基于光气化反应的嘧菌酯合成研究  

Synthesis of Azoxystrobin Based on Phosgenation

作　　者：吴春辉 李炜 WU Chunhui;LI Wei(Jiangsu Kuaida Agrochemical Co.,Ltd.,Nantong226400,China;College of Biotechnology and Pharmaceutical Engineering,Nanjing Tech University,Nanjing211816,China)

机构地区：[1]江苏快达农化股份有限公司,南通226400 [2]南京工业大学生物与制药工程学院,南京211816

出　　处：《现代农药》2023年第1期41-44,共4页MODERN AGROCHEMICALS

摘　　要：为了研究嘧菌酯绿色经济的合成方法,以4-氯-6-甲氧基嘧啶与水杨酰胺作原料,经醚化反应、光气化反应得到关键中间体2-((6-氯嘧啶-4-基)氧基)苯甲腈,再与2-(2-羟基苯基)-3,3-二甲氧基丙酸甲酯经醚化、脱甲醇反应得到目标产物嘧菌酯。结果表明,新合成方法总收率达80.4%,嘧菌酯含量达98%,产物及中间体结构经核磁确证。与现有生产工艺相比,新方法克服了副产物4-氯-6-甲氧基嘧啶量大,操作复杂,收率低等缺陷,具有绿色环保、原料易得、收率高、成本低廉等优点,适合工业化生产。The green and economic synthesis method of azoxystrobin was developed by using the raw materials 4-chloro-6-methoxypyrimidine and 2-hydroxybenzamide.The key intermediate 2-((6-chloropyrimidin-4-yl)oxy)benzonitrile was obtained through etherification and phosgenation.The intermediate was etherified with methyl 2-(2-hydroxyphenyl)-3,3-dimethoxypropanoate and then demethanolized to obtain the target product azoxystrobin.The results showed that the total yield of the new synthesis method was 80.4%,the content of azoxystrobin was 98%,and the structure of the product and intermediates were confirmed by NMR.Compared with the existing production process,the new method overcame the defects of large amount of by-product 4-chloro-6-methoxypyrimidine,complex operation and low yield.The process,which was suitable for industrialized production,had the advantages of environmental protection,easy availability of raw materials,high yield and low cost.

关 键 词：嘧菌酯 水杨酰胺 光气 嘧啶 合成 

分 类 号：TQ450[化学工程—农药化工]