摘要
5,6,7,8-四氢喹啉及衍生物是医药和农药的重要中间体。2-羟基-5,6,7,8-四氢-5,8-亚甲基喹啉-3-羧酸是合成HIF脯氨酰羟化酶抑制剂的重要中间体,其合成方法目前无文献报道。本文以降冰片烯为起始原料,经水合、氧化、缩合、环合和水解5步反应合成目标产物,总收率43.09%,结构经1H NMR、13C NMR和MS确证。该路线具有原料廉价易得、操作简单、后处理方便且收率较高等优点,适合工业化生产。
5,6,7,8-Tetrahydroquinoline and derivatives are important intermediates for medicines and pesticides.2-Hydroxy-5,6,7,8-tetrahydro-5,8-methylenequinoline-3-carboxylic acid is an important intermediate for the synthesis of HIF prolyl hydroxylase inhibitors,but its synthesis method is currently No literature reported.In this paper,the target product was synthesized by the five steps of hydration,oxidation,condensation,cyclization and hydrolysis with norbornene as the starting material.The total yield was 43.09%.The structure was confirmed by 1 H NMR,13 C NMR and MS.The route has the advantages of low cost and easy availability,simple operation,convenient post-treatment and high yield,and is suitable for industrial production.
作者
曹小江
周志旭
赵春深
李天祥
CAO Xiao-jiang;ZHOU Zhi-xu;ZHAO Chun-shen;LI Tian-xiang(College of Chemistry and Chemical Engineering,Guizhou University,Guiyang Guizhou 550025;School of Pharmaceutical Sciences,Guizhou University,Guiyang Guizhou 550025)
出处
《合成化学》
CAS
北大核心
2019年第11期913-916,共4页
Chinese Journal of Synthetic Chemistry
基金
贵州省科技厅社发公关项目(黔科合SY字[2014]3054号)
贵州省科技计划项目(黔科合[2017]1049和黔科合平台人才[2018]5781号)
