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1. 发明授权

US11634377B2 Fenfluramine compositions and methods of preparing the same 有权
公开(公告)号：US11634377B2
公开(公告)日：2023-04-25
申请号：US17159367
申请日：2021-01-27
申请人： ZOGENIX INTERNATIONAL LIMITED
发明人： Derek J. Londesbrough , Marc W. Andersen
IPC分类号： C07C209/28 , C07C51/43 , C07C51/08 , C07C45/80 , C07C45/72 , C07C209/84
摘要： Methods of preparing a fenfluramine active pharmaceutical ingredient are provided. Aspects of the method include (a) hydrolyzing a 2-(3-(trifluoromethyl)phenyl)acetonitrile composition to produce a 2-(3-(trifluoromethyl)phenyl)acetic acid composition; (b) reacting the 2-(3-(trifluoromethyl)phenyl)acetic acid composition with acetic anhydride and a catalyst to produce a 1-(3-(trifluoromethyl)phenyl)propan-2-one composition; and (c) reductively aminating the 1-(3-(trifluoromethyl)phenyl)propan-2-one composition with ethylamine using a borohydride reducing agent to produce a fenfluramine composition. Also provided are compositions and pharmaceutical ingredients prepared according to the subject methods including a pharmaceutically acceptable salt of fenfluramine and having less than 0.2% by weight in total of trifluoromethyl regioisomers.

2. 发明申请

US20210284602A1 2-(4-chloro-2,6-dimethyl-phenyl)propanedinitrile 有权
公开(公告)号：US20210284602A1
公开(公告)日：2021-09-16
申请号：US17337615
申请日：2021-06-03
申请人： SYNGENTA PARTICIPATIONS AG
发明人： Martin ZELLER , Nicolas FEDOU
IPC分类号： C07C255/35 , C07C51/08 , C07C53/134 , C07C255/33 , C07C253/30
摘要： 2-(4-chloro-2,6-dimethyl-phenyl)propanedinitrile.

3. 发明申请

US20210147335A1 FENFLURAMINE COMPOSITIONS AND METHODS OF PREPARING THE SAME 有权
公开(公告)号：US20210147335A1
公开(公告)日：2021-05-20
申请号：US17159367
申请日：2021-01-27
申请人： ZOGENIX INTERNATIONAL LIMITED
发明人： Derek J. LONDESBROUGH , Marc W. ANDERSEN
IPC分类号： C07C209/28 , C07C51/43 , C07C51/08 , C07C45/80 , C07C45/72 , C07C209/84
摘要： Methods of preparing a fenfluramine active pharmaceutical ingredient are provided. Aspects of the method include (a) hydrolyzing a 2-(3-(trifluoromethyl)phenyl)acetonitrile composition to produce a 2-(3-(trifluoromethyl)phenyl)acetic acid composition; (b) reacting the 2-(3-(trifluoromethyl)phenyl)acetic acid composition with acetic anhydride and a catalyst to produce a 1-(3-(trifluoromethyl)phenyl)propan-2-one composition; and (c) reductively aminating the 1-(3-(trifluoromethyl)phenyl)propan-2-one composition with ethylamine using a borohydride reducing agent to produce a fenfluramine composition. Also provided are compositions and pharmaceutical ingredients prepared according to the subject methods including a pharmaceutically acceptable salt of fenfluramine and having less than 0.2% by weight in total of trifluoromethyl regioisomers.

