- Phosphorus-containing bicyclic compound and preparation method and application thereof
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The invention belongs to the technical field of electroluminescent materials, and particularly relates to a phosphorus-containing bicyclic compound and a preparation method and application thereof. The phosphorus-containing bicyclic compound has the struc
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Paragraph 0042-0049
(2019/12/25)
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- LIGHT-EMITTING MATERIAL FOR ORGANIC ELECTROLUMINESCENT DEVICE, ORGANIC ELECTROLUMINESCENT DEVICE USING SAME, AND MATERIAL FOR ORGANIC ELECTROLUMINESCENT DEVICE
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Disclosed are a novel aromatic compound having excellent light emitting efficiency and thermal stability, a manufacturing method thereof, and an organic electroluminescent device comprising the novel aromatic compound. According to the present invention, provided are an aromatic compound forming a ring, and a novel aromatic derivative represented by chemical formula 1, which improves performance of a device. In the chemical formula 1, Z is equally or differently N (nitrogen), O (oxygen), or S (sulfur) in each case. Also, when Z is N (nitrogen), L1 is an integer of 1, and when Z is O (oxygen) or S (sulfur), L1 is an integer of 0.COPYRIGHT KIPO 2015
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Paragraph 0144-0147
(2016/10/08)
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- Transition-metal-free atropo-selective synthesis of biaryl compounds based on arynes
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A modular way towards biaryls: Highly enantioenriched biphenyls can be prepared based on a transition-metal-free aryl-aryl coupling followed by efficient desymmetrization or deracemization and chemoselective functionalization (see scheme). Copyright
- Leroux, Frédéric R.,Berthelot, Ana?s,Bonnafoux, Laurence,Panossian, Armen,Colobert, Fran?oise
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supporting information
p. 14232 - 14236
(2013/01/15)
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- Renin Inhibitors
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Disclosed are compounds having the formula (I): wherein the R1, R2, R3, X, Y, A, L, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
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Page/Page column 47
(2010/12/29)
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- Ring opening of aziridines with ortho-bromophenyl metal reagents: synthesis of 2-substituted indolines
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Stabilized ortho-bromo phenyllithium reagents, generated via lithium-halogen exchange of aryl iodides, undergo regioselective ring opening of mono-substituted N-Boc, N-Cbz, and N-tosyl-protected aziridines in good to excellent yields. The resulting ortho-
- Michaelis, David J.,Dineen, Thomas A.
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body text
p. 1920 - 1923
(2009/08/17)
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- RENIN INHIBITORS
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Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
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Page/Page column 103
(2008/12/04)
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- RENIN INHIBITORS
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Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
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Page/Page column 86-87
(2008/12/04)
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- RENIN INHIBITORS
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Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration
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Page/Page column 69
(2008/12/04)
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- Generation and suppression of 3-/4-functionalized benzynes using zinc ate base (TMP-Zn-ate): New approaches to multisubstituted benzenes
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We present full details of our new methods for preparing functionalized benzynes with lithium di-alkyl(2,2,6,6-tetramethylpiperidino)zincate (R 2Zn(TMP)Li) through deprotonative zincation as a key reaction. In this system, by choosing appropriate ligands for the zincate, either regioselective zincation of functionalized haloaromatics or the generation of substituted benzynes can be controlled in good yields with excellent chemoselectivity, using the same substrate. Zincation with tBu 2Zn(TMP)Li followed by electrophilic trapping or zincation with Me2Zn(TMP)Li followed by nucleophilic or diene trapping is shown to be a powerful tool for the chemoselective preparation of 1,2,3-/1,2,4- trisubstituted benzene derivatives. These methods offer far greater generality than previous methods for the synthesis of multifunctionalized benzenes. Computational/theoretical studies of the reaction mechanism of this unique benzyne formation indicated that preferential coordination of the dialkylzinc moiety of zincate to halogen is the reason for the reduced activation energy of the elimination, that is, for the formation of the benzyne. The role of the ligands on Zn in accelerating/decelerating the elimination is also discussed.
