首页> 外国专利> ELUTION OF FLUORINE-18 FLUORIDE FROM ANION EXCHANGE POLYMER SUPPORT CARTRIDGE USING PROTIC SOLVENTS WHICH DISSOLVE SALT IN AND ITS APPLICATION OF FLUORINE-18 FLUORINATION METHOD

ELUTION OF FLUORINE-18 FLUORIDE FROM ANION EXCHANGE POLYMER SUPPORT CARTRIDGE USING PROTIC SOLVENTS WHICH DISSOLVE SALT IN AND ITS APPLICATION OF FLUORINE-18 FLUORINATION METHOD

机译:离子交换聚合物支持溶质中质子溶剂从阴离子交换聚合物中洗脱氟18的研究及其在氟18氟化方法中的应用

摘要

A method for labeling fluorine-18 in alkyl halides or alkyl sulfonates is provided to reduce the overall time required for carrying out labeling of fluorine-18, and to obtain a labeled compound with high purity and high yield. A method for labeling fluorine-18 comprises the steps of: (i) adsorbing [18F] fluoride onto a quaternary ammonium-supported polymer support; (ii) eluting the [18F]fluoride adsorbed in step (i) with an ammonium salt represented by the following formula 2 or a solution containing a metal salt dissolved in an alcohol solvent represented by the following formula 1; and (iii) reacting the [18F]fluoride eluted in step (ii) with an alkyl halide or alkyl sulfonate in the presence of a reaction solvent to perform fluorine-18 labeling. In formula 1, each of R1, R2 and R3 is H or a C1-C8 alkyl. In formula 2, R4 is H or a C1-C5 primary or secondary alkyl group; and X- is -OH, -OTf, -OMs, HCO3^-, CO3^2-,H2PO4^-,HPO4^2- or PO4^3-.
机译:提供了一种在烷基卤或烷基磺酸盐中标记氟-18的方法,以减少进行氟-18标记所需的总时间,并获得高纯度和高产率的标记化合物。标记氟18的方法包括以下步骤:(i)将[18F]氟化物吸附到季铵负载的聚合物载体上; (ii)用下式2表示的铵盐或将金属盐溶解在下式1表示的醇溶剂中的溶液洗脱步骤(i)中吸附的[18 F]氟化物; (iii)使步骤(ii)中洗脱的[18 F]氟化物与卤代烷或磺酸烷基酯在反应溶剂的存在下反应,以进行氟18标记。在式1中,R 1,R 2和R 3各自为H或C 1 -C 8烷基。式2中,R 4为H或碳数1〜5的伯或仲烷基。 X-为-OH,-OTf,-OMs,HCO 3-,CO 3-,H 2 PO 4-,HPO 4 -2-或PO 4 -3-。

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