Chen Hui, Li Peng, Qin Rongfei, Yan Hong, Li Gang, Huang Haihong
Beijing Key Laboratory of Environmental and Viral Oncology, College of Life Science and Bio-engineering, Beijing University of Technology, Beijing 100124, P. R. China.
Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation & Chinese Academy of Medical Sciences Key Laboratory of Anti-DR TB Innovative Drug Research, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, P. R. China.
ACS Omega. 2020 Apr 16;5(16):9614-9623. doi: 10.1021/acsomega.0c01104. eCollection 2020 Apr 28.
The one-pot synthesis of quinazoline-2,4-diones was developed in the presence of 4-dimethylaminopyridine (DMAP) by metal-free catalysis. The commercially available (Boc)O acted as a key precursor in the construction of the 2-position carbonyl of quinazolinediones. The -methoxybenzyl (PMB)-activated heterocyclization could smoothly proceed at room temperature instead of the microwave condition. This strategy is compatible with a variety of substrates with different functional groups. Furthermore, this protocol was utilized to smoothly prepare Zenarestat with a total yield of 70%.
在4-二甲氨基吡啶（DMAP）存在下，通过无金属催化开发了喹唑啉-2,4-二酮的一锅法合成。市售的（Boc）O作为构建喹唑啉二酮2-位羰基的关键前体。对甲氧基苄基（PMB）活化的杂环化反应可以在室温下顺利进行，而无需微波条件。该策略与具有不同官能团的多种底物兼容。此外，该方案被用于顺利制备泽那司他，总收率为70%。
Zotero 插件