4. 发明申请

US20180079713A1 THERMAL CONVERSION VESSEL USED IN A PROCESS FOR AMIDIFICATION OF ACETONE CYANOHYDRIN 审中-公开
公开(公告)号：US20180079713A1
公开(公告)日：2018-03-22
申请号：US15820632
申请日：2017-11-22
申请人： Arkema France
发明人： Yves Bernardin , Xavier MARCARIAN , Romain BILLON
IPC分类号： C07C231/12 , C07C305/06 , B01J14/00 , C07C235/06 , C07C233/09 , C07C231/06 , C07C69/54 , C07C67/20 , C07C57/04 , C07C51/08 , C07C303/24 , B01J19/00 , B01J19/02 , B01J19/24
CPC分类号： C07C231/12 , B01J14/00 , B01J19/0013 , B01J19/002 , B01J19/006 , B01J19/02 , B01J19/245 , B01J19/249 , B01J2219/0004 , B01J2219/00058 , B01J2219/00063 , B01J2219/00065 , B01J2219/00162 , B01J2219/00166 , B01J2219/00182 , B01J2219/0027 , B01J2219/00272 , B01J2219/00768 , B01J2219/0286 , B01J2219/029 , B01J2219/182 , B01J2219/1943 , B01J2219/2475 , C07C51/08 , C07C57/04 , C07C67/20 , C07C69/54 , C07C231/06 , C07C233/09 , C07C235/06 , C07C303/24 , C07C305/06
摘要： The invention relates to a thermal conversion vessel (200) used during amidification step of acetone cyanohydrin (ACH), in the industrial process for production of a methyl methacrylate (MMA) or methacrylic acid (MAA). The thermal conversion vessel (200) is used for converting an hydrolysis mixture of α-hydroxyisobutyramide (HIBAM), α-sulfatoisobutyramide (SIBAM), 2-methacrylamide (MACRYDE) and methacrylique acid (MAA), into a mixture of 2-methacrylamide (MACRYDE). It comprises: at least one compartment (C1, C2, C3, . . . Ci) comprising an inner wall (206a, 206b, 206i) separating said compartment into two communicating parts (C1a, C1b) by a passage provided between the bottom of said vessel and said inner wall, said compartment having a space above said inner wall, for separating gas phase from liquid phase during thermal conversion, said compartment being connected to an outlet valve (204a, 204b, . . . 204i). Such vessel allows obtaining a high yield thermal conversion in very safe conditions.

5. 发明授权

US09458083B2 Method for hydrolysing acetone cyanohydrin 有权
标题翻译：水解丙酮氰醇的方法
公开(公告)号：US09458083B2
公开(公告)日：2016-10-04
申请号：US14384273
申请日：2013-03-06
申请人： Arndt Selbach , Lorenza Sartorelli , Andreas Perl , Joachim Deinken , Stefanie Sohnemann , Norbert Mnich , Matthias Groemping , Udo Gropp , Thomas Mertz
发明人： Arndt Selbach , Lorenza Sartorelli , Andreas Perl , Joachim Deinken , Stefanie Sohnemann , Norbert Mnich , Matthias Groemping , Udo Gropp , Thomas Mertz
IPC分类号： B01J19/18 , B01J19/24 , C07C231/06 , C07C253/30 , C07C51/06 , C07C51/08 , C07C51/377 , C07C67/22 , B01J19/00 , B01J4/00
CPC分类号： C07C67/22 , B01J4/008 , B01J19/0013 , B01J19/1868 , B01J19/2415 , B01J2219/00033 , B01J2219/30261 , B01J2219/30265 , C07C51/06 , C07C51/08 , C07C51/377 , C07C231/06 , C07C253/30 , C07C57/04 , C07C233/09 , C07C255/08
摘要： The present invention relates to a process for hydrolysis of acetone cyanohydrin (ACH) by means of sulphuric acid within the ACH sulpho process for preparation of methacrylic acid (MAA) or methyl methacrylate (MMA).
摘要翻译：本发明涉及在用于制备甲基丙烯酸（MAA）或甲基丙烯酸甲酯（MMA）的ACH硫酸法中用硫酸水解丙酮氰醇（ACH）的方法。

