Fully automated synthesis and purification of 4-(2'-methoxyphenyl)-1-[2'-(N-2?-pyridinyl)-p-[18F]fluorobenzamido]ethylpiperazine

被引：3
|
作者：
Hayashi, Kazutaka [1 ,2 ]
Furutsuka, Kenji [2 ,3 ]
Ito, Takehito [2 ,3 ]
Muto, Masatoshi [4 ]
Aki, Hatsumi [5 ]
Fukumura, Toshimitsu [2 ]
Suzuki, Kazutoshi [2 ]
机构：
[1] RIKEN Ctr Mol Imaging Sci CMIS, Mol Imaging Integrat Unit, Chuo Ku, Hyogo 6500047, Japan
[2] Natl Inst Radiol Sci, Radiopharmaceut Prod Team, Mol Probe Grp, Mol Imaging Ctr,Inage Ku, Chiba 2638555, Japan
[3] SHI Accelerator Serv Co Ltd, Shinagawa Ku, Tokyo 1410032, Japan
[4] Tokyo Nucl Serv Co Ltd, Tokyo 1100016, Japan
[5] Fukuoka Univ, Fac Pharmaceut Sci, Dept Pharmaceut, Jonan Ku, Fukuoka 81480, Japan
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2012年 / 55卷 / 03期
关键词：
5-HT1A receptor; p-[18F]MPPF; 18F]fluoride; automated synthesis; preparative HPLC separation; RECEPTORS; RADIOLIGAND; MONKEY; PET;
D O I：
10.1002/jlcr.1958
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
We have developed an efficient synthesis method for the rapid and high-yield automated synthesis of 4-(2'-methoxyphenyl)-1-[2'-(N-2-pyridinyl)-p-[18F]fluorobenzamido]ethylpiperazine (p-[18F]MPPF). No-carrier-added [18F]F- was trapped on a small QMA cartridge and eluted with 70% MeCN(aq) (0.4mL) containing Kryptofix 222 (2.3mg) and K2CO3 (0.7mg). The nucleophilic [18F]fluorination was performed with 3mg of the nitro-precursor in DMSO (0.4mL) at 190 degrees C for 20min, followed by the preparative HPLC purification (column: COSMOSIL Cholester, Nacalai Tesque, Kyoto, Japan; mobile phase: MeCN/25mm AcONH4/AcOH=200/300/0.15; flow rate: 6.0mL/min) to afford p-[18F]MPPF (retention time=9.5min). p-[18F]MPPF was obtained automatically with a radiochemical yield of 38.6 +/- 5.0% (decay corrected, n=5), a specific activity of 214.3 +/- 21.1GBq/mu mol, and a radiochemical purity of >99% within a total synthesis time of about 55min. Copyright (C) 2012 John Wiley & Sons, Ltd.
引用
收藏
页码：120 / 124
页数：5
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