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首页> 外文期刊>Journal of labelled compounds & radiopharmaceuticals. >Fully automated synthesis and purification of 4-(2'-methoxyphenyl)-1 -2'-(N-2'-pyridinyf)-p~(18)Ffluorobenza-midoethylpiperazine
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Fully automated synthesis and purification of 4-(2'-methoxyphenyl)-1 -2'-(N-2'-pyridinyf)-p~(18)Ffluorobenza-midoethylpiperazine

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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"-pyridinyI)-p-~(18)FfluorobenzamidoethyIpiperazine (p-~(18)FMPPF). No-carrier-added ~(18)FF~ was trapped on a small QMA cartridge and eluted with 70 MeCN(aq) (0.4 mL) containing Kryptofix 222 (2.3 mg) and K2CO3 (0.7 m§). The nucleophi-lic ~(18)Ffluorination was performed with 3mg of the nitro-preeyrsor in DMSO (0.4 mL) at 190 degC for 20 min, followed by the preparative HPLC pyrification (column: COSMOSIL Cholester, Naealai Tesque, Kyoto, Japan; mobile phase: MeCN/25mM AcQNH4/Ac0H = 200/300/0.15; flow rate: 6.0mL/min5 to afford p-~(18)FMPPF (retention time = 9.5 min). p-~(18)FMPPF was obtained automatically with a radioehemieal yield of 38.6 +- 5.0 (decay corrected, n = 5), a specific activity of 214.3 +- 21.1 GBq/p.mol, and a radioehemieal purity of >99 within a total synthesis time of about 55 min.

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