- Preparation of complexes of 1-amino-6,7-O-cyclohexylidene-4-azaheptane with transition metal acetates
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1-Amino-6,7-O-cyclohexylidene-4-azaheptane (L) has been synthesized starting from 1-chloro-2,3-O-cyclohexylidenepropane prepared by the reaction of epichlorohydrin with cyclohexanone, catalyzed by BF3OEt2. Complexes of this ligand with Co(II), Ni(II) and Cu(II) acetates were prepared. The structures of the ligand and its complexes are proposed based on the elemental analyses, IR, UV-VIS, and 1H and 13C NMR spectra, magnetic susceptibilities, and conductomety data. Pleiades Publishing, Inc. 2006.
- Oeztirk,Sekerci,Oezdemir
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- TETRAFLUOROBORIC ACID - A NEW CATALYST FOR THE SYNTHESIS OF 1,3-DIOXOLANES. PREPARATION OF HYDROXYACETONE
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It is established that tetrafluoroboric acid (HBF4) is an effective catalyst for halogen substitution reactions of oxiranes (epichlorohydrin and 1-bromo-3-methyl-2,3-epoxybutane) with aldehydes and ketones, forming 1,3-dioxolanes in high yield.
- Gevorkyan, A. A.,Kazaryan, P. I.,Avakyan, O. V.,Vardanyan, R. A.
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- 1,3-Dioxolane-based ligands as a novel class of α1-adrenoceptor antagonists
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1,3-Dioxolane-based compounds (2-14) were synthesized, and the pharmacological profiles at α1-adrenoceptor subtypes were assessed by functional experiments in isolated rat vas deferens (α1A), spleen (α1B), and aorta (α1D). Compound 9, with a pA2 of 7.53, 7.36, and 8.65 at α1A, α1B, and α1D, respectively, is the most potent antagonist of the series, while compound 10 with a pA2 of 8.37 at α1D subtype and selectivity ratios of 162 (α1D/α1A) and 324 (α1D/α1B) is the most selective. Binding assays in CHO cell membranes expressing human cloned α1-adrenoceptor subtypes confirm the pharmacological profiles derived from functional experiments, although the selectivity values are somewhat lower. Therefore, it is concluded that 1,3-dioxolane-based ligands are a new class of α1-adrenoceptor antagonists.
- Brasili, Livio,Sorbi, Claudia,Franchini, Silvia,Manicardi, Massimo,Angeli, Piero,Marucci, Gabriella,Leonardi, Amedeo,Poggesi, Elena
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p. 1504 - 1511
(2007/10/03)
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- Enzymatic resolution of 2,2-disubstituted-1,3-dioxolane-4-methanol carboxylic esters
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The enantioselectivity of enzymatic hydrolysis of carboxylic esters of various 1,2-ketals of glycerol has been investigated. The influence of the ketal group has been studied. A number of lipases and proteinases have been tested and the best enantioselectivity was obtained with proteinase from Aspergillus oryzae which gave an E-value of 9 with 2,2-dimethyl-1,3-dioxolane-4-methanol butanoate. Variations in the acyl part revealed that butanoyl was optimal. All hydrolysis products have been synthesised in homochiral forms from homochiral starting materials.
- Partali,Melbye,Alvik,Anthonsen
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- PERFLUORINATED RESINSULFONIC ACID - A CATALYST FOR CERTAIN ORGANIC REACTIONS.
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The purpose of this work was to examine the possibility of using, as a catalyst in certain organic reactions, the perfluorinated resinsulfonic acid F-4SK in the H form, which is an analog of the perfluorinated resinsulfonic acid Nafion-H. To compare catalyst activity of the perfluorinated resinsulfonic acid in decomposition of cumene hydroperoxide, CHP was also decomposed in presence of KU-2 resin. It was found that during repeated use over a period of 150 h the activity of KU-2 catalyst under analogous conditions fell by 4-6%. During the same time the activity of the perfluorinated resinsulfonic acid remained unchanged. It is also known that the presence of a strong acid in the reaction mixture causes formation of by-products, namely the products of condensation of phenol with acetone and dimethylphenylcarbinol, and of dehydration of dimethylphenylcarbinol, with formation of alpha -methylstyrene and products of greater complexity.
- Etlis,Beshenova,Semenova,Shomina,Dreiman,Balaev
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p. 551 - 555
(2007/10/02)
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- Imidazole derivatives and salts thereof and pharmaceutical formulations useful in thrombo-embolic disorders
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Imidazoles of formula (I) STR1 wherein A is a chemical bond or a straight or branched, saturated or unsaturated, aliphatic residue having from 1 to 6 carbon atoms wherein 1, 2 or 3 of such carbon atoms may be replaced by a corresponding number of heteroatoms selected from oxygen, sulphur and nitrogen providing (in the case of 2 or 3 heteroatoms) that any such heteroatom is not located adjacent to a further such heteroatoms or heteroatoms R is a fused, saturated or unsaturated, non-aromatic carbocyclic, polycyclic ring system; a saturated or unsaturated, carbocyclic spirocyclic ring system, optionally containing one or more ring heteroatoms selected from oxygen, sulphur and nitrogen; or a saturated or unsaturated, carbocyclic bridged-polycyclic ring system, optionally containing one or more ring heteroatoms selected from oxygen, sulphur and nitrogen and having one or more bridges; or AR together represent a straight or branched, saturated or unsaturated, aliphatic residue having 3 to 6 carbon atoms, wherein 1, 2 or 3 of such carbon atoms may be replaced by a corresponding number of heteroatoms selected from oxygen, sulphur and nitrogen providing (in the case of 2 or 3 heteroatoms) that any such heteroatom is not located adjacent to a further such heteroatom or heteroatoms; which aliphatic residue is substituted by at least two groups, which may be the same or different, selected from the groups specified for R above. and acid addition salts and pharmaceutically acceptable bioprecursors thereof. Methods of preparing the imidazoles are disclosed. The imidazoles and their acid addition salts and bioprecursors are useful in the treatment or prophylaxis of thrombo-embolic conditions.
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- FORMATION DE DIOXOLANNES A PARTIR DE L'EPICHLORHYDRINE DU GLYCEROL. HYDROLYSE AISEE DE DIOXOLANNES PAR LE TOSYLATE DE PYRIDINIUM
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We described a versatile synthesis of dioxolanne from 1-chlor 2,3-epoxypropane epichlorhydrine and different carbonyl compounds in presence of activated montmorillonite which is easily eliminated after the reaction.The hydrolysis was performed in mild conditions with pyridinium p-toluene sulfonate.
- Thuy, Vu Moc,Petit, Huguette,Maitte, Pierre
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p. 759 - 762
(2007/10/02)
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