 4,4′-[1-(trifluoromethyl)alkylidene]-bis-(2,6-diphenylphenols) 有权
标题翻译：制备4,4' - [1-（三氟甲基）亚烷基] - 双（2,6-二苯基苯酚）
公开(公告)号：USRE46151E1
公开(公告)日：2016-09-20
申请号：US14321865
申请日：2014-07-02
申请人： BASF SE
发明人： Gabriele Gralla , Gunnar Heydrich , Klaus Ebel , Wolfgang Krause
IPC分类号： C07C39/16 , C07C39/12 , C07C45/74 , C07C37/07 , C07C37/20 , C07C37/62
CPC分类号： C07C45/74 , C07C37/07 , C07C37/20 , C07C37/62 , C07C49/613 , C07C49/653 , C07C39/15 , C07C39/367
摘要： The present invention relates to a process for preparing 4,4′-[1-(trifluoromethyl)alkylidene]bis(2,6-diphenylphenols), in particular for preparing 4,4′-[1-(trifluoromethyl)ethylidene]bis(2,6-diphenylphenol), which comprises the self-condensation of cyclohexanone in the presence of a basic catalyst to form tricyclic condensation products, dehydrogenation of the resulting tricyclic condensation products in the presence of a supported transition metal catalyst in the condensed phase to form 2,6-diphenylphenol and reaction of the 2,6-diphenylphenol with a trifluoromethyl ketone. The invention further provides an improved process for preparing 2,6-diphenylphenol by aldol self-condensation of cyclohexanone.
摘要翻译：本发明涉及一种制备4,4' - [1-（三氟甲基）亚烷基]双（2,6-二苯基苯酚）的方法，特别是制备4,4' - [1-（三氟甲基）亚乙基]双（ 2,6-二苯基苯酚），其包括环己酮在碱性催化剂存在下的自缩合以形成三环缩合产物，所得三环缩合产物在冷凝相中负载的过渡金属催化剂存在下脱氢形成 2,6-二苯基苯酚和2,6-二苯基苯酚与三氟甲基酮的反应。本发明还提供了通过环己酮的醛醇自缩合制备2,6-二苯基苯酚的改进方法。

5. 发明授权

US08975447B2 Process for asymetric methylallylation in the presence of a 2,2′-substituted 1,1′-BI-2-naphthol catalyst 有权
标题翻译：在2,2'-取代的1,1'-二-2-萘酚催化剂的存在下进行不对称甲基化反应的方法
公开(公告)号：US08975447B2
公开(公告)日：2015-03-10
申请号：US14003248
申请日：2012-03-06
申请人： Wenjie Li , Zhi-Hui Lu , Chris Hugh Senanayake , Yongda Zhang
发明人： Wenjie Li , Zhi-Hui Lu , Chris Hugh Senanayake , Yongda Zhang
IPC分类号： C07C33/48 , C07C39/38 , C07C29/38 , C07C29/40 , C07C39/14 , C07C37/055 , C07C41/48 , C07C29/143 , C07C37/62
CPC分类号： C07C39/14 , C07B2200/07 , C07C29/143 , C07C29/38 , C07C37/055 , C07C37/62 , C07C39/38 , C07C41/48 , C07C43/313 , C07C33/483
摘要： Disclosed are a process and catalysts useful for carrying out asymmetric methlyallylations. The catalysts used in the invention have the formula (IV): wherein X1, X2, R3 and R4 are as defined herein. Compounds made by the process of the invention can be used to prepare pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors including 1,3-disubstituted oxazinan-2-ones.
摘要翻译：公开了用于进行不对称甲基化反应的方法和催化剂。用于本发明的催化剂具有式（Ⅳ）：其中X 1，X 2，R 3和R 4如本文所定义。通过本发明的方法制备的化合物可用于制备药物活性化合物，例如11-＆bgr-羟基类固醇氢化酶1型（11-＆amp; bgr-HSD1）抑制剂，包括1,3-二取代的恶嗪烷-2-酮。

