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Module-assisted one-pot synthesis of [18F]SFB for radiolabeling proteins.pdf

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Module-assisted one-pot synthesis of [18F]SFB for radiolabeling proteins

Module-assisted one-pot synthesis of [18F]SFB for radiolabeling proteins Ming-Wei Wang ? Yong-Ping Zhang ? Ying-Jian Zhang ? Clifton Kwang-Fu Shen Received: 10 March 2011 / Accepted: 17 March 2011 / Published online: 30 March 2011 Akade?miai Kiado?, Budapest, Hungary 2011 Abstract The need of reliable production of N-succinim- idyl 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-(trime- thylammonium)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-cor- rected) 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% radio- chemical purity. Keywords [18F]SFB Radiosynthesis One-pot Module Protein 18F-labeling Introduction Biomolecules, such as antibodies, proteins, and their engi- neered derivatives are gaining important roles as molecular imaging probes [1]. They serve not only as therapeutics but also potential Positron Emission Tomography (PET) imaging probes once labeled with positron-emitters, e.g. 18F [2, 3]. The use of radiolabeled biomolecules to target receptor-(over)expressed tissues in vivo has opened up a new avenue for immunoPET as a potentially useful diag- nostic tool to visu