Precursors for radiofluorination
    2.
    发明授权

    公开(公告)号:US10759760B2

    公开(公告)日:2020-09-01

    申请号:US16348997

    申请日:2017-11-17

    Abstract: A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A1 to the bonding unit and via bond A2 to the ring, wherein the bonding unit has second substituent(s) —OH, —CONH, and/or —COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is —N+(R1R2R3), —NO2, —Cl, —Br, —F, or —I, and R1, R2, and R3 are independently C1-C6 alkyl; and (b) reacting the precursor with a [18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N+(R4R5R6R7) with R4, R5, R6, and R7 being independently C1-C6 alkyl, wherein the substituent Y is replaced by [18F] fluoride.

    DEVICE AND METHOD FOR THE PRODUCTION OF RADIOCHEMICAL COMPOUNDS
    3.
    发明申请
    DEVICE AND METHOD FOR THE PRODUCTION OF RADIOCHEMICAL COMPOUNDS 有权
    用于生产放射化学化合物的装置和方法

    公开(公告)号:US20160115092A1

    公开(公告)日:2016-04-28

    申请号:US14990567

    申请日:2016-01-07

    Abstract: The invention relates to a method for the preparation of radiochemical compounds using a device having at least a reaction module, a dosing module, and a storage module, wherein the reaction module has at least one reaction vessel having a closable opening through which substances needed for the preparation of a predetermined radiochemical compound can be introduced into the reaction vessel of the reaction module and through which the prepared radiochemical compound can be removed from the reaction vessel of the reaction module; the dosing module has at least one pipetting head which can be moved relative to the storage module and the reaction module and in x, y, and z directions and also has at least one dosing unit; and at least one reservoir for one of the substances needed for the preparation of the respective radiochemical compound is formed in the storage module. Substances needed for the preparation of the respective radiochemical compound are introduced into the reaction vessel of the reaction module by means of dosing units, wherein the dosing units can be moved via a pipetting head in x, y directions or in x, y, and z directions.

    Abstract translation: 本发明涉及使用至少具有反应模块,剂量模块和储存模块的装置来制备放射化学化合物的方法,其中反应模块具有至少一个具有可闭合的开口的反应容器, 可以将预定的放射化学化合物的制备物引入反应模块的反应容器中,通过该反应装置可以从反应模块的反应容器中除去所制备的放射化学化合物; 所述计量模块具有至少一个移液头,其可相对于所述储存模块和所述反应模块以及x,y和z方向移动,并且还具有至少一个计量单元; 并且在储存模块中形成用于制备各放射化学化合物所需的物质之一的至少一个贮存器。 制备相应的放射化学化合物所需的物质通过计量单元被引入反应模块的反应容器中,其中计量单元可以通过移液头沿x,y方向或x,y和z移动 方向。

    PRECURSORS FOR RADIOFLUORINATION
    4.
    发明申请

    公开(公告)号:US20200165204A1

    公开(公告)日:2020-05-28

    申请号:US16778155

    申请日:2020-01-31

    Abstract: A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A1 to the bonding unit and via bond A2 to the ring, wherein the bonding unit has second substituent(s) —OH, —CONH, and/or —COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is —N+(R1R2R3), —NO2, —Cl, —Br, —F, or —I, and R1, R2, and R3 are independently C1-C6 alkyl; and (b) reacting the precursor with a [18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N+(R4R5R6R7) with R4, R5, R6, and R7 being independently C1-C6 alkyl, wherein the substituent Y is replaced by [18F] fluoride.

    PRECURSORS FOR RADIOFLUORINATION
    6.
    发明申请

    公开(公告)号:US20190263756A1

    公开(公告)日:2019-08-29

    申请号:US16348997

    申请日:2017-11-17

    Abstract: A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A1 to the bonding unit and via bond A2 to the ring, wherein the bonding unit has second substituent(s) —OH, —CONH, and/or —COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is —N+(R1R2R3), —NO2, —Cl, —Br, —F, or —I, and R1, R2, and R3 are independently C1-C6 alkyl; and (b) reacting the precursor with a [18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N+(R4R5R6R7) with R4, R5, R6, and R7 being independently C1-C6 alkyl, wherein the substituent Y is replaced by [18F] fluoride.

    Precursors for radiofluorination
    7.
    发明授权

    公开(公告)号:US11053200B2

    公开(公告)日:2021-07-06

    申请号:US16778155

    申请日:2020-01-31

    Abstract: A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A1 to the bonding unit and via bond A2 to the ring, wherein the bonding unit has second substituent(s) —OH, —CONH, and/or —COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is —N+(R1R2R3), —NO2, —Cl, —Br, —F, or —I, and R1, R2, and R3 are independently C1-C6 alkyl; and (b) reacting the precursor with a [18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N+(R4R5R6R7) with R4, R5, R6, and R7 being independently C1-C6 alkyl, wherein the substituent Y is replaced by [18F] fluoride.

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