Improved synthesis of anti-[18F]FACBC: improved preparation of labeling precursor and automated radiosynthesis.

Academic Article

Abstract

  • The non-natural amino acid anti-1-amino-3-[18F]fluorocyclobutyl-1-carboxylic acid (FACBC) has shown promise for tumor imaging with positron emission tomography. An improved synthesis of the precursor of anti-[18F]FACBC has been devised which demonstrates high stereoselectivity and suitability for large-scale preparations. An automated radiosynthesis has been developed which provides anti-[18F]FACBC in 24% decay-corrected yield. Additionally, the major non-radioactive species present in doses of anti-[18F]FACBC has been identified as anti-1-amino-3-hydroxycyclobutane-1-carboxylic acid. Together, these results are important steps towards the routine production of anti-[18F]FACBC for human use.
  • Published In

    Keywords

  • Carboxylic Acids, Cyclobutanes, Humans, Isotope Labeling, Neoplasms, Quality Control, Radiopharmaceuticals, Tomography, Emission-Computed
  • Digital Object Identifier (doi)

    Pubmed Id

  • 22865137
  • Author List

  • McConathy J; Voll RJ; Yu W; Crowe RJ; Goodman MM
  • Start Page

  • 657
  • End Page

  • 666
  • Volume

  • 58
  • Issue

  • 6