- Silicon-directed oxa-Pictet-Spengler cyclization and an unusual dimerization of 2-trimethylsilanyl tryptophols
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(Chemical Equation Presented) The tetrahydro-pyrano[3,4-b]indoles 6 were synthesized from 2-(2-trimethylsilanyl-1H-indol-3-yl)-ethanols 5 and various ketones or aldehydes through silicon-directed oxa-Pictet-Spengler cyclizations. An unusual reaction led to the dimeric products 7 when some of 5 was treated with acetone using BF3 as the catalyst.
- Zhang, Xuqing,Li, Xiaojie,Lanter, James C.,Sui, Zhihua
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Read Online
- 5, 10-dihydroindolo [3, 2-b] indole derivative and synthesis method and application thereof
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The invention discloses a synthesis method of a 5, 10-dihydroindolo [3, 2-b] indole derivative, the method comprises the following steps: mixing a 2-((2-halogen phenyl) ethynyl)-N, N-dimethylaniline derivative (II), N, N-di-tert-butyl diazacycloketone (III), a palladium catalyst, a monophosphine ligand, alkali and a first organic solvent, and carrying out a diamidation reaction under the protection of inert gas to realize the synthesis of the 5, 10-dihydroindolo [3, 2-b] indole derivative(I). The method is easy to operate, mild in reaction condition and high in reaction yield, and the synthesized 5, 10-dihydroindolo [3, 2-b] indole derivative can be used for preparing an organic light-emitting device.
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Paragraph 0139; 0141-0142
(2021/07/17)
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- New indolo[1,2-c]quinazolines for single-crystal field-effect transistor: A united experimental and theoretical studies
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Here, we account the synthesis and characterization of a series of symmetrical fused heterocyclic aromatic hydrocarbons (HAHs) with an indolo[1,2-c]quinazoline (IQ) as the core moiety. All the new HAHs IQ series were systematically investigated by using various spectroscopic methods. Furthermore, their photo-physical properties were supported by density functional theory (DFT) and time-dependent density functional theory (TDDFT) studies to support the experimental findings. The tetramethyl-substituted indolo[1,2-c]quinazoline (TMIQ) compound is shown to exhibit the shifted type of π–π stacking interactions, which render this series as a new semiconducting material. Single-crystal-based field-effect transistor devices of TMIQ exhibited efficient charge transport behavior, giving a p-channel field-effect mobility of 0.25 cm2?V?1?s?1 with an on/off ratio of 5 × 105.
- Puli, Venkat Swamy,Kilaru, Suresh,Bhongiri, Yadagiri,Marri, Sreenath Reddy,Tripathi, Anuj,Chetti, Prabhakar,Chatterjee, Anindita,Vukoti, Kiran Kumar,Pola, Someshwar
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- SULFONYL-SUBSTITUTED BICYCLIC COMPOUND WHICH ACTS AS ROR INHIBITOR
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Provided is a sulfonyl-substituted bicyclic compound (A) which acts as a RORγ inhibitor, said compound has good RORγ inhibitory activity and is expected to be used for treating diseases mediated by a RORγ receptor in mammals.
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Paragraph 0259; 0260
(2020/08/16)
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- One-Pot Access to Benzo[a]carbazoles via Palladium(II)-Catalyzed Hetero- and Carboannulations
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A Pd(II)-catalyzed direct synthesis of benzo[a]carbazoles has been achieved through aminopalladation of alkynes, followed by intramolecular nucleophilic addition of the generated carbon-palladium bond to a tethered cyano/aldehyde group. Compared to literature procedures, this synthetic approach is operationally simple, uses simple substrates, and offers a fast intramolecular assembly resulting in the direct synthesis of benzo[a]carbazoles in which a wide variation of substituents at different sites is well-tolerated, leaving enough opportunity for diversification.
- Jash, Moumita,Das, Bimolendu,Chowdhury, Chinmay
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supporting information
p. 10987 - 10999
(2016/11/28)
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- METHOD FOR PROMOTING PLANT GROWTH
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The present invention provides a method for promoting plant growth, which comprises treating a plant with at least one compound represented by the following Formula (1) The compounds indicated by formula (1) are used to promote the growth of plants. A pla
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Paragraph 1208; 1209
(2015/11/17)
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- Gold(I)-catalyzed iodination of arenes
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A wide variety of electron-rich arenes were efficiently converted into the corresponding iodinated compounds via a gold(I)-catalyzed reaction under mild conditions. Georg Thieme Verlag Stuttgart. New York.
- Leboeuf, David,Ciesielski, Jennifer,Frontier, Alison J.
