Method for the production of 18F-labeled active esters and their application exemplified by the preparation of a PSMA-specific PET-tracer

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United States of America Patent

PATENT NO 10112974
APP PUB NO 20170267717A1
SERIAL NO

15506351

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Abstract

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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.

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Patent Owner(s)

  • MAX-PLANCK GESELLSCHAFT ZUR FOERDERUNG DER WISSENSCHAFTEN E.V.; UNIVERSITAT ZU KOLN

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Krapf, Phillip Much, DE 1 4
Neumaier, Bernd Hurth, DE 4 11
Richarz, Raphael Leverkusen, DE 2 11
Zlatopolskiy, Boris Cologne, DE 2 11

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