- PGDH INHIBITORS AND METHODS OF MAKING AND USING
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Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.
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Paragraph 0271; 0278; 0283; 0400-0401; 0438-0439
(2021/07/31)
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- Method for selective catalytic hydrogenation of aromatic heterocyclic compounds in non-hydrogen participation manner
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The invention discloses a method for selective catalytic hydrogenation of aromatic heterocyclic compounds in a non-hydrogen participation manner. The method comprises the following steps: by taking 1, 5-cyclooctadiene iridium chloride dimer as a catalyst and phenylsilane as a hydrogen source, carrying out stirring reaction under mild conditions without adding a ligand, namely catalytically hydrogenating the aromatic heterocyclic compounds to obtain hydrogenated products of the aromatic heterocyclic compounds. The method has the advantages of low cost, mild reaction conditions, high selectivity and the like, and special equipment such as a high-pressure kettle and the like and high-temperature conditions which are required when hydrogen is used are avoided.
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Paragraph 0025-0029; 0163-0167
(2021/08/19)
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- Catalytic Hydrogenation of Substituted Quinolines on Co–Graphene Composites
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A set of 20 composites was prepared by pyrolysis of Co2+ complexes with 1,10-phenanthroline, melamine and 1,2-diaminobenzene. These composites were tested as the catalysts for the hydrogenation of quinolines. As shown by powder X-ray diffraction and TEM, the composited contained Co particles of several dozen nm sizes. The composition (elements content), Raman spectra X-ray photoelectron spectra parameters of the composites were analyzed. It was found that there was no distinct factor that controlled the yield of 1,2,3,4-tetrahydroquinolines in the investigated process. The yields of the respective products were in the range 90–100 %. The three most active composites were selected for scale-up and hydrogenation of a series of substituted quinolines. Up to 97 % yield of 1,2,3,4-tetrahydroquinoline was obtained on a 50 g scale. Five representative substituted quinolines were synthesized on a 10–20 grams scale using the Co-containing composites as the catalysts.
- Asaula, Vitalii M.,Buryanov, Volodymyr V.,Solod, Bohdan Y.,Tryus, Daryna M.,Pariiska, Olena O.,Kotenko, Igor E.,Volovenko, Yulian M.,Volochnyuk, Dmitriy M.,Ryabukhin, Sergey V.,Kolotilov, Sergey V.
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p. 6616 - 6625
(2021/12/24)
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- Ring size changes in the development of class I HDAC inhibitors
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Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.
- Cho, Er-Chieh,Liu, Chi-Yuan,Tang, Di-Wei,Lee, Hsueh-Yun
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p. 1387 - 1401
(2021/07/06)
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- Simple manganese carbonyl catalyzed hydrogenation of quinolines and imines
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Manganese-catalyzed hydrogenation of unsaturated molecules has made tremendous progresses recently benefiting from non-innocent pincer or bidentate ligands for manganese. Herein, we describe the hydrogenation of quinolines and imines catalyzed by simple manganese carbonyls, Mn2(CO)10 or MnBr(CO)5, thus eliminating the prerequisite pincer-type or bidentate ligands.
