Beilstein J. Org. Chem.2017,13, 2922–2927, doi:10.3762/bjoc.13.285
Psychiatric Institute, New York, NY, USA 10.3762/bjoc.13.285 Abstract Continuous-flow microfluidics has shown increased applications in radiochemistry over the last decade, particularly for both pre-clinical and clinical production of fluorine-18 labeled radiotracers. The main advantages of microfluidics are
receptor, [18F]FEMPT (pKi = 9. 79; Ki = 0.16 nM) by microfluidic radiochemistry. [18F]FEMPT was obtained in ≈7% isolated radiochemical yield and in >98% radiochemical and chemical purity. The molar activity of the final product was determined to be >148 GBq/µmol (>4 Ci/µmol).
Keywords: agonist; fluorine
longer half-life enables imaging protocols that can provide a better match of the pharmacokinetics of binding to the half-life of the radionuclide, as well as simplified radiochemistry protocols and the long-term goal of distribution for multicenter clinical trials.
Several reports on the use of
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Graphical Abstract
Figure 1:
Representative examples of recent 5-HT1AR agonists [3-9].
Beilstein J. Org. Chem.2013,9, 1002–1011, doi:10.3762/bjoc.9.115
of the analogous fluoroacetamide.
Keywords: fluorine-18; hydrolytic metabolism; prosthetic groups; radiochemistry; sulfonamides; Introduction
The importance of molecular imaging, i.e., the characterisation and measurement of biological processes in living organisms at the molecular level using
to be modified with fluorine. For this purpose, generic groups that allow both derivatisation with fluorine as well as convenient introduction of radiofluorine are often used. These groups are referred to as prosthetic groups in preparative radiochemistry. For labelling with fluorine-18, a variety of
multipolar contacts including hydrogen bonds [35], as observed herein. To our knowledge, all sulfonamides shown in Scheme 2 and Scheme 3 have not been described so far.
Radiochemistry
The sulfonate precursor molecules 3 and 4 were subjected to nucleophilic substitution with [18F]fluoride. The reaction
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Graphical Abstract
Figure 1:
Selection of prosthetic agents for 18F-labelling via acylation.