Radiosynthesis of a carbon-11 labeled tetrahydrobenzisoxazole derivative as a new PET probe for γ-secretase imaging in Alzheimer's disease.
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2019
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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 [C]8 was prepared from its corresponding precursor 9 with [C]CHOTf through O-C-methylation and isolated by RP-HPLC combined with SPE in 45-50% radiochemical yield, based on [C]CO and decay corrected to EOB. The radiochemical purity was >99%, and the molar activity (A) at EOB was 555-740 GBq/μmol.| Reference Key |
xu2019radiosynthesisapplied
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| Authors | Xu, Zhidong;Miao, Caihong;Dong, Fugui;Jia, Limeng;Li, Wei;Wang, Min;Liu, Wenqing;Zheng, Qi-Huang; |
| Journal | Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine |
| Year | 2019 |
| DOI | S0969-8043(19)30821-8 |
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