利用无溶剂研磨反应制备3-取代异吲哚啉-1-酮类化合物  

Synthesis of 3-Substituted Isoindolin-1-ones by Solvent-Free Grinding Reaction

作　　者：王平安 姚琳 张东旭 聂慧芳 李穆琼 姜茹 Pingan Wang;Lin Yao;Dongxu Zhang;Huifang Nie;Muqiong Li;Ru Jiang(Department of Medicinal Chemistry and Pharmaceutical Analysis,School of Pharmacy,The Air Force Medical University of PLA,Xi’an 710032,China.)

机构地区：[1]空军军医大学药学系,药物化学与药物分析学教研室,西安710032

出　　处：《大学化学》2021年第6期160-167,共8页University Chemistry

基　　金：国家自然科学基金(21372259)。

摘　　要：以2-氰基芳醛和活泼亚甲基化合物(如丙二酸二甲酯、乙酰乙酸乙酯等)为原料,在无水碳酸钾催化下,通过无溶剂室温研磨反应,一步得到3-取代异吲哚啉-1-酮类化合物,产物无需柱层析。产物的结构通过核磁共振波谱和质谱解析确定。该反应具有操作步骤简单、反应时间短、适用范围广、产率高、高原子经济性等优点,是绿色有机合成反应,在新药设计与合成、天然产物合成中具有应用价值。A solvent-free grinding reaction for the synthesis of 3-substituted isoindolin-1-ones from 2-cyanoarylaldehydes and various activated methylene compounds(such as dimethyl malonate and ethyl acetoacetate)has been developed.All the products were obtained without the tedious column chromatographic purification and were characterized using NMR spectroscopy and mass spectrometry.This method is advantageous because of its simple manipulation,short reaction time,wide substrate scope,high product yield,and high atom economy.It also has potential uses in novel-drug designing and natural product synthesis.

关 键 词：2-氰基芳醛 活泼亚甲基化合物 3-取代异吲哚啉-1-酮 无溶剂 研磨反应 

分 类 号：G64[文化科学—高等教育学] O6[文化科学—教育学]