[EN] METHOD FOR THE PRODUCTION OF 18F-LABELED ACTIVE ESTERS AND THEIR APPLICATION EXEMPLIFIED BY THE PREPARATION OF A PSMA-SPECIFIC PET-TRACER<br/>[FR] PROCÉDÉ DE PRODUCTION D'ESTERS ACTIFS MARQUÉS AU 18F ET LEUR APPLICATION ILLUSTRÉE PAR LA PRÉPARATION D'UN TRACEUR POUR PET SPÉCIFIQUE DE L'ANTIGÈNE MEMBRANAIRE SPÉCIFIQUE DE LA PROSTATE (PSMA)
申请人:MAX PLANCK GES ZUR FÖRDERUNG DER WISSENSCHAFTEN E V
公开号:WO2016030329A1
公开(公告)日:2016-03-03
Novel efficient, time-saving and reliable radiofluorination procedures for the production of 18F-labelled active esters via nucleophilic substitution of the corresponding onium precursors with 18F- are described. The active ester including [18F]F-Py-TFP and [18F]TFB produced by one of these methods was used to prepare PSMA-specific PET tracers such as [18F]DCFPyL. The key advantages of these inventive methods are efficiency, short time of preparation and excellent amenability to automation. A pharmaceutical composition containing at least one PSMA-specific PET tracers prepared by the inventive method is useful for positron emission tomography (PET) imaging, especially imaging prostate tumor.
本文描述了一种高效、省时和可靠的放射性氟化程序,通过将相应的离子前体与18F-的亲核取代反应制备18F标记的活性酯。其中包括通过其中一种方法制备的[18F]F-Py-TFP和[18F]TFB的活性酯,用于制备PSMA特异性PET示踪剂,如[18F]DCFPyL。这些创新方法的关键优势是高效、制备时间短,且易于自动化。通过这些创新方法制备的至少一种PSMA特异性PET示踪剂的药物组合物,对于正电子发射断层扫描(PET)成像特别是前列腺肿瘤成像非常有用。