A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride.

Kim K, Miller NR, Sulikowski GA, Lindsley CW
Bioorg Med Chem Lett. 2008 18 (16): 4467-9

PMID: 18674906 · PMCID: PMC3177602 · DOI:10.1016/j.bmcl.2008.07.065

This Letter describes a new multi-gram synthetic protocol for the preparation of the classic tosylate labeling precursor for the D(2/3) PET agent [(18)F]fallypride. In the course of our studies, we also discovered two novel labeling precusors, the previously undescribed mesylate and chloro congeners of fallypride.

MeSH Terms (12)

Benzamides Chemistry, Pharmaceutical Chlorine Dopamine D2 Receptor Antagonists Drug Design Mesylates Models, Chemical Positron-Emission Tomography Pyrrolidines Radiopharmaceuticals Receptors, Dopamine D2 Receptors, Dopamine D3

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