首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Synthesis of radiolabeled protein disulfide isomerase (PDI) inhibitors as new potential PET agents for imaging of the enzyme PDI in neurological disorders and cancer
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Synthesis of radiolabeled protein disulfide isomerase (PDI) inhibitors as new potential PET agents for imaging of the enzyme PDI in neurological disorders and cancer

机译:放射性标记的蛋白质二硫键异构酶(PDI)抑制剂的合成,作为在神经系统疾病和癌症中对PDI酶成像的新型潜在PET试剂

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Carbon-11-labeled substituted ??-tetrahydrocarbolines were prepared from their corresponding phenolic hydroxyl precursors with [11C]CH3OTf through O-[11C]methylation and isolated by simplified SPE in 50-60& decay corrected radiochemical yields at EOB with 185-370GBq/??mol specific activity at EOS. A fluorine-18-labeled substituted ??-tetrahydrocarboline was prepared from its corresponding halo-precursors (X=Cl, Br, I) with K[18F]F/Kryptofix 2.2.2 via the nucleophilic substitution and isolated by HPLC combined with SPE in 25-40& decay corrected radiochemical yield with 37-222GBq/??mol specific activity at EOB. ? 2013 Elsevier Ltd.
机译:用O [[11C]甲基化]由相应的酚羟基前体与[11C] CH3OTf制备碳-11标记的取代的ε-四烃基,并通过简化的SPE在50-60处经衰变校正的放射化学产率为185-370GBq /在EOS处的摩尔比活性。通过亲核取代反应,由其相应的卤素前体(X = Cl,Br,I)经K [18F] F / Kryptofix 2.2.2制备氟-18标记的取代的α-四氢咔啉,并通过HPLC与SPE结合进行分离在25-40℃和衰减校正的放射化学收率下,在EOB处的比活为37-222GBq /Δmol。 ? 2013爱思唯尔有限公司

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