- Rh(III)-Catalyzed C7-Thiolation and Selenation of Indolines
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The rhodium(III)-catalyzed intermolecular C7-thiolation and selenation of indolines with disulfides and diselenides were developed. This protocol relies on the use of a removable pyrimidyl directing group to access valuable C-7 functionalized indoline scaffolds with ample substrate scope and broad functional group tolerance.
- Xie, Wucheng,Li, Bin,Wang, Baiquan
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- Effect of C7-substitution of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indolines on the selectivity towards a subclass of histone deacetylases
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This study focused on the substitution effect at position C7 of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indolines. Compound 9, (E)-3-(7-amino-1-(4-methoxyphenylsulfonyl)indolin-5-yl)-N-hydroxyacrylamide, displayed 4- to 14-fold more potent antiproliferative
- Lee, Hsueh-Yun,Wang, Li-Ting,Li, Yu-Hsuan,Pan, Shiow-Lin,Chen, Yi-Lin,Teng, Che-Ming,Liou, Jing-Ping
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- Pd/C-Catalyzed transfer hydrogenation ofN-H indoles with trifluoroethanol and tetrahydroxydiboron as the hydrogen source
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Under the guidance of the known mechanism of the hydrogenation of indoles and transfer hydrogenation with tetrahydroxydiboron (B2(OH)4), Pd/C catalyzed transfer hydrogenation ofN-H indoles with trifluoroethanol and tetrahydroxydiborane as the hydrogen source has been developed. This provides an efficient strategy and catalytic system for the reduction of un-activatedN-H indoles, andN-H indolines are obtained with good to excellent yields. In addition, a series of the isotopic labelling experiments were carried out to probe the mechanism.
- Zhou, Xiao-Yu,Chen, Xia
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- Expedient cobalt(II)-catalyzed site-selective C7-arylation of indolines with arylboronic acids
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Cobalt(ii)-catalyzed pyrimidyl directing group-assisted C7 arylation of indolines with arylboronic acids has been developed using Mn(OAc)2·4H2O as an oxidant. The use of cobalt(ii)-PCy3 as a catalyst and broad substrate scope are the important practical features.
- De, Pinaki Bhusan,Pradhan, Sourav,Banerjee, Sonbidya,Punniyamurthy, Tharmalingam
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- Heterogeneous catalytic hydrogenation of unprotected indoles in water: A green solution to a long-standing challenge
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An environmentally benign procedure for the hydrogenation of unprotected indoles is described. The hydrogenation reaction is catalyzed by Pt/C and activated by p-toluenesulfonic acid in water as a solvent. The efficacy of the method is illustrated by the hydrogenation of a variety of substituted indoles to their corresponding indolines which were obtained in excellent yields.
- Kulkarni, Aditya,Zhou, Weihong,Toeroek, Bela
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- 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; 0460-0461
(2021/07/31)
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- Manganese(III) Acetate Catalyzed Aerobic Dehydrogenation of Tertiary Indolines, Tetrahydroquinolines and an N-Unsubstituted Indoline
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A Mn(OAc)3 ? 2H2O-catalyzed aerobic dehydrogenation of five and six-membered N-heterocycles for the synthesis of N-heteroarenes is reported. Of note, this protocol can be applied to the dehydrogenation of tertiary indolines with various electron-deficient N-substituents. Preliminary mechanistic investigations support that a single-electron transfer pathway might be involved. (Figure presented.).
- Niu, Xiaokang,Yang, Lei
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supporting information
p. 4209 - 4215
(2021/08/06)
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- Hydrogenation or Dehydrogenation of N-Containing Heterocycles Catalyzed by a Single Manganese Complex
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A highly chemoselective base-metal catalyzed hydrogenation and acceptorless dehydrogenation of N-heterocycles is presented. A well-defined Mn complex operates at low catalyst loading (as low as 2 mol %) and under mild reaction conditions. The described catalytic system tolerates various functional groups, and the corresponding reduced heterocycles can be obtained in high yields. Experimental studies indicate a metal-ligand cooperative catalysis mechanism.
- Borghs, Jannik C.,Rueping, Magnus,Zubar, Viktoriia
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supporting information
(2020/05/19)
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- Aerobic Dehydrogenation of N-Heterocycles with Grubbs Catalyst: Its Application to Assisted-Tandem Catalysis to Construct N-Containing Fused Heteroarenes
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An aerobic dehydrogenation of nitrogen-containing heterocycles catalyzed by Grubbs catalyst is developed. The reaction is applicable to various nitrogen-containing heterocycles. The exceptionally high functional group compatibility of this method was confirmed by the oxidation of an unprotected dihydroindolactam V to indolactam V. Furthermore, by taking advantage of the oxygen-mediated structural change of the Grubbs catalyst, we integrated ring-closing metathesis and subsequent aerobic dehydrogenation to develop the novel assisted-tandem catalysis using molecular oxygen as a chemical trigger. The utility of the assisted-tandem catalysis was demonstrated by the concise synthesis of N-containing fused heteroarenes including a natural antibiotic, pyocyanine.
