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Copper acetylides are readily available and especially convenient reagents for the alkynylation of a broad range of heteronucleophiles. Upon simple activation with molecular oxygen in the presence of suitable ligands and solvents, they readily transfer their alkyne moiety at room temperature, notably yielding a variety of nitrogen- and phosphorus-substituted alkynes. We report in this manuscript an extensive study of the chemoselectivity of this alkynylation based on quantitative 13C NMR analyses. With suitable ligand/solvent combinations, various phosphorus-based nucleophiles can be alkynylated with excellent levels of selectivity, even in the presence of a large excess of a nitrogen-nucleophile. This chemoselective alkynylation could be further extended to an even more challenging selective alkynylation of a nitrogen-nucleophile over another one, further highlighting the synthetic potential of copper acetylides as alkynylating agents that can selectively ?fish? a nucleophile without affecting others.

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Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.

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The synthesis of racemic Carvedilol ((±)-1) has been achieved starting from 2-(chloromethyl) oxirane ((±)-2) in a four-step sequence. 5-(Chloromethyl) oxazolidin-2-one ((±)-3) and 5-((9Hcarbazol-4-yloxy) methyl) oxazolidin-2-one ((±)-4) are intermediates. A similar sequence starting from (R)- or (S)-2-(chloromethyl)oxirane 2 give corresponding chiral 5-((9Hcarbazol-4-yloxy)methyl) oxazolidin-2-one 4 followed by chiral Carvedilol 1. The synthetic sequence followed avoids the formation of impurity B (bis impurity). This approach can be useful for the preparation of pharmaceutically important moieties containingbeta-amino alcohols without formation of bis impurity.

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Chemistry can be defined as the study of matter and the changes it undergoes. Recommanded Product: 5-(Chloromethyl)oxazolidin-2-one. You’ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.Recommanded Product: 5-(Chloromethyl)oxazolidin-2-one, Name is 5-(Chloromethyl)oxazolidin-2-one, molecular formula is C4H6ClNO2, introducing its new discovery.

(Chemical Equation Presented) Halohydrin dehalogenase from Agrobacterium radiobacter catalyzed the enantioselective ring opening of terminal epoxides with cyanate as a nucleophile, yielding 5-substituted oxazolidinones in high yields and with high enantiopurity (69-98% ee). This is the first example of the biocatalytic conversion of a range of epoxides to the corresponding oxazolidinones.

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Objective: The main objective of our present study, is to potentiate the antibacterial activity of biphenyl chalcones and oxazolidinones, thus in order to achieve the potent antibacterial agents, we coupled both derivatives by using green chemistry approach for Buchwald?s protocol under ultrasound irradiation. Methodology: Ultrasonication technique was used to couple a series of 24 novel bromo-biphenyl-chalcone derivatives and 5-chloromethyl-oxazolidinone in the presence of copper iodide (CuI) (10 mol %) for the amidation of chalcones and (±)-trans-1,2-diaminocyclohexane was used to solubilize CuI and potassium carbonate (K2CO3) as base, which provided the products in good yields after short reaction times under mild conditions. Results and Discussion: Herewith we report the synthesis of 24 novel oxazolidinone-biphenyl chalcone hybrid derivatives (7a-7x). All the synthesized compounds were characterized by spectral data and evaluated for in vitro antibacterial and antifungal activities. Antibacterial and antifungal activities were tested using the serial dilution method. From the screening studies it was observed that compounds 7c to 7g have shown significant antibacterial activities against the both the strains of gram-positive and gram-negative bacteria at 3.125 mug/ml when compared to the standard drugs ciprofloxacin and linezolid and were as other compounds showed moderate to weak activities. In case of antifungal studies the compounds 7e-7g showed moderate activities at 12.5 mug/ml compared to standard fluconazole and whereas other compounds showed weak activities. Conclusion: We have developed an experimentally simple, efficient, short time and high yielding CuI-mediated N-arylation of oxazolidinones under ultrasound irradiation with a simple set up at room temperature. This approach would be a worthwhile in the development of green chemistry protocols. Compounds 7c to 7g have shown significant antibacterial activities against the both the strains of gram-positive and gram-negative bacteria.

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An efficient and practical aluminium-catalysed approach towards a range of functional oxazolidinones is reported. The method is based on cheap and readily available starting materials including terminal and internal (bicyclic) epoxides and phenyl carbamate. The oxazolidinones serve as highly useful synthons for the high yield preparation of non-symmetrical ureas by nucleophilic ring-opening affording the targeted urea compounds with excellent functional group diversity, high regioselectivity and isolated yields up to >99%.

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Objective: The main objective of our present study, is to potentiate the antibacterial activity of biphenyl chalcones and oxazolidinones, thus in order to achieve the potent antibacterial agents, we coupled both derivatives by using green chemistry approach for Buchwald?s protocol under ultrasound irradiation. Methodology: Ultrasonication technique was used to couple a series of 24 novel bromo-biphenyl-chalcone derivatives and 5-chloromethyl-oxazolidinone in the presence of copper iodide (CuI) (10 mol %) for the amidation of chalcones and (±)-trans-1,2-diaminocyclohexane was used to solubilize CuI and potassium carbonate (K2CO3) as base, which provided the products in good yields after short reaction times under mild conditions. Results and Discussion: Herewith we report the synthesis of 24 novel oxazolidinone-biphenyl chalcone hybrid derivatives (7a-7x). All the synthesized compounds were characterized by spectral data and evaluated for in vitro antibacterial and antifungal activities. Antibacterial and antifungal activities were tested using the serial dilution method. From the screening studies it was observed that compounds 7c to 7g have shown significant antibacterial activities against the both the strains of gram-positive and gram-negative bacteria at 3.125 mug/ml when compared to the standard drugs ciprofloxacin and linezolid and were as other compounds showed moderate to weak activities. In case of antifungal studies the compounds 7e-7g showed moderate activities at 12.5 mug/ml compared to standard fluconazole and whereas other compounds showed weak activities. Conclusion: We have developed an experimentally simple, efficient, short time and high yielding CuI-mediated N-arylation of oxazolidinones under ultrasound irradiation with a simple set up at room temperature. This approach would be a worthwhile in the development of green chemistry protocols. Compounds 7c to 7g have shown significant antibacterial activities against the both the strains of gram-positive and gram-negative bacteria.

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Reference:
Oxazolidine – Wikipedia,
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In the present study, in order to synthesize broad-spectrum antibacterial agents, we coupled both the oxazolidinone and novel thiophene chalcone derivatives by using Buchwald’s protocol under ultrasound irradiation. All the newly synthesized 20 oxazolidinone-thiophene chalcone hybrid compounds were characterized by IR,1HNMR and Mass spectral analysis and evaluated for in vitro antibacterial and antifungal activities. Antibacterial and antifungal activities were tested using the serial dilution method. The test compounds 7e to 7g exhibited very high activities at 3.125 mug/ml when compared to the standard drug linezolid and were as other compounds showed moderate to weak activities. In case of antifungal activities, the test compounds 7e to 7g, 7i,7j, and 7m to 7o exhibited moderate activities compared to the standard fluconazole, whereas the rest of the compounds showed weak activities against tested fungal strains. The binding mode analysis of the test compounds 7e to 7g were investigated by the docking studies using Glide 6.6., inside the active site of peptidyl transferase center of E.coli ribosome (PDB ID: 2AW4), revealed that the experimental results were comparable to that of co-crystallized ligand linezolid.

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Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

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