- Chemical Consequences of the Mechanical Bond: A Tandem Active Template-Rearrangement Reaction
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We report the unexpected discovery of a tandem active template CuAAC-rearrangement process, in which N2 is extruded on the way to the 1,2,3-triazole product to give instead acrylamide rotaxanes. Mechanistic investigations suggest this process i
- Modicom, Florian,Jamieson, Ellen M. G.,Rochette, Elise,Goldup, Stephen M.
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supporting information
p. 3875 - 3879
(2019/02/24)
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- Organoiridium complex for organic electroluminescent elements
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The present invention provides an organometallic complex having a high quantum efficiency even in a polymer thin film as a emitting material for organic electroluminescent (EL) element. The present invention relates to an organoiridium complex for an organic electroluminescent element represented by the following Formula; wherein a C—N ligand including two atomic groups (A1, A2), and a β-diketone ligand in line symmetry having two tert-butyl-substituted phenyl groups are coordinated with an iridium atom. The organoiridium complex of the present invention has a high quantum efficiency even in a polymer thin film with respect to green to yellow electroluminescence. (In the aforementioned Formula, R1, R2, and R3 are each a tert-butyl group or a hydrogen atom, and have at least one tert-butyl group; they may bond each other to thereby form a saturated hydrocarbon ring, when having two tert-butyl groups; A1, A2 are each an unsaturated hydrocarbon ring, at least one is a single ring, and at least one is a heterocyclic ring).
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Page/Page column 22; 23
(2018/02/02)
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- Tropylium Ion Catalyzes Hydration Reactions of Alkynes
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The hydration of alkynes is one of the most atom-economic and versatile synthetic protocols to access carbonyl compounds. This fundamental reaction, however, often requires transition-metal catalysts or harsh reaction conditions to promote the addition of water to the carbon–carbon triple bond. In this work, it is demonstrated that the non-benzenoid aromatic tropylium ion can be used as an organic Lewis acid promoter for the hydration of alkynes under simple reaction conditions with excellent outcomes.
- Oss, Giulia,Ho, Junming,Nguyen, Thanh Vinh
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supporting information
p. 3974 - 3981
(2018/08/17)
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- ORGANIC IRIDIUM COMPLEX FOR ORGANIC ELECTROLUMINESCENCE ELEMENT
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A metallo-organic complex, which can realize an electroluminescence of high quantum efficiency and has high heat resistance as a luminescence material for an organic electroluminescence (EL) element. More particularly, an organic iridium complex for an organic EL element, wherein a C-N ligand having a substituent group of three-ring structure in which a hetero ring and two benzene rings are ring-fused and a β-diketone ligand including a propane-1,3-dione having two tert-butyl-substituted phenyl groups are coordinated with an indium atom. The present complex has a high heat resistance enough to contribute to increase in long service life of an organic EL element
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Paragraph 0036
(2016/12/01)
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- Design, synthesis and biological evaluation of nuclear receptor-degradation inducers
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Compounds that regulate the function(s) of nuclear receptors (NRs) are useful for biological studies and as candidate therapeutic agents. Most such compounds are agonists or antagonists. On the other hand, we have developed specific protein degradation in
- Itoh, Yukihiro,Kitaguchi, Risa,Ishikawa, Minoru,Naito, Mikihiko,Hashimoto, Yuichi
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experimental part
p. 6768 - 6778
(2012/01/13)
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- 4-PHENYL-1,3-THIAZOLES AND 4-PHENYL-1,3-OXAZOLES DERIVATIVES AS CANNABINOID RECEPTOR LIGANDS
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The present invention relates to new 4-phenyl-1,3-azole derivatives having the general formula (I) wherein R1, R2, R3, R4, X, A, B, and n are variable, in a racemic form, an enantiomeric form or any combinations thereof. These compounds exhibit affinity f
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- Inhibition of protein kinase C-driven nuclear factor-κB activation: Synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules
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A unique series of biologically active chemical probes that selectively inhibit NF-κB activation induced by protein kinase C (PKC) pathway activators have been identified through a cell-based phenotypic reporter gene assay. These 2-aminobenzimidazoles represent initial chemical tools to be used in gaining further understanding on the cellular mechanisms driven by B and T cell antigen receptors. Starting from the founding member of this chemical series 1a (notated in PubChem as CID-2858522), we report the chemical synthesis, SAR studies, and pharmacological profiling of this pathway-selective inhibitor of NF-κB activation.
- Peddibhotla, Satyamaheshwar,Shi, Ranxin,Khan, Pasha,Smith, Layton H.,Mangravita-Novo, Arianna,Vicchiarelli, Michael,Su, Ying,Okolotowicz, Karl J.,Cashman, John R.,Reed, John C.,Roth, Gregory P.
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supporting information; experimental part
p. 4793 - 4797
(2010/10/19)
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- The palladium-catalyzed aerobic kinetic resolution of secondary alcohols: Reaction development, scope, and applications
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The first palladium-catalyzed enantioselective oxidation of secondary alcohols has been developed, utilizing the readily available diamine (-)-sparteine as a chiral ligand and molecular oxygen as the stoichiometric oxidant. Mechanistic insights regarding the role of the base and hydrogen-bond donors have resulted in several improvements to the original system. Namely, addition of cesium carbonate and tert-butyl alcohol greatly enhances reaction rates, promoting rapid resolutions. The use of chloroform as solvent allows the use of ambient air as the terminal oxidant at 23°C, resulting in enhanced catalyst selectivity. These improved reaction conditions have permitted the successful kinetic resolution of benzylic, allylic, and cyclopropyl secondary alcohols to high enantiomeric excess with good-toexcellent selectivity factors. This catalyst system has also been applied to the desymmetrization of meso-diols, providing high yields of enantioenriched hydroxyketones.