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supporting information
p. 399 - 402
(2014/03/21)
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- Au-catalyzed formation of functionalized quinolines from 2-alkynyl arylazide derivatives
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A new method for converting 2-alkynyl arylazide derivatives into functionalized polysubstituted quinolines following a gold-catalyzed 1,3-acetoxy shift/cyclization/1,2-group shift sequence has been developed. This transformation proceeds under mild reaction conditions, is efficient, and tolerates a large variety of functional groups.
- Gronnier, Colombe,Boissonnat, Guillaume,Gagosz, Fabien
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p. 4234 - 4237
(2013/09/12)
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- NEW COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.
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Paragraph 0627-0628
(2013/10/22)
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- NOVEL COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1), wherein R1, R2, R4, R5, R6, E, n, Y1, Y2, Y3, Y4, Y5, B, R8, and m are as defined in the claims.
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Paragraph 0510; 0532-0533
(2013/11/06)
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- Spiro heterocycles as potential inhibitors of SIRT1: Pd/C-mediated synthesis of novel N-indolylmethyl spiroindoline-3,2′-quinazolines
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Novel N-indolylmethyl substituted spiroindoline-3,2′-quinazolines were designed as potential inhibitiors of SIRT1. These compounds were synthesized in good yields by using Pd/C-Cu mediated coupling-cyclization strategy as a key step involving the reaction of 1-(prop-2-ynyl)-1′H- spiro[indoline-3,2′-quinazoline]-2,4′(3′H)-dione with 2-iodoanilides. Some of the compounds synthesized have shown encouraging inhibition of Sir 2 protein (a yeast homologue of mammalian SIRT1) in vitro and three of them showed dose dependent inhibition of Sir 2. The docking results suggested that the benzene ring of 1,2,3,4-tetrahydroquinazolin ring system of these molecules occupied the deep hydrophobic pocket of the protein and one of the NH along with the sulfonyl group participated in strong H-bonding interaction with the amino acid residues.
- Rambabu,Raja, Guttikonda,Yogi Sreenivas,Seerapu,Lalith Kumar,Deora, Girdhar Singh,Haldar, Devyani,Rao, M.V.Basaveswara,Pal, Manojit
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supporting information
p. 1351 - 1357
(2013/03/14)
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- NOVEL COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1), wherein R1, R2, R4, R5, R6, E, n, Y1, Y2, Y3, Y4, Y5, B, R8, and m are as defined in the claims.
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Page/Page column 71; 75
(2012/06/30)
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- NEW COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.
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Page/Page column 84-85
(2012/06/30)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 196
(2011/10/05)
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- Potassium tert-butoxide promoted intramolecular arylation via a radical pathway
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Potassium tert-butoxide mediated intramolecular cyclization of aryl ethers, amines, and amides was efficiently performed under microwave irradiation to provide the corresponding products in high regioisomeric ratios. The reaction proceeds via single-electron transfer to initiate the formation of an aryl radical, followed by a kinetically favored 5-exo-trig and subsequent ring expansion.
- Roman, Daniela Sustac,Takahashi, Yoko,Charette, Andre B.
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supporting information; scheme or table
p. 3242 - 3245
(2011/08/02)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 91
(2010/06/11)
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- Synthesis and evaluation of a series of C5′-substituted duocarmycin SA analogs
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The synthesis and evaluation of a key series of analogs of duocarmycin SA, bearing a single substituent at the C5′ position of the DNA binding subunit, are described.
- Robertson, William M.,Kastrinsky, David B.,Hwang, Inkyu,Boger, Dale L.
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supporting information; experimental part
p. 2722 - 2725
(2011/07/06)
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- INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES
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This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
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Page/Page column 187
(2010/12/29)
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- Synthesis of α-ketoester- and α-hydroxyester-substituted isoindazoles via the thermodynamic coarctate cyclization of ester-terminated azo-ene-yne systems
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(Chemical Equation Presented) The synthesis of isoindazoles bearing α-ketoester and R-hydroxyester groups via the coarctate cyclization of ester-terminated azo-ene-yne precursors is described. Whereas previous studies on isoindazole formation have shown t
- McClintock, Sean P.,Forster, Nathan,Herges, Rainer,Haley, Michael M.
