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1. 发明授权

US09738584B2 Fluorination of acrylate esters and derivatives 有权
公开(公告)号：US09738584B2
公开(公告)日：2017-08-22
申请号：US15287105
申请日：2016-10-06
申请人： Relypsa, Inc.
发明人： YongQi Mu
IPC分类号： C07C51/36 , C07C51/363 , C07C51/62 , C07C67/307 , C07C67/22 , C07C253/30 , C07C253/32 , C07C51/50 , C07C51/64 , C07C67/03 , C07C67/62
CPC分类号： C07C51/36 , C07C51/363 , C07C51/50 , C07C51/62 , C07C51/64 , C07C67/03 , C07C67/22 , C07C67/307 , C07C67/62 , C07C253/30 , C07C253/32 , C07C69/63 , C07C53/21 , C07C53/50 , C07C255/03
摘要： The present invention generally relates to processes for converting acrylate esters or a derivative thereof to difluoropropionic acid or a derivative thereof. This process is generally performed using fluorine gas in a hydrofluorocarbon solvent.

2. 发明申请

US20170190648A1 3,6-DICHLOROSALICYLIC ACID COMPOUNDS AND RELATED SYNTHETIC PROCESSES 有权
公开(公告)号：US20170190648A1
公开(公告)日：2017-07-06
申请号：US15313728
申请日：2015-06-03
申请人： Monsanto Technology LLC
发明人： Terri L. Boehm , Mangesh Bore , Jeffery N. Carroll , G. Davis Harris, JR. , Matthew D. McReynolds , Justin R. Struble , Daniel P. Walker
IPC分类号： C07C51/363 , C07C67/035 , C07C51/377
CPC分类号： C07C51/363 , C07C51/367 , C07C51/377 , C07C67/035 , C07C65/05 , C07C65/21
摘要： The present disclosure relates, in general, to 5-halo-3,6-dichlorosalicylic acid compounds, 5-halo-3,6-dichlorosalicy-aldehyde compounds, processes for preparing 5-halo-3,6-dichlorosalicylic acid compounds, processes for preparing 5-halo-3,6-di-chlorosalicyaldehyde compounds, processes for preparing 3,6-dichlorosalicylic acid compounds, and processes that employ such compounds as intermediates in the preparation of the herbicide dicamba.

3. 发明授权

US09650469B2 Process or producing polyhydroxyalkanoates from precursors obtained by anaerobic fermentation from fermentable biomass 有权
公开(公告)号：US09650469B2
公开(公告)日：2017-05-16
申请号：US15053666
申请日：2016-02-25
申请人： AFYREN
发明人： Régis Nouaille , Jérémy Pessiot , Marie Thieulin
IPC分类号： C08G64/00 , C08G63/06 , C08G63/78 , C07C51/363 , C07C51/367 , C12P7/40 , C12P7/42 , C12P7/62 , C08G63/02
CPC分类号： C08G63/06 , C07C51/363 , C07C51/367 , C08G63/78 , C12P7/40 , C12P7/42 , C12P7/625 , C07C53/16 , C07C53/19 , C07C59/06 , C07C59/08 , C07C59/01
摘要： The process for producing polyhydroxyalkanoates or PHA from volatile fatty acid (VFA) molecules, referred to as precursors, produced by anaerobic fermentation from fermentable biomass, characterized in that it comprises at least the following steps: a) extracting the volatile fatty acid (VFA) molecules, without stopping the fermentation, via an extraction means chosen from means that are, at least, insoluble in the fermentation medium, b) collecting, outside the fermentation reactor, the volatile fatty acid (VFA) molecules once they have been extracted, c) synthesizing, by halogenation, using a type of volatile fatty acid (VFA) chosen from the volatile fatty acids collected in step b) and defined according to the desired type of PHA, a given α-halo acid, d) synthesizing from this α-halo acid molecules of a given α-hydroxy acid by reaction with a base, e) polymerizing using the α-hydroxy acid obtained a defined polyhydroxyalkanoate (PHA).

4. 发明申请

US20140315831A1 Synthesis of Libraries of Peptide Tertiary Amides 审中-公开
标题翻译：肽三级酰胺的文库的合成
公开(公告)号：US20140315831A1
公开(公告)日：2014-10-23
申请号：US14354031
申请日：2012-10-25
申请人： The Scripps Research Institute
发明人： Thomas Kodadek , Yu Gao
IPC分类号： C07K7/06 , C07K1/04 , C07K5/062 , A61K38/08 , C07K5/083 , G01N33/68
CPC分类号： C07K7/06 , A61K38/08 , C07C51/363 , C07C231/02 , C07K1/042 , C07K1/047 , C07K5/06026 , C07K5/0806 , C07K14/001 , G01N33/6845 , C07C237/22 , C07C53/19
摘要： The present disclosure is directed to a novel class of peptide-like oligomers called peptide tertiary amides (PTAs) and a combinatorial library of PTAs along with synthetic routes for the preparation of large combinatorial libraries of these compounds. The peptide tertiary amides provide an exceptional source of high affinity and selective protein ligands that are useful as tools for biological research and as drug leads, among others.
摘要翻译：本公开涉及一类新型的肽样低聚物，称为肽叔酰胺（PTAs），以及PTAs的组合文库以及用于制备这些化合物的大组合文库的合成途径。肽叔酰胺提供了高亲和力和选择性蛋白质配体的特殊来源，可用作生物研究的工具以及作为药物引导的工具。

