Radiosynthesis of a carbon-11 labeled tetrahydrobenzisoxazole derivative as a new PET probe for γ-secretase imaging in Alzheimer's disease

Zhidong Xu, Caihong Miao, Fugui Dong, Limeng Jia, Wei Li, Min Wang, Wenqing Liu, Qi Huang Zheng

Research output: Contribution to journalArticlepeer-review

Abstract

To develop PET radiotracers for imaging of Alzheimer's disease, a new carbon-11 labeled potent and selective γ-secretase modulator (GSM) has been synthesized. The reference standard tetrahydrobenzisoxazole derivative 8 and its desmethylated precursor 9 were synthesized from cyclohex-2-en-1-one and 3-hydroxy-4-nitrobenzaldehyde in eight and nine steps with 11% and 5% overall chemical yield, respectively. The radiotracer [11C]8 was prepared from its corresponding precursor 9 with [11C]CH3OTf through O–11C-methylation and isolated by RP-HPLC combined with SPE in 45–50% radiochemical yield, based on [11C]CO2 and decay corrected to EOB. The radiochemical purity was >99%, and the molar activity (Am) at EOB was 555–740 GBq/μmol.

Original languageEnglish (US)
Article number108915
JournalApplied Radiation and Isotopes
Volume155
DOIs
StatePublished - Jan 2020

Keywords

  • Alzheimer's disease (AD)
  • Carbon-11 labeled γ-secretase modulator (GSM)
  • Positron emission tomography (PET)
  • Radiosynthesis
  • γ-Secretase

ASJC Scopus subject areas

  • Radiation

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