6. 发明授权

US09428427B2 Process for nitrile removal from hydrocarbon feeds 有权
标题翻译：从碳氢化合物进料中除去腈的方法
公开(公告)号：US09428427B2
公开(公告)日：2016-08-30
申请号：US14233183
申请日：2012-06-14
申请人： Hans K. T. Goris , Machteld M. W. Mertens , Luc R. M. Martens
发明人： Hans K. T. Goris , Machteld M. W. Mertens , Luc R. M. Martens
IPC分类号： C07C2/02 , C07C7/12 , C07C7/00 , C07C7/148 , B01J20/06 , B01J20/08 , B01J20/12 , B01J20/18 , B01J20/20 , B01J21/04 , B01J29/70 , C07C2/12 , C07C51/06 , C07C51/08 , C07C51/47 , C07C53/08 , C07C53/122 , B01J20/10
CPC分类号： C07C7/1485 , B01J20/06 , B01J20/08 , B01J20/103 , B01J20/12 , B01J20/186 , B01J20/20 , B01J21/04 , B01J29/70 , B01J2220/606 , C07C2/12 , C07C7/005 , C07C7/12 , C07C7/148 , C07C7/14866 , C07C51/06 , C07C51/08 , C07C51/47 , C07C53/08 , C07C53/122 , C07C2521/04 , C07C2529/06 , C07C2529/70 , Y02P20/52 , C07C11/02 , C07C11/06
摘要： A process is described, such process comprising i) contacting a hydrocarbon feed with a heterogeneous catalyst under conditions suitable to hydrolyze nitriles present in the feed to form a nitrile hydrolysis product comprising ammonia, carboxylic acid and carboxylate salts or a mixture thereof; and ii) removing the nitrile hydrolysis product from the feed. In an embodiment, the hydrocarbon feed comprises olefins and is intended for use in an olefin oligomerization process.
摘要翻译：描述了一种方法，该方法包括：i）在适于水解进料中存在的腈的条件下使烃进料与多相催化剂接触以形成含有氨，羧酸和羧酸盐的腈水解产物或其混合物; 和ii）从进料中除去腈水解产物。在一个实施方案中，烃进料包含烯烃并且用于烯烃低聚方法。

7. 发明申请

US20140012033A1 METHOD FOR PREPARING DIFLUOROACETONITRILE AND THE DERIVATIVES THEREOF 有权
标题翻译：制备二氟乙酸乙酯及其衍生物的方法
公开(公告)号：US20140012033A1
公开(公告)日：2014-01-09
申请号：US14003118
申请日：2012-03-08
申请人： Olivier Buisine
发明人： Olivier Buisine
IPC分类号： C07C253/14 , C07C51/08
CPC分类号： C07C253/14 , C07C51/08 , C07C255/10
摘要： The present invention relates to a method for preparing difluoracetonitrile and the derivatives thereof. The method for preparing difluoroacetonitrile according to the invention is characterized in that it includes reacting halogenodifluoromethane and a source of cyanide anions in an alkaline medium. The invention also relates to the use of difluoroacetonitrile as an intermediate in the manufacture of difluoroacetic acid and the salts, esters, or amide thereof
摘要翻译：本发明涉及二氟乙腈及其衍生物的制备方法。根据本发明的制备二氟乙腈的方法的特征在于其包括在碱性介质中使卤代二氟甲烷和氰化物阴离子源反应。本发明还涉及二氟乙腈作为制备二氟乙酸及其盐，酯或酰胺的中间体的用途

8. 发明申请

US20130018201A1 New Process 有权
标题翻译：新进程
公开(公告)号：US20130018201A1
公开(公告)日：2013-01-17
申请号：US13541795
申请日：2012-07-05
申请人： Beat Birrer , Leo Clarke , Walter Deichtmann , John Hayes , Julius Jeisy , Christian Lautz , Rainer E. Martin , Michael Meade , Joaquim Pintao , Michelangelo Scalone , Juergen Schaefer , Dennis Smith , Andreas Staempfli , Joachim Veits , Christian Walch , Andrew Walsh , Andreas Zogg
发明人： Beat Birrer , Leo Clarke , Walter Deichtmann , John Hayes , Julius Jeisy , Christian Lautz , Rainer E. Martin , Michael Meade , Joaquim Pintao , Michelangelo Scalone , Juergen Schaefer , Dennis Smith , Andreas Staempfli , Joachim Veits , Christian Walch , Andrew Walsh , Andreas Zogg
IPC分类号： C07C327/30 , C07C319/06 , C07C319/22 , C07C51/08 , C07C51/60
CPC分类号： C07C319/20 , C07C51/02 , C07C51/06 , C07C51/08 , C07C319/06 , C07C327/30 , C07C2601/14 , C07C323/40 , C07C61/08
摘要： A process for the preparation of a compound of formula (I): which is useful as an intermediate in the preparation of pharmaceutically active compounds.
摘要翻译：制备式（I）化合物的方法：其可用作药物活性化合物的制备中的中间体。

