| 新型除草剂丙酯草醚A环14C均标记合成和鉴定 |
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| 引用本文： | 杨征敏,叶庆富,唐庆红,吕龙,陈子元.新型除草剂丙酯草醚A环14C均标记合成和鉴定[J].化学学报,2005,63(21):1999-2003. |
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| 作者姓名： | 杨征敏 叶庆富 唐庆红 吕龙 陈子元 |
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| 作者单位： | 杨征敏（西北农林科技大学生命科学学院,咸阳,712100;中国科学院上海有机化学研究所,上海,200032）
叶庆富（浙江大学原子核农业科学研究所,杭州,310029）
唐庆红（中国科学院上海有机化学研究所,上海,200032）
吕龙（中国科学院上海有机化学研究所,上海,200032）
陈子元（浙江大学原子核农业科学研究所,杭州,310029） |
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| 基金项目： | 973课题“绿色化学农药先导结构及作用靶标的发现与研究”（No.2003CB114406）资助项目. |
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| 摘 要： | 以U-14C-对氨基苯甲酸为前体, 通过酯化、缩合、还原和取代四步反应获得了A环14C均标记的丙酯草醚, 用PHPLC对其进行纯化. 采用HPLC-MS(ESI), MS(EI)和1H NMR验证了其结构, 通过HPLC(外标法)确定其化学纯度大于98%; HPLC-LSC和TLC-IIA两种方法分析表明, 其放射化学纯度大于98%, 其比活度为1.089±0.011 mCi/mmol. 合成的化学收率和放化收率均为53%.
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| 关 键 词： | 丙酯草醚(A-环-U-14C) 放射性标记合成 鉴定 除草剂 |
| 收稿时间： | 2005-05-20 |
| 修稿时间： | 2005-05-202005-07-18 |
Radiolabeled Synthesis and Identification of a Novel Herbicide, Propyl 4-[2-(4,6-Dimethoxy-2-pyrimidinyloxy)benzylamino]benzoate with All Six Benzoic Ring Carbons Labeled by 14C |
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| YANG,Zheng-Mina,c YE,Qing-Fub TANG,Qing-Hongc LU,Long,c CHEN,Zi-Yuanb.Radiolabeled Synthesis and Identification of a Novel Herbicide, Propyl 4-[2-(4,6-Dimethoxy-2-pyrimidinyloxy)benzylamino]benzoate with All Six Benzoic Ring Carbons Labeled by 14C[J].Acta Chimica Sinica,2005,63(21):1999-2003. |
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| Authors: | YANG Zheng-Mina c YE Qing-Fub TANG Qing-Hongc LU Long c CHEN Zi-Yuanb |
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| Institution: | ( College of Life Science, Northwest Science and Technology University of Agriculture and Forestry, Xianyang 712100)(Institute of Nuclear-Agricultural Science, Zhejiang University, Hangzhou 310029)(Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032) |
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| Abstract: | A radiochemical, propyl 4-2-(4,6-dimethoxy-2-pyrimidinyloxy)benzylamino]benzoate with all six benzoic ring carbons labeled by 14C was made from 4-aminobenzoic acid with all six benzoic ring carbons labeled by 14C through esterification, condensation, reduction and substitution, and purified by preparative HPLC. Its structure was identified by LC-MS and 1H NMR. HPLC test showed its chemical purity exceeded 98%. HPLC-LSC and TLC-IIA demonstrated that its radiochemical purity exceeded 98% and specific activity was 1.089±0.011 mCi/mmol. The total chemical yield and radiochemical yield were all 53%. |
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| Keywords: | propyl 4-[2-(4 6-dimethoxy-2-pyrimidinyloxy)benzylamino]benzoate with all six benzoic ring carbons labeled by 14C (A-ring-U-14C) radiolabelled synthesis identification herbicide |
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