- Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones
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The synthesis and antibacterial activity of several new 5-((3-oxoisothiazol-2(3H)-yl)methyl)-3-phenyloxazolidin-2-ones 8 and analogous 2-(4-substituted phenyl)-3(2H)-isothiazolones 3 and 4 substituted at 4 and/or 3-positions of the phenyl moiety with different groups of which some have shown to increase the antibacterial activity of both 3-aryl-2-oxazolidinones and 3(2H)-isothiazolones is described. The most active compounds were isothiazolyl oxazolidinones 8a,j with unsubstituted and 8b with 4-F substituted phenyl rings which showed activities higher than analogous 3(2H)-isothiazolones and comparable or superior to linezolid, vancomycin, and ciprofloxacin against some tested microorganisms. The change in position of F and/or the use of larger substituents gave compounds with reduced or no activity. Evaluation of cytotoxicity to mouse fibroblast (NIH/3T3) cells indicated that these compounds exhibit antibacterial activity at non-cytotoxic concentrations.
- Adibpour, Neda,Khalaj, Ali,Rajabalian, Saeed
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scheme or table
p. 19 - 24
(2010/03/24)
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- Substituent effect on aniline carbonylation reaction in the presence of the PdCl2/Fe/I2/Py catalytic system
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A study of the effect of substituents in the aromatic ring on the aniline carbonylation reaction in the presence of the PdCl2/Fe/I 2/Py catalytic system, where oxygen or nitrobenzene were used as oxidants, showed that the electronodonor substituents accelerate the aniline carbonylation reaction, when the reaction is conducted in the presence of oxygen. For nitrobenzene used as an oxidant in this reaction substituent was found to have no effect on the carbamate yield. The nitrobenzene reduction is the rate-determining step in the aniline carbonylation process.
- Karpinska,Baran,Skupinska
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p. 1105 - 1116
(2008/09/21)
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- Cyanomethyl anion/carbon dioxide system: An electrogenerated carboxylating reagent. Synthesis of carbamates under mild and safe conditions
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A new carboxylating reagent (-CH2CN/CO2) was obtained by bubbling CO2 in a CH3CN-TEAP (tetraethylammonium perchlorate) solution previously electrolyzed under galvanostatic control. Organic carbamates were isolated from these solutions after addition of amines and an alkylating agent. In this paper, we describe the optimized conditions for the electrochemical synthesis of carbamates from amines and CO2, in mild and safe conditions, without any addition of bases, probases, or catalysts. Carbamates were isolated from primary and secondary aliphatic amines in high to excellent yields and from aromatic amines in moderate yields (dependent on the nucleophilicity of the nitrogen atom).
- Feroci, Marta,Casadei, Maria Antonietta,Orsini, Monica,Palombi, Laura,Inesi, Achille
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p. 1548 - 1551
(2007/10/03)
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- BENZIMIDAZOLIDINONE DERIVATIVES
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The present invention can provide novel compounds useful as orally administrable growth hormone releaser, more specifically a benzimidazolidinone derivative of formula (1) or a pharmaceutically acceptable salt thereof:(1) wherein R1 is optional
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Page/Page column 28
(2010/02/07)
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- The reaction of amines with an electrogenerated base. Improved synthesis of arylcarbamic esters
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The electrogenerated base of 2-pyrrolidone reacts with amines and anilines yielding the corresponding alkyl and aryl carbamates, after addition of carbon dioxide and ethyl iodide. Arylcarbamic esters are obtained in very good yields under mild reaction conditions with respect to the methods so far reported. (C) 2000 Elsevier Science Ltd.
- Feroci, Marta,Inesi, Achille,Rossi, Leucio
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p. 963 - 966
(2007/10/03)
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- A simple method for the synthesis of carbamates
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A new method for carbamate synthesis using aryl and alkylamines with sodium hydride and diethylcarbonate in dry benzene is described.
- Angeles,Santillan,Martinez,Ramirez,Moreno,Salmon,Martinez
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p. 2441 - 2447
(2007/10/02)
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