Simple and Efficient Synthesis of -Succinimidyl-4-[F]fluorobenzoate ([F]SFB)-An Important Intermediate for the Introduction of Fluorine-18 into Complex Bioactive Compounds.

-succinimidyl-[F]fluorobenzoate ([F]SFB) is commonly prepared through a three-step procedure starting from [F]fluoride ion. A number of methods for the single-step radiosynthesis of [F]SFB have been introduced recently, including the radiofluorination of diaryliodonium salts and the Cu-mediated F-fluorination of pinacol aryl boronates and aryl tributyl stannanes, but they still have the drawbacks of lengthy product purification procedures. In the present work, two approaches for the direct labeling of [F]SFB from diaryliodonium (DAI) salt () and pinacol aryl boronate () are evaluated, with a major focus on developing a fast and simple SPE-based purification procedure.

One-Pot Radiosynthesis of [F]Anle138b-5-(3-Bromophenyl)-3-(6-[F]fluorobenzo[][1,3]dioxol-5-yl)-1-pyrazole-A Potential PET Radiotracer Targeting α-Synuclein Aggregates.

Availability of PET imaging radiotracers targeting α-synuclein aggregates is important for early diagnosis of Parkinson's disease and related α-synucleinopathies, as well as for the development of new therapeutics. Derived from a pyrazole backbone, C-labelled derivatives of anle138b (3-(1,3-benzodioxol-5-yl)-5-(3-bromophenyl)-1-pyrazole)-an inhibitor of α-synuclein and prion protein oligomerization-are currently in active development as the candidates for PET imaging α-syn aggregates. This work outlines the synthesis of a radiotracer based on the original structure of anle138b, labelled with fluorine-18 isotope, eminently suitable for PET imaging due to half-life and decay energy characteristics (97% β+ decay, 109.

Preliminary Assessment of the Anti-inflammatory Activity of New Structural Honokiol Analogs with a 4'--(2-Fluoroethyl) Moiety and the Potential of Their F-Labeled Derivatives for Neuroinflammation Imaging.

Neolignans honokiol and 4'--methylhonokiol (MH) and their derivatives have pronounced anti-inflammatory activity, as evidenced by numerous pharmacological studies. Literature data suggested that cyclooxygenase type 2 (COX-2) may be a target for these compounds in vitro and in vivo. Recent studies of [C]MPbP () biodistribution in LPS (lipopolysaccharide)-treated rats have confirmed the high potential of MH derivatives for imaging neuroinflammation.