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A Simple and Efficient Enantioselective Synthesis of (S)-Esmolol
A. Venkat Narsaiah,J. Kranthi Kumar
International Journal of Industrial Chemistry , 2010,
Abstract: The stereoselective synthesis of (S)-methyl-2-[4-(2-hydroxy-2-(isopropyl amino)-ethoxy]-phenylacetate has been carried out in six steps with an overall yield of 65.6%. The key intermediate is chiral epoxide (7), which was achieved by applying Sharpless asymmetric dihydroxylation method with high enantiomeric purity and in excellent yields.
SYNTHESIS, CHARACTERIZATION AND ANALGESIC ACTIVITY OF VARIOUS PYRIDINE DERIVATIVES
Chaubey Ajit kumar,Pandeya S.N
International Journal of Research in Ayurveda and Pharmacy , 2011,
Abstract: The treatment of 2-amino pyridine (1) with isatine (2) affords (3Z)-3-(pyridin-2-ylimino)-1,3-dihydro-2H-indol-2-one (3) & then treatment with formaldehyde along with secondary amine, various N-substituted of (3Z)-3-(pyridin-2-ylimino)-1,3-dihydro-2H-indol-2-one (Schiff base) in the presence of glacial acetic acid results Mannich bases (4-8). (3Z)-3-(pyridin-2-ylimino)-1,3-dihydro-2H-indol-2-one (3) were synthesized by refluxing (1-2) in glacial acetic acid.The Mannich bases (4-8) of above condensed products were prepared by refluxing them with various secondary amines i.e., dimethylamine, diethylamine, piperazine, isopropyle amine , morpholine & with formaldehyde in the presence of glacial acetic acid in scheme 1. In scheme 2 the compound (2) was brominated and condensed with substituted pyridine (1) to give Schiff base (5-bromo-1H-indole-2,3-dione)(9) & also Mannich bases of (9) were synthesized(11-15) with secondary amines, in glacial acetic acid. Further the compound(2) was treated with conc. nitric acid in presence of sulfuric acid & condensed with 2- amino pyridine(1) & results 5-nitro-3-(pyridin-2-ylimino)-1,3-dihydro-2H-indol-2-one, the Mannich bases (18-22) of above condensed products were prepared by refluxing them with various secondary amines. The synthesized compounds were characterized by IR, NMR & elemental analysis. These compounds were screened for their analgesic activity using acetic acid induced writhing test & hot plate test. Some of these compounds (3,7,8,11,12,13,14,18,19,20 ) exhibit promising activities.
Analysis and Characterization of Isopropyl Carbanilate Herbicide and Its Photoproducts  [PDF]
Mohammed Fehmi Zaater
American Journal of Analytical Chemistry (AJAC) , 2011, DOI: 10.4236/ajac.2011.27092
Abstract: The phototransformation of the herbicide Isopropyl carbanilate (IPC) has been investigated under UV light. Irradiation of the herbicide at room temperature in aqueous and organic solvents such as hexane and methanol afforded new photo-products formed as a consequence of various processes including photo-Fries rearrangement, ring solvolysis, hydrolysis of the amide/carbamoyl and ester bonds, ring coupling and polymerization. The percentage remaining of the herbicide as a function of time was followed periodically starting from zero time up to three hours. Analyses were performed by GC-FID equipped with a semipolar glass column operated at 170?C. The rate of photo disappearance of IPC under controlled lab condition followed 1st order kinetics and found to be solvent dependent in the manner of non polar > polar solvents. The photo-products were successfully separated by GC and preparative TLC (Silica gel F-254) and were identified using either GC-MS and/or MS. Identifications were assigned on the bases of molecular ions, mass fragmentation pattern and whenever possible by comparison with the mass spectra of literature analogues.
Improvements to the Fluoride Reactivation Method by Simple Organic Extraction for Retrospective Detection of Exposure to the Organophosphorus Nerve Agents in Human Plasma  [PDF]
Jin Young Lee, Yong Han Lee
International Journal of Analytical Mass Spectrometry and Chromatography (IJAMSC) , 2014, DOI: 10.4236/ijamsc.2014.23007
Abstract: A rapid and simple organic extraction method for the determination of the chemical warfare agent, isopropyl methylphosphonofluoridate (sarin, GB) in human plasma has been developed using gas chromatography-tandem mass spectrometry (GC-MS/MS). In the course of method development, several organic solvents have been screened and chloroform show a low background and increase signal to noise ratio of GB among other organic solvents. Especially, the organic extraction method of reactivated GB from the human plasma has a 30% greater recovery yield than solid-phase ex-traction (SPE). This simple extraction method was successfully applied to the trace analysis of nerve agents in human plasma in the 3rd Organisation for the Prohibition of Chemical Weapons (OPCW) confidence building exercise on biomedical sample analysis.
