Enhanced copper-mediated 18 F-fluorination of aryl boronic esters provides eight radiotracers for PET applications
Sean Preshlock
(1)
,
Samuel Calderwood
(1)
,
Stefan Verhoog
(1)
,
Matthew Tredwell
(1)
,
Mickael Huiban
(2)
,
Antje Hienzsch
(3)
,
Stefan Gruber
(1)
,
Thomas L. Wilson
(4)
,
Nicholas Taylor
(1)
,
Thomas Cailly
(5)
,
Michael Schedler
(6)
,
Thomas Collier
(7)
,
Jan Passchier
(8)
,
René Smits
(3)
,
Jan Mollitor
(3)
,
Alexander Hoepping
(3)
,
Marco Mueller
(3)
,
Christophe Genicot
(9)
,
Joël Mercier
(9)
,
Veronique Gouverneur
(1)
1
Chemistry Research Laboratory [Oxford, UK]
2 Hammersmith Hospital NHS Imperial College Healthcare
3 ABX GmbH - ABX advanced biochemical compounds GmbH
4 ESO - European Southern Observatory
5 CERMN - Centre d'Etudes et de Recherche sur le Médicament de Normandie
6 Organisch-Chemisches Institut der Westfälischen Wilhelms-Universität Münster
7 ADVION
8 Erasmus MC - Erasmus University Medical Center [Rotterdam]
9 UCB Pharma S.A.[Braine-l'Alleud]
2 Hammersmith Hospital NHS Imperial College Healthcare
3 ABX GmbH - ABX advanced biochemical compounds GmbH
4 ESO - European Southern Observatory
5 CERMN - Centre d'Etudes et de Recherche sur le Médicament de Normandie
6 Organisch-Chemisches Institut der Westfälischen Wilhelms-Universität Münster
7 ADVION
8 Erasmus MC - Erasmus University Medical Center [Rotterdam]
9 UCB Pharma S.A.[Braine-l'Alleud]
Thomas Cailly
- Fonction : Auteur
- PersonId : 170651
- IdHAL : thomas-cailly
- ORCID : 0000-0002-5262-4494
- IdRef : 112090672
Résumé
[18F]FMTEB, [18F]FPEB, [18F]flumazenil, [18F]DAA1106, [18F]MFBG, [18F]FDOPA, [18F]FMT and [18F]FDA are prepared from the corresponding arylboronic esters and [18F]KF/K222 in the presence of Cu(OTf)2py4. The method was successfully applied using three radiosynthetic platforms, and up to 26 GBq of non-carrier added starting activity of 18F-fluoride.