- Wang, Zelong,Chen, Lei,Mao, Guoliang,Wang, Congyang
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p. 1890 - 1894
(2020/03/04)
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- Dual-Active-Sites Design of Co@C Catalysts for Ultrahigh Selective Hydrogenation of N-Heteroarenes
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The dual-active-sites Co@C catalyst provides a general powerful strategy to break the limitation of scaling relation on traditional metal surfaces and thus affords unprecedentedly selective hydrogenation of various N-heteroarenes as well as high activity and stability. A porous carbon shell not only allows H2 diffusion to Co sites for activation but also blocks accessibility of N-heteroarenes, and the hydrogenation of N-heteroarenes is achieved on carbon by the spilled hydrogen from Co sites. In addition, the presence of surface/subsurface carbon at the Co sites shows high anti-sulfur poisoning and anti-oxidant capability. Ideal heterogeneous metal hydrogenation catalysts are featured by simultaneously high activity, selectivity, and stability. Herein, we report a general yet powerful strategy to design and fabricate dual-active-sites Co@C core-shell nanoparticle for boosting selective hydrogenation of various N-heteroarenes. It can break the limitation of scaling relation on traditional metal surfaces, and thus afford unprecedentedly high selectivity, activity, and stability. Combining kinetics analysis and DFT calculations with multiple techniques directly unveil that the critical porous carbon shell with a pore size of 0.53 nm not only allows H2 diffusion to Co sites for activation and blocks accessibility of N-heteroarenes but also catalyzes hydrogenation of N-heteroarenes via hydrogen spillover from Co sites. In addition, the presence of surface/subsurface carbon at the Co sites shows high anti-sulfur poisoning and anti-oxidant capability. This work is valuable for guiding the design and manipulation of cost-effective and robust hydrogenation catalysts. Our research can provide an environmentally friendly approach to afford unprecedentedly selective N-heteroarenes hydrogenation, which will greatly reduce the resource and energy consumption and decrease the amount of waste discharge and water pollution. Therefore, these results could help in achieving the “Clean water and sanitation” goal in the 10 UN Sustainable Development Goals. Meanwhile, the products of N-heteroarenes hydrogenation are the core structural motifs in both fine and bulk chemicals, which will make our life more beautiful. Thus, our research also benefits the “Good health and well-being” goal.
- Zhang, Sai,Gan, Jie,Xia, Zhaoming,Chen, Xiao,Zou, Yong,Duan, Xuezhi,Qu, Yongquan
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supporting information
p. 2994 - 3006
(2020/09/04)
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- Nanolayered Cobalt-Molybdenum Sulfides as Highly Chemo- and Regioselective Catalysts for the Hydrogenation of Quinoline Derivatives
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Herein, a general protocol for the preparation of a broad range of valuable N-heterocyclic products by hydrogenation of quinolines and related N-heteroarenes is described. Interestingly, the catalytic hydrogenation of the N-heteroarene ring is chemoselectively performed when other facile reducible functional groups, including alkenes, ketones, cyanides, carboxylic acids, esters, and amides, are present. The key to successful catalysis relies on the use of a nanolayered cobalt-molybdenum sulfide catalyst hydrothermally synthesized from earth-abundant metal precursors. This heterogeneous system displays a tunable composition of phases that allows for catalyst regeneration. Its catalytic activity depends on the composition of the mixed phase of cobalt sulfides, being higher with the presence of Co3S4, and could also be associated with the presence of transient Co-Mo-S structures that mainly vanish after the first catalytic run.
- Sorribes, Iván,Liu, Lichen,Doménech-Carbó, Antonio,Corma, Avelino
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p. 4545 - 4557
(2018/05/22)
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- NHC-Based Iridium Catalysts for Hydrogenation and Dehydrogenation of N-Heteroarenes in Water under Mild Conditions
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We present a set of iridium complexes containing triazolylidene ligands that are highly active for the reduction of quinoline under 5 atm of H2 pressure and using water as a solvent. This reduction is effective also with a wide variety of quinolines having functionalities at the 2-, 3-, 6-, and 8-positions. One complex is active as well in catalyzing the reverse, viz., the dehydrogenation of tetrahydroquinoline, in high yields and in the same medium without the need of an external hydrogen scavenger. The use of a single catalyst for both hydrogenation and dehydrogenation processes is highly attractive for reversible hydrogen storage in liquid organic hydrogen carriers.
- Vivancos, ángela,Beller, Matthias,Albrecht, Martin
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- A General and Highly Selective Cobalt-Catalyzed Hydrogenation of N-Heteroarenes under Mild Reaction Conditions
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Herein, a general and efficient method for the homogeneous cobalt-catalyzed hydrogenation of N-heterocycles, under mild reaction conditions, is reported. Key to success is the use of the tetradentate ligand tris(2-(diphenylphosphino)phenyl)phosphine). This non-noble metal catalyst system allows the selective hydrogenation of heteroarenes in the presence of a broad range of other sensitive reducible groups.
