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

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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%.

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作者机构：

[ 1 ] [Li, Peng]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 ] [Qin, Rongfei]Peking Union Med Coll & Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Inst Mat Med, Beijing 100050, Peoples R China
[ 3 ] [Li, Gang]Peking Union Med Coll & Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Inst Mat Med, Beijing 100050, Peoples R China
[ 4 ] [Huang, Haihong]Peking Union Med Coll & Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Inst Mat Med, Beijing 100050, Peoples R China
[ 5 ] [Li, Peng]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
[ 6 ] [Qin, Rongfei]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
[ 7 ] [Li, Gang]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
[ 8 ] [Huang, Haihong]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
[ 9 ] [Chen, Hui]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Beijing 100124, Peoples R China
[ 10 ] [Yan, Hong]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Beijing 100124, Peoples R China

通讯作者信息：

李港
[Li, Gang]Peking Union Med Coll & Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Inst Mat Med, Beijing 100050, Peoples R China;;[Huang, Haihong]Peking Union Med Coll & Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Inst Mat Med, Beijing 100050, Peoples R China;;[Li, Gang]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;;[Huang, Haihong]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

电子邮件地址：

ligang@imm.ac.cn |
joyce@imm.ac.cn

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