5. 发明申请

US20140221681A1 FLUORINATION OF ACRYLATE ESTERS AND DERIVATIVES 有权
标题翻译：丙烯酸酯和衍生物的氟化
公开(公告)号：US20140221681A1
公开(公告)日：2014-08-07
申请号：US14128899
申请日：2012-06-27
申请人： YongQi Mu
发明人： YongQi Mu
IPC分类号： C07C67/307 , C07C51/363
CPC分类号： C07C51/36 , C07C51/363 , C07C51/50 , C07C51/62 , C07C51/64 , C07C67/03 , C07C67/22 , C07C67/307 , C07C67/62 , C07C253/30 , C07C253/32 , C07C69/63 , C07C53/21 , C07C53/50 , C07C255/03
摘要： The present invention generally relates to processes for converting acrylate esters or a derivative thereof to difluoropropionic acid or a derivative thereof. This process is generally performed using fluorine gas in a hydrofluorocarbon solvent.
摘要翻译：本发明一般涉及将丙烯酸酯或其衍生物转化为二氟丙酸或其衍生物的方法。该方法通常在氢氟烃溶剂中使用氟气进行。

6. 发明申请

US20120309973A1 PREPARATION OF 2-(4-BROMOPHENYL)-2-METHYLPROPANOIC ACID 审中-公开
标题翻译： 2-（4-溴苯基）-2-甲基丙酸的制备
公开(公告)号：US20120309973A1
公开(公告)日：2012-12-06
申请号：US13219971
申请日：2011-08-29
申请人： Murali Krishna Prasad Divi , Gundu Rao Padakandla , Nageswara Rao Bolneni , Krishnaji Rao Mutyala
发明人： Murali Krishna Prasad Divi , Gundu Rao Padakandla , Nageswara Rao Bolneni , Krishnaji Rao Mutyala
IPC分类号： C07D211/22 , C07C51/363
CPC分类号： C07C51/363 , C07D211/32 , C07C57/58
摘要： Selective bromination of 2-methyl-2-phenylpropanoic acid in aqueous medium is described to obtain pure 2-(4-bromophenyl)-2-methylpropanoic acid, which is a useful key intermediate in the process of manufacturing pure fexofenadine.
摘要翻译：描述了2-甲基-2-苯基丙酸在水性介质中的选择性溴化，得到纯的2-（4-溴苯基）-2-甲基丙酸，其是制造纯非索非那定的过程中的有用关键中间体。

7. 发明授权

US08022247B2 Process for production of 2,3,4-trifluoro-5-(iodo or bromo)-benzoic acid 失效
标题翻译：制备2,3,4-三氟-5-（碘或溴） - 苯甲酸的方法
公开(公告)号：US08022247B2
公开(公告)日：2011-09-20
申请号：US11887843
申请日：2006-04-06
申请人： Hiroshi Koyano , Hitoshi Iikura , Yoshiaki Isshiki , Yasunori Kohchi
发明人： Hiroshi Koyano , Hitoshi Iikura , Yoshiaki Isshiki , Yasunori Kohchi
IPC分类号： C07C63/00
CPC分类号： C07C51/363 , C07C63/70
摘要： The invention provides a process for production of 2,3,4-trifluoro-5-(iodo or bromo)benzoic acid, the process comprising a halogenation step in which direct iodination or bromination of 2,3,4-trifluorobenzoic acid is performed with an iodinating agent or brominating agent in a reaction solvent in the presence of an oxidizing agent. According to the invention, there is provided a process for convenient production of 2,3,4-trifluoro-5-(iodo or bromo)benzoic acid in high yield and high purity in a highly regioselective manner.
摘要翻译：本发明提供了一种生产2,3,4-三氟-5-（碘或溴）苯甲酸的方法，该方法包括一个卤化步骤，其中对2,3,4-三氟苯甲酸进行直接碘化或溴化，碘化剂或溴化剂在反应溶剂中在氧化剂存在下进行。根据本发明，提供了以高度区域选择性方式以高产率和高纯度方便生产2,3,4-三氟-5-（碘或溴）苯甲酸的方法。

