铁催化三组分羰基化Suzuki反应合成非诺贝特

Synthesis of Fenofibrate Through Three-component Carbonylative Suzuki Reaction in the Presence of Iron Catalysts

改进了非诺贝特的合成工艺。以2-(4-碘苯氧基)-2-甲基丙酸异丙酯和4-氯苯硼酸为底物,安全环保的N-甲酰基糖精替代一氧化碳为羰基源,廉价的FeCl_(2)为催化剂,Na_(2)CO_(3)为碱,NaI为添加剂,绿色溶剂聚乙二醇(PEG-400)为溶剂,经过三组分羰基化Suzuki反应制得非诺贝特,收率86%,产物结构经1H NMR和13C NMR表征。改进后的工艺操作简便、安全、副产物少、收率高。为非诺贝特的合成提供了一条新途径。

The method for the synthesis of Fenofibrate was improved.The target product was synthesized from isopropyl 2-(4-iodophenoxy)-2-methylpropionate and 4-chlorophenylboronic by using safety and environmental N-formyl saccharin as carbonyl source instead of CO,low-cost FeCl_(2) as catalysts,Na_(2)CO_(3) as base,NaI as additive and green PEG-400 as solvent.The yield reached 86%and the product was characterized by NMR.This improved process realized safe production,simplified operation,reduced generation of waste and increased yield,which provided a new way to synthesis Fenofibrate.