9. 发明授权

US08334399B2 Method for producing acetone cyanohydrin and the subsequent products thereof by specific cooling 有权
标题翻译：通过特定冷却生产丙酮氰醇的方法及其后续产物
公开(公告)号：US08334399B2
公开(公告)日：2012-12-18
申请号：US12442123
申请日：2007-08-31
申请人： Udo Gropp , Robert Weber , Thomas Schaefer , Andreas Perl , Rudolf Sing , Thomas Mertz
发明人： Udo Gropp , Robert Weber , Thomas Schaefer , Andreas Perl , Rudolf Sing , Thomas Mertz
IPC分类号： C07C253/00 , C07C57/02 , C07C51/08
CPC分类号： C07C231/14 , C07C51/06 , C07C67/20 , C07C231/06 , C07C253/00 , C07C57/04 , C07C69/54 , C07C233/09 , C07C255/16
摘要： The present invention relates in general terms to a process for preparing acetone cyanohydrin, comprising as steps: A. contacting acetone and hydrocyanic acid in a reactor to give a reaction mixture, the reaction mixture being circulated, to obtain acetone cyanohydrin; B. cooling at least some of the reaction mixture by flowing it through a cooling region of a cooler, the cooler including one cooling element or at least two cooling elements; C. discharging at least a portion of the acetone cyanohydrin obtained from the reactor, the volume of the cooling region of the cooler based on the total internal volume of the cooler being greater than the volume of the cooling element or of the at least two cooling elements of the cooler, to a process for preparing an alkyl methacrylate, to a process for preparing a methacrylic acid, to an apparatus for preparing alkyl methacrylates, to a process for preparing polymers based at least partly on alkyl methacrylates, to the use of the alkyl methacrylates obtainable from the process according to the invention in chemical products, and to chemical products based on the alkyl methacrylates obtainable by the processes according to the invention.
摘要翻译：本发明总体上涉及制备丙酮氰醇的方法，其包括如下步骤：A.在反应器中使丙酮和氢氰酸接触，得到反应混合物，使反应混合物循环，得到丙酮氰醇; B.通过使至少一些反应混合物流过冷却器的冷却区域来冷却反应混合物，冷却器包括一个冷却元件或至少两个冷却元件; C.排出从反应器获得的丙酮氰醇的至少一部分，冷却器的冷却区域的体积基于冷却器的总内部容积大于冷却元件的体积或至少两个冷却冷却器的元件，制备甲基丙烯酸烷基酯的方法，制备甲基丙烯酸的方法，制备甲基丙烯酸烷基酯的设备，至少部分地基于甲基丙烯酸烷基酯制备聚合物的方法，以使用可从本发明的方法获得的甲基丙烯酸烷基酯化学产品，以及基于通过本发明的方法获得的甲基丙烯酸烷基酯的化学产品。

10. 发明申请

US20120283470A1 PROCESS TO PREPARE TREPROSTINIL, THE ACTIVE INGREDIENT IN REMODULIN® 有权
标题翻译：制备TREPROSTINIL，REMODULIN®中的活性成分的方法
公开(公告)号：US20120283470A1
公开(公告)日：2012-11-08
申请号：US13548446
申请日：2012-07-13
申请人： Hitesh Batra , Sudersan M. Tuladhar , Raju Penmasta , David A. Walsh
发明人： Hitesh Batra , Sudersan M. Tuladhar , Raju Penmasta , David A. Walsh
IPC分类号： C07C51/08 , C07C59/72
CPC分类号： A61K31/192 , A01N37/10 , C07C39/12 , C07C39/17 , C07C51/08 , C07C51/41 , C07C51/412 , C07C59/60 , C07C59/72 , C07C213/08 , C07C253/00 , C07C405/0075 , C07C2103/12
摘要： This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.
摘要翻译：本发明涉及制备前列环素衍生物的改进方法。一个实施方案提供了通过曲前列腺素盐将苯三烯三醇转化成曲前列腺素并净化曲前列素的改进方法。

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