文章摘要
张首琪,曹阳.磷酸二苯酯催化的2-吲哚甲烷胺衍生物的合成[J].精细化工,2021,(8):0
磷酸二苯酯催化的2-吲哚甲烷胺衍生物的合成
Synthesis of 2-indolyl methanamine derivatives catalyzed by diphenyl phosphate
投稿时间:2021-01-22  修订日期:2021-03-12
DOI:
中文关键词: 3-甲基吲哚  亚胺  磷酸二苯酯  2-吲哚基甲烷胺  Friedel-Crafts 反应
英文关键词: 3-methylindole  imine  diphenyl phosphate  2-indolyl methanamine  Friedel-Crafts reaction
基金项目:江苏海洋大学人才引进科研基金项目
作者单位E-mail
张首琪 天津大学 药物科学与技术学院 2604596801@qq.com 
曹阳 江苏海洋大学 2020000088@jou.edu.cn 
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中文摘要:
      以磷酸二苯酯为催化剂,3-甲基吲哚类化合物与亚胺通过Friedel-Crafts加成反应一步合成了具有广泛药理活性的2-吲哚基甲烷胺类化合物,对反应条件进行优化。结果表明,当n(3-甲基吲哚类)∶n(亚胺)∶n(磷酸二苯酯)=1.0∶2.0∶0.1,其中,磷酸二苯酯0.0025 mmol,1 mL无水二氯甲烷作溶剂,室温下反应0.5 h时,即可得到高收率2-吲哚基甲烷胺类衍生物(85%~90%)。产物经 1HNMR、13CNMR 和 HRMS 进行了结构确定。
英文摘要:
      Friedel-Crafts reaction of 3-methylindoles and imines catalyzed by diphenyl phosphate can be used to synthesize 2-indolyl methanamines in one step, which has a wide range of pharmacological activities. The reaction conditions were optimized and the optimal reaction conditions were obtained as follows: n (3-methylindoles) ∶ n (imines) ∶ n(diphenyl phosphate) = 1.0 : 2.0∶0.1, the amount diphenyl phosphate is 0.0025 mmol, 1 mL anhydrous dichloromethane as solvent, room temperature, reaction time 0.5 h. 2-indolyl methanamine derivatives can be obtained in good yields (85~90%). The structures of the products were confirmed by 1HNMR, 13CNMR and HRMS.
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