Chlorination of sucrose-6-esters
    2.
    发明授权

    公开(公告)号:US10081651B2

    公开(公告)日:2018-09-25

    申请号:US15502372

    申请日:2015-06-16

    IPC分类号: C07H5/02 C07H13/04

    CPC分类号: C07H5/02 C07H13/04

    摘要: There is provided a method for the chlorination of a sucrose-6-acylate to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate, wherein said method comprises the following steps (i) to (v): (i) providing a first component comprising sucrose-6-acylate; (ii) providing a second component comprising a chlorinating agent; (iii) combining said first component and said second component to afford a mixture; (iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1′ and 6′ positions thereof; (v) quenching said mixture to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate; wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; and wherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises dimethylacetamide (DMAc).

    MODULAR RADIOCHEMISTRY SYNTHESIS SYSTEM
    6.
    发明申请
    MODULAR RADIOCHEMISTRY SYNTHESIS SYSTEM 有权
    模块化放射化学合成系统

    公开(公告)号:US20150329583A1

    公开(公告)日:2015-11-19

    申请号:US14582885

    申请日:2014-12-24

    摘要: A modular chemical production system includes multiple modules for performing a chemical reaction, particularly of radiochemical compounds, from a remote location. One embodiment comprises a reaction vessel including a moveable heat source with the position thereof relative to the reaction vessel being controllable from a remote position. Alternatively the heat source may be fixed in location and the reaction vial is moveable into and out of the heat source. The reaction vessel has one or more sealing plugs, the positioning of which in relationship to the reaction vessel is controllable from a remote position. Also the one or more reaction vessel sealing plugs can include one or more conduits there through for delivery of reactants, gases at atmospheric or an elevated pressure, inert gases, drawing a vacuum and removal of reaction end products to and from the reaction vial, the reaction vial with sealing plug in position being operable at elevated pressures. The modular chemical production system is assembled from modules which can each include operating condition sensors and controllers configured for monitoring and controlling the individual modules and the assembled system from a remote position. Other modules include, but are not limited to a Reagent Storage and Delivery Module, a Cartridge Purification Module, a Microwave Reaction Module, an External QC/Analysis/Purification Interface Module, an Aliquotting Module, an F-18 Drying Module, a Concentration Module, a Radiation Counting Module, and a Capillary Reactor Module.

    摘要翻译: 模块化化学生产系统包括从远程位置进行化学反应,特别是放射化学化合物的多个模块。 一个实施例包括一个包括可移动热源的反应容器,其相对于反应容器的位置可从远程位置控制。 或者,热源可以固定在位置,并且反应小瓶可移动进入和离开热源。 反应容器具有一个或多个密封塞,其与反应容器相关的定位可从远程位置控制。 此外,一个或多个反应容器密封塞可以包括一个或多个管道,用于输送反应物,大气压或高压气体,惰性气体,抽真空和从反应小瓶中除去反应终产物, 具有密封塞位置的反应小瓶可在升高的压力下操作。 模块化化学生产系统由模块组装,每个模块可以包括操作状态传感器和配置成用于从远程位置监控和控制各个模块和组装系统的控制器。 其他模块包括但不限于试剂储存和输送模块,滤芯净化模块,微波反应模块,外部QC /分析/纯化界面模块,等分模块,F-18干燥模块,浓缩模块 ,辐射计数模块和毛细管反应堆模块。

    Purification of tertiary formamide contaminated with tertiary acetamide
    8.
    发明授权
    Purification of tertiary formamide contaminated with tertiary acetamide 有权
    用叔乙酰胺污染的叔甲酰胺的纯化

    公开(公告)号:US08981079B2

    公开(公告)日:2015-03-17

    申请号:US13378531

    申请日:2010-06-18

    摘要: A chlorinating agent such as a chloroiminium species is used to remove or neutralize tertiary acetamide present as a contaminant in a tertiary formamide solvent. Tertiary formamide solvent purified or treated in this manner can be used as a reaction vehicle for the chlorination of sucrose-6-acylates, thereby improving the yields of the desired sucralose-6-acylate (an intermediate in the production of sucralose).

    摘要翻译: 使用氯化剂如氯亚胺鎓物质来除去或中和作为叔甲酰胺溶剂中的污染物存在的叔乙酰胺。 以这种方式纯化或处理的叔甲酰胺溶剂可用作蔗糖-6-酰化物氯化反应载体,从而提高所需三氯半乳蔗糖-6-酰化物(三氯蔗糖生产中的中间体)的产率。

    STABILISATION OF RADIOPHARMACEUTICAL PRECURSORS
    9.
    发明申请
    STABILISATION OF RADIOPHARMACEUTICAL PRECURSORS 审中-公开
    无脊椎动物前列腺的稳定

    公开(公告)号:US20150018541A1

    公开(公告)日:2015-01-15

    申请号:US14258247

    申请日:2014-04-22

    IPC分类号: C07H13/04 C07H1/00

    摘要: The present invention relates to a method for improving stability of non fluoridated sugar derivatives, and in particular glucose derivatives such as 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-β-D-mannopyranose which are used as precursors for production of radiofluoridated sugar derivatives for use in in vivo imaging procedures such as positron emission tomography (PET). The method comprises storing the non fluoridated sugar derivative in an organic solvent. The resultant formulations of the non fluoridated sugar derivative and cassettes for automated synthesis apparatus comprising the same are also claimed.

    摘要翻译: 本发明涉及一种改善非氟化糖衍生物,特别是诸如1,3,4,6-四-O-乙酰基-2-O-三氟甲磺酰基-β-甘露吡喃糖等葡萄糖衍生物的稳定性的方法,其中 用作生产放射性氟化糖衍生物的前体,用于体内成像过程如正电子发射断层扫描(PET)。 该方法包括将非氟化糖衍生物储存在有机溶剂中。 还要求保护所得的非氟化糖衍生物制剂和包含其的自动化合成装置的盒。