Robertson Thomas B R, Antonides Lysbeth H, Gilbert Nicolas, Benjamin Sophie L, Langley Stuart K, Munro Lindsey J, Sutcliffe Oliver B, Mewis Ryan E
Department of Natural Sciences Manchester Metropolitan University John Dalton Building, Chester St. Manchester, M1 5GD UK.
Leverhulme Research Centre for Forensic Science University of Dundee Dundee DD1 5EH UK.
ChemistryOpen. 2019 Nov 8;8(12):1375-1382. doi: 10.1002/open.201900273. eCollection 2019 Dec.
Fentanyl, also known as 'jackpot', is a synthetic opiate that is 50-100 times more potent than morphine. Clandestine laboratories produce analogues of fentanyl, known as fentalogues to circumvent legislation regarding its production. Three pyridyl fentalogues were synthesized and then hyperpolarized by signal amplification by reversible exchange (SABRE) to appraise the forensic potential of the technique. A maximum enhancement of -168-fold at 1.4 T was recorded for the pyridyl H nuclei. Studies of the activation parameters for the three fentalogues revealed that the ratio of ligand loss to hydride and hydride loss in the complex [Ir(IMes)(L)(H)] (IMes=1,3-(2,4,6-trimethylphenyl)imidazole-2-ylidene) ranged from 0.52 to 1.83. The fentalogue possessing the ratio closest to unity produced the largest enhancement subsequent to performing SABRE at earth's magnetic field. It was possible to hyperpolarize a pyridyl fentalogue selectively from a matrix that consisted largely of heroin (97 : 3 heroin:fentalogue) to validate the use of SABRE as a forensic tool.
芬太尼，也被称为“大奖”，是一种合成阿片类药物，其效力比吗啡强50至100倍。秘密实验室生产芬太尼的类似物，即所谓的芬太尼类似物，以规避有关其生产的法规。合成了三种吡啶基芬太尼类似物，然后通过可逆交换信号放大（SABRE）进行超极化，以评估该技术的法医潜力。在1.4 T时，吡啶基H核的最大增强倍数为-168倍。对这三种芬太尼类似物的活化参数研究表明，在配合物[Ir(IMes)(L)(H)]（IMes = 1,3-(2,4,6-三甲基苯基)咪唑-2-亚基）中，配体损失与氢化物和氢化物损失的比率在0.52至1.83之间。在地球磁场中进行SABRE后，比率最接近1的芬太尼类似物产生了最大的增强。从主要由海洛因组成的基质（海洛因：芬太尼类似物为97:3）中选择性地超极化一种吡啶基芬太尼类似物是可能的，以验证SABRE作为法医工具的用途。
