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The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

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A simple combination of copper(II) acetate (Cu(OAc)2) and an appropriate base could promote oxidative cross-coupling of H-phosphonates and amides using air as a terminal oxidant. The substrate scope was broad with respect to both dialkyl H-phosphonates and nitrogen nucleophiles (including oxazolidinone, lactam, pyrrolidinone, urea, indole, and sulfonamide derivatives), giving the corresponding P-N coupling products in moderate to high yields.

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Two new classes of highly active yet air- and moisture-stable pi-R-allylpalladium complexes containing bulky biaryl- and bipyrazolylphosphines with extremely broad ligand scope have been developed. Neutral pi-allylpalladium complexes incorporated a range of biaryl/bipyrazolylphosphine ligands, while extremely bulky ligands were accommodated by a cationic scaffold. These complexes are easily activated under mild conditions and are efficient for a wide array of challenging C-C and C-X (X = heteroatom) cross-coupling reactions. Their high activity is correlated to their facile activation to a 12-electron-based L-Pd(0) catalyst under commonly employed conditions for cross-coupling reactions, noninhibitory byproduct release upon activation, and suppression of the off-cycle pathway to form dinuclear (mu-allyl)(mu-Cl)Pd2(L)2 species, supported by structural (single crystal X-ray) and kinetic studies. A broad scope of C-C and C-X coupling reactions with low catalyst loadings and short reaction times highlight the versatility and practicality of these catalysts in organic synthesis.

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Oxazolidine – Wikipedia,
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Bicyclo[1.1.1]pentane (BCP) replacement as a bioisostere in drug molecules has an influence on their permeability, aqueous solubility and in vitro metabolic stability. Thus, the chemical installation of the BCP unit into a chemical entity remains a significant challenge from a synthetic point of view. Here, we have presented a new approach for the installation of the BCP unit on the xanthate moiety by means of a radical exchange process.

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This review article surveys literature methods for the carboxylative cyclization of N-propargylamines with CO2 to provide 2-oxazolidinones. We have classified these reactions based on the type of catalysts.

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Oxazolidine – Wikipedia,
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A flexible, modular ynamide synthesis is reported that uses trichloroethene as an inexpensive two carbon synthon. A wide range of amides and electrophiles can be converted to the corresponding ynamides, importantly including acyclic carbamates, hindered amides, and aryl amides. This method thus overcomes many of the limitations of other approaches to this useful functionality. This journal is

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4-Aminopyridines are valuable scaffolds for the chemical industry in general, from life sciences to catalysis. We report herein a collection of structurally diverse polycyclic fused and spiro-4-aminopyridines that are prepared in only three steps from commercially available pyrimidines. The key step of this short sequence is a [4 + 2]/retro-[4 + 2] cycloaddition between a pyrimidine and an ynamide, which constitutes the first examples of ynamides behaving as electron-rich dienophiles in [4 + 2] cycloaddition reactions. In addition, running the ihDA/rDA reaction in continuous mode in superheated toluene, to overcome the limited scalability of MW reactions, results in a notable production increase compared to batch mode. Finally, density functional theory investigations shed light on the energetic and geometric requirements of the different steps of the ihDA/rDA sequence.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H508NO – PubChem

 

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In the present study, we report the solar-photocatalytic disinfection (SPCD) of a multidrug resistant (MDR) bacterium, Bacillus sp. CBEL-1 using Ag@SnO2@ZnO core-shell nanocomposites (NCs) as catalyst. Complete disinfection was observed within 210 min with a catalyst concentration of 500 mg/L when subjected to NCs mediated PCD under solar irradiation. H2O2 was found to be the key reactive oxygen species (ROS) involved in SPCD of targeted bacteria. Increase in production of 4-HNE along with change in fatty acid profile of bacteria after SPCD induced oxidative stress indicates the compromisation of bacterial cell membrane. Irreversible change in antibiotic resistance profile of the target bacteria was notice after SPCD, without recovery even after 96 h post disinfection experiments. Traditional disinfectants and UV-250 nm were found to have marginal impact on the resistance profile of the bacteria compared to that of SPCD. Disinfection achieved using the NCs were also validated for real water samples.

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Ferula orientalis L. stalks were liquefied in an autoclave in supercritical organic solvents (methanol, ethanol, 2-propanol, acetone and 2-butanol) with (NaOH, Na2CO3, ZnCl2) and without catalyst at five different temperatures ranging from 240 C to 320 C. The amounts of solid (unconverted raw material), liquid (bio-oil) and gas produced, as well as the composition of the resulting liquid phase, were determined. The effects of various parameters such as temperature, solvent, catalyst and ratio of catalyst on product yields were investigated. The results showed that conversion highly depends on the temperature and catalyst. The highest bio-oil yield (53.97%) was obtained using acetone with 10% zinc chloride at 300 C. The liquid products were extracted with benzene and diethyl ether. Some of selected liquid products (bio-oils) were analyzed by elemental, FT-IR and GC-MS. 126 different compounds were identified by GC-MS in the liquid products obtained in ethanol at 300 C.

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Oxazolidine | C3H322NO – PubChem

 

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Disclosed is a process for preparing an aryloxyalkylene amine compound via an aminoethylation reaction comprising: a) reacting an aromatic hydroxyl compound in the presence of a basic catalyst with a 2-oxazolidinone compound of the formula II to form an intermediate reaction product; wherein R3 is selected from the group consisting of hydrogen or lower alkyl having 1 to 6 carbon atoms, R4 is selected from the group consisting of hydrogen, straight or branched chain alkyl having from one to six carbon atoms, phenyl, alkaryl, or arylalkyl; and b) reacting the intermediate product of step a) with a polyalkylene polyamine.

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Oxazolidine – Wikipedia,
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