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

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4467-9. doi: 10.1016/j.bmcl.2008.07.065. Epub 2008 Jul 20.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzamides / pharmacology*
  • Chemistry, Pharmaceutical / methods
  • Chlorine / chemistry
  • Dopamine D2 Receptor Antagonists
  • Drug Design
  • Mesylates / chemistry
  • Models, Chemical
  • Positron-Emission Tomography / instrumentation*
  • Positron-Emission Tomography / methods
  • Pyrrolidines / pharmacology*
  • Radiopharmaceuticals / pharmacology*
  • Receptors, Dopamine D2 / chemistry
  • Receptors, Dopamine D3 / antagonists & inhibitors
  • Receptors, Dopamine D3 / chemistry

Substances

  • Benzamides
  • Dopamine D2 Receptor Antagonists
  • Mesylates
  • N-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamide
  • Pyrrolidines
  • Radiopharmaceuticals
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3
  • Chlorine