- A highly efficient copper-catalyzed method for the synthesis of 2-hydroxybenzamides in water
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An efficient copper-catalyzed synthetic method for the preparation of 2-hydroxybenzamides is described for the first time from 2-chlorobenzamide substrates using copper iodide/1,10-phenanthroline and a base, potassium hydroxide, in neat water. By using this reaction, a series of 2-hydroxybenzamides with functional groups such as fluoro, chloro, iodo, methoxy, amide, and alcohol have been obtained in 33-96% yield. Other aromatic 2-chloroarylamides such as naphthalene, pyridine, and thiophene are found to be equally compatible to the reaction. It is proposed that the reaction proceed via formation of copper-amide complex, which may facilitate the hydroxylation in water. Overall, the first report on copper-catalyzed hydroxylation reaction in water and first catalytic route for the synthesis of 2-hydroxybenzamides is presented. Simple purification procedure and convenience of employing low-cost reagents in neat water make this method practical and economical for the synthesis of 2-hydroxybenzamides. Georg Thieme Verlag Stuttgart · New York.
- Balkrishna, Shah Jaimin,Kumar, Sangit
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p. 1417 - 1426
(2012/06/30)
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- Synthesis, antibacterial activities and molecular docking studies of peptide and Schiff bases as targeted antibiotics
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A series of peptide and Schiff bases (PSB) were synthesized by reacting salicylic acid, primary diamines with salicylaldehyde or its derivatives, and 40 of which were newly reported. The inhibitory activities against Escherichia coli β-ketoacyl-acyl carrier protein synthase III (ecKAS III) were investigated in vitro and molecular docking simulation also surveyed. Top 10 PSB compounds which posses both good inhibitory activity and well binding affinities were picked out, and their antibacterial activities against Gram-negative and Gram-positive bacterial strains were tested, expecting to exploit potent antibacterial agent with broad-spectrum antibiotics activity. The results demonstrate compound N-(3-(5-bromo-2-hydroxybenzylideneamino)propyl)-2-hydroxybenzamide (2d) can be as a potential antibiotics agent, displaying minimal inhibitory concentration values in the range of 0.39-3.13 μg/mL against various bacteria. Crown Copyright
- Cheng, Kui,Zheng, Qing-Zhong,Qian, Yong,Shi, Lei,Zhao, Jing,Zhu, Hai-Liang
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experimental part
p. 7861 - 7871
(2010/03/24)
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- Hydrazide-containing inhibitors of HIV-1 integrase
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Inhibitors of HIV integrase are currently being sought as potential new therapeutics for the treatment of AIDS. A large number of inhibitors discovered to date contain the o-bis-hydroxy catechol structure. In an effort to discover structural leads for the
- Zhao, He,Neamati, Nouri,Sunder, Sanjay,Hong, Huixiao,Wang, Shaomeng,Milne, George W. A.,Pommier, Yves,Burke Jr., Terrence R.
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p. 937 - 941
(2007/10/03)
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- A Convenient Method for Preparing Some New Macrocyclic Diamides
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A simple and convenient method for preparing macrocyclic diamides containing two sulfur atoms or two to four oxygen atoms of various ring sizes was developed.This two-step procedure is simply composed of reacting salicylic acid or 2-mercaptobenzoic acid w
- Liu, Lilian Kao,Hsieh, Tsing-Pai,Kuo, Sung-Ming
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p. 309 - 312
(2007/10/02)
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