Suzuki交叉偶联法合成非甾体抗炎药二氟尼柳  

Synthesis of NSAID-diflunisal with Suzuki Cross-coupling Reaction

作　　者：刘世文[1] 张苗[1] 王腊生[1] 李伟[1] 郭孟萍[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：《化学世界》2015年第2期94-97,共4页Chemical World

基　　金：国家自然科学基金(NO:21063015)

摘　　要：以5-溴水杨酸和2,4-二氟苯硼酸为原料,1 mol%新型结构钯配合物[(NH2CH2COOH)2PdCl2]为催化剂,纯水为溶剂,碳酸钾为碱,经Suzuki交叉偶联反应在25℃反应6h可一步合成原料药二氟尼柳,分离产率高达90%,粗产品通过简单的重结晶处理后,纯度高达99.1%(HPLC)。反应中所使用的催化剂易于合成、结构简单、性质稳定,催化效率高。该Suzuki交叉偶联反应步骤少、操作简单、产品产率好、纯度高,具有工业应用前景。NSAID-diflunisal was synthesized from 5-bromosalicylic acid and 2,4-difluorophenylboronic acid with 1% [（NH2CH2COOH）2PdCl2]as catalyst and three equivalent of base（K2CO3）under air in water at room temperature for 6hthrough Suzuki cross-coupling reaction.The yield was 90% and the purity after recrystallization was 99.1%according to HPLC.The catalyst used in the reaction was simple,stable and easy to synthesize.High purity product can be obtained through this method with less reaction steps and easy process,showing great potential of industrial application.

关 键 词：钯催化剂 Suzuki交叉偶联 催化合成 二氟尼柳 

分 类 号：TQ245.4[化学工程—有机化工]