Discovery of Oxazolidin-2-one

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Analogs of 3,4,5 trimethoxybenzamide: synthesis and effects on CNS

A series of new heterocyclic derivatives of 3,4,5 trimethoxybenzamide was synthesized and tested for C.N.S. depressant activity. The oxazolidino and imidazolino derivatives (VI c) and (VI g) were subjected to more detailed pharmacological evaluation in comparison with trimetozine, and proved to be particularly active on conditioned and aggressive behavior of rodents.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H899NO – PubChem

 

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Diaminotetrafluoroethoxybenzenes

Tetrafluoroethoxybenzenes, and their acid addition salts, of the general formula: STR1 in which R1 may represent hydrogen or an alkyl having from 1 to 4 carbon atoms and R2, R3 and R4 represent one or more of the same or different substituents selected from hydrogen, an alkyl having 1 to 4 carbon atoms or mono- or dihydroxylalkyls having 1 to 4 carbon atoms, provided that the amino groups are situated relative to one another in an ortho- or meta- position and R1, R2, R3 and R4 do not simultaneously represent hydrogen when the amino groups are arranged in a 2,4- position. The compounds of the invention, along with 2,4-diaminotetrafluoroethoxybenzene, are useful as coupler components in oxidative hair coloring agents. A process for making the compounds, as well as a separate process for making the mono-N-beta-hydroxylethyl compounds, is provided.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H149NO – PubChem

 

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A novel and efficient (NHC)CuI (NHC = N-heterocyclic carbene) catalyst for the oxidative carbonylation of amino compounds

Oxidative carbonylation of amino compounds to prepare corresponding 2-oxazolidinones, ureas, and carbamates selectively in the presence of (NHC)CuI without any additives was firstly achieved in good yields and selectivities.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1214NO – PubChem

 

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Cysteine-Aminoethylation-Assisted Chemical Ubiquitination of Recombinant Histones

Histone ubiquitination affects the structure and function of nucleosomes through tightly regulated dynamic reversible processes. The efficient preparation of ubiquitinated histones and their analogs is important for biochemical and biophysical studies on histone ubiquitination. Here, we report the CAACU (cysteine-aminoethylation assisted chemical ubiquitination) strategy for the efficient synthesis of ubiquitinated histone analogs. The key step in the CAACU strategy is the installation of an N-alkylated 2-bromoethylamine derivative into a recombinant histone through cysteine aminoethylation, followed by native chemical ligation assisted by Seitz’s auxiliary to produce mono- and diubiquitin (Ub) and small ubiquitin-like modifier (SUMO) modified histone analogs. This approach enables the rapid production of modified histones from recombinant proteins at about 1.5-6 mg/L expression. The thioether-containing isopeptide bonds in the products are chemically stable and bear only one atomic substitution in the structure, compared to their native counterparts. The ubiquitinated histone analogs prepared by CAACU can be readily reconstituted into nucleosomes and selectively recognized by relevant interacting proteins. The thioether-containing isopeptide bonds can also be recognized and hydrolyzed by deubiquitinases (DUBs). Cryo-electron microscopy (cryo-EM) of the nucleosome containing H2BKC34Ub indicated that the obtained CAACU histones were of good quality for structural studies. Collectively, this work exemplifies the utility of the CAACU strategy for the simple and efficient production of homogeneous ubiquitinated and SUMOylated histones for biochemical and biophysical studies.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H441NO – PubChem

 

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Method for treating glaucoma IIB

Provided is a method of decreasing intraocular pressure or improving ocular accommodation in an animal, including a human, comprising administering an intraocular pressure decreasing amount or ocular accommodation improving amount of a compound of the formula I or IA, 1wherein J is oxygen, sulfur, or N?Rd.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H75NO – PubChem

 

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Ag@SnO2@ZnO core-shell nanocomposites assisted solar-photocatalysis downregulates multidrug resistance in Bacillus sp.: A catalytic approach to impede antibiotic resistance

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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Oxazolidine – Wikipedia,
Oxazolidine | C3H472NO – PubChem

 

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Process for producing oxazolidin-2-one derivative

An industrial process for preparing an oxazolidin-2-one derivative represented by the following general formula (3) wherein R1, R2, R3 and R4 are hydrogen atom, straight, branched or cyclic alkyl group, straight or branched alkyl group substituted by alkoxy, substituted amino or alkylthio, substituted or unsubstituted aralkyl group, or substituted or unsubstituted aryl group, and R5 is are hydrogen atom, straight, branched or cyclic alkyl group, substituted or unsubstituted aralkyl group, or substituted or unsubstituted aromatic ring,which is characterized in reacting a 1,3-dioxolan-2-one derivative and a carbamate derivative or an urea derivative in the presence of a fluoride salt.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H143NO – PubChem

 

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Chirality and stereoselectivity in photochromic reactions

In this review, the chirality and stereoselectivity in photochromic reactions are broadly discussed. Stereoselectivity is categorized into the two main areas of enantioselectivity and diastereoselectivity. Enantioselective photochromism was discussed according to the methods of generating chirality, that is: (1) optical resolution of chiral and racemic compounds, (2) spontaneous separation of racemic compounds during crystallization, (3) chiral template-assisted photochromic reactions to preferentially generate an enantiomer or cause chirality-based events, and (4) the generation of a non-racemic mixture of the photoisomers by irradiation of circularly polarized light to the racemic starting photoisomer. Diastereoselective photochromism was discussed for each family of photochromic reactions, namely, (1) fulgides, (2) diarylethenes, (3) spiro-compounds, (4) azobenzenes, and (5) organometallic complexes. Chirality-related reactions in overcrowded alkenes are discussed in a separate chapter. These include: (1) the discovery of the light-driven molecular motor, (2) the first generation of light-driven molecular motors with unidirectional rotation, which have two chiral carbon atoms in a molecule, (3) the second generation of light-driven molecular motors with unidirectional rotation, which have a single chiral carbon atom in a molecule. Finally, two distinctive novel photochromic systems are introduced in which the reactions proceed stereoselectively, although their enantio- or diastereoselectivity during photochromic reactions have yet to be examined.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H853NO – PubChem

 

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Enantioselective N-Alkylation of Indoles via an Intermolecular Aza-Wacker-Type Reaction

The development of an intermolecular and enantioselective aza-Wacker reaction is described. Using indoles as the N-source and a selection of alkenols as the coupling partners selective beta-hydride elimination toward the alcohol was achieved. This strategy preserves the newly formed stereocenter by preventing the formation of traditionally observed enamine products. Allylic and homoallylic alcohols with a variety of functional groups are compatible with the reaction in high enantioselectivity. Isotopic-labeling experiments support a syn amino-palladation mechanism for this new class of aza-Wacker reactions.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H288NO – PubChem

 

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Investigation of pyramidal inversion of nitrogen atom in carbamate and thiocarbamate ions formed at the reaction of ??2, ?OS, CS2 with 2-aminoethanol

Dynamic NMR was applied to measuring the value DeltaG? characterizing the height of the barrier to the pyramidal inversion of the nitrogen atom in carbamate and thiocarbamate anions formed at the reaction of 2-aminoethanol with CO2 and COS. The refinement was introduced in formerly suggested cyclic structures of anions containing an intramolecular hydrogen bond NHO(S), which contradicted the found large values of the barrier of inversion (DeltaG? ? 70 kJ mol?1). The hydrogen bond in the cyclic anions of carbamates and thiocarbamates is two-electron and three-center. Analogous cyclic structure with a multicenter hydrogen bond does not form in the case of dithiocarbamate anion that is the product of 2-aminoethanol reaction with CS2.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H1040NO – PubChem