Fenfluramine compositions and methods of preparing the same

    公开(公告)号:US11634377B2

    公开(公告)日:2023-04-25

    申请号:US17159367

    申请日:2021-01-27

    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.

    FENFLURAMINE COMPOSITIONS AND METHODS OF PREPARING THE SAME

    公开(公告)号:US20210147335A1

    公开(公告)日:2021-05-20

    申请号:US17159367

    申请日:2021-01-27

    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.

    METHOD FOR PREPARING DIFLUOROACETONITRILE AND THE DERIVATIVES THEREOF
    7.
    发明申请
    METHOD FOR PREPARING DIFLUOROACETONITRILE AND THE DERIVATIVES THEREOF 有权
    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

    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

    Method for producing acetone cyanohydrin and the subsequent products thereof by specific cooling
    9.
    发明授权
    Method for producing acetone cyanohydrin and the subsequent products thereof by specific cooling 有权
    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

    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。