河北师范大学学报—

以4-氯N-甲基-2-吡啶甲酰胺和对氨基苯酚为原料，经亲核取代反应一步合成索拉非尼关键中间体4-（4-氨基苯氧基）N-甲基-2-吡啶甲酰胺，考察了溶剂、温度、碱和催化剂对反应收率的影响.以N，N-二甲基甲酰胺（DMF）为溶剂，叔丁醇钾为碱，碘化钾作催化剂，120℃时反应收率为90.5%.目标产物经IR，¹HNMR，MS得到确证.

Abstract：

The key intermediate of Sorafeni 4-(4-aminophenoxy)-N-methylpicolinamide was synthesized by nucleophilic substitution using 4-chloro-N-methylpicolinamide and 4-aminophenol as raw materials. The effect of solvent, temperature, base and catalyst were studied. At 120℃, DMF as solvent, and potassium tert-butanolate as base, 4-(4-aminophenoxy)-N-methylpicolinamide was get catalysted by potassium iodide with a 90.5% yield. The structure of target compound was characterized by IR, ¹HNMR, and MS.

关键词

关键词： 4-（4-氨基苯氧基）N-甲基-2-吡啶甲酰胺 ; 索拉非尼 ; 合成

Key words： 4-(4-aminophenoxy)-N-methylpicolinamide ; Sorafeni ; synthesis

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