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NOVEL CYCLIC HYDROCARBON COMPOUNDS FOR THE TREATMENT OF DISEASES

The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H90NO – PubChem

 

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Efficient and Divergent Synthesis of alpha-Halogenated Amides and Esters by Double Electrophilic Activation of Ynamides

An efficient and modular entry to alpha-halogenated amides and esters is reported. This reaction is based on an underestimated double electrophilic activation of ynamides sequentially involving highly reactive activated keteniminium and iminium ions. Upon simple reaction with HCl and an electrophilic halogenation reagent in the presence of water or an alcohol, a broad range of ynamides can be transformed, in a highly divergent manner, to alpha-halo amides and esters with high efficiency and under mild conditions.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1054NO – PubChem

 

The important role of Oxazolidin-2-one

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Highly exo-selective and enantioselective cycloaddition reactions of nitrones catalyzed by a chiral binaphthyldiimine-Ni(II) complex

(Chemical Equation Presented) Significant levels of exo-selectivity (exo:endo = >99:1 to 86:14) and enantioselectivity (95-82% ee) were obtained in the 1,3-dipolar cycloadditions of a number of nitrones with 3-(2-alkenoyl)-2-thiazolidinethiones, using the chiral binaphthyldiimine-Ni(II) complex (5-20 mol %), which was easily prepared form N,N?-bis(3,5- dichrolo-2-hydroxybenzylidene)-1,1?-binaphthyl-2,2?-diamine and Ni(ClO4)2·6H2O in CHCl3 in the presence of 4 A molecular sieves, as a chiral Lewis acid catalyst.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1029NO – PubChem

 

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Azides. Part VIII. Thermolysis of ethyl azidoformate in acetic and propionic anhydrides: facilitation of intramolecular cyclization of the resultant carbethoxynitrene to 2-oxazolidinone

The thermolysis of ethyl azidoformate in acetic and propionic anhydrides as solvent yielded the corresponding N-acyl-2-oxazolidinones (2a,b) in relatively significant yields.The other major products isolated were N-carboxyethyl-N,O-diacyl hydroxylamine (1a.b) and N,N,O-triacetyl hydroxylamine (3).The intramolecular cyclization is facilitated by the solvent.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H323NO – PubChem

 

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Nitroimidazoles: Part XVI – Some 1-Methyl-4-nitro-5-substituted Imidazoles

Treatment of 1-methyl-4-nitro-5-chloroimidazole (3) with 5-membered lactames, e.g. imidazolidinones, oxazolidinone and thiazolidinone affords N-imidazolyl derivatives (4a-d).Reaction of 3 with imidazole yields 4e; amino derivatives (4f-h) are similarly obtained. 2-Hydroxypyrazine, 4-hydroxyquinazoline and 3,4,5-trichlorophenol and 3 react to form O-derivatives (4i-k).Imidazole (11) is formed from 1-methyl-4-chloro-5-nitroimidazole (10).

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H319NO – PubChem

 

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Synthesis of allenamides by Pd-catalyzed coupling of 3-alkoxycarbonyloxy ynamides or 1-alkoxycarbonyloxy allenamides with arylboronic acids

An efficient palladium-catalyzed method is reported for the synthesis of multi-substituted allenamides by Suzuki-Miyaura cross-coupling reaction between easily prepared 3-alkoxycarbonyloxy ynamides or 1-alkoxycarbonyloxy allenamides and arylboronic acids. The Royal Society of Chemistry 2012.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H394NO – PubChem

 

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AgOTf-catalyzed reaction of sulfonyl hydrazones with ynamides led to stereoselective synthesis of alpha-amino alkenyl-substituted hydrazone derivatives

A novel method for the synthesis of alpha-amino alkenyl-substituted hydrazone derivatives was disclosed through silver-catalyzed reaction of sulfonyl hydrazones with ynamides. The present method features mild conditions, high stereoselectivity and good yields. The proposed mechanism involves silver-mediated generation of a keteniminium ion intermediate to facilitate the stereoselective addition of hydrazones in the presence of K2CO3, while pyrazole ring could not be constructed under the current conditions.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H397NO – PubChem

 

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Enantioselective organocatalytic michael addition of nitroalkanes and other nucleophiles to beta-trifluoromethylated acrylamides

An organocatalytic asymmetric Michael addition of nitroalkanes to trifluoromethylated acrylamides in good yields and with good to excellent diastereoselectivities and excellent enantioselectivities is described. The Michael adducts could be readily transformed into optically pure trifluoromethylated gamma-aminobutyric acid 7 in high yields without loss in enantioselectivities.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1129NO – PubChem

 

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History of antimicrobial drug discovery: Major classes and health impact

The introduction of antibiotics into clinical practice revolutionized the treatment and management of infectious diseases. Before the introduction of antibiotics, these diseases were the leading cause of morbidity and mortality in human populations. This review presents a brief history of discovery of the main antimicrobial classes (arsphenamines, beta-lactams, sulphonamides, polypeptides, aminoglycosides, tetracyclines, amphenicols, lipopeptides, macrolides, oxazolidinones, glycopeptides, streptogramins, ansamycins, quinolones, and lincosamides) that have changed the landscape of contemporary medicine. Given within a historical timeline context, the review discusses how the introduction of certain antimicrobial classes affected the morbidity and mortality rates due to bacterial infectious diseases in human populations. Problems of resistance to antibiotics of different classes are also extensively discussed.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H297NO – PubChem

 

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 497-25-6, name is Oxazolidin-2-one, introducing its new discovery. Application In Synthesis of Oxazolidin-2-one

Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors

Mutant isocitrate dehydrogenase 1 (IDH1) is an attractive therapeutic target for the treatment of various cancers such as AML, glioma, and glioblastoma. We have evaluated 3-pyrimidin-4-yl-oxazolidin-2-ones as mutant IDH1 inhibitors that bind to an allosteric, induced pocket of IDH1R132H. This Letter describes SAR exploration focused on improving both the in vitro and in vivo metabolic stability of the compounds, leading to the identification of 19 as a potent and selective mutant IDH1 inhibitor that has demonstrated brain penetration and excellent oral bioavailability in rodents. In a preclinical patient-derived IDH1 mutant xenograft tumor model study, 19 efficiently inhibited the production of the biomarker 2-HG.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1207NO – PubChem