Automated, Transferable, and Ethanol-Free Radiosynthesis of [11C]Butanol

ACS Chem Neurosci. 2024 Oct 2;15(19):3535-3542. doi: 10.1021/acschemneuro.4c00455. Epub 2024 Sep 13.

Abstract

Cerebral blood flow and blood-brain barrier permeability assessment are crucial hemodynamic parameters to measure under neurological conditions. In conjunction with positron emission tomography (PET), oxygen-15-labeled water has emerged as a gold standard for measuring cerebral perfusion; however, at higher flow rates, [15O]water extraction becomes nonlinear. In such a scenario, freely diffusible [11C]butanol can provide a truer estimate. Radiosyntheses of [11C]butanol reported to date are protracted, are not automated, or require ethanol in the final formulation. By using a flow-based, captive solvent approach on a commercially available radiosynthesizer, we automated and reduced the synthesis time to 28 min. Forgoing cartridge-based purification for an aqueous high-performance liquid chromatography method, we obtained high purity [11C]butanol in ethanol-free phosphate buffered saline in sufficient yields for clinical PET studies. We here report our expedited, automated, and ethanol-free radiosynthesis of [11C]butanol along with preliminary imaging of a porcine subject.

Keywords: PET; [11C]butanol; automated radiosynthesize; blood–brain barrier; cerebral blood flow.

MeSH terms

  • Animals
  • Brain / diagnostic imaging
  • Butanols* / chemical synthesis
  • Butanols* / chemistry
  • Carbon Radioisotopes*
  • Ethanol / chemistry
  • Positron-Emission Tomography* / methods
  • Radiopharmaceuticals* / chemical synthesis
  • Swine

Substances

  • Carbon Radioisotopes
  • Butanols
  • Radiopharmaceuticals
  • Ethanol
  • Carbon-11