氟丙嘧草酯的合成新工艺  

A Novel Process for Synthesis

作　　者：李爱军[1] 廖道华[1] 高倩[1] 郭栋[1] 陈立鹏[1] 

机构地区：[1]华东理工大学药学院,上海200237

出　　处：《合成化学》2015年第4期358-360,364,共4页Chinese Journal of Synthetic Chemistry

摘　　要：以2-氯-5-硝基苯甲酸甲酯为原料,经还原、缩合得2-氯-5-(乙氧羰基)氨基苯甲酸甲酯(3);3与3-氨基-4,4,4-三氟巴豆酸乙酯进行环合得脲嘧啶环中间体(4);4经甲基化、水解、酰化和缩合反应合成了氟丙嘧草酯,总收率55.2%,纯度99.1%。中间体和产物结构经1H NMR和EI-MS确证。Methyl 2-chloro-5-（ethoxycarbonylamino） benzoate（3） was obtained by reduction and condensation reaction using methyl 2-chloro-5-nitrobenzoate as the material.Butafenacil in total yield of 55.2% with 99.1% purity was synthesized by cyclization reaction of 3 with（Z）-ethyl 3-amino-4,4,4-trifluorobut-2-enoate,and then through methylation,hydrolysis,acylation and consideration.The structures of products and intermediates were confirmed by1 H NMR and EI-MS.

关 键 词：氟丙嘧草酯 2-氯-5-硝基苯甲酸甲酯 除草剂 药物合成 

分 类 号：O621.3[理学—有机化学] R914.5[理学—化学]