8. 发明授权

US07473803B2 Process for production of optically active 2-halogeno-carboxylic acids 失效
标题翻译：光学活性2-卤代羧酸的制备方法
公开(公告)号：US07473803B2
公开(公告)日：2009-01-06
申请号：US10503264
申请日：2003-02-04
申请人： Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C53/19 , C07B39/00
CPC分类号： C07C51/412 , C07C51/363 , C07C51/43 , C07C53/19
摘要： The invention provides processes for producing efficiently optically active 2-halogenocarboxylic acids useful in the preparation of drugs or the like and salts thereof with amines. Specifically, an optically active 2-halogenocarboxylic acid is produced by halogenating an optically active amino acid in water in the presence of a hydrophobic organic solvent and nitrous acid with the configuration retained and with the racemization inhibited through the removal of 2-hydroxy-bromocarboxylic acid formed as a by-product; the obtained optically active 2-halogenocarboxylic acid is transferred to an aqueous phase by converting it into a salt thereof with a base, followed by the removal of the organic phase; and the optically active 2-halogenocarboxylic acid is transferred again to an organic solvent phase, followed by the removal of the aqueous phase, whereby an optically active 2-halogenocarboxylic acid is obtained through the removal of a halogen component. Further, a high-quality salt of an optically active 2-halogenocarboxylic acid with an amine can be obtained by a crystallization method wherein the amine is added over the period of ½ hour or longer either continuously or in portions and/or wherein the crystallization solvent consists of a hydrophobic organic solvent and a hydrophilic organic solvent.
摘要翻译：本发明提供了可用于制备药物等的有效光学活性2-卤代羧酸的方法及其与胺的盐。具体地说，光学活性2-卤代羧酸是通过在疏水性有机溶剂和亚硝酸的存在下在水中卤化光学活性氨基酸而形成的，其中保留了结构，并且通过除去2-羟基 - 溴羧酸，外消旋化被抑制形成副产品; 将得到的光学活性2-卤代羧酸通过将其转化为其盐与碱反应，然后除去有机相，转移到水相中。并将光学活性2-卤代羧酸再次转移到有机溶剂相中，然后除去水相，由此通过除去卤素组分获得光学活性的2-卤代羧酸。此外，光学活性2-卤代羧酸与胺的高品质盐可以通过结晶方法获得，其中胺在连续或部分加入0.5小时或更久的时间内和/或其中结晶溶剂由疏水性有机溶剂和亲水性有机溶剂构成。

9. 发明申请

US20080200731A1 Polyhalogen-substituted cinnamic acids and cinnamic acid derivatives and a process for the preparation of polyhalogen-substituted cinnamic acids and cinnamic acid derivatives 审中-公开
公开(公告)号：US20080200731A1
公开(公告)日：2008-08-21
申请号：US12148752
申请日：2008-04-22
申请人： Walter Lange , Joachim Komoschinski , Markus Eckert , Michael Dockner
发明人： Walter Lange , Joachim Komoschinski , Markus Eckert , Michael Dockner
IPC分类号： C07C45/62
CPC分类号： C07C57/60 , C07C45/46 , C07C45/62 , C07C49/697 , C07C51/363
摘要： Polyhalogenated cinnamic acids and cinnamic acid derivatives are prepared by reacting diazonium salts accessible from polyhalogenated anilines with acrylic acid or acrylic acid derivatives in the presence of a homogeneous, palladium-containing catalyst at about −5 to about +100° C. Some of the cinnamic acids and cinnamic acid derivatives obtainable in this way are new. Cinnamic acids and cinnamic acid derivatives which can be prepared according to the invention can be used for the preparation of indanones which are precursors for agro- and pharmaceutical chemicals and for substances having liquid-crystalline properties.

10. 发明申请

US20070213569A1 Processes for conversion of tyrosine to p-hydroxystyrene and p-acetoxystyrene 失效
标题翻译：将酪氨酸转化为对羟基苯乙烯和对乙酰氧基苯乙烯的方法
公开(公告)号：US20070213569A1
公开(公告)日：2007-09-13
申请号：US11369422
申请日：2006-03-07
申请人： Steven Shuey
发明人： Steven Shuey
IPC分类号： C07C39/10
CPC分类号： C07C37/50 , C07C51/363 , C07C67/08 , C07C59/56 , C07C69/017 , C07C69/157 , C07C39/20
摘要： Tyrosine was converted to p-hydroxystyrene in a two-step reaction without purification of individual intermediates. Conditions were determined for bromination of tyrosine in which reactive intermediates were formed. The mixture of these intermediates was used directly in a second step reaction to produce p-hydroxystyrene. The p-hydroxystyrene was further acetylated to produce p-acetoxystyrene in the second step reaction vessel.
摘要翻译：酪氨酸在两步反应中转化为对羟基苯乙烯，而不需要纯化各个中间体。确定形成反应性中间体的酪氨酸溴化条件。这些中间体的混合物直接用于第二步反应以产生对羟基苯乙烯。进一步乙酰化对羟基苯乙烯以在第二步反应容器中产生对乙酰氧基苯乙烯。

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