一步法合成[F]氟-4-(乙烯砜基)苯：一种用于肽类选择性放射性氟代的巯基反应前体。
One-Step Synthesis of [F]Fluoro-4-(vinylsulfonyl)benzene: A Thiol Reactive Synthon for Selective Radiofluorination of Peptides.
机构信息
Department of Molecular and Medical Pharmacology and Crump Institute for Molecular Imaging, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, California 90095, United States.
Department of Chemistry and Biochemistry, University of California Los Angeles, Los Angeles, California 90095, United States.
出版信息
Org Lett. 2021 Jan 15;23(2):530-534. doi: 10.1021/acs.orglett.0c04054. Epub 2020 Dec 29.
Radiolabeled peptide-based molecular imaging probes exploit the advantages of large biologics and small molecules, providing both exquisite selectivity and favorable pharmacokinetic properties. Here, we report an operationally simple and broadly applicable approach for the F-fluorination of unprotected peptides via a new radiosynthon, [F]fluoro-4-(vinylsulfonyl)benzene. This reagent demonstrates excellent chemoselectivity at the cysteine residue and rapid F-labeling of a diverse scope of peptides to generate stable thioether constructs.
放射性核素标记的肽基分子成像探针利用了大分子生物和小分子的优势，兼具了极高的选择性和良好的药代动力学特性。在这里，我们报告了一种通过新的放射性合成子[F]氟-4-（乙烯砜基）苯实现未保护肽的 F-氟代的操作简单且广泛适用的方法。该试剂在半胱氨酸残基上表现出极好的化学选择性，并能快速标记各种肽，生成稳定的硫醚结构。
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