Synthesis optimization of 2-(4-N-[11C]methylaminophenyl)-6-hydroxybenzothiazole ([11C]PIB), β-amyloid PET imaging tracer for Alzheimer's disease diagnosis

Appl Radiat Isot. 2015 Nov:105:66-71. doi: 10.1016/j.apradiso.2015.07.003. Epub 2015 Jul 17.

Abstract

[11C]PIB is the most used amyloid plaques-specific positron-emitting radiotracers. The radiosynthesis of this compound, carried out by methylation of its precursor with [11C]methyl triflate in 2-butanone, has been improved optimizing the initial concentration and the purification method. Two HPLC methods were compared: good radiochemical yields, specific activities, and chemical purity above 98% were achieved by using as eluant acetonitrile/citrate and formulation in 10% ethanol.

Keywords: Alzheimer's disease; Cyclotron; [11C]MeOTf; [11C]PIB; β-amyloid.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / diagnosis
  • Alzheimer Disease / diagnostic imaging*
  • Alzheimer Disease / metabolism
  • Amyloid beta-Peptides / metabolism*
  • Aniline Compounds
  • Benzothiazoles / chemical synthesis*
  • Benzothiazoles / isolation & purification
  • Benzothiazoles / standards
  • Carbon Radioisotopes* / isolation & purification
  • Carbon Radioisotopes* / standards
  • Humans
  • Positron-Emission Tomography / methods*
  • Quality Control
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / isolation & purification
  • Radiopharmaceuticals / standards
  • Thiazoles

Substances

  • 2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole
  • Amyloid beta-Peptides
  • Aniline Compounds
  • Benzothiazoles
  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • Thiazoles