The reference standard IUR-1601 ((S)-N-(2-chloro-3-(trifluoromethyl)benzyl)-1-(2-fluoroethyl)-5-oxopyrrolidine-2-carboxamide) was synthesized from tert-butyl (S)-5-oxopyrrolidine-2-carboxylate, fluoroethylbromide, and 2-chloro-3-(trifluoromethyl)benzylamine with overall chemical yield 12% in three steps. The target tracer [¹⁸F]IUR-1601 ((S)-N-(2-chloro-3-(trifluoromethyl)benzyl)-1-(2-[¹⁸F]fluoroethyl)-5-oxopyrrolidine-2-carboxamide) was synthesized from desmethyl-GSK1482160 with 2-[¹⁸F]fluoroethyl tosylate, prepared from 1,2-ethylene glycol-bis-tosylate and K[¹⁸F]F/Kryptofix2.2.2, in two steps and isolated by HPLC combined with SPE in 1–3% decay corrected radiochemical yield. The radiochemical purity was >99%, and the molar activity at end of bombardment (EOB) was 74–370 GBq/μmol. The potency of IUR-1601 in comparison with GSK1482160 was determined by a radioligand competitive binding assay using [¹¹C]GSK1482160, and the binding affinity K_i values for IUR-1601 and GSK1482160 are 4.31 and 5.14 nM, respectively.

由叔丁基（S）合成参考标准IUR-1601（（S）-N-（2-氯-3-（三氟甲基）苄基）-1-（2-氟乙基）-5-氧吡咯烷-2-羧酰胺））-5-氧吡咯烷-2-羧酸盐，氟乙基溴化物和2-氯-3-（三氟甲基）苄胺的总化学收率在三个步骤中为12％。目标示踪物[ ¹⁸ F] IUR-1601（（S）-N-（2-氯-3-（三氟甲基）苄基）-1-（2- [ ¹⁸ F]氟乙基）-5-氧吡咯烷-2-羧酰胺）由去甲基-GSK1482160与2- [ ¹⁸ F]氟乙基甲苯磺酸酯合成，由1,2-乙二醇双甲苯磺酸酯和K [ ¹⁸ F] F / Kryptofix2.2.2，分两步进行，并通过HPLC与SPE结合以1-3％的衰减进行分离，从而校正了放射化学的收率。放射化学纯度> 99％，轰击结束时的摩尔活性（EOB）为74-370 GBq /μmol。通过使用[ ¹¹ C] GSK1482160的放射性配体竞争结合测定法确定了IUR-1601与GSK1482160的效力，并且IUR-1601和GSK1482160的结合亲和力K _i值分别为4.31和5.14 nM。