- Substituent Effects on the Acid Hydration of Acetylenes
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The rates of hydration in aqueous sulfuric acid of 1-butyne, 2-butyne, 1-hexyne, 1-cyclopropylacetylene, and 1-butene are reported, together with rates in D2SO4 for the alkynes plus 3-hexyne.All of the compounds are proposed to react through the AdE2 mechanism of rate-limiting protonation on carbon.A general correlation of logkH+(alkyne)/log kH+(alkene) is observed, whose slope of 1.25 is a quantitative measure of the greater sensitivity to substituent effects of alkynes compared to alkenes in protonation.
- Allen, Annette D.,Chiang, Yvonne,Kresge, A. Jerry,Tidwell, Thomas T.
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Read Online
- Nickel-Catalyzed Reductive Cross-Coupling of N-Acyl and N-Sulfonyl Benzotriazoles with Diverse Nitro Compounds: Rapid Access to Amides and Sulfonamides
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Herein we report a Ni-catalyzed reductive transamidation of conveniently available N-acyl benzotriazoles with alkyl, alkenyl, and aryl nitro compounds, which afforded various amides with good yields and a broad substrate scope. The same catalytic reaction conditions were also applicable for N-sulfonyl benzotriazoles, which could undergo smooth reductive coupling with nitroarenes and nitroalkanes to afford the corresponding sulfonamides.
- Qu, Erdong,Li, Shangzhang,Bai, Jin,Zheng, Yan,Li, Wanfang
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supporting information
p. 58 - 63
(2021/12/27)
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- Rationally designed N-phenylsulfonylindoles as a tool for the analysis of the non-basic 5-HT6R ligands binding mode
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Among all of the monoaminergic receptors, the 5-HT6R has the highest number of non-basic ligands (approximately 5% of compounds stored in 25th version of ChEMBL database have the strongest basic pKa below 5, calculated using the Instant JChem c
- Staroń, Jakub,Bugno, Ryszard,Pietru?, Wojciech,Sata?a, Grzegorz,Mordalski, Stefan,Warszycki, Dawid,Hogendorf, Agata,Hogendorf, Adam S.,Kalinowska-T?u?cik, Justyna,Lenda, Tomasz,Pilarski, Bogus?aw,Bojarski, Andrzej J.
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supporting information
(2020/10/26)
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- Construction of Oxepino[3,2-b]indoles via [4+3] Annulation of 2-Ylideneoxindoles with Crotonate-Derived Sulfur Ylides
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A [4+3] annulation of 2-ylideneoxindoles with crotonate-derived sulfur ylides has been developed. A series of oxepino[3,2-b]indoles were prepared in moderate to excellent yields (62-93%) under mild conditions. Moreover, the synthetic oxepino[3,2-b] indoles can be further transformed into more complex cyclopropa[5,6]oxepino[3,2-b]indoles via a [2+1] cyclopropanation. In addition, the synthetic compounds show certain antiproliferative activity against K562 and MCF-7 cells, and its IC50 values for these two kinds of tumor cells up to 5.40±0.88 μM and 18.41±0.50 μM, respectively. (Figure presented.).
- Fei, Xing-Hai,Guan, Xiang,He, Bin,Li, Zong-Qin,Wang, Da-Peng,Yang, Fen-Fen,Yang, Yuan-Yong,Zhao, Yong-Long,Zhou, Meng
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supporting information
p. 3018 - 3024
(2021/06/26)
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- Transition-Metal-Free and Visible-Light-Mediated Desulfonylation and Dehalogenation Reactions: Hantzsch Ester Anion as Electron and Hydrogen Atom Donor
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Novel approaches for N- and O-desulfonylation under room temperature (rt) and transition-metal-free conditions have been developed. The first methodology involves the transformation of a variety of N-sulfonyl heterocycles and phenyl benzenesulfonates to the corresponding desulfonylated products in good to excellent yields using only KOtBu in dimethyl sulfoxide (DMSO) at rt. Alternately, a visible light method has been used for deprotection of N-methyl-N-arylsulfonamides with Hantzsch ester (HE) anion serving as the visible-light-absorbing reagent and electron and hydrogen atom donor to promote the desulfonylation reaction. The HE anion can be easily prepared in situ by reaction of the corresponding HE with KOtBu in DMSO at rt. Both protocols were further explored in terms of synthetic scope as well as mechanistic aspects to rationalize key features of desulfonylation processes. Furthermore, the HE anion induces reductive dehalogenation reaction of aryl halides under visible light irradiation.
- Heredia, Micaela D.,Guerra, Walter D.,Barolo, Silvia M.,Fornasier, Santiago J.,Rossi, Roberto A.,Budén, Mariá E.
