非甾体抗炎药联苯乙酸的环境友好催化合成  

Catalytic Synthesis of NSAID-felbinac

作　　者：郭孟萍[1] 刘世文[1] 周秀玲[1] 王腊生[1] 

机构地区：[1]宜春学院化学与生物工程学院配位催化研究所,江西宜春336000

出　　处：《化学试剂》2015年第1期82-84,共3页Chemical Reagents

基　　金：国家自然科学基金资助项目(21063015)

摘　　要：以苯硼酸和对溴苯乙酸为原料,0.5 mmol%(NH2CH2COOH)2Pd Cl2为催化剂,纯水为溶剂,碳酸钾为碱,经Suzuki交叉偶联反应在温和的反应条件下,2 h内可一步合成原料药联苯乙酸。反应中所使用的催化剂易于合成、结构简单、性质稳定,该合成反应高效经济、环境友好,通过简单的后处理就能获得纯度为99.1%(HPLC)的产物,分离产率高达93%。NSAID-felbinac can be synthesized from 4-bromophenylacetic acid and phenyl boronic acid with 0. 5 mmol% catalyst and three equivalent of base（ K2CO3） under air in water at room temperature in 2 h via Suzuki cross-coupling reaction. The separate yield is up to 93%. Besides the catalyst used in the reaction is simple,stable and easy to synthesize. The HPLC purity of99. 1% can be obtained through the method with an advantage of convenience,simplicity,shorter reaction time and friendly environment.

关 键 词：钯配合物催化剂 SUZUKI偶联 联苯乙酸 纯水相 

分 类 号：R914.5[医药卫生—药物化学]