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Citation: Pingan Wang, Lin Yao, Dongxu Zhang, Huifang Nie, Muqiong Li, Ru Jiang. Synthesis of 3-Substituted Isoindolin-1-ones by Solvent-Free Grinding Reaction[J]. University Chemistry, ;2021, 36(6): 200804. doi: 10.3866/PKU.DXHX202008040 shu

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

Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, The Air Force Medical University of PLA, Xi'an 710032, China

Corresponding author: Pingan Wang, ping_an1718@outlook.com
Received Date: 17 August 2020

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.
- 2-Cyanoarylaldehyde,
- Activated methylene compound,
- 3-Substituted isoindolin-1-one,
- Solvent-free,
- Grinding reaction
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