期刊
TETRAHEDRON LETTERS
卷 51, 期 36, 页码 4723-4726出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2010.07.010
关键词
Benzimidazole; Antagonist; Anti-viral; Chelators synthesis
资金
- University of Hull Clinical Biosciences Institute
- EPSRC
The synthesis of 1-(4-nitrobenzyl)-2-chloromethyl benzimidazole, which undergoes a nucleophilic substitution with pyridine in the absence of additional base, is reported. The key steps are the reaction of 1,2-phenylenediamine to give exclusively the mono-substituted product and the avoidance of minor by-products via the use of glycolic acid for the cyclisation step. The X-ray structures of 1-(4-nitrobenzyl)-2-chloromethyl benzimidazolium chloride and 1-[1-(4-nitrobenzyl)benzimidazol-2-ylmethyl]pyridinium chloride are presented. (C) 2010 Elsevier Ltd. All rights reserved.
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