- Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a -agonist δ-antagonist and δ-inverse agonists
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Enantiomeric N-phenethyl-m-hydroxyphenylmorphans with various substituents in the ortho, meta or para positions of the aromatic ring in the phenethylamine side-chain (chloro, hydroxy, methoxy, nitro, methyl), as well as a pyridylethyl and a indolylethyl m
- Cheng, Kejun,Kim, In Jong,Lee, Mei-Jing,Adah, Steven A.,Raymond, Tyler J.,Bilsky, Edward J.,Aceto, Mario D.,May, Everette L.,Harris, Louis S.,Coop, Andrew,Dersch, Christina M.,Rothman, Richard B.,Jacobson, Arthur E.,Rice, Kenner C.
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- Probing the TCDD receptor: Synthesis of 5,6-dihydro-6a,11,11b- triazabenzo[a]fluorene · PF6, a potential ligand
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With the aim of investigating whether the ability of omeprazole (3) to activate the TCDD receptor is due to an internal cyclization process, 5,6- dihydro-6a,11,11b-triazabenzo[a]fluorene · PF6 (6) (X=PF6) has been designed and synthe
- Tholander, Joakim,Bergman, Jan
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- Longer-Lived Ruthenium Olefin Metathesis Catalysts Supported by Hemi-Labile Carbene Ligands
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Contemplated subject matter disclosed herein relates generally to organometallic olefin metathesis catalysts, and more particularly to longer-lived olefin metathesis catalysts supported by hemi-labile carbene ligands that bear an arm with one or more donor ligands, as well as the use of such catalysts in metathesis reactions of olefins and olefin compounds. The contemplated subject matter has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry. This contemplated subject matter serves to reduce the cost of olefin metathesis (OM) processes including in olefin metathesis polymerizations, conversion of vegetable oils into chemicals, and processes in the petrochemical industry. This contemplated subject matter reduces the cost of OM processes by providing OM catalysts that are longer-lived and lead to higher turnover numbers, hence requiring less catalyst to convert a given amount of substrate(s). Considering that the OM catalyst is the most expensive part of some OM processes, longer-lived OM catalysts have the benefit of reducing the overall cost of the OM processes.
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Paragraph 0074
(2021/05/14)
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- Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy
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Tuberculosis, caused by Mycobacterium tuberculosis, is still one of the leading infectious diseases globally. Therefore, novel approaches are needed to face this disease. Efflux pumps are known to contribute to the emergence of M. tuberculosis drug resistance. Thioridazine has shown good anti-TB properties both in vitro and in vivo, likely due to its capacity to inhibit efflux mechanisms. Here we report the design and synthesis of a number of putative efflux inhibitors inspired by the structure of thioridazine. Compounds were evaluated for their in vitro and ex vivo activity against M. tuberculosis H37Rv. Compared to the parent molecule, some of the compounds synthesized showed higher efflux inhibitory capacity, less cytotoxicity, and a remarkable synergistic effect with anti-TB drugs both in vitro and in human macrophages, demonstrating their potential to be used as coadjuvants for the treatment of tuberculosis.
- Pieroni, Marco,Machado, Diana,Azzali, Elisa,Santos Costa, Sofia,Couto, Isabel,Costantino, Gabriele,Viveiros, Miguel
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supporting information
p. 5842 - 5853
(2015/08/24)
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- Copper-chelating azides for efficient click conjugation reactions in complex media
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The concept of chelation-assisted copper catalysis was employed for the development of new azides that display unprecedented reactivity in the copper(I)-catalyzed azide-alkyne [3+2] cycloaddition (CuAAC) reaction. Azides that bear strong copper-chelating moieties were synthesized; these functional groups allow the formation of azide copper complexes that react almost instantaneously with alkynes under diluted conditions. Efficient ligation occurred at low concentration and in complex media with only one equivalent of copper, which improves the biocompatibility of the CuAAC reaction. Furthermore, such a click reaction allowed the localization of a bioactive compound inside living cells by fluorescence measurements. Chelating azides were designed to form clickable copper complexes for efficient ligation with alkynes in complex biological media. Among a series of azides that bear nitrogen heterocycles, a bis(triazole) azide allowed ultra-fast click reactions with alkynes within seconds under diluted conditions. The reactivity and stability of this copper complex enabled efficient click reactions inside living cells.
- Bevilacqua, Valentina,King, Mathias,Chaumontet, Manon,Nothisen, Marc,Gabillet, Sandra,Buisson, David,Puente, Celine,Wagner, Alain,Taran, Frederic
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supporting information
p. 5872 - 5876
(2014/06/10)
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- Addition/elimination reactions of ethylsulfonyl pyridines: Stereoselective synthesis of vinylpyridine allylic alcohols
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2-(Phenylsulfonyl)ethyl pyridines can be coupled with aldehydes leading directly to sulfone-eliminated vinylpyridine allylic alcohols. These products are obtained in good yield and with high levels of stereocontrol.
- O'Neil, Gregory W.,Drake, Nathan D.,Storvick, Jennifer M.
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supporting information
p. 715 - 717
(2013/02/23)
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- Synthesis, structures of (aminopyridine)nickel complexes and their use for catalytic ethylene polymerization
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A series of α-aminopyridines in the form of (2,6-C6H 3N)(R1)(CHR2NR3R4) (R1 = R2 = H R3 = H R4 = iPr (L1a), R4 = tBu (L1b), R4 = Ph (L1c), R4 = 2,6-Me2C6H3 (L1d), R4 = 2,6-iPr2C6H3 (L1e), R1 = R2 = H R3 = R4 = Et (L1f), R1 = H R2 = Me R3 = H R4 = iPr (L2a), R4 = Ph (L2c), R4 = 2,6-Me 2C6H3 (L2d), R4 = 2,6- iPr2C6H3 (L2e), R1 = Me R2 = H R3 = H R4 = 2,6-iPr 2C6H3 (L3e)) and β-aminopyridines in the form of (2-C6H4N)(CH2CH2NR 1R2) (R1 = H R2 = iPr (4a), R2 = tBu (L4b), R1 = R2 = Et (L4f)) have been prepared. Their corresponding halonickel complexes 1a-4f are synthesized by ligand substitution from (DME)NiBr2 and the molecular structures are characterized. Four types of coordination modes include four-coordinate mononuclear species with one ligand, five-coordinate mononuclear species with two ligands, five-coordinate dinuclear species with two ligands, and a six-coordinate polymeric framework were determined by X-ray crystallography. Using methylaluminoxanes (MAO) as the activator, the nickel complexes can catalyze ethylene polymerization under moderate pressure and ambient temperature. The activity reaches 105 g PE mol-1 Ni h. The PE products with high branching and high crystallinity have M n ~ 103 with PDI 2.
- Lin, Ya-Chi,Yu, Kuo-Hsuan,Lin, Ya-Fan,Lee, Gene-Hsiang,Wang, Yu,Liu, Shiuh-Tzung,Chen, Jwu-Ting
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experimental part
p. 6661 - 6670
(2012/08/08)
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