Automated synthesis of [18F]Florbetaben as Alzheimer's disease imaging agent based on a synthesis module system

Appl Radiat Isot. 2013 Jan;71(1):41-6. doi: 10.1016/j.apradiso.2012.09.014. Epub 2012 Sep 28.

Abstract

An automated synthesis procedure of [(18)F]Florbetaben ([(18)F]BAY94-9172), a radiolabeled imaging agent in phase III study for in vivo mapping of fibrillar amyloid β (Aβ) with PET, was developed using the commercial PET-MF-2V-IT-1 synthesizer. The automated radiosynthesis was carried out via a one-step nucleophilic fluorination of methanesulfonic acid 2-[2-(2-{4-[2-(4-methylamino-phenyl)-vinyl]-phenoxy}-ethoxy)-ethoxy]-ethyl ester, as a new precursor, and separation with semi-preparative high performance liquid chromatography (HPLC). The total synthesis time amounted to 50 min with 20-25% yield (uncorrected for decay) and radiochemical purities of more than 95% in all runs. The described automated radiosynthesis allows the production of [(18)F]Florbetaben using a commercial radiosynthesis module and enables clinical trials of this compound.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / diagnostic imaging*
  • Aniline Compounds / chemical synthesis*
  • Automation*
  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes / chemistry*
  • Humans
  • Quality Control
  • Radionuclide Imaging
  • Stilbenes / chemical synthesis*

Substances

  • Aniline Compounds
  • Fluorine Radioisotopes
  • Stilbenes
  • 4-(N-methylamino)-4'-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)stilbene