- Synthesis of Some Aromatic and Aliphatic Esters Using WO3/ZrO2 Solid Acid Catalyst under Solvent Free Conditions
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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.
- Guguloth, Vijaya Charan,Battu, Satyanarayana
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p. 2153 - 2157
(2020/09/16)
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- FUSED BICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE
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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.
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Paragraph 00196; 00277
(2019/03/05)
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- Pyridyl Radical Cation for C?H Amination of Arenes
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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.
- R?ssler, Simon L.,Jelier, Benson J.,Tripet, Pascal F.,Shemet, Andrej,Jeschke, Gunnar,Togni, Antonio,Carreira, Erick M.
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supporting information
p. 526 - 531
(2019/01/04)
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- Direct and practical synthesis of primary anilines through iron-catalyzed C-H bond amination
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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.
- Legnani, Luca,Cerai, Gabriele Prina,Morandi, Bill
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p. 8162 - 8165
(2018/05/22)
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- Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis
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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.
- 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
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supporting information
p. 2423 - 2435
(2016/04/10)
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- TRANSITION METAL-CATALYZED IMIDATION OF ARENES
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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).
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Paragraph 00260; 00261
(2015/03/13)
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- 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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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.
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Paragraph 0416; 0417
(2014/06/23)
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- Pd-catalyzed aryl C-H imidation with arene as the limiting reagent
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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.
- Boursalian, Gregory B.,Ngai, Ming-Yu,Hojczyk, Katarzyna N.,Ritter, Tobias
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supporting information
p. 13278 - 13281
(2013/09/24)
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- DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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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.
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Paragraph 0740
(2013/04/10)
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- DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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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.
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Page/Page column 146
(2013/04/13)
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- Structure-activity relationship of the 7-hydroxy benzimidazole analogs as glycogen synthase kinase 3β inhibitor
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Design, synthesis and the GSK3β inhibitory activities of the 7-hydroxy benzimidazole analogs are described. The solid-phase synthetic route was also developed for preparation of the analogs consisting of the novel ATP competitive scaffold. In addition, th
- Lee, Seung-Chul,Shin, Dongkyu,Cho, Joong Myung,Ro, Sunggu,Suh, Young-Ger
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scheme or table
p. 1891 - 1894
(2012/04/04)
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- Antileishmanial activity screening of 5-nitro-2-heterocyclic benzylidene hydrazides
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A series of 53 nitro derivatives rationally designed were obtained by parallel synthesis and screened against Leishmania donovani. Six compounds exhibited IC50 values lower than standard drugs. Brief SAR analysis revealed that substitution is important to the activity. Nitrothiophene analogues were more potent than the nitrofuran ones. This was attributed to the ability of sulfur atoms in accommodating electrons from nitro group, which facilitate its reduction and therefore the formation of free radicals lethal to parasites.
- Rando, Daniela G.,Avery, Mitchell A.,Tekwani, Babu L.,Khan, Shabana I.,Ferreira, Elizabeth I.
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p. 6724 - 6731
(2008/12/22)
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- UREA DERIVATIVES USEFUL AS CALCIUM RECEPTOR MODULATORS
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The present invention provides compounds of formula (I): in which Y is oxygen or sulphur; R1 and R”1 are optionally substituted aryl, heteroaryl or a fused ring structure, R2and R'2 are each H, or optionally substituted alkyl, alkylaminoalkyl or dialkylaminoalkyl, or R2 and R'2 and their N form a saturated or unsaturated optionally substituted heterocycle, R3 represents a group of formula -(CH2)P-Ar-Rn, wherein p is 0 or 1 and, when p is 1, is optionally substituted, Ar is aryl or heteroaryl, and each R is H, halogen; hydroxyl; trifiuoromethyl; linear and branched alkyl, alkenyl, alkynyl, and alkoxyl groups, all optionally further substituted by one or more of hydroxy groups, halogen atoms, alkoxy groups, amino groups, and alkylthio groups; linear and branched alkoxyl groups; linear and branched thioalkyl groups; aryl groups; aralkyl groups; aralkoxy groups; aryloxy groups; perfluoroalkyl; -CN; -NR4R5, -C(=X)NR4R5,-O-C(=X)NR4R5, -SO2NR4R5, - Alk-NR4R5, -NZC(=X)(NH)qR6, -Alk-NZC(=X)(NH)qR6, -C(=X)R6, -Alk-C(=X)(NH)qR6, -NHSO2R7, -SO2R7, -SOR7, -SR7, or is a saturated or unsaturated heterocyclyl group, and salts and esters thereof, are useful in the treatment of conditions susceptible to modulating ion channels, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.
