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学科主题: 药学
题名:
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
作者: Li, Gong1; Wang, Xiaowei1; Tian, Chao1; Zhang, Tongbo1; Zhang, Zhili1; Liu, Junyi1
关键词: Pyrimidodiazepine ; Pyrimido[4,5-b][1,4]diazepine-2,4,6-trione ; Pyrimido[4,5-b][1,41diazepine-2,4-dione
刊名: TETRAHEDRON LETTERS
发表日期: 2012-09-26
DOI: 10.1016/j.tetlet.2012.06.143
卷: 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
所属项目编号: 21042009 ; 2009ZX09301-010 ; 20972011 ; 21172014
项目资助者: National Science Foundation of China
WOS记录号: WOS:000308628900001
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/53012
Appears in Collections:北京大学药学院_化学生物学系_期刊论文

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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

Recommended Citation:
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.
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