劳拉替尼中间体5-氟-2-碘苯乙醇的合成研究  

Synthesis of Lauratinib Intermediate 5-fluoro-2-iodophenyl Ethanol

作　　者：尹小丹 郑莉 张峻华 杨维清 YIN Xiao-dan;ZHENG Li;ZHANG Jun-hua;YANG Wei-qing(School of Science,Xihua University,Sichuan Chengdu 610041,China)

机构地区：[1]西华大学理学院,四川成都610041

出　　处：《广州化工》2023年第8期53-55,共3页GuangZhou Chemical Industry

基　　金：教育部春晖计划(Z2016163);四川省创新训练项目(201710623074)。

摘　　要：5-氟-2-碘苯乙醇是一种重要合成中间体,同时也是抗癌药物劳拉替尼的关键中间体,目前其合成方法国内外鲜见报道。先以5-氟-2-氨基苯甲酸为原料经过重氮化反应、碘化和酰氯化反应得到5-氟-2-碘苯甲酰氯;该中间体再在碱性条件下发生取代反应后,进一步水解和硼氢化钠发生还原反应后得到目标化合物5-氟-2-碘苯乙醇。并对关键反应步骤反应条件进行条件筛选。该合成路线单步反应收率最高90%,四步反应总收率24%,具有一定应用价值。5-fluorine-2-iophenylethanol is an important synthesis intermediate,but also a key intermediate of anticancer drug Lauratinib.Its synthesis method is rarely reported at home and abroad.The synthesis of 5-fluoro-2-iodophenethyl alcohol,which was the key intermediate of lorlatinib,was studied.First,5-fluoro-2-iodobenzoyl chloride was obtained using raw material of 5-fluoro-2-aminobenzoic acid through diazotization reaction,iodination and acid chloride reaction.The target compound 5-fluoro-2-iodophenethyl alcohol was obtained after further hydrolysis and reduction reaction with sodium borohydride.The optimal reaction conditions were screened.The maximum single-step reaction yield was 90%,and the total 4-step reaction yield was 24%,which had a certain application value.

关 键 词：5-氟-2-碘苯乙醇 劳拉替尼中间体 5-氟-2-碘苯乙酮 合成 

分 类 号：R914[医药卫生—药物化学]