Verfahren zur Synthese trägerarmer ·18·F markierter Verbindungen

摘要

The invention relates to a method for the synthesis of <18>F marked compounds which are low in carriers. Nucleophilic phase-transfer catalyzed <18>F- fluoridation was previously the only way to produce <18>F marked radiotracers having a high molar activity (> 3,7 . 10<16> Bq/mol) for nuclear medicinal diagnosis. However, this marking method pre-supposes that educts having high nucleofugic leaving groups are accessible and that the requisite chemical stability of said compounds is guaranteed in said marking conditions. Complex natural substances and the derivatives thereof do not fulfil said conditions. They are irreversibly damaged or denatured. The inventive method makes it possible to mark natural substances and the derivatives thereof with <18>F, especially in a stereoselective manner in mild reaction conditions. According to the inventive method, <18>F marked compounds which are low in carriers can be synthesized, by <18>F fluoridating perfluoroalkyl sulfonimides and by subsequent esterization with a hydroxy function. According to the inventive method it is also possible to work with small amounts of educts and therefore to increase the cost-effectiveness of the method.