(2S,3S)-2-[(4-iodophenyl)-(2-ethoxyphenoxy)methyl]-N-tert-butoxycarbonylmorpholine | 1075221-99-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: (2S,3S)-2-[(4-iodophenyl)-(2-ethoxyphenoxy)methyl]-N-tert-butoxycarbonylmorpholine
• CAS: 1075221-99-6
• 化学式: C₂₄H₃₀INO₅
• 分子量: 539.41
• InChiKey: WQWFXENNLJKKBG-VXKWHMMOSA-N

反应信息

• 作为反应物：
  描述：

  (2S,3S)-2-[(4-iodophenyl)-(2-ethoxyphenoxy)methyl]-N-tert-butoxycarbonylmorpholine 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 以60%的产率得到(2S,3S)-Iodoreboxetine
  参考文献：
  名称：

  New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter

  摘要：

  A new route for the stereoselective synthesis of iodinated reboxetine analogues has been developed for the generation of SPECT imaging agents for the noradrenaline transporter (NAT). (2S,3S)- and (2R,3R)-iodoreboxetine were prepared and biological testing against various mono-amine transporters showed these compounds to be potent and selective for NAT. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.08.041
• 作为产物：
  描述：

  η⁶-(1-ethoxy-2-fluorobenzene)tricarbonylchromium 、 (2S,3S)-2-[α-hydroxy-4-(4-iodophenyl)methyl]-N-tert-butoxycarbonylmorpholine 在 sodium hydride 、 碘 作用下， 以 N,N-二甲基甲酰胺 、 四氢呋喃 为溶剂， 反应 5.5h， 以63%的产率得到(2S,3S)-2-[(4-iodophenyl)-(2-ethoxyphenoxy)methyl]-N-tert-butoxycarbonylmorpholine
  参考文献：
  名称：

  New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter

  摘要：

  A new route for the stereoselective synthesis of iodinated reboxetine analogues has been developed for the generation of SPECT imaging agents for the noradrenaline transporter (NAT). (2S,3S)- and (2R,3R)-iodoreboxetine were prepared and biological testing against various mono-amine transporters showed these compounds to be potent and selective for NAT. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.08.041