• Title/Summary/Keyword: Arylpiperazines

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Rapid Synthesis of Arylpiperazine Derivatives for Imaging 5-HT1A Receptor under Microwave Irradiation

  • Park, Sang-Hyun;Gwon, Hui-Jeong;Lee, Hyo-Sun;Park, Kyung-Bae
    • Bulletin of the Korean Chemical Society
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    • v.26 no.11
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    • pp.1701-1705
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    • 2005
  • We have established an efficient method for the synthesis of the arylpiperazine derivatives in which the acylation of 2-aminopyridine, the coupling reaction of the acyl compound with piperazines, and reduction of the arylpiperazines were performed under a microwave irradiation (300 W) to afford the corresponding target compounds in quantitative yields. In all cases, the reaction times were remarkably reduced when compared with those of the conventional method.

99mTc(CO)3-Labeled Histidine-Arylpiperazines as Potential Radiotracers for a Neuroreceptor Targeting

  • Choi, Kang-hyuk;Hong, Young-Don;Choi, Ok-Ja;Choi, Sun-Ju
    • Bulletin of the Korean Chemical Society
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    • v.27 no.8
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    • pp.1189-1193
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    • 2006
  • In order to develop radiopharmaceuticals for targeting a serotonin receptor such as $5-HT_{1A}$, histidine-$C_n$-arylpiperazines (AP) (C = alkyl, n = 2, 3, 4) were prepared in five steps with yields of 25%, 37% and 51%, respectively, and radiolabeled with the $[^{99m}Tc(CO)_3(H_2O)+3]^+$. The $^{99m}Tc(CO)_3$-Histidine-Cn-APs were prepared with a high yield (>99%) and characterized as a tridentate complex with a neutral charge to pass through the blood-brain barrier (BBB). The rhenium complexes with $Re(CO)_3$ were also synthesised and comparative experiments were achieved to evaluate the nature of the $^{99m}Tc$ complexes.