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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

 

Awesome Chemistry Experiments For 5-(Chloromethyl)oxazolidin-2-one

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3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models

Cyclin-dependent kinases are therapeutic targets frequently deregulated in various cancers. By convenient alkylation of the 5-sulfanyl group, we synthesized 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with various substitutions at position 5 with potent antiproliferative activity in non-Hodgkin lymphoma cell lines. The most potent derivative 4.35 also displayed activities across more than 60 cancer cell lines. The kinase profiling confirmed high selectivity of 4.35 toward cyclin-dependent kinases (CDKs) 2, 5, and 9, and the cocrystal with CDK2/cyclin A2 revealed its binding in the active site. Cultured lymphoma cell lines treated with 4.35 showed dephosphorylation of CDK substrates, cleavage of PARP-1, downregulation of XIAP and MCL-1, and activation of caspases, which collectively confirmed ongoing apoptosis. Moreover, 4.35 demonstrated significant activity in various cell line xenograft and patient-derived xenograft mouse models in vivo both as a monotherapy and as a combination therapy with the BCL2-targeting venetoclax. These findings support further studies of combinatorial treatment based on CDK inhibitors.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1442NO – 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

 

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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The important role of (R)-4-Benzyl-3-(3-methylbutanoyl)oxazolidin-2-one

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Lead optimization of 5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)- 4-hydroxyhexanamides to reduce a cardiac safety issue: Discovery of DS-8108b, an orally active renin inhibitor

With the aim to address an undesired cardiac issue observed with our related compound in the recently disclosed novel series of renin inhibitors, further chemical modifications of this series were performed. Extensive structure-activity relationships studies as well as in vivo cardiac studies using the electrophysiology rat model led to the discovery of clinical candidate trans-adamantan-1-ol analogue 56 (DS-8108b) as a potent renin inhibitor with reduced potential cardiac risk. Oral administration of single doses of 3 and 10 mg/kg of 56 in cynomolgus monkeys pre-treated with furosemide led to significant reduction of mean arterial blood pressure for more than 12 h.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2606NO – PubChem

 

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New progress in azole compounds as antimicrobial agents

The increasing incidence of microbial resistance and newly emerging pathogens have become a serious challenge for public health. More and more efforts have been directed to the development of new antimicrobial agents with distinct mechanisms from the well-known classes of clinical drugs. The extensive clinical utilization of azole-based medicinal drugs has evoked numerous attentions, and their researches and developments have been a quite rapid developing and active highlight topic with an infinite space. Consideration of our researches on azole compounds and other literature in recent three years, this review scientifically reviewed the new progress of azole derivatives as antibacterial, antifungal, antitubercular and antiviral agents, including mono-nitrogen azoles (oxazoles, thiazoles and carbazoles), bis-nitrogen azoles (imidazoles, pyrazoles and benzimidazoles) and tri-nitrogen azoles (triazoles and benzotriazoles) as well as tetrazole derivatives. It was hoped that this review would be helpful for the design and development of highly efficient azole derivatives with high bioactivity and low toxicity.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1196NO – PubChem

 

New explortion of 189028-95-3

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Reference of 189028-95-3, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 189028-95-3, Name is (S)-3-((S)-5-(4-Fluorophenyl)-5-hydroxypentanoyl)-4-phenyloxazolidin-2-one, molecular formula is C20H20FNO4. In a Patent£¬once mentioned of 189028-95-3

PROCESSES FOR PRODUCTION OF PHENOLIC 4-BIPHENYLYLAZETIDIN-2-ONES

The present invention relates to processes for the production of phenolic 4-biphenylylazetidin-2-one derivatives Formula (1)

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2823NO – PubChem

 

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An intermolecular hydroamination of allenamides with arylamines catalyzed by cationic Au(I) salts

(Figure presented) An intermolecular hydroamination of allenamides with arylamines has been achieved under mild Au(I) catalysis conditions delivering allylamino E-enamides stereoselectively and in high yield. The reaction is made possible via a convenient method for conjugated N-acyliminium formation.

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Can You Really Do Chemisty Experiments About 875444-08-9

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PYRIDYL OXAZOLIDINONE CETP INHIBITOR

The compound of Formula I, including pharmaceutically acceptable salts, is a CETP inhibitor, and is useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula 1, R is H or C1-6alkyl optionally substituted with 1-3 halogens: (Formula I).

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Oxazolidine – Wikipedia,
Oxazolidine | C3H2778NO – PubChem

 

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PESTICIDAL COMPOSITIONS AND RELATED METHODS

A pesticidal composition comprises at least one compounds selected from a compound of formula, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, Q, Z, L, La, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.

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Oxazolidine – Wikipedia,
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