- Synthesis and antibacterial activity of aromatic and heteroaromatic amino alcohols
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Two series of aromatic and heteroaromatic amino alcohols were synthesized from alcohols and aldehydes and evaluated for their antibacterial activities. All the octylated compounds displayed a better activity against the four bacteria tested when evaluated by the agar diffusion method and were selected for the evaluation of minimal inhibitory concentration. The best results were obtained for p-octyloxybenzyl derivatives against Staphylococcus epidermidis (minimal inhibitory concentrations = 32μm).
- de Almeida, Camila G.,Reis, Samira G.,de Almeida, Angelina M.,Diniz, Claudio G.,da Silva, Vania L.,Le Hyaric, Mireille
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experimental part
p. 876 - 880
(2012/06/18)
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- AMIDOPYRAZOLE DERIVATIVE
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A platelet coagulation inhibitor which inhibits neither COX-1 nor COX-2 is provided. The inhibitor is a compound represented by general formula (I): wherein Ar1 and Ar2 independently represent a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents, or a phenyl group optionally substituted with 1 to 3 substituents; R1 represents a lower acyl group, carboxyl group, a lower alkoxycarbonyl group, a lower alkoxy group, a lower alkyl group optionally substituted with 1 or 2 substituents, a carbamoyl group optionally substituted with 1 or 2 substituents, an oxamoyl group optionally substituted with 1 or 2 substituents, an amino group optionally substituted with 1 or 2 substituents, a 4- to 7-membered alicyclic heterocyclic group optionally substituted with 1 or 2 substituents, a phenyl group optionally substituted with 1 to 3 substituents, or a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents; and R2 represents hydrogen atom, a halogeno group, or the like.
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Page/Page column 83-84
(2010/11/23)
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- Improved syntheses of fluorinated tertiary butylamines
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Two new and efficient methods using cyclic sulfamidate and nitrone chemistry were developed for the synthesis of the sterically congested 1,1- dimethyl-2-fluoroethylamine (1), 2-fluoro-1-(fluoromethyl)-1-methylethylamine (2) and 2-fluoro-1,1-bis-(fluoromethyl)-ethylamine (3).
- Ok, Dong,Fisher, Michael H.,Wyvratt, Matthew J.,Meinke, Peter T.
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p. 3831 - 3834
(2007/10/03)
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- Bicyclic and tricyclic compounds with β-amino alcohol groups as chiral ligands in the enantioselective reaction of diethylzinc with aldehydes
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Reduction of the enantiomerically pure allyloxy esters 9 or ent-9 with DIBAH afforded the corresponding aldehydes which were treated in situ with chiral or achiral hydroxylamines 8 to give nitrones 10. These underwent a spontaneous intramolecular 1,3-dipolar cycloaddition, affording the bicyclic compounds 11 and 12, respectively. In an analogous manner, a mixture of the tricyclic compounds 14 and 15 was prepared. Treatment of compound 16 with cyclohexene oxide afforded a mixture of diastereomers 17 and 18. Diastereomers 14 and 15 as well as 17 and 18 could be separated by chromatography. X-ray analyses of compounds 11Ff, 17, and 11Af · HCI were performed. The bicyclic and tricyclic compounds were used as chiral ligands in the reaction of diethylzinc with aldehydes 19, in particular with benzaldehyde (19a). Using bicyclic compounds with a tertiary β-hydroxyalkyl substituent at the N atom as ligands, ee's in the range of 78 to 95% were found. Whereas for the best ligands 11Ae and Af the enantioselectivity in the reaction of 4-tolualdehyde was only slightly decreased, with the aliphatic aldehydes 19c and d distinctly lower enantioselectivities were determined. VCH Verlagsgesellschaft mbH, 1997.
- Aurich, Hans Guenter,Biesemeier, Frank,Geiger, Michael,Harms, Klaus
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p. 423 - 434
(2007/10/03)
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- Regio- and Diastereoselectivity in the Reaction Sequence from Secondary 3-Oxa-5-hexen-1-ylamines to Bicyclic Compounds via Nitrones
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Secondary amines 2 and 8 are oxidized by hydrogen peroxide in the presence of sodium tungstate providing nitrones. It the amino function is substituted by one primary and one secondary alkyl moiety, oxidation proceeds with high regioselectivity at the primary alkyl group affording aldonitrones. Thus, compound 2b gives exclusively 3b that undergoes an intramolecular cycloaddition yielding 4b. From 2c, however, in addition to 4c nitrone 5 is formed as by-product, which affords the bridged compound 6 on heating in toluene. Oxidation of compounds 8 yields nitrones 9 which are converted to bridged compounds 10 as major products along with small amounts of regioisomers 11 at elevated temperatures. The intramolecular cycloaddition of the chiral nitrones 3b and c as well as 9b proceeds with high diastereoselectivity.
- Aurich, Hans Günter,Geiger, Michael,Sievers, Ulrich
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p. 1004 - 1006
(2007/10/03)
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- ELECTROREDUCTION OF 2-OXAZOLINES
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The cathodic behavior of 2-phenyl-4,4-dimethyl-2-oxazoline (4), 2,4,4-trimethyl-2-oxazoline (7) and 2-(1,1-dimethylethyl)-4,4-dimethyl-2-oxazoline (8) at Hg electrodes was investigated.A reduction peak for 4 at -2.49V (SCE), was observed by cyclic voltamm
- Ryan, Christopher M.,Kariv-Miller, Essie
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p. 6807 - 6810
(2007/10/02)
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- HYDROXY SCHIFF BASE-OXAZOLIDINE TAUTOMERISM: APPARENT BREAKDOWN OF BALDWIN'S RULES
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The tautomerism between hydroxy Schiff bases, X=C6H4CR=NCMe2CH2OH (R=H, Me, C6H5; X is a range of substituents) and X=C6H4CR=NC6H4(o-CH2OH), and the corresponding ring closed systems, oxazolidines and dihydrobenzoxazines, has been investigated.In all case
- Astudillo, Mario E. Alva,Chokotho, Norris C. J.,Jarvis, Terence C.,Johnson, C. David,Lewis, Colin C.,McDonnell, Peter D.
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p. 5919 - 5928
(2007/10/02)
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