Rotation Barriers in Pyridinium Salts Depend on the Number of Available Ground State Conformations
Balaban, Alexandru T.,Czerwinski, Edmund W.,Ghiviriga, Ion
- , 2004,
Abstract: Sa？etak The enthalpy and entropy of activation for the rotation about the C–N bond were measured in a series of five N-(1-hydroxybutan-2-yl)pyridinium salts, the 2,6-substituents being methyl, ethyl and isopropyl. Replacement of a methyl by an ethyl does not change the activation parameters, while replacement by an isopropyl increases both the activation enthalpy and the activation entropy. The latter is due to the decreased number of conformations available in the ground state. The activation entropies fit a simple model based on entropy of mixing
Chiral palladium complexes based on derivatives of benzylamine and 2α-hydroxypinan-3-one  [PDF]
Olga A. Zalevskaya, Yana A. Gur'eva, Larisa L. Frolova, Igor N. Alekseev, Alexander V. Kutchin
Natural Science (NS) , 2010, DOI: 10.4236/ns.2010.211147
Abstract: Synthesized and characterized new chiral palladium complexes, some of which contain asymmetric donor nitrogen atom. Nitrogen-containing derivatives (+) - and (-)-2α-hydroxypinan-3-one- (1R,2R,5R)-3-(benzylimino)-2,6,6-trimethylbicy- clo[3.1.1]heptane-2-ol (HL1), (1S,2S,3S,5S)-3- (benzylamino)-2,6, 6-trimethylbicyclo[3.1.1]- heptane-2-ol (HL2), (1R,2R,5R)-3-((S)-α-methyl- benzylimino)-2,6,6-trimethylbicyclo[3.1.1]- heptane-2-ol (HL3), (1R,2R,3R,5R)-3-((S)-α-methyl- benzylamino)-2,6,6-trimethylbicyclo[3.1.1]- heptane-2-ol (HL4) -were studied as optically active ligands.
Determination of ETM, Histamine and Mycotoxins in Garba, a Traditional Ivoirian Meal  [PDF]
Adjo Thérèse Anoman, Kouamé Mathias Koffi, Kouassi Narcisse Aboua, Marina Koussemon
American Journal of Analytical Chemistry (AJAC) , 2018, DOI: 10.4236/ajac.2018.94019
Abstract: The methods of preparation, conservation and sale of Garba, the traditional Ivorian street meal, abundantly consumed in Côte d’Ivoire, can be exposed to various infections resulting in the poisoning of consumers. The aim of this study was to evaluate the hygienic quality of Garba through the analysis and the determination of certain toxic chemicals. In three hundred (300) samples of Garba collected in four districts in Abidjan, toxic metals (cadmium, mercury, lead), biogenic amine (histamine) and mycotoxins (aflatoxins and ochratoxin A) were detected and quantified using official standardized methods. Different toxics analyzed were present at various levels in the Garba. The mercury, lead, cadmium and histamine levels in the Garba were respectively 0.19 mg/kg, 0.19 mg/kg, 0.03 mg/kg and 32.69 mg/kg. The detected mycotoxins included aflatoxins B1, B2, G1, G2 and ochratoxin A, with respective average proportions of 3.44 μg/kg, 1.90 μg/kg, 8.07 μg/kg, 0.56 μg/kg and 0.42 μg/kg. The mycotoxins levels in the Garba are higher than the recommended toxic levels, particularly the ones in aflatoxin B1 and G1. This suggests a sanitary risk associated with the consumption of this meal. Consequently, awareness campaigns and training of the Garba sellers in hygiene and a better regulation of this sector by the competent authorities are required.
An Aminopyrrolidinyl Phosphonates—A New Class of Antibiotics: Facile Synthesis and Predicted Biological Activity  [PDF]
Abed Al Aziz Al Quntar, Hasan Dweik, Ahmad Jabareen, Tatyana A. Gloriozova, Valery M. Dembitsky
International Journal of Organic Chemistry (IJOC) , 2020, DOI: 10.4236/ijoc.2020.104013
Abstract: A novel class of aminopyrrolidinyl phosphonates was synthesized in 74% - 80% isolated yield by the addition of three-fold excess of primary amines to diethyl 4-chloro-1-butynylphosphonates. The reaction was carried out at room temperature and in the absence of solvent or catalyst to give solely compounds which showed predicted biological activity based on PASS program. Some of the synthesized derivatives of antibiotics exhibit properties for the treatment of stroke, the treatment of acute neurological disorders, and can also be acetyl esterase inhibitors.
Synthesis and Characterization of N,N’-(propane-1,2 diyldicarbamothioyl)dibenzamide
Gül？ah Kurt,Bedrettin Mercimek
Molbank , 2008, DOI: 10.3390/m578
Abstract: No abstract available
3-[(Benzylsulfonyl)methyl]aniline hydrochloride
Daniel G. Grohmann,Bruce A. Hathaway
Molbank , 2006, DOI: 10.3390/m503
Abstract: No abstract available
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