农药学学报2017，Vol.19Issue(6)：672-678,7.DOI:10.16801/j.issn.1008-7303.2017.0092
高比活度碳-14标记毒氟磷的合成与分析
Synthesis and analysis of carbon-14 labelled Dufulin with high specific activity
摘要
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.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Key words
isotopically labelled synthesis/Dufulin/carbon-14/radiotracer/plant antiviral agent分类
化学化工引用本文复制引用
许亚军,张贵华,杨征敏,周兵,徐鹏飞,陈沪飞,叶庆富..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):672-678,7.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). （201609-FX-A2008-002）
