多巴胺转运体示踪剂[¹⁸F]FECNT的高效合成。
An efficient synthesis of dopamine transporter tracer [¹⁸F]FECNT.
作者信息
Murali D, Barnhart T E, Vandehey N T, Christian B T, Nickles R J, Converse A K, Larson J A, Holden J E, Schneider M L, Dejesus O T
机构信息
Department of Medical Physics, University of Wisconsin-Madison, Madison, 1111 Highland Ave, 1005 WIMR, Madison, WI 53705, United States.
出版信息
Appl Radiat Isot. 2013 Feb;72:128-32. doi: 10.1016/j.apradiso.2012.10.010. Epub 2012 Oct 23.
A simple synthesis of the dopamine transporter ligand [(18)F]FECNT with high radiochemical yield and short synthesis time, suitable for routine production is reported. Reaction of 2β-carbomethoxy-3β-(4-chlorophenyl)nortropane with [(18)F]2-fluoroethyl triflate ([(18)F]FEtOTf) at room temperature for 4 min provided [(18)F]FECNT in 84% decay corrected radiochemical yield. Since [(18)F]FEtOTf was prepared from [(18)F]2-fluoroethyl bromide that was isolated from its starting material, formation of unwanted side products and the amount of expensive precursor used could be greatly reduced. The overall radiochemical yields of [(18)F]FECNT were 40% (n=29) and the total synthesis time was ca. 100 min. The average specific activity of [(18)F]FECNT was 377.4 GBq/μmol (10.2 Ci/μmol).
报道了一种简单合成多巴胺转运体配体[(18)F]FECNT的方法，其放射化学产率高、合成时间短，适用于常规生产。2β-甲氧羰基-3β-(4-氯苯基)去甲托烷与[(18)F]2-氟乙基三氟甲磺酸酯([(18)F]FEtOTf)在室温下反应4分钟，得到[(18)F]FECNT，校正衰变后的放射化学产率为84%。由于[(18)F]FEtOTf是由从起始原料中分离出的[(18)F]2-氟乙基溴制备的，因此可以大大减少不需要的副产物的形成以及昂贵前体的使用量。[(18)F]FECNT的总放射化学产率为40%（n = 29），总合成时间约为100分钟。[(18)F]FECNT的平均比活度为377.4 GBq/μmol（10.2 Ci/μmol）。
Zotero 插件