Published July 17, 2015 | Version v1
Journal article Open

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

  • 1. Vita-Salute S.RaffaeleUniversity,Milan,Italy
  • 2. CNR-IBFM c/oDepartmentofNuclearMedicine,OspedaleSanRaffaele,ViaOlgettina60,20132Milan,Italy
  • 3. Nuclear MedicineDepartment,IRCCSOspedaleSanRaffaele,Milan,Italy
  • 4. CNR-ISTM, Milan,Italy
  • 5. Vita-Salute S.RaffaeleUniversity,Milan,Italy and CNR-IBFM c/oDepartmentofNuclearMedicine,OspedaleSanRaffaele,ViaOlgettina60,20132Milan,Italy
  • 6. CNR-IBFM c/oDepartmentofNuclearMedicine,OspedaleSanRaffaele,ViaOlgettina60,20132Milan,Italy and Nuclear MedicineDepartment,IRCCSOspedaleSanRaffaele,Milan,Italy

Description

[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.

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Funding

INMIND – Imaging of Neuroinflammation in Neurodegenerative Diseases 278850
European Commission