- Ebner, David C.,Bagdanoff, Jeffrey T.,Ferreira, Eric M.,McFadden, Ryan M.,Caspi, Daniel D.,Trend, Raissa M.,Stoltz, Brian M.
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supporting information; experimental part
p. 12978 - 12992
(2010/06/19)
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- THIAZOLE DERIVATIVES AS CXCR3 RECEPTOR MODULATORS
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The invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, which are antagonist of the CXCR3 chemokine receptor useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
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Page/Page column 57-58
(2008/06/13)
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- Aza-retinoids as novel retinoid X receptor-specific agonists
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A new structurally simple series of potent lipophilic aza-retinoids RXR agonists has been developed. SAR studies for the N-alkyl-azadienoic acids described here demonstrate that the RXR activity profile is sensitive to the N-alkyl chain length. Further, we have expanded the work to include azadienoic acids, which exhibited many accessible conformations leading to a better understanding of the SAR around the series.
- Farmer, Luc J.,Marron, Kristen S.,Canan Koch, Stacie S.,Hwang,Kallel, E. Adam,Zhi, Lin,Nadzan, Alex M.,Robertson, Dave W.,Bennani, Youssef L.
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p. 2352 - 2356
(2007/10/03)
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- Novel anti-Markovnikov regioselectivity in the Wacker reaction of styrenes
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The Wacker reaction is one of the longest known palladium-catalysed organic transformations, and in the vast majority of cases proceeds with Markovnikov regioselectivity. Palladium(II)-mediated oxidation of styrenes was examined and in the absence of reoxidants was found to proceed in an anti-Markovnikov sense, giving aldehydes. Studies on the mechanism of this unusual transformation were carried out, and indicate the possible involvement of a η4-palladium-styrene complex. With a heteropolyacid as the terminal oxidant, oxidation of styrene to give the anti-Markovnikov aldehyde as the major product was found to be catalytic.
- Wright, Joseph A.,Gaunt, Matthew J.,Spencer, Jonathan B.
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p. 949 - 955
(2007/10/03)
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- Secondary isotope effects on the deslipping reaction of rotaxanes: High-precision measurement of steric size
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A supramolecular measuring instrument for determining steric size: The deslipping reaction of the rotaxane shown with deuterated stopper groups senses the smaller steric size of the deuterium atom and proceeds with a 10% higher reaction rate than the reaction of the unlabeled rotaxane. This result sheds new light from a supramolecular point of view on the classical problem of determining steric demand.
- Felder, Thorsten,Schalley, Christoph A.
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p. 2258 - 2260
(2007/10/03)
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- Trienoic retinoid compounds and methods
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Novel trienoic retinoid compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.
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- Pyridinium N-phenoxide betaines and their application to the determination of solvent polarities, XXIV. Syntheses and UV-vis spectroscopic properties of new lipophilic tert-butyl- and 1-adamantyl substituted, negatively solvatochromic pyridinium N-phenolate betaine dyes
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Syntheses and negative solvatochromism of two new lipophilic pentaphenyl pyridinium N-phenolate betaine dyes, substituted with seven tert-butyl groups (9) or with three tert-butyl and two 1-adamantyl groups (13) in the peripheral phenyl rings, are described in order to get zwitterionic dyes that are more soluble in nonpolar solvents such as the standard betaine dye, 1, which has been used for the construction of an empirical scale of solvent polarity, called the E(T)(30) scale.
- Reichardt, Christian,L?bbecke, Stefan,Mehranpour, Abdol Mohammed,Sch?fer, Gerhard
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p. 686 - 694
(2007/10/03)
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- Trienoic retinoid compounds and methods
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Novel trienoic compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.
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- Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells
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Retinoic acid receptor (RAR) active retinoids have proven therapeutically useful for treating certain cancers and dermatological diseases. Herein, we describe the discovery of two new RAR active trienoic acid retinoids, (2E,4E,6E)-7-(3,5-di-tert-butylphen
- Zhang, Lin,Nadzan, Alex M.,Heyman, Richard A.,Love, Deborah L.,Mais, Dale E.,Croston, Glenn,Lamph, William W.,Boehm, Marcus F.
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p. 2659 - 2663
(2007/10/03)
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- Retinobenzoic Acids. 1. Structure-Activity Relationships of Aromatic Amides with Retinoidal Activity
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Two types of aromatic amides, terephthalic monoanilides and (arylcarboxamido)benzoic acids, have been shown to possess potent retinoidal activities and can be classified as retinoids.The structure-activity relationships of these amides are discussed on the basis of differentiation-inducing activity on human promyelocytic leukemia cells HL-60.In generic formula 4 (X = NHCO or CONH), the necessary factors to elicit the retinoidal activities are a medium-sized alkyl group (isopropyl, tert-butyl, etc.) at the meta position and a carboxyl group at the para position of the other benzene ring.The bonding of the amide structure can be reversed, this moiety apparently having the role of locating the two benzene rings at suitable positions with respect to each other.Substitution at the ring position ortho to the amide group or N-methylation of the amido group caused loss of activity, presumably owing to the resultant change of conformation.It is clear that the mutual orientation of the benzylic methyl group(s) and the carboxyl group and their distance apart are essential factors determining the retinoidal activity.Among the synthesized compounds, 4-benzoic acid (Am80) and 4-benzoic acid (Am580) were several times more active than retinoic acid in the assay.They are structurally related to retinoic acid, as is clear from the biological activity of the hybrid compounds (M2 and R2).
- Kagechika, Hiroyuki,Kawachi, Emiko,Hashimoto, Yuichi,Himi, Toshiyuki,Shudo, Koichi
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p. 2182 - 2192
(2007/10/02)
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