Position: Home > Articles > Synthesis of 1-Methyl-3-(trifluoromethyl)-1H-pyrazole-4-carbonyl Chloride
Agrochemicals
2012,51
(8)
27-30
1-甲基-3-三氟甲基-1H-吡唑-4-甲酰氯的合成
作 者：
陈倩;廖道华;张曙光;牛纪凤;汤阿萍
单 位：
华东理工大学药学院
关键词：
1-甲基-3-三氟甲基-1H-吡唑-4-甲酰氯;吡噻菌胺;杀菌剂;合成
摘 要：
[目的]旨在优化合成1-甲基-3-三氟甲基-1H-吡唑-4-甲酰氯并寻找一条适用于工业化生产的工艺路线。[方法]以3-二甲胺基丙烯酸乙酯为原料,经三氟乙酰化、环合后生成1-甲基-3-三氟甲基-1H-吡唑-4-甲酸乙酯,再经过水解并酰氯化得到目标产物1-甲基-3-三氟甲基-1H-吡唑-4-甲酰氯。[结果]反应总收率为46.8%,1-甲基-3-三氟甲基-1H-吡唑-4-甲酸含量为96.1%(HPLC),所有中间体及产物经MS或1H NMR等进行表征。[结论]该路线操作简便、收率较高,适用于工业生产。
译 名：
Synthesis of 1-Methyl-3-(trifluoromethyl)-1H-pyrazole-4-carbonyl Chloride
作 者：
CHEN Qian,LIAO Dao-hua,ZHANG Shu-guang,NIU Ji-feng,TANG A-ping(Pharmacy School,East China University of Science and Technology,Shanghai 200237,China)
关键词：
1-methyl-3-(trifluoromethyl)-1H-pyrazole-4-carbonyl chloride;penthiopyrad;fungicide;synthesis
摘 要：
This article aims to optimize a reasonable route of 1-methyl-3-(trifluoromethyl)-1H-pyrazole-4-carbonyl chloride on industrial scale.[Methods] 1-methyl-3-(trifluoromethyl)-1H-pyrazole-4-carbonyl chloride was synthesized from ethyl 3-(dimethylamino)arylate via four steps including acylation,cyclization,hydrolysis,chlorination.[Results] The total yield was 46.8%,and the purity of 1-methyl-3-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid was 96.1%(HPLC).The products and intermediates were determined by 1H NMR or MS and so on.[Conclusions] The yield is improved and the operation process is simple,which is suitable for industrial production.
导出引用
计量
文章访问数: 13
HTML全文浏览量: 0
PDF下载量: 0
所属期刊
