2-氟-5-甲酰基苯甲酸的合成及工艺优化  

Synthesis and Process Optimization of 2-Fluoro-5-formylbenzoic Acid

作　　者：徐康 薛登峰 李贝贝[1] 王立强[1] 邱飞[1] XU Kang;XUE Dengfeng;LI Beibei;WANG Liqiang;QIU Fei(Institutes of Molecular Medicine,School of Biomedical Science,Engineering Research Center of Molecular Medicine,Ministry of Education,Huaqiao University,Quanzhou,Fujian 362021,China)

机构地区：[1]华侨大学分子药物研究院生物医学学院,分子药物教育部工程研究中心,福建泉州362021

出　　处：《化学世界》2018年第8期507-510,共4页Chemical World

基　　金：福建省自然科学基金(No.2013J01338);华侨大学中青年教师科研提升资助计划(No.ZQN-PY219)资助项目

摘　　要：2-氟-5-甲酰基苯甲酸是合成奥拉帕尼等的关键中间体。以2-氟-5-甲酰基苯腈为原料,经乙二醇保护醛基、氰基水解、脱保护三步得到目标化合物2-氟-5-甲酰基苯甲酸,并对各步反应条件进行了优化,三步反应平均收率77.8%。目标化合物2-氟-5-甲酰基苯甲酸经1 H NMR和MS表证。2-Fluoro-5-formylbenzoic acid,an important intermediate of olperapib,was synthesized by using2-fluoro-5-formylbenzonitrile as starting material via reacting with ethylene glycol to protect the aldehyde group,followed by cyanide hydrolyzation and deprotection with an overall yield of 77.8%.The reaction conditions of all steps were optimized.The chemical structure of product was confirmed by 1 H NMR and MS.

关 键 词：2-氟-5-甲酰基苯甲酸 合成 正交设计 

分 类 号：O625.56[理学—有机化学]