24812-90-6Relevant academic research and scientific papers
Synthesis of Some Aromatic and Aliphatic Esters Using WO3/ZrO2 Solid Acid Catalyst under Solvent Free Conditions
Guguloth, Vijaya Charan,Battu, Satyanarayana
, p. 2153 - 2157 (2020/09/16)
A simple method is delineated for the synthesis of substituted ester products in superior yields by esterification reaction under solvent unbound condition using tungsten upgraded ZrO2 solid acid catalyst at 353 K. The WO3/ZrO2 catalyst has been prepared by using impregnation method followed by calcination at 923 K over a period of 6 h in air atmosphere. SEM, XRD, FTIR, and BET surface area techniques were used to categorize this catalyst. Zirconia has both acidic and basic possessions which can be changed by incorporating suitable promoter atom like tungsten which in turn increases the surface area thereby enhancing the surface acidity. Impregnation of W6+ ions exhibits a strong influence on phase modification of zirconia from thermodynamically solid monoclinic to metastable tetragonal phase. Amalgamation of promoter W6+ will stabilize tetragonal phase which is active in catalyzing reactions. In esterification reaction WO3/ZrO2 catalyst was found to be stable, efficient and environmental friendly, effortlessly recovered by filtration, excellent yield of product and can be reusable efficiently.
FUSED BICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE
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Paragraph 00196; 00277, (2019/03/05)
Fused bicyclic compounds and uses thereof in medicine. In particular, provided are fused bicyclic compounds used as ASK1 active regulator and and use of the compounds in the manufacture of a drug for treating a disease regulated by ASK1. Further provided are a pharmaceutical composition and a method of treating a disease regulated by ASK1 comprising administering the compounds or pharmaceutical composition thereof.
Pyridyl Radical Cation for C?H Amination of Arenes
R?ssler, Simon L.,Jelier, Benson J.,Tripet, Pascal F.,Shemet, Andrej,Jeschke, Gunnar,Togni, Antonio,Carreira, Erick M.
supporting information, p. 526 - 531 (2019/01/04)
Electron-transfer photocatalysis provides access to the elusive and unprecedented N-pyridyl radical cation from selected N-substituted pyridinium reagents. The resulting C(sp2)?H functionalization of (hetero)arenes furnishes versatile intermediates for the development of valuable aminated aryl scaffolds. Mechanistic studies that include the first spectroscopic evidence of a spin-trapped N-pyridyl radical adduct implicate SET-triggered, pseudo-mesolytic cleavage of the N?X pyridinium reagents mediated by visible light.
Direct and practical synthesis of primary anilines through iron-catalyzed C-H bond amination
Legnani, Luca,Cerai, Gabriele Prina,Morandi, Bill
, p. 8162 - 8165 (2018/05/22)
The direct C-H amination of arenes is an important strategy to streamline the discovery and preparation of functional molecules. Herein, we report an operationally simple arene C-H amination reaction that, in contrast to most literature precedent, affords directly the synthetically versatile primary aniline products without relying on protecting group manipulations. Inexpensive Fe(II)-sulfate serves as a convenient catalyst for the transformation. The reaction tolerates a wide scope of arenes, including structurally complex drugs. Importantly, the arene substrates are used as limiting reagents in the transformation. This operationally simple transformation should considerably accelerate the discovery of medicines and functional molecules.
Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis
Heimburg, Tino,Chakrabarti, Alokta,Lancelot, Julien,Marek, Martin,Melesina, Jelena,Hauser, Alexander-Thomas,Shaik, Tajith B.,Duclaud, Sylvie,Robaa, Dina,Erdmann, Frank,Schmidt, Matthias,Romier, Christophe,Pierce, Raymond J.,Jung, Manfred,Sippl, Wolfgang
supporting information, p. 2423 - 2435 (2016/04/10)
Schistosomiasis is a major neglected parasitic disease that affects more than 265 million people worldwide and for which the control strategy consists of mass treatment with the only available drug, praziquantel. In this study, a series of new benzohydroxamates were prepared as potent inhibitors of Schistosoma mansoni histone deacetylase 8 (smHDAC8). Crystallographic analysis provided insights into the inhibition mode of smHDAC8 activity by these 3-amidobenzohydroxamates. The newly designed inhibitors were evaluated in screens for enzyme inhibitory activity against schistosome and human HDACs. Twenty-seven compounds were found to be active in the nanomolar range, and some of them showed selectivity toward smHDAC8 over the major human HDACs (1 and 6). The active benzohydroxamates were additionally screened for lethality against the schistosome larval stage using a fluorescence-based assay. Four of these showed significant dose-dependent killing of the schistosome larvae and markedly impaired egg laying of adult worm pairs maintained in culture.
TRANSITION METAL-CATALYZED IMIDATION OF ARENES
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Paragraph 00260; 00261, (2015/03/13)
The present invention provides novel transition metal complexes (e.g., complexes of any one of Formulae (C1) to (C25)) that include an amine-N-oxide motif. The invention also provides methods of using these transition metal complexes in preparing N-aryl or N- heteroaryl sulfonimides (e.g., compounds of Formula (I)) and aryl or heteroaryl amines (e.g., compounds of Formula (II)). The inventive methods involve imidation of arenes and heteroarenes (e.g., compounds of Formula (A)) using an imidating agent (e.g., a compound of Formula (B), such as N-fluorobenzenesulfonimide (NFBS or NFSI)) in the presence of a single-electron reductant (e.g., an Ag(I) or Ru(II) salt).
1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Paragraph 0416; 0417, (2014/06/23)
Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
Pd-catalyzed aryl C-H imidation with arene as the limiting reagent
Boursalian, Gregory B.,Ngai, Ming-Yu,Hojczyk, Katarzyna N.,Ritter, Tobias
supporting information, p. 13278 - 13281 (2013/09/24)
An amine-N-oxide-ligated palladium complex, in conjunction with a silver cocatalyst, catalyzes imidation of arenes by the reagent N- fluorobenzenesulfonimide. The reaction enables imidation of a variety of arenes at or below room temperature, requires no coordinating directing group on the substrate, and gives synthetically useful yields with only 1 equiv of arene. Mechanistic data implicate an unusual mechanism devoid of commonly invoked organometallic intermediates: oxidation of the Pd catalyst occurs as the turnover-limiting step, while C-H bond functionalization occurs subsequently at a high oxidation state of the catalyst.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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Paragraph 0740, (2013/04/10)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 146, (2013/04/13)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
