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本文引用的文献

1
Facile, novel two-step syntheses of benzimidazoles, bis-benzimidazoles, and bis-benzimidazole-dihydroquinoxalines.简便、新颖的两步法合成苯并咪唑、双苯并咪唑和双苯并咪唑二氢喹喔啉。
Mol Divers. 2012 Feb;16(1):73-9. doi: 10.1007/s11030-011-9354-x. Epub 2012 Jan 12.
2
Imides: forgotten players in the Ugi reaction. One-pot multicomponent synthesis of quinazolinones.酰亚胺:Ugi 反应中被遗忘的角色。一锅多组分合成喹唑啉酮。
Chem Commun (Camb). 2011 Jun 28;47(24):6966-8. doi: 10.1039/c1cc12067k. Epub 2011 May 17.
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Concise Two-Step Solution Phase Syntheses of four novel Dihydroquinazoline scaffolds.四种新型二氢喹唑啉支架的简洁两步溶液相合成。
Tetrahedron Lett. 2010 Jul 28;51(30):3951-3955. doi: 10.1016/j.tetlet.2010.05.108.
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1,4-Thienodiazepine-2,5-diones via MCR (I): synthesis, virtual space and p53-Mdm2 activity.1,4-噻吩并二氮杂*-2,5-二酮通过 MCR(I)合成:虚拟空间与 p53-Mdm2 活性。
Chem Biol Drug Des. 2010 Aug;76(2):116-29. doi: 10.1111/j.1747-0285.2010.00989.x. Epub 2010 May 18.
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Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2008.2008年用于药物发现和化学生物学的化学文库综合调查。
J Comb Chem. 2009 Sep-Oct;11(5):739-90. doi: 10.1021/cc9000828.
6
Application of multicomponent reactions to antimalarial drug discovery. Part 2: New antiplasmodial and antitrypanosomal 4-aminoquinoline gamma- and delta-lactams via a 'catch and release' protocol.多组分反应在抗疟药物发现中的应用。第2部分:通过“捕获与释放”方案合成新型抗疟原虫和抗锥虫的4-氨基喹啉γ-和δ-内酰胺。
Bioorg Med Chem. 2006 Aug 15;14(16):5605-15. doi: 10.1016/j.bmc.2006.04.035. Epub 2006 May 11.
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Recent developments in isocyanide based multicomponent reactions in applied chemistry.应用化学中基于异腈的多组分反应的最新进展。
Chem Rev. 2006 Jan;106(1):17-89. doi: 10.1021/cr0505728.
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The impact of microwave synthesis on drug discovery.微波合成对药物发现的影响。
Nat Rev Drug Discov. 2006 Jan;5(1):51-63. doi: 10.1038/nrd1926.
9
One-step construction of peptidomimetic 5-carbamoyl-4-sulfonyl-2-piperazinones.肽模拟物5-氨基甲酰基-4-磺酰基-2-哌嗪酮的一步构建。
J Comb Chem. 2005 May-Jun;7(3):360-3. doi: 10.1021/cc0500147.
10
Transport of anthelmintic benzimidazole drugs by breast cancer resistance protein (BCRP/ABCG2).抗蠕虫苯并咪唑类药物经乳腺癌耐药蛋白(BCRP/ABCG2)的转运
Drug Metab Dispos. 2005 May;33(5):614-8. doi: 10.1124/dmd.104.003319. Epub 2005 Feb 9.

通用一锅两步法获得具有高度骨架多样性的一系列新型多环杂环化合物。

General one-pot, two-step protocol accessing a range of novel polycyclic heterocycles with high skeletal diversity.

机构信息

College of Pharmacy, The University of Arizona, Oro Valley, 85737, United States.

出版信息

ACS Comb Sci. 2012 Aug 13;14(8):460-4. doi: 10.1021/co300046r. Epub 2012 Jul 12.

DOI:10.1021/co300046r
PMID:22746181
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3426865/
Abstract

An Ugi one-pot three-component four-center reaction was coupled with a subsequent acid mediated cyclodehydration step to furnish a multitude of unique scaffolds having in common an embedded or attached benzimidazole and often a ring system formed through lactamization. Using combinations of tethered Ugi inputs typically via tethered acid-ketone inputs and supporting reagents containing masked internal nucleophiles, such scaffolds were produced in good to excellent yields in an operationally friendly manner.

摘要

一种 Ugi 一锅三组分四中心反应与随后的酸介导的环脱水步骤相结合,提供了许多具有共同特点的独特支架,这些支架通常具有嵌入式或附着的苯并咪唑,并且经常通过内酰胺化形成环系统。通过通常使用连接的酸酮输入的组合以及含有掩蔽内部亲核试剂的支持试剂,以操作友好的方式以良好至优异的产率生产了这些支架。