- DIBENZOHETEROCYCLIC COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
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A dibenzoheterocyclic compound wherein band gaps of HOMO and LUMO energy levels of the dibenzoheterocyclic compound are wide, light can be emitted in a deep blue light-emitting region; and the LUMO energy level of the dibenzoheterocyclic compound is low, so the LUMO energy level matches with an electron transport layer for electrons injection and transport. The dibenzoheterocyclic compound has hole transport performance, so as a light-emitting layer material, the dibenzoheterocyclic compound balances the ratio of electrons to holes in a light-emitting layer increasing the combination probability and improving the device light-emitting efficiency. The spatial configuration of the dibenzoheterocyclic compound avoids material stacking molecules, reduces annihilation of excitons, and inhibits efficiency roll-off. The dibenzoheterocyclic compound has thermal stability, so deep blue light can be emitted efficiently and stably. With an organic light-emitting diode and a deep blue light-emitting device with high light-emitting efficiency, low working voltage can be obtained.
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Paragraph 0077; 0079-0080
(2020/12/18)
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- Cross-coupling strategy for the synthesis of diazocines
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Ethylene bridged azobenzenes are novel, promising molecular switches that are thermodynamically more stable in the (Z) than in the (E) configuration, contrary to the linear azobenzene. However, their previous synthetic routes were often not general, and yields were poorly reproducible, and sometimes very low. Here we present a new synthetic strategy that is both versatile and reliable. Starting from widely available 2-bromobenzyl bromides, the designated molecules can be obtained in three simple steps.
- Eleya, Nadi,Li, Shuo,Staubitz, Anne
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supporting information
p. 1624 - 1627
(2020/03/13)
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- tBuOK-Promoted Cyclization of Imines with Aryl Halides
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A transition-metal-free indole synthesis using radical coupling of 2-halotoluenes and imines via the later-stage C-N bond construction was reported for the first time. It includes an aminyl radical generation by C-H cleaving addition of 2-halotoluenes to imines via the carbanion radical relay and an intramolecular coupling of aryl halides with aminyl radicals. One standard condition can be used for all halides including F, Cl, Br, and I. No extra oxidant or transition metal is required.
- Li, Ya-Wei,Zheng, Hong-Xing,Yang, Bo,Shan, Xiang-Huan,Qu, Jian-Ping,Kang, Yan-Biao
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supporting information
p. 4553 - 4556
(2020/06/08)
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- A two-benzo heterocyclic compound and its preparation method and application (by machine translation)
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The present invention discloses a two-benzo heterocyclic compound, of formula (I) as shown in the structure. Dibenzofluorene and heterocyclic compounds of the LUMO energy level is low, with the electronic transmission material good matching, favorable to electronic injection and transmission. Dibenzofluorene and heterocyclic compound having good hole transmission performance, as luminescent material in the luminescent layer can balance the proportion of electrons and holes, improve the composite probability, make the device light-emitting efficiency is enhanced. Dibenzofluorene and heterocyclic compounds of space configuration can avoid material molecular stacking, and then prevent the intermolecular energy transfer result in high-energy exciton generation, reduce the exciton annihilation, inhibit efficiency roll-off. At the same time, dibenzo heterocyclic compound having good thermal stability, can achieve high-efficiency stable blue-light. The invention also discloses an organic electroluminescent device, at least one functional layer containing the above-mentioned in-diazepine heterocyclic compound, can be obtained with high blue light emitting efficiency and low operating voltage of blue light device. (by machine translation)
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Paragraph 0081-0089
(2019/05/08)
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- COMPOUNDS AND COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO NTRK
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This invention relates to inhibitors of NTRK that are active against wild-type NTRK and its resistant mutants.
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Page/Page column 100; 101
(2017/03/14)
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- Rhodium-Catalyzed, Enantioselective Hydroacylation of ortho-Allylbenzaldehydes
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The development of a rhodium catalyst for endo- and enantioselective hydroacylation of ortho-allylbenzaldehydes is reported. A catalyst generated in situ from [Rh(COD)Cl]2, (R)-DTBM-SEGPHOS, and NaBARF promotes the desired hydroacylation reactions and minimizes the formation of byproducts from competitive alkene isomerization and ene/dehydration pathways. These rhodium-catalyzed processes generate the 3,4-dihydronaphthalen-1(2H)-one products in moderate-to-high yields (49-91%) with excellent enantioselectivities (96-99% ee).
- Johnson, Kirsten F.,Schmidt, Adam C.,Stanley, Levi M.
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supporting information
p. 4654 - 4657
(2015/10/12)
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- NEW CRTH2 ANTAGONISTS
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The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
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Page/Page column 165
(2013/03/26)
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- Copper-catalyzed domino coupling reaction: An efficient method to synthesize oxindoles
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An efficient and novel procedure for a copper catalyzed domino coupling reaction has been developed, which afforded various oxindoles in good to excellent yields with tolerance of various substituents. In addition, this method could be applied to synthesize horsfiline and coerulescine in few steps with high total yields. The Royal Society of Chemistry 2012.
