Buccino Pablo, Kreimerman Ingrid, Zirbesegger Kevin, Porcal Williams, Savio Eduardo, Engler Henry
Centro Uruguayo de Imagenología Molecular (CUDIM), Ricaldoni 2010, Montevideo 11600, Uruguay.
Centro Uruguayo de Imagenología Molecular (CUDIM), Ricaldoni 2010, Montevideo 11600, Uruguay; Departamento de Química Orgánica, Facultad de Química, Universidad de la República, Gral. Flores 2124, Montevideo 11800, Uruguay.
Appl Radiat Isot. 2016 Apr;110:47-52. doi: 10.1016/j.apradiso.2015.12.051. Epub 2015 Dec 24.
Two (11)C-labelled PET tracers, (R)-N-[(11)C]methyl-N-(3,3-dideuteropropargyl)-1-phenylpropan-2-amine ([(11)C]L-deprenyl-D2, [(11)C]DED) and (S)-N-[(11)C]methyl-N-propargyl-1-phenylpropan-2-amine ([(11)C]D-deprenyl, [(11)C]DDE) were synthesised. One step N-alkylation with [(11)C]MeI or [(11)C]MeOTf was performed using the automated platform TRACERlab® FX-C Pro. The labelled products were obtained with (37±15)% (n=10) (end of synthesis, decay corrected from [(11)C]MeI) radiochemical yields from [(11)C]MeI after 38±3min synthesis time. In all cases, radiochemical purity was over 99% when [(11)C]MeOTf was used. This synthesis using a commercial platform makes these tracers more accessible for clinical research purposes.
合成了两种碳-11标记的正电子发射断层扫描（PET）示踪剂，即（R）-N-[(11)C]甲基-N-（3,3-二氘代炔丙基）-1-苯基丙-2-胺（[(11)C]L-司来吉兰-D2，[(11)C]DED）和（S）-N-[(11)C]甲基-N-炔丙基-1-苯基丙-2-胺（[(11)C]D-司来吉兰，[(11)C]DDE）。使用TRACERlab® FX-C Pro自动化平台进行与[(11)C]MeI或[(11)C]MeOTf的一步N-烷基化反应。在38±3分钟的合成时间后，以[(11)C]MeI为原料，获得了放射性化学产率为（37±15）%（n = 10）（合成结束时，经[(11)C]MeI衰变校正）的标记产物。在所有情况下，当使用[(11)C]MeOTf时，放射性化学纯度超过99%。使用商业平台进行的这种合成使得这些示踪剂更便于用于临床研究目的。
