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2-氨基甲基-3-氯-5-三氟甲基吡啶盐酸盐的合成

作  者:
陆阳;陶京朝;周志莲;张志荣
单  位:
郑州大学化学与分子工程学院;河南科易集团;信阳农林学院有机化学教研室;河南富邦农药化工公司
关键词:
2,3-二氯-5-三氟甲基吡啶;水解;脱羧
摘  要:
旨在寻找一条适用于工业化生产的合成2-氨基甲基-3-氯-5-三氟甲基吡啶盐酸盐的新路线。以2,3-二氯-5-三氟甲基吡啶为起始原料,经过亲核取代反应,得到反应物;再与10%HCl水溶液经过亚胺水解、脱羧"一锅法"反应制得目标化合物2-氨基甲基-3-氯-5-三氟甲基吡啶盐酸盐。反应总收率为79.4%,纯度为99.6%,所有中间体及产物经IR和1H NMR进行表征。该合成技术收率较高,经济合理,操作简单,为工业化生产奠定了基础。
译  名:
Synthesis of 2-Aminomethyl-3-Chloro-5-(Trifluoromethyl) Pyridine Hydrochloride
作  者:
Lu Yang;Tao Jingzhao;Zhou Zhilian;Zhang Zhirong;Office of Organic chemistry,Xinyang Agriculture College;Chemistry Department of ZhengZhou University;New Drug Research and Development Center Henan KeYi Group;Henan FuBang Pesticides Chemical Engineering Company;
关键词:
2,3-dichloro-5-trifluoromethyl-pyridine;;hydrolysis;;decarboxylic
摘  要:
This article aims to establish a new manufacturing process suitable for the industrial production of 2-aminomethyl-3-chloro-5-(trifluoromethyl) pyridine hydrochloride.(I) was synthesized through a nucleophilic substitution reaction using 2,3-dichloro-5-trifluoromethylpyridine as raw material. Then(I) and 10% Hydrochloric solution went through "one-pot" reaction of hydrolysis of imine and decarboxylic to produce target compound of 2-aminomethyl-3-chloro-5-(trifluoromethyl) pyridine hydrochloride. The total yield was 79. 4% and the purity of product was 99. 6%. The structure of the final product and all the intermediates were confirmed by IR and 1 H NMR. This synthetic technology has advantages of high yield, reasonable cost and simple operation, which laid the foundation for industrial production.

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