- Hsieh, Jen-Chieh,Cheng, An-Yi,Fu, Jun-Hao,Kang, Ting-Wei
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experimental part
p. 6404 - 6409
(2012/09/05)
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- Palladium-catalyzed intramolecular decarboxylative coupling of arene carboxylic acids/esters with aryl bromides
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Give me a ring? An efficient approach has been developed for the intramolecular decarboxylative coupling of arene carboxylic acids/esters with aryl bromides catalyzed by palladium (see scheme). From a synthetic viewpoint, this method is highly attractive because the catalyst loading is low, the optimized reaction conditions are mild, and the substrate scope is broad. Copyright
- Shen, Zengming,Ni, Zhenjie,Mo, Song,Wang, Jing,Zhu, Yamin
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supporting information; experimental part
p. 4859 - 4865
(2012/06/04)
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- Synthesis of benzo- and naphtho-fused bicyclo[n.3.1]alkane frameworks with a bridgehead nitrogen function by palladium-catalyzed intramolecular α′-arylation of α-nitroketones
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The C-alkylation of cyclic α-nitroketones with α-halobenzyl halides in the presence of DBU followed by a Pd-catalyzed intramolecular C-arylation afforded benzo-and naphtho-fused bicyclo[n.3.1]alkane derivatives (n = 3, 4, 5) in excellent overall yields for the two-step sequence. In some of the reactions starting from α-nitrocyclooctanone, the major products were fused indane derivatives arising from an intramolecular attack of an intermediate Pd species onto the carbonyl group, followed by elimination.
- Giorgi, Giorgio,Maiti, Swarupananda,Lopez-Alvarado, Pilar,Menendez, J. Carlos
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supporting information; experimental part
p. 2722 - 2730
(2011/05/12)
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- PYRAZOLE AND TRIAZOLE CARBOXAMIDES AS CRAC CHANNEL INHIBITORS
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The present invention relates to amide compounds of formula (I) processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing these compounds and to their use in therapy.
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Page/Page column 42
(2010/11/05)
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- A concise synthesis of 6,7-dihydro-5H-dibenz[c,e]azepin-5-one
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A concise and efficient strategy for the synthesis of dibenz[c,e]azepin-5-ones has been developed. The approach relies on a key transformation involving Suzuki-Miyaura coupling of 2-bromobenzyl azides with 2-(methoxycarbonyl)phenylboronic acid, followed b
- Goh, Young-Hyoung,Kim, Guncheol,Kim, Bum Tae,Heo, Jung-Nyoung
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experimental part
p. 669 - 677
(2010/04/29)
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- Substituted aryl or heteroarylpiperidine derivatives as melanocortin-4 receptor modulators
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The present invention relates to substituted aryl or heteroarylpiperidine derivatives of structure (I) as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
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Page/Page column 68
(2009/03/07)
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- QUINAZOLINE AND PYRIDOPYRIMIDINE DERIVATIVES AS P38 KINASE INHIBITORS
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The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2/su
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Page/Page column 36-37
(2008/06/13)
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- Discovery of a series of aminopiperidines as novel iNOS inhibitors
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Nitric oxide (NO), a mediator of various physiological and pathophysiological processes, is synthesized by three isozymes of nitric oxide synthase (NOS). Potential candidate clinical drugs should be devoid of inhibitory activity against endothelial NOS (eNOS), since eNOS plays an important role in maintaining normal blood pressure and flow. A new series of aminopiperidines as potent inhibitors of iNOS were identified from a HTS lead. From this study, we identified compound 33 as a potent iNOS inhibitor, with >25-fold selectivity over eNOS and 16-fold selectivity over nNOS.
- Bourdonnec, Bertrand Le,Leister, Lara K.,Ajello, Christopher A.,Cassel, Joel A.,Seida, Pamela R.,O'Hare, Heather,Gu, Minghua,Chu, Guo-Hua,Tuthill, Paul A.,DeHaven, Robert N.,Dolle, Roland E.
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p. 336 - 343
(2008/09/18)
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- Phenylpiperidine derivatives as melanocortin-4 receptor modulators
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The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
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Page/Page column 51
(2008/06/13)
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- Substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators
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The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally, all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
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Page/Page column 34-35
(2010/11/28)
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- CETP INHIBITORS
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Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.
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Page/Page column 77
(2008/06/13)
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- TETRACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
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The present invention relates to tetracyclic indole compounds of formula (I); wherein R1, R2, A, Ar, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
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Page/Page column 28
(2010/11/08)
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- Benzimidazole derivatives bearing substituted biphenyls as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors: Structure-activity relationship studies and identification of a potent and highly selective inhibitor JTK-109
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Following the discovery of a new series of benzimidazole derivatives bearing a diarylmethyl group as inhibitors of hepatitis C virus NS5B RNA-dependent RNA polymerase (HCV NS5B RdRp), we extended the structure-activity relationship (SAR) study to analogue
- Hirashima, Shintaro,Suzuki, Takayoshi,Ishida, Tomio,Noji, Satoru,Yata, Shinji,Ando, Izuru,Komatsu, Masakazu,Ikeda, Satoru,Hashimoto, Hiromasa
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p. 4721 - 4736
(2007/10/03)
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- CETP INHIBITORS
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Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalky substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalky substituent connected directly to the ring or attached to the ring through a -CH2-.
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Page/Page column 87
(2010/10/19)
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- PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING METABOLIC BONE DISEASES CONTAINING ALPHA-ARYLMETHOXYACRYLATE DERIVATIVES
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The present invention relates to a use of a specific alpha-arylmethoxyacrylate derivative, or its pharmacologically acceptable salt or solvate for preventing and treating metabolic bone diseases.
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Page/Page column 25
(2008/06/13)
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- Fused-ring compounds and use thereof as drugs
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The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. Th
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- Fullerene tectonics. Part 2. Synthesis and pyrolysis of halogenated benzo[c]phenanthrenes
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Halogenated benzo[c]phenanthrenes with a halogen in the hindered fiord region are prepared by the photochemical cyclisation of appropriately substituted stilbenes. Pyrolysis gives the corresponding benzo[ghi]fluoranthrenes in moderate yields. At higher temperatures a competing rearrangement pathway to cyclopenta[cd]pyrene occurs.
- Plater, M. John
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p. 2903 - 2909
(2007/10/03)
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