- A practical and scaleable synthesis of A-224817.0, a novel nonsteroidal ligand for the glucocorticoid receptor
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A practical and scaleable synthesis of a novel nonsteroidal ligand for the glucocorticoid receptor A-224817.0 1A is described. The synthesis proceeds in seven steps starting from 1,3-dimethoxybenzene. The biaryl intermediate 5 was prepared by an optimized
- Ku, Yi-Yin,Grieme, Tim,Raje, Prasad,Sharma, Padam,Morton, Howard E.,Rozema, Mike,King, Steve A.
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Read Online
- Aryl boronic acid preparation method
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The invention belongs to the technical field of fine chemical engineering, and relates to an aryl boronic acid preparation method. In the prior art, aryl boronic acid as a novel safe and environmentally-friendly arylation reagent is widely used in scientific research and production of various fine chemicals containing aryl structures in the fields of medicines, pesticides, advanced materials and the like; and the aryl boronic acid compound preparation method reported in the disclosed literature has problems of harsh reaction conditions and high cost. A purpose of the invention is to provide amethod, wherein an aryl boron compound is formed by carrying out a reaction on a Grignard reagent and trialkyl borate under mild conditions, the composition of the aryl boron compound is converted from the main component diaryl borate into the main component aryl borate, and the aryl borate is hydrolyzed to obtain aryl boric acid, so that the preparation cost of the acyl aryl boric acid compound can be remarkably reduced, and the method has good practical application prospect.
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Paragraph 0033-0036; 0040
(2020/01/25)
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- Organic Compound for organic light emitting diode and an organic light emitting diode including the same
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The present invention relates to an anthracene derivative selected from among compounds represented by chemical formula A-1, chemical formula A-2, chemical formula B-1, and chemical formula B-2, and an organic light emitting diode comprising the same, whe
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Paragraph 0611-0617; 0707-0713
(2019/06/04)
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- Kolbe-Schmitt type reaction under ambient conditions mediated by an organic base
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The combined use of an organic base for resorcinols realized a Kolbe-Schmitt type reaction under ambient conditions. When resorcinols (3-hydroxyphenol derivatives) were treated with DBU under a carbon dioxide atmosphere, nucleophilic addition to carbon dioxide proceeded to afford the corresponding salicylic acid derivatives in high yields.
- Sadamitsu, Yuta,Okumura, Akira,Saito, Kodai,Yamada, Tohru
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supporting information
p. 9837 - 9840
(2019/08/20)
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- Novel organic compounds for organic light-emitting diode and organic light-emitting diode including the same
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The present invention relates to a compound for organic light-emitting diodes that can operate organic light-emitting diodes at a low driving voltage and an organic light-emitting diode comprising the same and, more particularly, to a compound for use as a fluorescent host in organic light-emitting diodes, which can bring about excellent diode properties by operating organic light-emitting diodes at a low driving voltage, and an organic light-emitting diode comprising the same.
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Paragraph 0097-0098
(2018/02/22)
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- Organic light-emitting element capable of low-voltage drive and having long life
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The present invention relates to an organic light-emitting element capable of low-voltage drive and also having a long life, and, more specifically, relates to an organic light-emitting element comprising: a first electrode; a second electrode facing the first electrode; and a light-emitting layer interposed between the first electrode and the second electrode, wherein the light-emitting layer comprises at least one amine compound represented by [chemical formula A] or [chemical formula B], and at least one compound represented by [chemical formula D], and the structures of [chemical formula A], [chemical formula B] and [chemical formula D] are the same as given in the detailed description of the invention.
