公开(公告)号：US20150045548A1

公开(公告)日：2015-02-12

申请号：US14375412

申请日：2012-12-21

Applicant: THE ASAN FOUNDATION

Inventor： Sang Ju Lee ,  Seung Jun Oh ,  Dae Hyuk Moon ,  Jin Sook Ryu ,  Jae Seung Kim ,  Jong Jin Lee

IPC: C07C303/32 ,  C07D213/64 ,  C07D451/02 ,  C07H19/06 ,  C07D233/91 ,  C07C309/01 ,  C07C217/80

CPC classification number: C07C303/32 ,  A61K51/04 ,  A61K51/0455 ,  C07B59/00 ,  C07B2200/05 ,  C07C213/08 ,  C07C217/80 ,  C07C253/30 ,  C07C309/01 ,  C07D213/64 ,  C07D233/91 ,  C07D403/06 ,  C07D451/02 ,  C07D471/04 ,  C07H19/06 ,  C07C309/04 ,  C07C255/42

Abstract: The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [18F]fluoride in a method for preparing an organic [18F]fluoro compound by reacting an alkyl halide or an alkyl sulfonate with a [18F]fluoride, wherein a [18F]fluoride supported on a quaternary alkyl ammonium polymer support is eluted using a solution containing a metal salt or a quaternary ammonium salt with an adjusted pH, and a base is not additionally used. The present invention enables a labeling reaction without an additional base after precisely reflecting the concentration of a base absolutely necessary for the nucleophilic substitution of a [18F]fluoride or eluting a [18F]fluoride using a [18F]fluoride eluent with an adjusted pH, thereby stably obtaining a [18F]fluoride-labelled compound in a high yield, and is thus useful for production of fluorine-18-labelled radioactive medical supplies.

Abstract translation: 本发明涉及一种放射性同位素标记氟-18的方法，更具体地说，涉及通过使烷基卤化物或烷基卤反应制备有机[18 F]氟化合物的方法中的[18 F]氟化物的标记方法 具有[18 F]氟化物的烷基磺酸盐，其中使用含有调节pH的金属盐或季铵盐的溶液洗脱负载在季烷基铵聚合物载体上的[18 F]氟化物，并且不另外使用碱 。 本发明能够在精确反映[18 F]氟化物的亲核取代绝对必需的碱的浓度或使用具有调节pH的[18 F]氟化物洗脱液洗脱[18 F]氟化物时，无需附加碱的标记反应， 从而以高产率稳定地获得[18 F]氟化物标记的化合物，因此可用于生产氟-18-标记的放射性医疗用品。

公开(公告)号：US10392344B2

公开(公告)日：2019-08-27

申请号：US14375412

申请日：2012-12-21

Applicant: THE ASAN FOUNDATION

Inventor： Sang Ju Lee ,  Seung Jun Oh ,  Dae Hyuk Moon ,  Jin Sook Ryu ,  Jae Seung Kim ,  Jong Jin Lee

IPC: C07C303/32 ,  C07B59/00 ,  C07C217/80 ,  C07C309/01 ,  C07D213/64 ,  C07D233/91 ,  C07D451/02 ,  C07H19/06 ,  C07D403/06 ,  C07C213/08 ,  C07D471/04 ,  C07C253/30 ,  A61K51/04

Abstract: The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [18F]fluoride in a method for preparing an organic [18F]fluoro compound by reacting an alkyl halide or an alkyl sulfonate with a [18F]fluoride, wherein a [18F]fluoride supported on a quaternary alkyl ammonium polymer support is eluted using a solution containing a metal salt or a quaternary ammonium salt with an adjusted pH, and a base is not additionally used. The present invention enables a labeling reaction without an additional base after precisely reflecting the concentration of a base absolutely necessary for the nucleophilic substitution of a [18F]fluoride or eluting a [18F]fluoride using a [18F]fluoride eluent with an adjusted pH, thereby stably obtaining a [18F]fluoride-labelled compound in a high yield, and is thus useful for production of fluorine-18-labelled radioactive medical supplies.