6. 发明申请

US20100312020A1 METHOD FOR THE PRODUCTION OF 4,4'-[1-TRIFLUOROMETHYL)ALKYLIDENE]-BIS-(2,6-DIPHENYLPHENOLS) 有权
标题翻译：生产4,4' - [1-三氟甲基）亚苄基] -BIS-（2,6-二苯基苯酚）的方法
公开(公告)号：US20100312020A1
公开(公告)日：2010-12-09
申请号：US12808865
申请日：2008-12-17
申请人： Gabriele Gralla , Gunnar Heydrich , Klaus Ebel , Wolfgang Krause
发明人： Gabriele Gralla , Gunnar Heydrich , Klaus Ebel , Wolfgang Krause
IPC分类号： C07C37/62 , C07C37/00
CPC分类号： C07C45/74 , C07C37/07 , C07C37/20 , C07C37/62 , C07C49/613 , C07C49/653 , C07C39/15 , C07C39/367
摘要： The present invention relates to a process for preparing 4,4′-[1-(trifluoromethyl)alkylidene]bis(2,6-diphenylphenols), in particular for preparing 4,4′-[1-(trifluoromethyl)ethylidene]bis(2,6-diphenylphenol), which comprises the self-condensation of cyclohexanone in the presence of a basic catalyst to form tricyclic condensation products, dehydrogenation of the resulting tricyclic condensation products in the presence of a supported transition metal catalyst in the condensed phase to form 2,6-diphenylphenol and reaction of the 2,6-diphenylphenol with a trifluoromethyl ketone. The invention further provides an improved process for preparing 2,6-diphenylphenol by aldol self-condensation of cyclohexanone.
摘要翻译：本发明涉及一种制备4,4' - [1-（三氟甲基）亚烷基]双（2,6-二苯基苯酚）的方法，特别是制备4,4' - [1-（三氟甲基）亚乙基]双（ 2,6-二苯基苯酚），其包括环己酮在碱性催化剂存在下的自缩合以形成三环缩合产物，所得三环缩合产物在冷凝相中负载的过渡金属催化剂存在下脱氢形成 2,6-二苯基苯酚和2,6-二苯基苯酚与三氟甲基酮的反应。本发明还提供了通过环己酮的醛醇自缩合制备2,6-二苯基苯酚的改进方法。

7. 发明申请

US20050148570A1 Novel substituted alkane compounds and uses thereof 审中-公开
标题翻译：新型取代烷烃化合物及其用途
公开(公告)号：US20050148570A1
公开(公告)日：2005-07-07
申请号：US10495141
申请日：2002-11-07
申请人： Liren Huang , Alenka Tomazic , Joanns Clancy , Weitao Pan , Vito Esposito
发明人： Liren Huang , Alenka Tomazic , Joanns Clancy , Weitao Pan , Vito Esposito
IPC分类号： A61K31/075 , A61K31/375 , A61K31/397 , A61K31/43 , A61K31/545 , A61K31/56 , A61K31/715 , A61K45/06 , C07C37/20 , C07C37/50 , C07C37/62 , C07C39/16 , C07C39/17 , C07C39/23 , C07C39/42 , C07C43/21 , C07C49/39 , A61K38/46 , A61K38/47
CPC分类号： C07C49/39 , A61K31/075 , A61K31/375 , A61K31/397 , A61K31/43 , A61K31/545 , A61K31/56 , A61K31/715 , A61K45/06 , C07C37/055 , C07C37/20 , C07C37/62 , C07C39/16 , C07C39/17 , C07C39/42 , C07C43/21 , C07C2601/02 , C07C2601/04 , C07C2603/18 , A61K2300/00 , C07C39/23
摘要： The present invention includes compounds, methods of making the compounds, compositions including the compounds and/or use of the compounds and compositions, wherein the compounds of the following formulas
摘要翻译：本发明包括化合物，制备化合物的方法，包括化合物的组合物和/或化合物和组合物的用途，其中下列化学式

8. 发明申请

US20050049440A1 Bromination of hydroxyaromatic compounds 有权
标题翻译：溴化羟基芳族化合物
公开(公告)号：US20050049440A1
公开(公告)日：2005-03-03
申请号：US10650566
申请日：2003-08-28
申请人： Ryan Mills , John Ofori
发明人： Ryan Mills , John Ofori
IPC分类号： C07B39/00 , C07C37/62 , C07C39/27 , C07C39/34
CPC分类号： C07B39/00 , C07C37/62 , C07C39/27
摘要： A method for brominating hydroxyaromatic compounds to form products, such as p-bromophenol, is disclosed. The method uses elemental bromine as the brominating agent and comprises contacting a hydroxyaromatic compound with bromine and oxygen in the presence of metal catalyst. Suitable catalysts include elemental copper, copper compounds, and compounds of Group IV-VIII transition metals.
摘要翻译：公开了用于溴化羟基芳族化合物以形成产物的方法，例如对溴苯酚。该方法使用元素溴作为溴化剂，并且包括在金属催化剂存在下使羟基芳族化合物与溴和氧接触。合适的催化剂包括元素铜，铜化合物和IV-VIII族过渡金属的化合物。

