Synthesis method of trifluoro-imidazole amide

The invention relates to a synthesis method of trifluoro-imidazole amide, which comprises the following steps: step 1, microwave cyclization reaction: carrying out microwave cyclization reaction on 2-amino-3-chloro-5-trifluoromethylpyridine and halogenated pyruvic acid in the presence of a solvent A...

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Hauptverfasser: XU HUI, GUAN TONG, GE FENGMIN, LI XINSHENG, FENG XIAODONG, SUN JINGQUAN, LI LINHU
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to a synthesis method of trifluoro-imidazole amide, which comprises the following steps: step 1, microwave cyclization reaction: carrying out microwave cyclization reaction on 2-amino-3-chloro-5-trifluoromethylpyridine and halogenated pyruvic acid in the presence of a solvent A and acid to generate 8-chloro-6-(trifluoromethyl)-imidazole [1, 2a] pyridine-2-formic acid, and crystallizing the 8-chloro-6-(trifluoromethyl)-imidazole [1, 2a] pyridine-2-formic acid; and step 2, microwave condensation reaction: carrying out microwave condensation reaction on the 8-chloro-6-(trifluoromethyl)-imidazole [1, 2a] pyridine-2-formic acid and 2-chloro-5-methoxybenzenesulfonamide in a solvent B under the action of a catalyst to generate the trifluoro-imidazole amide. The method is mild in reaction condition, short in time consumption, free of dechlorination impurities, high in yield and good in purity. 本发明涉及一种三氟咪啶酰胺的合成方法,包括如下步骤:步骤1、微波环化反应:2-氨基-3-氯-5-三氟甲基吡啶与卤代丙酮酸在溶剂A和酸的存在下进行微波环化反应,生成8-氯-6-(三氟甲基)-咪唑[1,2a]吡