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experimental part
p. 6631 - 6636
(2009/12/31)
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- Indole Compounds, Method of Preparing Them and Uses Thereof
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Indole compounds corresponding to the formula (I): as defined in the claims, pharmaceutically acceptable addition salts of such compounds, pharmaceutical compositions containing such compounds, the process for their preparation, and their use as pharmacol
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Page/Page column 7
(2008/12/06)
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- Acetonitrile-mediated synthesis of 2,4-dichloroquinoline from 2-ethynylaniline and 2,4-dichloroquinazoline from anthranilonitrile
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2,4-Dichloroquinolines and 2,4-dichloroquinazolines were synthesized from 2-ethynylanilines and anthranilonitriles, respectively, using diphosgene in acetonitrile and heating at 130 °C or 150 °C for 12 hours. This reaction was applied to the synthesis of 4,6-dichloropyrazolo[3,4-d]pyrimidine (dichloro-9H-isopurine). The postulated mechanism is also described. Georg Thieme Verlag Stuttgart.
- Lee, Jae Hak,Lee, Byoung Se,Shin, Hyunik,Nam, Do Hyun,Chi, Dae Yoon
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- Nickel-catalyzed cyclization of 2-iodoanilines with aroylalkynes: An efficient route for quinoline derivatives
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An efficient and convenient nickel-catalyzed cyclization of 2-iodoanilines with alkynyl aryl ketones to give 2,4-disubstituted quinolines was developed. The reaction can be employed for the synthesis of naturally occurring quinoline derivatives in good yields. On the basis of the regiochemistry of the products, the possible pathway for the reaction is via the formation of o-aminochalcone.
- Korivi, Rajendra Prasad,Cheng, Chien-Hong
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p. 7079 - 7082
(2007/10/03)
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- 1,1,1-TRIFLUORO-4-PHENYL-4-METHYL-2-(1H-PYRROLO
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Compounds of Formula (IA), IB), IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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Page/Page column 187
(2010/02/11)
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- Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
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The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
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Page/Page column 34
(2010/02/11)
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- TREATMENT FOR ALZHEIMER'S DISEASE AND RELATED CONDITIONS
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Compounds of formula (I): are useful in the treatment of diseases associated with deposition of β-amyloid in the brain.
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Page/Page column 47-49
(2010/02/10)
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- Nonmetal-catalyzed iodination of arenes with iodide and hydrogen peroxide
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Oxidative iodination of arenes was carried out with one equivalent of KI and two equivalents of 30% hydrogen peroxide in MeOH in the presence of strong acid. Reactions of various substituted anisoles, phenols and anilines, as well as mesitylene and uracil, were selective and effective with very good yields of isolated halogenated aromatic molecules.
- Iskra, Jernej,Stavber, Stojan,Zupan, Marko
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p. 1869 - 1873
(2007/10/03)
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- Novel 3,4-Dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a
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The preparation of a series of substituted indoles coupled to six- and seven-membered cyclic lactams is described and their role as human glycogen phosphorylase a inhibitors discussed. The SAR of the indole moiety and lactam ring are presented.
- Rosauer, Keith G.,Ogawa, Anthony K.,Willoughby, Chris A.,Ellsworth, Kenneth P.,Geissler, Wayne M.,Myers, Robert W.,Deng, Qiaolin,Chapman, Kevin T.,Harris, Georgianna,Moller, David E.
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p. 4385 - 4388
(2007/10/03)
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- Practical syntheses of 5-trifluoromethyl-1H-indoles
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Short and convenient syntheses of 5-trifluoromethyltryptamine and 5-trifluoromethyltryptophole have been realized via a regioselective, palladium catalyzed, coupling/annulation method involving functionalized alkynes and 2-iodo-4-trifluoromethylaniline. A new and improved approach for the preparation of 5-trifluoromethyl-1H-indole is also described.
- Parmentier, Jean-Gilles,Poissonnet, Guillaume,Goldstein, Solo
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p. 465 - 476
(2007/10/03)
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- Preparation and pharmacological profile of 2-trifluoromethyl-benzo(8,9)-1,3-diaza-spiro(4,6)-undeca-2,8-diene and its enantiomers as new anti-obesity agents
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Obesity affects a large population of industrialised countries in which occurrence may reach 20%. The multifactorial aspect of the pathology prompted us to develop new entities associating favourable effects on both eating behaviour and metabolic paramete
- Boussard,Guette,Wierzbicki,Beal,Fournier,Boulanger,Della-Zuana,Duhault
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p. 1084 - 1092
(2007/10/03)
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- Amide-based protecting/radical translocating (PRT) groups. Generation of radicals adjacent to carbonyls by 1,5-hydrogen transfer reactions of o-iodoanilides
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The o-iodoanilide group is shown to be broadly useful for the generation and subsequent reactions of radicals adjacent to carboxyl groups. The results indicate that this group is one of the best 'protecting/radical translocating' (PRT) groups introduced t
- Curran, Dennis P.,Yu, Hosung,Liu, Hongtao
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p. 7343 - 7366
(2007/10/02)
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