Syntheses and structure–activity relationships of a novel class of 2-[3-oxospiro[isobenzofuran-1(3H),1′-cyclohexan]-4′-yl]benzimidazole NPY Y5 receptor antagonists are described. Optimization of the lead compound 2a by incorporating substituents into the 5-position or into both the 5- and 6-p...
Design, syntheses, and structure–activity relationships of a novel class of 2-{3-oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole NPY Y5 receptor antagonists are described. The benzimidazole structures were newly designed based on the urea linkage of our prototype Y5 receptor an...
An efficient and novel two step synthetic procedure to prepare various substituted 3H,3′H-spiro[benzofuran-2,1′-isobenzofuran]-3,3′-diones A, was established from very simple and easily available starting materials. The developed method is a robust and general approach for the synthesis of th...
Formal syntheses of both cis and trans 3-hydroxy pipecolic acids is achieved from l-ascorbic acid. Present synthesis describes use of chiral pool approach in which epimerization, Staudinger reaction and Cyclization reactions were employed as key steps.
N-protected dehydroamino acid methyl esters have been converted to α-fluoro-β-halo amino acid derivatives under halofluorination reaction conditions. The influences of the nitrogen protecting group of the substrates and of the halonium electrophile on the reaction outcome and the stability of ...
Routes to single enantiomers of hydroxy, methoxy and ketomycolic acids containing an α-methyl-trans-alkene unit as well as related trehalose, glucose, arabinose and glycerol esters are described. In serodiagnostic assays to detect antibodies to mycobacterial lipids, the trehalose esters give hi...
Addition reactions of the chiral lithium (2S)-enolates of the (2S,5S)-2-tert-butyl-5-methyl-[1,3]dioxolan-4-one and (2S,5S)-2-tert-butyl-2,5-dimethyl-[1,3]dioxolan-4-one with linear aliphatic acylsilanes yield the corresponding (2S,5R,1′R)-1′-trimethylsilyl-dioxolanone alcohols. Sodium methoxi...
(S)-Aspartyl-(7,7-dimenthylnorborn-2R-yl)-(S)-alanine methyl ester (1) was synthesized in nine steps from (+)-α-fenchyl alcohol (3) as a chiral synthon. Crucial steps for controlling the side-chain stereochemistry of 1, required for the manifestation of sweetness, were the catalytic hydroformyl...
In this study, the LLE data of ternary system (water + 1,6-diaminohexane + 2-methyl-1-propanol) and (water + 1,6-diaminohexane + 3-methyl-1-butanol) were measured at (293.15, 303.15 and 313.15) K under atmospheric pressure. Reliability of the experimental tie-line data was checked by empirical H...
This study presented the effects of lipids extraction from waste activated sludge (WAS) via in-situ transesterification on anaerobic digestion performance. The nonpolar transesterified product (TP) yield through the extraction was 9.68% of the dried mass of WAS and its fatty acid methyl esters (...
With molecular dynamics simulations of phospholipid membranes becoming a reality, there is a growing need for experiments that provide the molecular details necessary to test these computational results. Pyridine is used here to explore the interaction of planar aromatic groups with the water-li...
1H and 2H NMR spectra of pyridine and pyridine-N-oxide in nematic phase have been obtained. Three solvents (EBBA, Phase IV, and ZLI 1132) have successfully been used for pyridine, while only two (EBBA and Phase IV) gave reasonable spectra for pyridine-N-oxide. The values obtained for the deuteri...
Crystals of bis(2,6-dimethylpyridine-N-oxide) sulphate are monoclinic, space group P21c, a = 14.098(2) Å, b = 7.855(1) Å, c = 15.203(3) Å, β = 104.84(1)°. The crystal structure has been refined to R = 0.0373 (2052 reflections). The disordered SO2−4 anion accepts hydrogen bonds from two prot...
The thermal reaction between the electron-rich iridium complex, [IrCOD(PMe3)3]Cl, 1a, and pyrrolic or anilinic N–H bonds results in the oxidative addition of the N–H bond and the formation of an amido iridium hydride complex, HIr(amido)(Cl)(PMe3)3 with loss of COD. The only isomer formed in th...
Transition metal ion complexes of the potentially bidentate ligand 2-pyridylcarbinol N-oxide have been prepared. They are characterized and identified by chemical analysis and physical measurements. Their IR and electronic spectra are discussed with regard to monodentate or bidentate bonding of ...
Complexes of the anion 2-thio-6-picoline N-oxide (6MOS) have been isolated with the following stoichiometry: M(6MOS)3 (M = Cr, Fe, and Co) and M(6MOS)2 (M = Co, Ni, Cu and Zn). The spectral properties of these complexes are compared with those of 2-thiopyridine N-oxide in order to determine the ...
Three new alkaloids, galanthamine N-oxide, sanguinine N-oxide and lycoramine N-oxide were isolated from Lycoris sanguinea var. Kiushiana Makino.
We have synthesized a series of novel 4-((2,4,5-triphenyl-1H-imidazol-1-yl)methyl)pyridine derivatives. The structures of these compounds were confirmed by IR, HR-MS, 1H and 13C NMR spectra. The compound 5g was also confirmed by single crystal XRD. The geometry of the synthesized compounds 5a–5...
Medroxyprogesterone acetate (MPA) (1) has been transformed by two filamentous fungi, including Absidia griseolla var. igachii and Acremonium chrysogenum, into 11α-hydroxy-medroxyprogesterone acetate (2) as the major metabolite. The structure of the product was identified by different spectrosco...
Cellulose acetate (CA) membranes were prepared via phase inversion using methyl lactate as a green solvent and 2-methyltetrahydrofuran as a green co-solvent with or without evaporation period prior to immersion of the cast polymer solution in the coagulation bath. The membrane morphologies were ...
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