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Cobalt-Copper Catalyzed C(sp2) ? N Cross Coupling of Amides or Nitrogenated Heterocycles with Styrenyl or Aryl Halides

An efficient C(sp2) ? N cross coupling of cyclic and acyclic amides with styrenyl/aryl/heteroaryl halides catalyzed by cobalt acetylacetonate in combination with copper(I) iodide, has been achieved. A library of diversely substituted cyclic and acyclic enamides have been obtained in high yields by this procedure. The reaction is stereoselective producing (E)?enamides from trans-styrenyl halides and (Z)- products from cis-halides. This procedure has been successfully employed for the coupling of other N-heterocycles such as pyrazole, imidazole and triazole with aryl/styrenyl/heteroaryl halides to produce the corresponding N-coupled products. A probable mechanism has been suggested.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H556NO – PubChem

 

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Electrolytic partial fluorination of organic compounds. Part 78: Regioselective anodic fluorination of 2-oxazolidinones

Various 2-oxazolidinones were galvanostatically electrooxidized in the presence of various fluoride salts. It was found that a fluorine atom was introduced to the alpha-position of the nitrogen atom of N-acyl- and N-alkoxycarbonyl-2-oxazolidinones to provide the corresponding alpha-fluorinated products in moderate to good yields. In the case of N-phenoxycarbonyl derivative, fluorination took place on the phenyl group selectively.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H396NO – PubChem

 

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The role of oxazolidine derivatives in the treatment of infectious and chronic diseases

Background: Despite being known for their antibacterial activity, the oxazolidines are molecules with wide pharmacological action and may act as anticonvulsants, anti-inflammatory and antineoplasic agents. However, such activities have been poorly explored and only two oxazolidinic derivatives hit the market until now. Therefore, this review covers the main biological activities of oxazolidines, indicating which of the classes and substituents have the best biological results as well as the synthesis methodology used to obtain them. Methods: The search for bibliographic data was made using a question focused on the oxazolidine structure and their respective activities, besides using inclusion/exclusion criteria clearly defined. The selected papers were subjected to qualitative content analysis methodology to be used in this review. Results: The oxazolidines remain excellent candidates for antibacterial, presenting three compounds in clinical testing phase (Radezolide, Cadezolide and Sutezolide), besides being a good candidate as antitubercular agents. Other less explored activities have niches with a great therapeutic potential such as the oxazolidines acting on 5-HT receptors (anticonvulsant) and Zolmitriptan (anti-migraine), and also mefloquine-oxazolidine derivatives which may act as antineoplasic and antitubercular agents. Conclusion: This review summarizes the versatility and great therapeutic potential that oxazolidines can offer, reinforcing the need for further studies and investments for this class of molecules.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H366NO – PubChem

 

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NOVEL BENZODIOXANE-PIPERIDINE DERIVATIVES AND THEIR THERAPEUTIC APPLICATIONS FOR TREATING NEUROPSYCHIATRIC DISORDERS

The present invention concerns benzodioxane-piperidine with general formula I: wherein notably: R1 represents one or more identical or different substituent(s) on the benzene ring, each independently representing a hydrogen or halogen atom, or a C1-4 alkyl group, or a C1-4 alkoxy group or a C1-4 hydroxyalkyl group or a C1-4 alkylcarbonyl or an alkoxycarbonyl group or an OH group or an SO2R group with R alkyl, or a CN group, or a CF3 group, or an OCF 3 group; n=1, 2 or 3; m=0 or 1, and R2 represents one or more identical or different substituent(s) on the oxazolidinone or morpholinone ring, each independently representing: a hydrogen atom, a C1-4 alkyl group, or a C1-4 alkoxy group, or a C1-4 hydroxyalkyl group, or an alkylcarbonyl group, or an alkoxycarbonyl group, or an alkoxyphenyl group.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H225NO – PubChem

 

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Simultaneous quantification of haemoglobin adducts of ethylene oxide, propylene oxide, acrylonitrile, acrylamide and glycidamide in human blood by isotope-dilution GC/NCI-MS/MS