- Kawauchi, Daichi,Noda, Kenta,Komatsu, Yoshiyuki,Yoshida, Kei,Ueda, Hirofumi,Tokuyama, Hidetoshi
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supporting information
p. 15793 - 15798
(2020/10/12)
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- HETEROBICYCLIC AROMATIC DERIVATIVES FOR THE TREATMENT OF FERROPTOSIS-RELATED DISORDERS
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The present application discloses heterobicyclic and non-heterobicyclic aromatic derivative compounds and compositions, and methods for treating ferroptosis-related disorders and diseases in patients using the compounds and compositions as disclosed herei
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Paragraph 120
(2019/06/17)
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- INDOLINE COMPOUNDS FOR TREATMENT AND/OR PREVENTION OF INFLAMMATION DISEASES
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The invention is based on the discovery that 1-arylsulfonyl-5-(N-hydroxyacrylamide)indolines and 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles has great potential as a novel agent to be used in the treatment of inflammation-associated diseases, particular
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Paragraph 0072
(2016/01/15)
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- FUSED 1,4-DIHYDRODIOXIN DERIVATIVES AS INHIBITORS OF HEAT SHOCK TRANSCRIPTION FACTOR 1
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The present invention relates to compounds of formula I wherein A1, A2 R4 and Q are as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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Paragraph 0043
(2015/04/22)
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- Selective reduction of condensed N-heterocycles using water as a solvent and a hydrogen source
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The reduction of unprotected indoles and quinolines is described using water as a hydrogen source. The method is based on the application of a RANEY type Ni-Al alloy in an aqueous medium. During the reaction the Al content of the alloy, used as reductants, reacts with water in situ providing hydrogen and a RANEY Ni catalyst, thus the alloy serves as a hydrogen generator as well as a hydrogenation catalyst. The simplicity and efficacy of the method are illustrated by the selective reduction of a variety of substituted indoles and quinolines to indolines and tetrahydroquinolines, respectively.
- Cho, Hyejin,T?r?k, Fanni,T?r?k, Béla
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p. 1209 - 1215
(2013/04/10)
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- HISTONE DEACETYLASE INHIBITORS
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Provided herein are isoform selective histone deacetylase inhibitors of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, metabolites, prodrugs, solvates, pharmaceutically acceptable salts and compositions thereof. These compounds are isoform selective inhibitors of HDACs and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as cancer, malignant tumors, autoimmune diseases, skin diseases, fungal infections, protozoal infections, HIV, inflammation and CNS disorders.
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Page/Page column 41-42
(2012/09/21)
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- AMINO-PYRROLIDINE-AZETIDINE DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
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Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula
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Page/Page column 54; 55
(2012/05/04)
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- INDOLYL OR INDOLINYL HYDROXAMATE COMPOUNDS
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Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.
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Page/Page column 10
(2011/10/13)
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- NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO
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New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2, X3, X4, Y1
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Page/Page column 51
(2011/01/12)
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- Design, synthesis and antiviral efficacy of a series of potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitors
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Design, synthesis and biological evaluation of a series of 5-chloropyridine ester-derived severe acute respiratory syndrome-coronavirus chymotrypsin-like protease inhibitors is described. Position of the carboxylate functionality is critical to potency. I
- Ghosh, Arun K.,Gong, Gangli,Grum-Tokars, Valerie,Mulhearn, Debbie C.,Baker, Susan C.,Coughlin, Melissa,Prabhakar, Bellur S.,Sleeman, Katrina,Johnson, Michael E.,Mesecar, Andrew D.
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scheme or table
p. 5684 - 5688
(2009/05/30)
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- Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5- carboxamide, an agonist of the α7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: Synthesis and structure-activity relationship
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N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the α7 neuronal nicotinic acetylcholine receptor (α7 nAChR), has been identified as a potential treatment of cognitive deficits in schizophrenia. Compound 14 is a potent and selective a7 nAChR agonist with an excellent in vitro profile. The compound is characterized by rapid brain penetration and high oral bioavailability in rat and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition.
- Wishka, Donn G.,Walker, Daniel P.,Yates, Karen M.,Reitz, Steven C.,Jia, Shaojuan,Myers, Jason K.,Olson, Kirk L.,Jacobsen, E. Jon,Wolfe, Mark L.,Groppi, Vincent E.,Hanchar, Alexander J.,Thornburgh, Bruce A.,Cortes-Burgos, Luz A.,Wong, Erik H. F.,Staton, Brian A.,Raub, Thomas J.,Higdon, Nicole R.,Wall, Theron M.,Hurst, Raymond S.,Walters, Rodney R.,Hoffmann, William E.,Hajos, Mihaly,Franklin, Stanley,Carey, Galen,Gold, Lisa H.,Cook, Karen K.,Sands, Steven B.,Zhao, Sabrina X.,Soglia, John R.,Kalgutkar, Amit S.,Arneric, Stephen P.,Rogers, Bruce N.
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p. 4425 - 4436
(2007/10/03)
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- INHIBITORS OF HISTONE DEACETYLASE
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The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
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Page/Page column 144
(2010/02/11)
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- Manganese(III) Acetate Oxidation of 1-Acetylindole Derivatives
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In the presence of malonic acid, the reaction of 1-acetylindole (2) with manganese(III) acetate resulted in the formation of 4-acetyl-3,3a,4,8b-tetrahydro-2H-furoindol-2-one (5).The same reaction of 1-acetyl-2,3-dimethylindole yielded a mixture of 2-acetoxymethyl-1-acetyl-3-methylindole and 4-acetyl-3a,8b-dimethyl-3,3a,4,8b-tetrahydro-2H-furoindol-2-one, furthermore, the oxidation of 1-acetylindoline proceeded to the formation of 2,5 and 1-acetylindoline-5-carboxylic acid.
- Izumi, Taeko,Kohei, Kunihiro,Murakami, Satoshi
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p. 1133 - 1136
(2007/10/02)
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- Pharmaceutical compounds
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A pharmaceutical compound of the formula STR1 in which A is selected from --NHCOR1, --NHCOOR1, --NHCONHR1, --NHCSNHR1, --CONHR1, where R1 is optionally halo-substituted C1-10 alk
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