Radiosynthesis of carbon-11 labeled PDE5 inhibitors as new potential PET radiotracers for imaging of Alzheimer's disease

被引：10

作者：

Dong, Fugui ^{[1
]}

Du, Jie ^{[1
]}

Miao, Caihong ^{[1
]}

Jia, Limeng ^{[1
]}

Li, Wei ^{[1
]}

Wang, Min ^{[2
]}

Zheng, Qi-Huang ^{[2
]}

Xu, Zhidong ^{[1
,3
,4
]}

机构：

[1] Hebei Univ, Coll Chem & Environm Sci, Key Lab Med Chem & Mol Diag, Minist Educ, Baoding 071002, Hebei, Peoples R China

[2] Indiana Univ Sch Med, Dept Radiol & Imaging Sci, 1345 West,16th St,Room 202, Indianapolis, IN 46202 USA

[3] Hebei Univ Sci & Technol, Coll Chem & Pharmaceut Engn, Key Lab Mol Chem Med Hebei Prov, Shijiazhuang 050018, Hebei, Peoples R China

[4] Shijiazhuang Vince Pharmatech Co Ltd, Shijiazhuang 050030, Hebei, Peoples R China

来源：

APPLIED RADIATION AND ISOTOPES | 2019年 / 154卷

关键词：

Phosphodiesterase 5 (PDE5); Carbon-11 labeled PDE5 inhibitors; Radiosynthesis; Positron emission tomography (PET); Alzheimer's disease (AD); AGENTS;

D O I：

10.1016/j.apradiso.2019.108873

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

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-11]5) and ([C-11]12) were prepared from their corresponding precursors 6 and 13 with [C-11]CH3OTf through O-C-11-methylation and isolated by HPLC combined with SPE in 40-50% radiochemical yield, based on [C-11]CO2 and decay corrected to EOB. The radiochemical purity was > 99%, and the molar activity (A(m)) at EOB was in a range of 370-740 GBq/mol.

引用

页数：8

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