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6-取代苯并噻唑苯胺类化合物的合成 总被引:1,自引:0,他引:1
以2-氨基苯并噻唑类化合物为原料, 通过碱性条件下水解, 与苯甲酸类化合物在PPA(聚磷酸)条件下脱水环化, 部分化合物通过BBr3去甲基化反应, 合成了一系列潜在的针对β-淀粉样蛋白的正电子放射性探针分子前体或作为参比的6-取代苯并噻唑苯胺类化合物, 并用1H NMR, IR, EI/ESI-MS, HRMS, 元素分析等对其进行了表征. 同时测定比较了6种化合物与早老性痴呆(Alzheimer’s disease, AD)死者脑匀浆的亲和力强弱. 相似文献
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Gu-Cai Li Ru Zhang Li-Jun Li Kai-Jun Jiang 《Journal of Radioanalytical and Nuclear Chemistry》2013,295(1):385-391
A potential dopamine D4 receptor ligand, 1-(4-(4-(4-fluorobenzyl)-1-piperazinyl)butyl)indolin-2-one (4) was synthesized through a four-step process and its affinity and selectivity for dopamine D2-like receptors was determined through in vitro receptor binding assay. [18F]4 was prepared using a one-pot two-step method with total radiochemical yield 21.2 % (decay-corrected). The molar radioactivity was around 135 GBq/μmol and the radiochemical purity was greater than 95.5 %. The partition coefficient (Log P) of [18F]4 was determined to be 2.10 ± 0.30 through octanol experiment. The in vivo biodistribution and the competitive distribution of [18F]4 in rat exposed that the tracer passes through blood–brain-barrier (BBB) and may specifically bind to D4 receptor. Metabolite analysis revealed that there was no metabolism of [18F]4 in brain. Conclusively, these preliminary results demonstrated that [18F]4 shows promises as a radioligand for the in vivo study of dopamine D4 receptor. 相似文献
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