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Rapid access to multi-substituted pyrimido[4,5-b][1,4]diazepine-2,4,6-trione and pyrimido[4,5-b][1,4]diazepine-2,4-dione as novel and versatile scaffolds for drug discovery
Li, Gong1; Wang, Xiaowei1; Tian, Chao1; Zhang, Tongbo1; Zhang, Zhili1; Liu, Junyi1
关键词Pyrimidodiazepine Pyrimido[4 5-b][1 Pyrimido[4 4]Diazepine-2 5-b][1 4 41diazepine-2 6-trione 4-dione
刊名TETRAHEDRON LETTERS
2012-09-26
DOI10.1016/j.tetlet.2012.06.143
53期:39页:5193-5196
收录类别SCI ; IC ; CCR
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]INHIBITORS ; DERIVATIVES ; REDUCTION ; DESIGN ; POTENT
英文摘要

A novel pyrimido[4,5-b][1,4]diazepine-2,4,6-trione was synthesized with an efficient strategy. Especially, the key intermediate 2,4-dimethoxypyrimido[4,5-b][1,4]diazepin-6-one was promoted by one pot tandem reduction-cyclization with Na2S2O4. Subsequently, reduction of lactams 6 with LiAIH(4) afforded a more flexible scaffold of pyrimidodiazepines. The synthetic strategy was versatile since it facilitated the sequential functionalization on the pyrimidodiazepine at three positions. Thus a convenient and effective method for the rapid preparing of multi-substituted pyrimido[4,5-b][1,4]diazepines was developed. (c) 2012 Elsevier Ltd. All rights reserved.

语种英语
WOS记录号WOS:000308628900001
项目编号21042009 ; 2009ZX09301-010 ; 20972011 ; 21172014
资助机构National Science Foundation of China
引用统计
被引频次:4[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/53012
专题北京大学药学院_化学生物学系
作者单位1.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Li, Gong,Wang, Xiaowei,Tian, Chao,et al. Rapid access to multi-substituted pyrimido[4,5-b][1,4]diazepine-2,4,6-trione and pyrimido[4,5-b][1,4]diazepine-2,4-dione as novel and versatile scaffolds for drug discovery[J]. TETRAHEDRON LETTERS,2012,53(39):5193-5196.
APA Li, Gong,Wang, Xiaowei,Tian, Chao,Zhang, Tongbo,Zhang, Zhili,&Liu, Junyi.(2012).Rapid access to multi-substituted pyrimido[4,5-b][1,4]diazepine-2,4,6-trione and pyrimido[4,5-b][1,4]diazepine-2,4-dione as novel and versatile scaffolds for drug discovery.TETRAHEDRON LETTERS,53(39),5193-5196.
MLA Li, Gong,et al."Rapid access to multi-substituted pyrimido[4,5-b][1,4]diazepine-2,4,6-trione and pyrimido[4,5-b][1,4]diazepine-2,4-dione as novel and versatile scaffolds for drug discovery".TETRAHEDRON LETTERS 53.39(2012):5193-5196.
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