Patrice Marchand1, Ali Ouadi2, Michel Pellicioli3, Jacky Schuler4, Patrice Laquerriere5, Frédéric Boisson6, David Brasse7. 1. Université de Strasbourg, IPHC, 23 rue du Loess, 67037 Strasbourg, France; CNRS, UMR 7178, 67037 Strasbourg, France. Electronic address: patrice.marchand@iphc.cnrs.fr. 2. Université de Strasbourg, IPHC, 23 rue du Loess, 67037 Strasbourg, France; CNRS, UMR 7178, 67037 Strasbourg, France. Electronic address: ali.ouadi@iphc.cnrs.fr. 3. Université de Strasbourg, IPHC, 23 rue du Loess, 67037 Strasbourg, France; CNRS, UMR 7178, 67037 Strasbourg, France. Electronic address: michel.pellicioli@iphc.cnrs.fr. 4. Université de Strasbourg, IPHC, 23 rue du Loess, 67037 Strasbourg, France; CNRS, UMR 7178, 67037 Strasbourg, France. Electronic address: jacky.schuler@iphc.cnrs.fr. 5. Université de Strasbourg, IPHC, 23 rue du Loess, 67037 Strasbourg, France; CNRS, UMR 7178, 67037 Strasbourg, France. Electronic address: patrice.laquerriere@iphc.cnrs.fr. 6. Université de Strasbourg, IPHC, 23 rue du Loess, 67037 Strasbourg, France; CNRS, UMR 7178, 67037 Strasbourg, France. Electronic address: frederic.boisson@iphc.cnrs.fr. 7. Université de Strasbourg, IPHC, 23 rue du Loess, 67037 Strasbourg, France; CNRS, UMR 7178, 67037 Strasbourg, France. Electronic address: david.brasse@iphc.cnrs.fr.
Abstract
INTRODUCTION: Since 1991 until now, many radiosyntheses of [(18)F]FLT have been published. Most of them suffer from side reactions and/or difficult purification related to the large amount of precursor necessary for the labeling step. A fully automated synthesis using only commercial and unmodified materials with a reduced amount of precursor would be desirable. METHODS: We first explored the possibility to elute efficiently [(18)F]fluorine from commercial and unmodified cartridges with various amount of base. Based on these results, 10mg and 5mg of precursors were used for the fluorination step. The best conditions were transposed in an automated process for a one pot two steps synthesis of labeled FLT. RESULTS: Using commercial and non-treated carbonate form of QMA cartridges, we were able to elute quantitatively the [(18)F]fluorine with a very low amount of base (0.59mg) and, with only 5mg of precursor, to perform an efficient fluorination reaction with up to 94% incorporation of [(18)F]fluorine. The synthesis was fully automated and radiochemical yields of 54% (decay corrected) were obtained within a synthesis time of 52minutes. CONCLUSION: We demonstrate that a fully automated and efficient radiosynthesis of [(18)F]FLT is feasible with only 5mg of precursor. Compare to the present state of the art, our method provides high yields of pure [(18)F]FLT and is broadly adaptable to other synthesis automates.
INTRODUCTION: Since 1991 until now, many radiosyntheses of [(18)F]FLT have been published. Most of them suffer from side reactions and/or difficult purification related to the large amount of precursor necessary for the labeling step. A fully automated synthesis using only commercial and unmodified materials with a reduced amount of precursor would be desirable. METHODS: We first explored the possibility to elute efficiently [(18)F]fluorine from commercial and unmodified cartridges with various amount of base. Based on these results, 10mg and 5mg of precursors were used for the fluorination step. The best conditions were transposed in an automated process for a one pot two steps synthesis of labeled FLT. RESULTS: Using commercial and non-treated carbonate form of QMA cartridges, we were able to elute quantitatively the [(18)F]fluorine with a very low amount of base (0.59mg) and, with only 5mg of precursor, to perform an efficient fluorination reaction with up to 94% incorporation of [(18)F]fluorine. The synthesis was fully automated and radiochemical yields of 54% (decay corrected) were obtained within a synthesis time of 52minutes. CONCLUSION: We demonstrate that a fully automated and efficient radiosynthesis of [(18)F]FLT is feasible with only 5mg of precursor. Compare to the present state of the art, our method provides high yields of pure [(18)F]FLT and is broadly adaptable to other synthesis automates.
Authors: Jeffrey Collins; Christopher M Waldmann; Christopher Drake; Roger Slavik; Noel S Ha; Maxim Sergeev; Mark Lazari; Bin Shen; Frederick T Chin; Melissa Moore; Saman Sadeghi; Michael E Phelps; Jennifer M Murphy; R Michael van Dam Journal: Proc Natl Acad Sci U S A Date: 2017-10-10 Impact factor: 11.205
Authors: James L Tatum; Joseph D Kalen; Paula M Jacobs; Lisa A Riffle; Amy James; Lai Thang; Chelsea Sanders; Melinda G Hollingshead; Falguni Basuli; Jianfeng Shi; James H Doroshow Journal: J Transl Med Date: 2022-08-18 Impact factor: 8.440