| 高比活度碳-14标记毒氟磷的合成与分析 |
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投稿时间：2017-10-17
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| 引用本文：许亚军,张贵华,杨征敏,等.高比活度碳-14标记毒氟磷的合成与分析[J].农药学学报,2017,19(6):672-678. |
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| 基金项目:上海张江国家自主创新示范区专项发展资金重点项目（201609-FX-A2008-002） |
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| 中文摘要:以[14C]碳酸钡为放射性同位素原料，通过格氏反应、Curtius重排、亲核加成、硫代及关环等7步反应，制备了同位素碳-14标记的毒氟磷粗品，经反相高效液相色谱（RP-HPLC）纯化获得标记物纯品14C-毒氟磷（N-[2-（4-甲基苯并[2-14C]噻唑基）]-2-氨基-2-氟代苯基-O，O-二乙基甲基膦酸酯，38.3 mCi）。7步反应的化学收率/放化收率为10%。其结构经核磁共振氢谱、质谱和放射性高效液相色谱（HPLC-FSA）分析确认。放射性薄层成像分析（TLC-IIA）、高效液相色谱-液体闪烁测量联用分析（HPLC-LSC）、高效液相色谱-流动液体闪烁测量/二极管阵列检测器/质谱联用分析（HPLC-FSA/PDA/MS）和LSC分析表明，14C-毒氟磷的放化纯度和化学纯度均大于98%，比活度为58.0 mCi/mmol，可作为放射性示踪剂，用于毒氟磷的代谢和环境行为等研究。 |
| 中文关键词:同位素标记合成 毒氟磷 碳-14 放射性示踪剂 植物抗病毒剂 |
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| Synthesis and analysis of carbon-14 labelled Dufulin with high specific activity |
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| Abstract:Carbon-14 labelled Dufulin, diethyl ((2-fluorophenyl)((4-methylbenzo[2-14C]thiazol-2-yl) amino)methyl)phosphonate was synthesized from barium [14C]carbonate via Grignard reaction, Curtius arrangement, nucleophilic addition, thionation reaction, cyclization reaction, etc. The labelled product (38.3 mCi) was obtained after RP-HPLC purification in the overall radiochemical/chemical yield of 10%. The product was characterized by ESI-MS, 1H NMR and HPLC-FSA. Its technical data (radiochemical purity > 98%, chemical purity > 98%, specific activity 58.0 mCi/mmol) was determined by TLC-IIA, HPLC-LSC, HPLC-FSA/PDA/MS and LSC. This carbon-14 labelled Dufulin can be used as radiotracer in the study on its metabolism and environmental behavior by employing radioisotope tracing techniques. |
| Key words:isotopically labelled synthesis Dufulin carbon-14 radiotracer plant antiviral agent |
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