Haemoglobin adducts are highly valuable biomarkers of cumulative exposure to carcinogenic substances. We have developed and applied an analytical method for the simultaneous quantification of five haemoglobin adducts of important occupational and environmental carcinogens. The N-terminal adducts were determined with gas chromatography as pentafluorophenylthiohydantoine derivatives according to the modified Edman-procedure and subsequent acetonization of the glycidamide adduct N-(R,. S)-2-hydroxy-2-carbamoylethylvaline (GAVal). The use of self-synthesized labelled internal standards in combination with tandem mass spectrometry using negative chemical ionisation guarantees both high accuracy and sensitivity of our determination. The limit of detection for N-2-hydroxyethylvaline (HEVal), N-(R,. S)-2-hydroxypropylvaline (HPVal), N-2-carbamoylethylvaline (AAVal) and N-(R,. S)-2-hydroxy-2-carbamoylethylvaline (GAVal) was 2 pmol/g globin, for N-2-cyanoethylvaline (CEVal) it was determined as 0.5 pmol/g globin, which was sufficient to determine the background levels of these adducts in the non-smoking general population. The between-day-precision for all analytes using a human blood sample as quality control material ranged from 4.7 to 12.3%. We investigated blood samples of a small group (n= 104) of non-smoking persons of the general population for the background levels of these haemoglobin adducts. The median values for HEVal, HPVal, CEVal, AAVal and GAVal in a group of 92 non-smoking persons were 18.1, 4.1, <0.5, 29.9 and 35.2 pmol/g globin, respectively. The adduct levels in 12 persons reporting exposure to passive smoke at home were similar for most adducts with median values of 17.2, 4.1, 1.0, 24.9 and 29.7 pmol/g globin for HEVal, HPVal, CEVal, AAVal and GAVal, respectively. Our results point to an elevated uptake of acrylonitrile caused by passive smoking as indicated by higher levels of the corresponding haemoglobin adduct CEVal. A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 497-25-6 Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H962NO – PubChem

 

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NEW PHOSPHORYLATING AGENTS FOR GENERAL SYNTHESIS OF MIXED PHOSPHATE ESTERS

An effective procedure has been developed for the general synthesis of mixed alkyl or aryl phosphate esters by metal-catalyzed phosphorylation of alcohols with aryl bis(2-oxo-3-oxazolinyl)phosphinate.Among metallic acetylacetonates examined as catalysts, the zirconium complex was the most effective as in activity order of Zr(IV)> Ce(III)> Zn(II)> Mn(III)> Mn(II)-complexes.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H851NO – PubChem

 

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Synthetic study of diversifolin: The construction of 11-oxabicyclo[6.2.1] undec-3-ene core using ring-closing metathesis

Stereoselective synthesis of a potential intermediate bearing 11-oxabicyclo[6.2.1]undec-3-ene core, a common scaffold of biologically active germacrane-type sesquiterpenes, has been achieved. Synthetic features involve formal 1,3-asymmetric induction, unusual ring-closing metathesis constructing a 10-membered carbocycle system, and unique lactone transposition.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H854NO – PubChem

 

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Cobalt-catalyzed intermolecular C(sp2)-O cross-coupling

Cobalt(II)-catalyzed C(sp2)-O cross-coupling between aryl/heteroaryl alcohols and vinyl/aryl halides in the presence of CuI has been achieved under ligand-free conditions. In this reaction, copper plays a significant role in transmetalation rather than being directly involved in the C-O coupling. This unique Co/Cu-dual catalyst system provides an easy access to a library of aryl-vinyl, heteroaryl-styryl, aryl-aryl, and heteroaryl-heteroaryl ethers in the absence of any ligand or additive.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H712NO – PubChem

 

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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Farrell and a compound is mentioned, 497-25-6, Oxazolidin-2-one, introducing its new discovery. 497-25-6

Revitalizing the drug pipeline: AntibioticDB, an open access database to aid antibacterial research and development

The current state of antibiotic discovery, research and development is insufficient to respond to the need for new treatments for drug-resistant bacterial infections. The process has changed over the last decade, with most new agents that are in Phases 1-3, or recently approved, having been discovered in small- and medium-sized enterprises or academia. These agents have then been licensed or sold to large companies for further development with the goal of taking them to market. However, early drug discovery and development, including the possibility of developing previously discontinued agents, would benefit from a database of antibacterial compounds for scrutiny by the developers. This article describes the first free, open-access searchable database of antibacterial compounds, including discontinued agents, drugs under pre-clinical development and those in clinical trials: AntibioticDB (AntibioticDB.com). Data were obtained from publicly available sources. This article summarizes the compounds and drugs in AntibioticDB, including their drug class, mode of action, development status and propensity to select drug-resistant bacteria. AntibioticDB includes compounds currently in pre-clinical development and 834 that have been discontinued and that reached varying stages of development. These may serve as starting points for future research and development.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H516NO – PubChem

 

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Regioselective 4-amino-de-chlorination of trichloro- and dichloro-pyrimidines with N-sodium carbamates

4-N-Alkoxycarbonylamino-2,6-dichloro- and -2-chloro-pyrimidines have been synthesized in good to excellent regioselectivity and yields from N-sodium carbamates and, respectively, 2,4,6-trichloropyrimidine and 2,4-dichloropyrimidine, in DMF, rt, 15-30 min. The reaction is effective also with 4,6-dichloropyrimidine, producing 4-N-alkoxycarbonylamino-6-chloropyrimidines in good yields. Some conformational features of 4-N-alkoxycarbonylamino-2,6-dichloro-pyrimidines have been investigated by X-ray diffraction and 1H NMR spectroscopy.

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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H832NO – PubChem