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Paragraph 0441; 0447; 0448; 0450; 0451
(2017/10/13)
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- ORGANIC LIGHT EMITTING DIODE FOR HIGH EFFICIENCY
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Disclosed herein is an organic light-emitting diode, comprising: a first electrode, a second electrode opposite the first electrode, and a light-emitting layer and an electron-density-controlling layer in that order between the first electrode and the sec
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Paragraph 0157-0158; 0183-0184
(2017/02/02)
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- Compound containing anthracene and pyrene and preparing method and application thereof
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The invention provides a compound containing anthracene and pyrene and a preparing method and application thereof. The compound has a structure shown in formula I, wherein R1 and R3 are independently selected from substituted or unsubstituted C1-C60 alkyl groups, substituted or unsubstituted C6-C60 aryl groups, substituted or unsubstituted C10-C60 condensed ring groups or substituted or unsubstituted C5-C60 heterocyclic groups; R2 is selected from hydrogen, substituted or unsubstituted C6-C60 aryl groups, substituted or unsubstituted C5-C60 heterocyclic groups, substituted or unsubstituted C10-C60 condensed ring groups or substituted or unsubstituted C5-C60 arylamine groups; n is 0 or 1. When current density is 20 mA/cm2, the current efficiency of the compound with the structure shown in formula I is as high as 8.9 cd/A, and service life is as long as 8500 h which is much longer than that of existing electroluminescent materials.
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Paragraph 0147-0149
(2017/02/24)
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- A preparing method of a dibenzofuran compound
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The invention relates to a preparing method of a dibenzofuran compound. The method includes subjecting m-dimethoxy benzene which is adopted as a raw material to a butyl lithium low-temperature reaction to prepare a boric acid compound, preparing the boric
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Paragraph 0059; 0060
(2016/10/07)
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- An efficient indenyl-derived phosphine ligand for the Suzuki-Miyaura coupling of sterically hindered aryl halides
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An air-stable aryl substituted indenyl phosphine used in combination with Pd(OAc)2 provides a highly efficient catalyst for the Suzuki-Miyaura cross-coupling reaction of sterically hindered aryl halides with aryl boronic acids.
- Liu, Yan,Peng, Hui,Yuan, Jia,Yan, Meng-Qi,Luo, Xue,Wu, Qing-Guo,Liu, Sheng-Hua,Chen, Jian,Yu, Guang-Ao
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supporting information
p. 4664 - 4668
(2016/06/09)
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- Novel antracene derivatives for organic light-emitting diode and organic light-emitting diode including the same
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The present invention relates to an organic light emitting compound represented by chemical formula A, and an organic light emitting device comprising the same. Substituent R_1 to R_8, R_11 to R_19, L, n, and X are the same as defined in the specification. The organic light emitting compound represented by chemical formula A can be used as an organic light emitting device, and can be used to manufacture an excellent device having stable and highly efficient characteristics.COPYRIGHT KIPO 2016
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Paragraph 0162; 0163; 0164; 0165; 0166; 0167; 0168
(2016/10/31)
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- Method for preparing aromatic boronic acid
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The invention discloses a method for preparing aromatic ring boric acid, which comprises the following steps of: (1) firstly, leading the mixed solution of aromatic ring compounds, n-butyllithium and a chelant with nitrogen heterocycle to have a reaction
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Paragraph 0044; 0045
(2017/04/04)
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- Synthesis of substituted azulenes via Pt(II)-Catalyzed ring-expanding cycloisomerization
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Substituted azulenes, valuable structures for electronic devices and pharmaceuticals, have been synthesized by the platinum(II)-catalyzed intramolecular ring-expanding cycloisomerization of 1-en-3-yne with ortho-disubstituted benzene. This novel method provides an alternative route for the efficient synthesis of substituted azulenes. The reaction mechanism of selected catalytic transformations was explored using density functional calculations.
- Usui, Kazuteru,Tanoue, Kensuke,Yamamoto, Kosuke,Shimizu, Takashi,Suemune, Hiroshi
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p. 4662 - 4665
(2015/01/16)
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- Towards allosteric receptors synthesis of β-cyclodextrin- functionalised 2,2'-bipyridines and their metal complexes
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Herein, we present three new 2,2'-bipyridines that carry two β-cyclodextrin moieties in different substitution patterns. When coordinated by zinc(II) or copper(I) ions (or their complexes), these compounds undergo conformational changes and switch between
- Kremer, Christopher,Schnakenburg, Gregor,Lutzen, Arne
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p. 814 - 824
(2014/05/06)
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- Robust acenaphthoimidazolylidene palladium complexes: Highly efficient catalysts for suzuki-miyaura couplings with sterically hindered substrates
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Robust acenaphthoimidazolylidene palladium complexes have been demonstrated as highly efficient and general catalysts for the sterically hindered Suzuki-Miyaura cross-coupling reactions in excellent yields even with low catalyst loadings under mild reaction conditions. The high catalytic activity of these complexes highlights that, besides the "flexible steric bulky" concept, σ-donor properties of the NHC ligands are also crucial to accelerate the transformations.