- Uchiyama, Masanobu,Kobayashi, Yuri,Furuyama, Taniyuki,Nakamura, Shinji,Kajihara, Yumiko,Miyoshi, Tomoko,Sakamoto, Takao,Kondo, Yoshinori,Morokuma, Keiji
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p. 472 - 480
(2008/10/09)
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- PIPERIDINE AND MORPHOLINE RENIN INHIBITORS
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Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.
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Page/Page column 169
(2008/06/13)
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- A practical transition metal-free aryl-aryl coupling method: Arynes as key intermediates
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Upon treatment of various aryllithium intermediates with 1,2-dibromobenzene or 1-bromo-2-iodobenzene, dissymmetrical ortho,ortho′-di-, tri-and even tetrasubstituted bromo- or iodobiaryls become readily available. The crucial steps in all these reactions were the nucleophilic addition of the organolithium precursor to a transient aryne species released from it by β-elimination of a lithium halide and, stabilization of the resulting 2-biaryllithium intermediate by in situ transfer of bromine or iodine from the starting material. This straightforward transition metal-free access to biaryls allows the preparation of highly valuable halobiaryls on a gram scale in excellent yields. These precursors can be subsequently functionalized by highly regioselective halogen/metal permutations into a vast variety of target molecules. This was demonstrated in the synthesis of several mono- and diphosphine ligands.
- Leroux, Frederic R.,Bonnafoux, Laurence,Heiss, Christophe,Colobert, Francoise,Lanfranchi, Don Antoine
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p. 2705 - 2713
(2008/09/19)
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- Formation of 3-halobenzyne: Solvent effects and cycloaddition adducts
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Noncoordinating solvents permit the halogen-metal exchange-induced formation of benzyne (aryne) from di- and trihalobenzene precursors in the presence of cyclopentadiene to give 1,4-dihydro-1,4-methano-naphthalenes. Studies with mixed halide precursors and nonacidic Diels-Alder diene traps reveal that ethereal and hydrocarbon solvents influence the halide leaving group facility, resulting in a reversal of 3-halobenzyne regioselectivity.
- Coe, Jotham W.,Wirtz, Michael C.,Bashore, Crystal G.,Candler, John
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p. 1589 - 1592
(2007/10/03)
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- The "Aryne" route to biaryls featuring uncommon substituent patterns
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1,2-Didehydroarenes ("arynes") mediate as extremely reactive, short-lived intermediates in selective aryl-aryl coupling processes to form biaryls with unprecedented substituent patterns (see scheme, X = H, F, Cl). Possible applications include the synthesis of novel ligands for asymmetric catalysis.
- Leroux, Frederic,Schlosser, Manfred
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p. 4272 - 4274
(2007/10/03)
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- Generation of functionalized asymmetric benzynes with TMP-zincates. Effects of ligands on selectivity and reactivity of zincates
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We have developed new methods for preparing functionalized benzynes through deprotonative zincation as a key reaction using R2Zn(TMP)Li, and we also describes dramatic ligand effects on the benzyne formation. Deprotonative zincation of various meta-substituted bromobenzenes with Me2Zn(TMP)Li proved effective for the one-pot generation of various 3-functionalized benzynes, particularly those electrophilic substituents such as ester, amide, and cyano. On the other hand, zincation with tBu2Zn(TMP)Li, followed by electrophilic trapping (with I2) proved a powerful tool for the preparation of 1,2,3-trisubstituted aromatic compounds.8 The resultant 1,2,3-trisubstituted benzenes are available as precursors for generation of 3-substituted benzynes by halogen-zinc exchange reactions with Me3ZnLi. These methods offer far greater generality than previous methods for the synthesis of functionalized asymmetric benzynes, and should be of value in new syntheses of various natural products and functional materials. In addition, these results underline the utility of spectator ligands on the central metal of ate complexes as a tunable functionality in the development of new ate complex-promoted reactions. Copyright
- Uchiyama, Masanobu,Miyoshi, Tomoko,Kajihara, Yumiko,Sakamoto, Takao,Otani, Yuko,Ohwada, Tomohiko,Kondo, Yoshinori
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p. 8514 - 8515
(2007/10/03)
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