摘要
以1-溴-3-氟-2-硝基苯为原料,经甲胺取代,锌粉还原,甲酸环化3步反应合成4-溴-1-甲基-1H-苯并咪唑,再与频哪醇硼酸酯在双(三环己基膦)二氯化钯催化下进行硼酸化,制得未见文献报道的目标化合物1-甲基-1H-苯并咪唑-4-硼酸,4步反应总收率27.4%。产品经MS和1H NMR确证。该合成工艺具有反应条件温和、操作简单的优点。
As an important intermediate for pharmaceuticals, the titled compound, which has never been reported in literatures, was prepared by bis （tricyclohexylphosphine） palladium （Ⅱ） dichloride catalyzed reaction of bis （pinacolato） di-boron with 4-bromo-l-methyl-1H-benzo [d] imidazole. The later compound was synthesized from 1-bromo-3-fluoro-2-nitrobenzene via substitution with methylamine, reduction with zinc, eyclization with formic acid. The structure of the target product was characterized by MS and 1H NMR spectra. This route has advantages of mild reaction conditions and simple procedures.
出处
《精细化工中间体》
CAS
2014年第6期26-28,共3页
Fine Chemical Intermediates
基金
国家自然科学基金青年科学基金(81202398)
中科院上海药物研究所新药研究国家重点实验室开放研究课题(SIMM1106KF-12)
广州市科技攻关项目(201300000147)
广东省科技计划项目([2013]137168)