- Tu, Tao,Sun, Zheming,Fang, Weiwei,Xu, Mizhi,Zhou, Yunfei
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supporting information; experimental part
p. 4250 - 4253
(2012/10/07)
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- Synthesis and evaluation of [11C]Cimbi-806 as a potential PET ligand for 5-HT7 receptor imaging
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2-(2′,6′-Dimethoxy-[1,1′-biphenyl]-3-yl)-N, N-dimethylethanamine has been identified as a potent ligand for the serotonin 7 (5-HT7) receptor. In this study, we describe the synthesis, radiolabeling and in vivo evaluation of [11C]2-(2
- Herth, Matthias M.,Hansen, Hanne D.,Ettrup, Anders,Dyssegaard, Agnete,Lehel, Szabolcs,Kristensen, Jesper,Knudsen, Gitte M.
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scheme or table
p. 4574 - 4581
(2012/09/07)
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- Guest-encapsulation properties of a self-assembled capsule by dynamic boronic ester bonds
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Two molecules of tetrakis(dihydroxyboryl)-cavitand 1a as an aromatic cavity and four molecules of 1,2-bis(3,4-dihydroxyphenyl)ethane 2 as an equatorial linker self-assemble into capsule 3a via the formation of eight dynamic boronic ester bonds in CDClsub
- Nishimura, Naoki,Yoza, Kenji,Kobayashi, Kenji
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supporting information; experimental part
p. 777 - 790
(2010/04/01)
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- Palladium-catalyzed cross-coupling of N-benzenesulfonyl-3,4-dibromopyrrole and its application to the total syntheses of lamellarins O, P, Q, and R
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Palladium-catalyzed Suzuki-Miyaura coupling of N-benzenesulfonyl-3,4-dibromopyrrole with a variety of arylboronic acids gave the corresponding 3,4-diarylpyrroles in high yields. The 3,4-differentially arylated pyrroles could also be prepared by stepwise cross-coupling approach. The total syntheses of lamellarins O, P, Q, and R have been achieved by using the cross-coupling and the directed lithiation as key reactions.
- Fukuda, Tsutomu,Sudo, Ei-ichi,Shimokawa, Kozue,Iwao, Masatomo
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p. 328 - 338
(2008/04/01)
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- Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT7 receptor
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The synthesis of novel C6-aryl substituted derivatives of 3-(dimethylamino)chroman is described. The novel derivatives display 5-HT 7 receptor affinities that varies from nM to μM, indicating that this small set of derivatives constitute a nove
- Holmberg, Paer,Tedenborg, Lars,Rosqvist, Susanne,Johansson, Anette M.
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p. 747 - 750
(2007/10/03)
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- METHOD FOR METAL-ORGANIC PRODUCTION OF ORGANIC INTERMEDIATE PRODUCTS BY MEANS OF ARYL LITHIUM-BASES
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The invention relates to a method for the production of substituted aromatic compounds by producing lithium arylene and by reacting it with suitable electrophiles. The method comprises the following steps (step 1); an aryl lithium compound ( auxiliary base'') is initially produced by reacting a halogen aromatic compound with lithium metal; said compound is subsequently (step 2) reacted for deprotonation of the aromatic substrate in order to form the corresponding lithium aromatic compound which is subsequently (step 3) reacted with a corresponding electrophile to form the desired substituted aromatic compound, see page 2 of the description.
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Page/Page column 13-14
(2010/02/06)
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- Glucocorticoid receptor antagonists for treatment of diabetes
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Compounds of formula I are useful for treating type II diabetes, obesity, hyperglycemia, inadequate glucose clearance, hyperinsulinemia, hypertriglyceridemia, and high-circulating glucocorticoid levels, preparations of the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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- Inhibitors of α4 mediated cell adhesion
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The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O-(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur, W is oxygen, sulfur, —CH═CH—, —NH— or —N═CH—; R1, R2and R3are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4is tetrazolyl, carboxyl group, amide or ester; R5is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl etc.; R6is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.; or a pharmaceutically acceptable salt thereof.
