DMAP-Catalyzed One-Pot Synthesis of Quinazoline-2,4-diones from 2-Aminobenzamides and Di-tert-butyl Dicarbonate

被引：19

作者：

Chen, Hui ^{[3
]}

Li, Peng ^{[1
,2
]}

Qin, Rongfei ^{[1
,2
]}

Yan, Hong ^{[3
]}

Li, Gang ^{[1
,2
]}

Huang, Haihong ^{[1
,2
]}

机构：

[1] Peking Union Med Coll & Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Inst Mat Med, Beijing 100050, Peoples R China

[2] Peking Union Med Coll & Chinese Acad Med Sci, Chinese Acad Med Sci, Key Lab AntiDR TB Innovat Drug Res, Inst Mat Med, Beijing 100050, Peoples R China

[3] Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Beijing 100124, Peoples R China

来源：

ACS OMEGA | 2020年 / 5卷 / 16期

基金：

中国国家自然科学基金;

关键词：

ALDOSE REDUCTASE; DERIVATIVES; QUINAZOLINE-2,4(1H,3H)-DIONES; INHIBITORS; EFFICIENT; DESIGN; CO2; TRANSFORMATION; DISCOVERY; ARYLATION;

D O I：

10.1021/acsomega.0c01104

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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)(2)O acted as a key precursor in the construction of the 2-position carbonyl of quinazolinediones. The p-methoxybenzyl (PMB)-activated hetero- cyclization 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%.

引用

收藏

页码：9614 / 9623

页数：10

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