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Page/Page column 49
(2008/06/13)
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- Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3β
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A hydroxy functional group was introduced as the hydrogen bond donor and acceptor at the hinge region of protein kinase in order to develop novel ATP-competitive inhibitors. Several derivatives of 7-hydroxyl-1H-benzoimidazole were designed as inhibitors o
- Shin, Dongkyu,Lee, Seung-Chul,Heo, Yong-Seok,Lee, Woon-Young,Cho, Yong-Soon,Kim, Yong Eun,Hyun, Young-Lan,Cho, Joong Myung,Lee, Yoon Sup,Ro, Seonggu
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p. 5686 - 5689
(2008/04/03)
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- 4-METHOXYACRIDINE-1-CARBOXAMIDE DERIVATIVES AND THE PHENAZINE AND OXANTHRENE ANALOGS AS PDE4-INHIBITORS FOR THE TREATMENT OF ASTHMA AND CHRONIC PULMONARY DISEASE (COPD)
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The present invention relates to new Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) for treatment of asthma: Ar is a substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heterocyclic ring or substituted or unsubstituted heteroaryl ring; each occurrence of L is O, S or NR 3; X and A are independently-CRaRb-,-CRa-,-C(=B)-, O, S(O)m, N or NR3; each occurrence of m is 0, 1, or 2; n is 0-4; p is 0-2; Y is-C(=B)C(=D)NR 4 or-C(=B)NR4 B is O, S or NRa; D is O, S or NRa; The other substituents are defined in the claims.
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Page/Page column 28
(2010/11/08)
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- GLYCOGEN SYNTHASE KINASE 3BETA INHIBITOR, COMPOSITION AND PROCESS FOR THE PREPARATION THEREOF
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Novel compounds having hydroxybenzoimidazole carboxylic amide are useful for inhibiting glycogen synthase kinase 3β (GSK-3β).
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- Antitumor agents 222. Synthesis and anti-androgen activity of new diarylheptanoids
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Fifteen new diarylheptanoids were synthesized and evaluated for antagonistic activity against androgen receptor (AR)-mediated reporter gene transcription using DU145, PC-3, and LNCaP prostate cancer cell lines. Most compounds showed activity in a 5α-dihydrotestosterone (DHT)-induced reporter gene expression assay in DU145 cells transfected with wild-type AR. Ten compounds (5, 8, 10, 14-15, and 18-22) were equipotent with hydroxyflutamide (HF), the anti-androgen currently available for the treatment of prostate cancer. However, except for compounds 5 and 10, none of the tested compounds was significantly effective in attenuating DHT-induced reporter gene expression in LNCaP cells, which contain endogenous mutant AR.
- Ohtsu, Hironori,Itokawa, Hideji,Xiao, Zhiyan,Su, Ching-Yuan,Shih, Charles C.-Y.,Chiang, Tzuying,Chang, Eugene,Lee, YiFen,Chiu, Shang-Yi,Chang, Chawnshang,Lee, Kuo-Hsiung
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p. 5083 - 5090
(2007/10/03)
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- Thiourea and benzamide compounds, compositions and methods of treating or preventing inflammatory diseases and atherosclerosis
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The present invention provides compounds of formula (I). The present invention also provides methods of treating or preventing inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of formula (I).
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