Position: Home > Articles > Synthesis of isopropyl 4-(2-chloro-6-(1H-1,2,4-triazol-1-yl)benzamido)benzoate
Agrochemicals
2022
(2)
91-95
4-(2-氯-6-(1H-1,2,4-三唑-1-基)苯甲酰胺基)苯甲酸异丙酯的合成
作 者：
孙连省;张芷嘉;蒋振华;闫景铭;允圆圆;王夏菲;孟颢光;程绎南;李洪连
单 位：
河南农业大学植物保护学院
关键词：
4-(2-氯-6-(1H-1,2,4-三唑-1-基)苯甲酰胺基)苯甲酸异丙酯;小麦全蚀病;合成路线;结构表征
摘 要：
[目的]开发具有全新结构的小麦全蚀病抑制剂4-(2-氯-6-(1H-1,2,4-三唑-1-基)苯甲酰胺基)苯甲酸异丙酯的合成路线。[方法]以2-氟-6-氯苯甲酸为原料,通过羧酸的酰胺化以及1,2,4-三唑的选择性取代等过程,更高效地合成4-(2-氯-6-(1H-1,2,4-三唑-1-基)苯甲酰胺基)苯甲酸异丙酯;以4-硝基苯甲酸为原料,通过酯化和还原,合成中间体4-氨基苯甲酸异丙酯。各中间体及产品通过1H NMR、13C NMR、元素分析等手段进行了结构表征和确证。[结果]所开发合成路线具有合成步骤少、中间体及产品分离容易,目标化合物的合成收率达到了62%,含量达到了98%。[结论]该合成路线为4-(2-氯-6-(1H-1,2,4-三唑-1-基)苯甲酰胺基)苯甲酸异丙酯的生理生化实验、田间试验及环境实验等样品的获得提供了有力的技术支持。
译 名：
Synthesis of isopropyl 4-(2-chloro-6-(1H-1,2,4-triazol-1-yl)benzamido)benzoate
作 者：
SUN Lian-sheng;ZHANG Zhi-jia;JIANG Zhen-hua;YAN Jing-ming;YUN Yuan-yuan;WANG Xia-fei;MENG Hao-guang;CHENG Yi-nan;LI Hong-lian;College of Plant Protection, Henan Agricultural University;
关键词：
isopropyl 4-(2-chloro-6-(1H-1,2,4-triazol-1-yl)benzamido)benzoate;;Gaeumannomyces graminis var.tritici;;synthetic route;;structure characterization
摘 要：
[Aims] This study aims to explore a new synthetic route of isopropyl 4-(2-chloro-6-(1 H-1,2,4-triazol-1-yl)benzamido)benzoate as an active compound against Gaeumannomyces graminis var. tritici. [Methods] Using2-chloro-6-fluorobenzoic acid as the starting material, isopropyl 4-(2-chloro-6-(1 H-1,2,4-triazol-1-yl)benzamido)benzoate was synthesized smoothly via amidation of carboxylic acid and the C-F selective substitution with 1,2,4-triazole. An important intermediate isopropyl 4-aminobenzoate was also synthesized by esterification and reduction from4-nitrobenzoic acid. The structures of intermediates and product were characterized and confirmed by1 H NMR,13 C NMR and elemental analysis. [Results] The developed procedure had fewer synthetic steps. The intermediates and products could be isolated easily. The yield of the target compound was up to 62% and the purity was up to 98%.[Conclusions] The results provide a technical support for the physiological and biochemical experiments, field experiments and environmental experiments of isopropyl 4-(2-chloro-6-(1 H-1,2,4-triazol-1-yl) benzoate.
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4-(2-氯-6-(1 H-1,2,4-三唑-1-基)苯甲酰胺基)苯甲酸异丙酯的合成 [孙连省, 张芷嘉, 蒋振华, 闫景铭, 允圆圆, 王夏菲, 孟颢光, 程绎南, 李洪连] 农药 2022,61 (2) 91-95