- Adam, Rosa,Cabrero-Antonino, Jose R.,Spannenberg, Anke,Junge, Kathrin,Jackstell, Ralf,Beller, Matthias
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supporting information
p. 3216 - 3220
(2017/03/17)
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- Cobalt-catalysed transfer hydrogenation of quinolines and related heterocycles using formic acid under mild conditions
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Herein, we report the first example of homogeneous non-noble metal-catalyzed transfer hydrogenation of N-heteroarenes. The combination of Co(BF4)2·6H2O with tris(2-(diphenylphosphino)phenyl)phosphine L1 is able to selectively reduce quinolines in the presence of other sensitive functional groups, under mild conditions, using formic acid as a hydrogen source.
- Cabrero-Antonino, Jose R.,Adam, Rosa,Junge, Kathrin,Jackstell, Ralf,Beller, Matthias
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p. 1981 - 1985
(2017/07/15)
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- TETRAHYDROISOQUINOLINE COMPOUNDS AND THEIR USE AS PYRUVATE DEHYDROGENASE KINASE INHIBITORS
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A compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 is H, Cl, F, CH3 or CF3; R2 is H, C1-C6 alkyl or optionally substituted heteroaryl or optionally substituted aryl; and R3 is (Alk)n-Rn-(Alk)n-Rn-(Alk)n-X. The compounds are useful as tetrahydroisoquinoline (THQ) compounds, which are suitable for use as PDK inhibitors, for example for inhibition of cancer cell proliferation.
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Page/Page column 49; 54
(2015/04/15)
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- Tetrahydroquinoline derivatives as opioid receptor antagonists
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Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.58 nM
- Zhang, Cunyu,Westaway, Susan M.,Speake, Jason D.,Bishop, Michael J.,Goetz, Aaron S.,Carballo, Luz Helena,Hu, Mike,Epperly, Andrea H.
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scheme or table
p. 670 - 676
(2011/03/18)
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- N-THIAZOL-2-YL-BENZAMIDE DERIVATIVES
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The invention relates to N-thiazol-2-yl-benzamide derivatives of the formula I in the description wherein the variables are as defined in the claims. The compounds are A2A-receptor ligands, such as antagonists, agonists, reverse agonists or partial agonists, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.
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Page/Page column 31-32
(2008/06/13)
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- Palladium(II)-catalyzed heterocyclisation of 8-arylethynyl-1,2,3,4- tetrahydroquinolines: A facile route to 2-aryl-5,6-dihydro-4H-pyrrolo[3,2,1-ij] quinoline derivatives
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Dihydropyrroloquinolines have been synthesized reacting 8-arylethynyl-1,2,3,4-tetrahydroquinolines in the presence of palladium(II) chloride catalyst. Heteroannulation has been achieved in good yields and tolerates substituents on the tetrahydroquinoline,
- Marchand, Pascal,Puget, Alain,Le Baut, Guillaume,Emig, Peter,Czech, Michael,Günther, Eckhard
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p. 4035 - 4041
(2007/10/03)
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- Regio- and chemoselective transfer hydrogenation of quinolines catalyzed by a Cp*Ir complex
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An efficient method for the transfer hydrogenation of quinolines catalyzed by a Cp*Ir complex was developed. A variety of 1,2,3,4-tetrahydroquinolines were obtained by regio- and chemoselective transfer hydrogenation of quinolines using 2-propanol as a hydrogen source.
- Fujita, Ken-Ichi,Kitatsuji, Chihiro,Furukawa, Shigetoyo,Yamaguchi, Ryohei
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p. 3215 - 3217
(2007/10/03)
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- Pharmaceutical compounds
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This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, m and n have the values defined in claim 1, their preparation and use as pharmaceuticals.
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- Heterocyclic esters of rapamycin
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A compound of the structure STR1 wherein R and R1 are each, independently, STR2 or hydrogen, R2 is a heterocyclic radical which may be optionally substituted; n=0-6; with the proviso that R and R1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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- Reduction of Quinolinecarboxylic Acids by Raney Alloy
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The heterocyclic nucleus in quinolinecarboxylic acids is reduced by Raney alloy (nickel-aluminium) in alkaline media to give 1,2,3,4-tetrahydro-2-,3-,4-,5-,6-, and 8-quinolinecarboxylic acids and 8-methyl-5-quinolinecarboxylic acid and their ethyl esters.
- Gracheva, I. N.,Tochilkin, A. I.
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