碳-11标记的磷酸二酯酶5抑制剂的放射性合成作为用于阿尔茨海默病成像的新型潜在正电子发射断层显像（PET）放射性示踪剂
Radiosynthesis of carbon-11 labeled PDE5 inhibitors as new potential PET radiotracers for imaging of Alzheimer's disease.
作者信息
Dong Fugui, Du Jie, Miao Caihong, Jia Limeng, Li Wei, Wang Min, Zheng Qi-Huang, Xu Zhidong
机构信息
Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, College of Chemistry and Environmental Science, Hebei University, Baoding, Hebei, 071002, China.
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th, Street, Room 202, Indianapolis, IN, 46202, USA.
出版信息
Appl Radiat Isot. 2019 Dec;154:108873. doi: 10.1016/j.apradiso.2019.108873. Epub 2019 Aug 22.
To develop PET tracers for imaging of Alzheimer's disease, new carbon-11 labeled potent and selective PDE5 inhibitors have been synthesized. The reference standards (5) and (12), and their corresponding desmethylated precursors (6) and (13) were synthesized from methyl 2-amino-5-bromobenzoate and (4-methoxyphenyl)methanamine in multiple steps with 2%, 1%, 1% and 0.2% overall chemical yield, respectively. The radiotracers ([C]5) and ([C]12) were prepared from their corresponding precursors 6 and 13 with [C]CHOTf through O-C-methylation and isolated by HPLC combined with SPE in 40-50% radiochemical yield, based on [C]CO and decay corrected to EOB. The radiochemical purity was >99%, and the molar activity (A) at EOB was in a range of 370-740 GBq/μmol.
为了开发用于阿尔茨海默病成像的正电子发射断层显像（PET）示踪剂，已经合成了新型的碳-11标记的强效且选择性的磷酸二酯酶5（PDE5）抑制剂。参考标准品（5）和（12）以及它们相应的去甲基化前体（6）和（13）由2-氨基-5-溴苯甲酸甲酯和（4-甲氧基苯基）甲胺经多步合成，总化学产率分别为2%、1%、1%和0.2%。放射性示踪剂（[C]5）和（[C]12）由它们相应的前体6和13通过[C]CHOTf经O-C-甲基化制备，并通过高效液相色谱（HPLC）结合固相萃取（SPE）分离，基于[C]CO并校正至给药结束时（EOB）的放射性化学产率为40%-50%。放射性化学纯度>99%，给药结束时的摩尔活度（A）在370-740 GBq/μmol范围内。
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