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.

Automated radiosynthesis and purification of [F]flumazenil with solid phase extraction.

This paper describes the novel approach for preparation of [F]flumazenil ([F]FMZ), well known radioligand for assessment of GABA receptors by PET. The optimized reaction conditions allowed us to implement commercially available SPE cartridges for [F]FMZ purification avoiding HPLC. All procedures were performed with TRACERlab FX N Pro synthesizer in 53 min.

Synthesis and biological evaluation of 2-(3,4-dimethoxyphenyl)-6-(2-[F]fluoroethoxy)benzothiazole ([F]FEDBT) for PET imaging of breast cancer.

Given the ever-present demand for improved PET radiotracer in oncology imaging, we have synthesized 2-(3,4-dimethoxyphenyl)-6-(2-[F]fluoroethoxy)benzothiazole ([F]FEDBT), a fluorine-18-containing fluoroethylated benzothiazole to explore its utility as a PET imaging tracer. [F]FEDBT was prepared via kryptofix-mediated nucleophilic substitution of the tosyl group precursor. Fractionated ethanol-based solid-phase (SPE cartridge-based) purification afforded [F]FEDBT in 60% radiochemical yield (EOB), with radiochemical purity in excess of 98% and the specific activity was 35GBq/μmol.