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

Appl Radiat Isot. 2003 Jun;58(6):657-66. doi: 10.1016/s0969-8043(03)00029-0.


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.

MeSH terms

  • Carboxylic Acids / chemical synthesis*
  • Carboxylic Acids / chemistry
  • Carboxylic Acids / isolation & purification*
  • Cyclobutanes / chemical synthesis*
  • Cyclobutanes / chemistry
  • Cyclobutanes / isolation & purification*
  • Humans
  • Isotope Labeling / methods*
  • Neoplasms / diagnostic imaging
  • Neoplasms / metabolism
  • Quality Control
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / isolation & purification
  • Tomography, Emission-Computed / methods


  • Carboxylic Acids
  • Cyclobutanes
  • Radiopharmaceuticals
  • fluciclovine F-18