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- Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.
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A series of substituted N-(3,5-dichlorobenzenesulfonyl)-(L)-prolyl- and (L)-azetidyl-beta-biaryl beta-alanine derivatives was prepared as selective and potent VLA-4 antagonists. The 2,6-dioxygenated biaryl substitution pattern is important for optimizing potency. Oral bioavailability was variable and may be a result of binding to circulating plasma proteins.
- Kopka, Ihor E,Lin, Linus S,Mumford, Richard A,Lanza Jr., Thomas,Magriotis, Plato A,Young, David,DeLaszlo, Stephen E,MacCoss, Malcolm,Mills, Sander G,Van Riper, Gail,McCauley, Ermengilda,Lyons, Kathryn,Vincent, Stella,Egger, Linda A,Kidambi, Usha,Stearns, Ralph,Colletti, Adria,Teffera, Yohannes,Tong, Sharon,Owens, Karen,Levorse, Dorothy,Schmidt, John A,Hagmann, William K
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p. 2415 - 2418
(2007/10/03)
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- A facile route to Aryl-substituted 1,10-phenanthrolines by means of Suzuki coupling reactions between substituted areneboronic acids and halogeno-1,10-phenanthrolines
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Twelve new mono- or diaryl-substituted 1,10-phenanthrolines (17 and 18) have been synthesized. The key step is a Suzuki coupling reaction between the substituted areneboronic acids 6, 11, and 15 and the mono- and dihalo-1,10-phenanthrolines 16. The syntheses of bis-ortho-substituted boronic acids 6, 11, and 15 from substituted arenes 5 or substituted bromoarenes 10 and 14 by lithiation and subsequent treatment with trimethyl borate is described. Not only 2,9-diiodo- (16c) but also 2,9-dichloro-1,10-phenanthroline (16b) can be used with good yields (65-92%) in the described Suzuki coupling. For the syntheses of unsymmetrically substituted 1,10-phenanthrolines 18b, 18i, and 18j, the use of 2- chloro-9-iodo-1,10-phenanthroline is not necessary; two different bis-ortho-substituted arene rings can be introduced stepwise in 46 to 64% total yield. ( Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002).
- Luening, Ulrich,Abbass, Michael,Fahrenkrug, Frank
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p. 3294 - 3303
(2007/10/03)
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- Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: Discovery of TR-14035, a dual α4β7/α4β1 integrin antagonist
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α4β1 and α4β7 integrins are key regulators of physiologic and pathologic responses in inflammation and autoimmune disease. The effectiveness of anti-integrin antibodies to attenuate a number of inflammatory/immune conditions provides a strong rationale to target integrins for drug development. Important advances have been made in identifying potent and selective candidates, peptides and peptidomimetics, for further development. Herein, we report the discovery of a series of novel N-benzoyl-L-biphenylalanine derivatives that are potent inhibitors of α4 integrins. The potency of the initial lead compound (1: IC50 α4β7/α4β1 =5/33 μM) was optimized via sequential manipulation of substituents to generate low nM, orally bioavailable dual α4β1/α4β7 antagonists. The SAR also led to the identification of several subnanomolar antagonists (134, 142, and 143). Compound 81 (TR-14035; IC50 α4β7/α4β1 =7/87 nM) has completed Phase I studies in Europe. The synthesis, SAR and biological evaluation of these compounds are described.
- Sircar, Ila,Gudmundsson, Kristjan S.,Martin, Richard,Liang, Jimmy,Nomura, Sumihiro,Jayakumar, Honnappa,Teegarden, Bradley R.,Nowlin, Dawn M.,Cardarelli, Pina M.,Mah, Jason R.,Connell, Samuel,Griffith, Ronald C.,Lazarides, Elias
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p. 2051 - 2066
(2007/10/03)
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- GLUCOCORTICOID RECEPTOR ANTAGONISTS FOR TREATMENT OF DIABETES
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are useful for treating type II diabetes, obesity, hyperglycemia, inadequate glucose clearance, hyperinsulinemia, hypertriglyceridemia, and high-circulating glucocorticoid levels, preparations of the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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