Automated radiosynthesis of [18F]PBR111 and [18F]PBR102 using the Tracerlab FXFN and Tracerlab MXFDG module for imaging the peripheral benzodiazepine receptor with PET.

[(18)F]PBR111 and [(18)F]PBR102 are selective radioligands for imaging of the Peripheral Benzodiazepine Receptor (PBR). We have developed a fully automated method for the radiosynthesis of [(18)F]PBR111 and [(18)F]PBR102 in the Tracerlab FX(FN) (30±2% radiochemical yield non-decay-corrected for both tracers) and Tracerlab MX(FDG) (25±2% radiochemical yield non-decay-corrected for both tracers) from the corresponding p-toluenesulfonyl precursors. For all tracers, radiochemical purity was >99% and specific activity was >150GBq/μmol after less than 60min of preparation time.

Bourdier T ，Pham TQ ，Henderson D ，Jackson T ，Lam P ，Izard M ，Katsifis A ... -  《-》

[18F]DPA-714, [18F]PBR111 and [18F]FEDAA1106-selective radioligands for imaging TSPO 18 kDa with PET: automated radiosynthesis on a TRACERLAb FX-FN synthesizer and quality controls.

Imaging of TSPO 18 kDa with PET is more and more considered as a relevant biomarker of inflammation in numerous diseases. Development of new radiotracers for TSPO 18 kDa has seen acceleration in the last years and the challenge today is to make available large amounts of such a radiotracer in compliance with GMP standards for application in humans. We present in this technical note automated productions of [(18)F]DPA-714, [(18)F]PBR111 and [(18)F]FEDAA1106, three promising radiotracers for TSPO 18 kDa imaging, using a TRACERlab FX-FN synthesizer. This note also includes the quality control data of the validation batches for the manufacturing qualification of clinical production of [(18)F]DPA-714.

Kuhnast B ，Damont A ，Hinnen F ，Catarina T ，Demphel S ，Le Helleix S ，Coulon C ，Goutal S ，Gervais P ，Dollé F ... -  《-》

Fully automated synthesis of PET TSPO radioligands [11C]DAA1106 and [18F]FEDAA1106.

[(11)C]DAA1106 was prepared by O-[(11)C]methylation of DAA1123 with [(11)C]CH(3)OTf and NaH in CH(3)CN at 80°C and isolated by HPLC combined with SPE purification in 60-70% decay corrected radiochemical yield. [(18)F]FEDAA1106 was synthesized by the nucleophilic substitution of tosyloxy-FEDAA1106 in DMSO with K[(18)F]F/Kryptofix 2.2.2 at 140°C and isolated by HPLC combined with SPE purification in 30-60% decay corrected radiochemical yield. The specific activity for [(11)C]DAA1106 and [(18)F]FEDAA1106 was 370-740GBq/μmol and 37-222GBq/μmol at EOB, respectively.

Wang M ，Gao M ，Zheng QH 《-》

Automated radiosynthesis of [(18)F]ciprofloxacin.

We transferred the previously published manual synthesis of [(18)F]ciprofloxacin (decay-corrected RCY: 5.5±1.0%) to an automated synthesis module (TRACERlab(TM) FXFDG, GE Healthcare) and observed a strong decrease in RCY (0.4±0.4%). When replacing the standard 15-mL glassy carbon reactor of the synthesis module with a 3-mL V-shaped borosilicate glass reactor a considerable improvement in RCY was observed. [(18)F]Ciprofloxacin was obtained in a RCY of 2.7±1.4% (n=23) with a specific activity at EOS of 1.4±0.5GBq/µmol in a synthesis time of 160min.

Stanek J ，Mairinger S ，Wanek T ，Kuntner C ，Müller M ，Langer O ... -  《-》

New approach to fully automated synthesis of sodium [18F]fluoroacetate -- a simple and fast method using a commercial synthesizer.

Sun LQ ，Mori T ，Dence CS ，Ponde DE ，Welch MJ ，Furukawa T ，Yonekura Y ，Fujibayashi Y ... -  《NUCLEAR MEDICINE AND BIOLOGY》