Module-assisted one-pot synthesis of [18F]SFB for radiolabeling proteins |
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| Authors: | Ming-Wei Wang Yong-Ping Zhang Ying-Jian Zhang and Clifton Kwang-Fu Shen |
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| Institution: | (1) Department of Nuclear Medicine, Fudan University Shanghai Cancer Center, Shanghai, 200032, China;(2) Department of Oncology, Shanghai Medical College, Fudan University, Shanghai, 200032, China;(3) The Joint Center For Biomedical Imaging of Department of Chemistry and Institute of Biomedical Science and Shanghai Cancer Center, Fudan University, Shanghai, 200032, China;(4) Department of Molecular and Medical Pharmacology, David Geffen School of Medicine at University of California Los Angeles (UCLA), Los Angeles, CA, USA;(5) Crump Institute for Molecular Imaging (CIMI), David Geffen School of Medicine at University of California Los Angeles (UCLA), Los Angeles, CA, USA;(6) California NanoSystems Institute (CNSI), University of California Los Angeles (UCLA), Los Angeles, CA, USA |
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| Abstract: | The need of reliable production of N-succinimidyl 4-18F]fluorobenzoate (18F]SFB), a versatile 18F-labeled prosthetic group for protein labeling, has increased dramatically due to the easy availability of proteins or their
engineered derivatives for targeted molecular imaging. A module-assisted radiosynthesis of 18F]SFB was developed using a three-step, one-pot procedure and ethyl 4-(trimethylammonium)benzoate triflate (1) as the starting material. The radiochemical transformations were carried out in a general-purpose, custom-made module and
streamlined by an anhydrous deprotection strategy using t-BuOK/DMSO. After HPLC-purification, 18F]SFB was synthesized in radiochemical yields of 20–30% (n > 10, not decay-corrected) and excellent radiochemical and chemical purities (>98%). The total synthesis and purification
time required is ~90 min. Using the purified 18F]SFB, three 18F-labeled proteins, bovine serum albumin (BSA), chicken egg albumin (CEA) and transferrin, were synthesized in yields of 61.0–79.5%.
The 18F-Annexin V for apoptosis imaging was also produced in 5% radiolabeling yield and >95% radiochemical purity. |
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