9. 发明授权

US5395994A Method for recovering methanol solvent 失效
标题翻译：甲醇溶剂回收方法
公开(公告)号：US5395994A
公开(公告)日：1995-03-07
申请号：US245949
申请日：1994-05-19
申请人： Robert E. Williams , William J. Cranston, III
发明人： Robert E. Williams , William J. Cranston, III
IPC分类号： C07C29/80 , C07C37/62 , C07C39/367 , C07C27/26 , C07C29/74 , C07C37/68
CPC分类号： C07C29/80 , C07C37/62
摘要： This invention provides an environmentally acceptable method for recovery of phenolic and brominated phenolic compounds, alcohol solvent, and bromide values from the a reaction medium liquid mixture formed in the production of a tetrabromobisphenol-A predominant product. The process comprises (a) separating the tetrabromobisphenol-A predominant product and alkyl bromide from the reaction medium thereby forming a liquid mixture containing alcohol, phenolic and brominated phenolic compounds, HBr, and water; (b) treating the liquid mixture with a sufficient amount of alkaline or alkaline earth metal hydroxide so as to form a treated aqueous mixture having a pH in the range of from about 9.5 to about 14.0, and containing MBr.sub.n, water, alcohol, and soluble salts of the phenolic and brominated phenolic compounds, wherein M is an alkaline or alkaline earth metal ion, and n is the valence of M; (c) distilling alcohol from the treated aqueous mixture of (b); (d) acidifying the treated aqueous mixture from (c) subsequent to distillation with a sufficient amount of acid to precipitate the phenolic and brominated phenolic compounds therefrom; and (e) separating the precipitated phenolic and brominated phenolic compounds from the acidified aqueous mixture of (d).
摘要翻译：本发明提供了一种用于从生产四溴双酚A主要产物中形成的反应介质液体混合物回收酚类和溴化酚类化合物，醇溶剂和溴化物值的环境可接受的方法。该方法包括（a）从反应介质中分离出四溴双酚A主要产物和烷基溴，从而形成含有醇，酚和溴化酚化合物HBr和水的液体混合物; （b）用足量的碱金属或碱土金属氢氧化物处理液体混合物，以形成pH在约9.5至约14.0范围内的处理过的水性混合物，并含有MBrn，水，醇和可溶的酚类和溴化酚类化合物的盐，其中M是碱金属或碱土金属离子，n是M的化合价; （c）从经处理的（b）水混合物中蒸馏出醇; （d）用（c）在蒸馏后用足够量的酸酸化经处理的含水混合物以从其中沉淀酚类和溴化酚类化合物; 和（e）从（d）的酸化含水混合物中分离出沉淀的酚类和溴化酚类化合物。

10. 发明授权

US5283375A Process for high purity tetrabromobisphenol-A 失效
标题翻译：高纯度四溴双酚A的工艺
公开(公告)号：US5283375A
公开(公告)日：1994-02-01
申请号：US990414
申请日：1992-12-15
申请人： Bonnie G. McKinnie , Gary L. Sharp , Robert E. Williams
发明人： Bonnie G. McKinnie , Gary L. Sharp , Robert E. Williams
IPC分类号： C07C37/62 , C07C37/68 , C07C37/70 , C07C37/82 , C07C39/367 , C07C39/38
CPC分类号： C07C37/70 , C07C37/62 , C07C37/685 , C07C37/86 , C07C39/367
摘要： This invention relates to a process for preparing a flame retardant product predominant in tetrabromobisphenol-A. The process comprises: (a) dissolving bisphenol-A in a methanol solvent containing up to about 5 weight percent water, wherein the ratio of methanol to bisphenol-A ranges from about 25 to about 43 moles of methanol per mole of bisphenol-A based on the total amount of methanol used and the total amount of bisphenol-A to be brominated; (b) adding to the solution in (a) from about 3.9 to about 4.2 moles of bromine per mole of bisphenol-A to be brominated while maintaining a reaction temperature in the range of from about 0.degree. to about 40.degree. C.; (c) after the bromination is substantially complete, adding water to precipitate the tetrabromobisphenol-A thus formed; and (d) purifying the precipitated tetrabromobisphenol-A so as to obtain a product predominant in tetrabromobisphenol-A containing less than about 20 ppm total ionic impurity.
摘要翻译：本发明涉及一种主要用于四溴双酚A的阻燃剂的制备方法。该方法包括：（a）将双酚-A溶解在含有至多约5重量％水的甲醇溶剂中，其中甲醇与双酚A的比例为约25至约43摩尔甲醇/摩尔双酚A基关于所用甲醇的总量和要被溴化的双酚A的总量; （b）在（a）中加入约3.9至约4.2摩尔溴/摩尔待溴化双酚A，同时保持反应温度在约0℃至约40℃的范围内; （c）在溴化基本完成后，加入水以沉淀由此形成的四溴双酚A; 和（d）纯化沉淀的四溴双酚A以获得在四溴双酚A中占优势的产物，其含有小于约20ppm的总离子杂质。

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