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p. 13481 - 13494
(2020/12/15)
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- The generation of Indole-2,3-quinodimethanes from the Deamination of 1,2,3,4-Tetrahydropyrrolo[3,4-b]indoles
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A novel generation of indole-2,3-quinodimethanes via the deamination of 1,2,3,4-tetrahydropyrrolo[s3,4-b]indoles is reported.
- Rinderspacher, Alison,Gribble, Gordon W.
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- Electron Transfer Photoredox Catalysis: Development of a Photoactivated Reductive Desulfonylation of an Aza-Heteroaromatic Ring
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Herein, we report a protocol for desulfonylation of aza-heteroaromatic rings via photoinduced electron transfer and hydrogen atom transfer. This general protocol has a wide substrate range and moderate to good yields. The utility of the method was demonstrated by the chemoselective desulfonylation of a molecule containing both an aliphatic and an aromatic sulfonamide. (Figure presented.).
- Qiang-Liu,Liu, Yu-Xiu,Song, Hong-Jian,Wang, Qing-Min
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supporting information
p. 3110 - 3115
(2020/07/04)
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- Design and synthesis of azaindole heterocycle decorated new scaffold in fluorometric sensing of F? and H2PO4?
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7-Azaindole has been used in designing new molecular structure 1 on enediyne spacer for its application in anion sensing. New structure 1 has been established as efficient fluorescent sensor of H2PO4? and F? ion
- Ghosh, Kumaresh,Ali, Sk. Sarfaraj,Joardar, Soumen
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p. 3558 - 3565
(2020/08/06)
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- Iodine-Mediated Electrochemical C(sp2)-H Amination: Switchable Synthesis of Indolines and Indoles
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A metal-free electrochemical intramolecular C(sp2)-H amination using iodine as a mediator was developed. This method enables a switchable synthesis of indoline and indole derivatives, respectively, from easily available 2-vinyl anilines.
- Hu, Kangfei,Zhang, Yan,Zhou, Zhenghong,Yang, Yu,Zha, Zhenggen,Wang, Zhiyong
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supporting information
p. 5773 - 5777
(2020/08/05)
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- Regioselective C3-Phosphonation of Free Indoles via Transition-Metal-Free Radical/Hydrolysis Cascade
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The selectivity is of great importance for the preparation of molecules in organic chemistry. Herein, a novel method to enable the highly regioselective C3-phosphonation of free indoles has been developed. This transformation involves a radical and a hydrolysis procedure, and tolerates a range of functional groups, which gives an efficient route toward the 1H-indol-3 – ylphosphonic acid monoesters in one step.
- Guo, Shengmei,Jie, Kun,Zhang, Zhebin,Fu, Zhengjiang,Cai, Hu
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supporting information
p. 1808 - 1814
(2019/02/13)
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- IMIDAZO-PYRIDINE COMPOUNDS AS PAD INHIBITORS
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Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis. The process of preparation of the compounds of Formula (I), (II), and (III), their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof, along with a pharmaceutical composition comprising a compound of Formula (I), Formula (II), Formula (III), or a pharmaceutically acceptable salt thereof have also been described.
- -
-
Paragraph 000133; 000348
(2019/05/10)
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- Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety
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Thirty-six N-arylsulfonyl-3-substituted indoles were designed and synthesized by combining the N-arylsulfonylindoles with aminoguanidine, semicarbazide, and thiosemicarbazide, respectively. Their antibacterial activities were screened, and cytotoxic activities were evaluated. The results showed that aminoguanidines (6) exhibited much better antibacterial activity than semicarbazides (7) and thiosemicarbazides (8). Most compounds in series 6 showed potent inhibitory activity against the tested bacterial strains, including multidrug-resistant strains, with MIC values in the range of 1.08–23.46 μM. The cytotoxic activity of the compounds 6c, 6d, 6h, 6j, 6k and 6l was assessed in two human cancer cell lines A590 and SGC7901, and one human normal cell line HEK 293T. The results indicated that compounds selected exhibited excellent activity against the tested cancer cells with IC50 values in the range of 1.51–15.12 μM suggesting the potential of them as new antibacterial and anticancer agents. What's more, the results of resistance study revealed that resistance of the tested bacteria toward 6d is not easily developed. Molecular docking studies revealed that the aminoguanidine and arylsulfonylindole moieties played a significant role in binding the target site of E. coli FabH-CoA receptor.
- Song, Mingxia,Wang, Shiben,Wang, Zengtao,Fu, Zhiyang,Zhou, Shengchao,Cheng, Huabin,Liang, Zhuo,Deng, Xianqing
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p. 108 - 118
(2019/01/28)
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- Asymmetric Construction of 4 H-Pyrano[3,2-b]indoles via Cinchonine-Catalyzed 1,4-Addition of 2-Ylideneoxindole with Malononitrile
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A highly enantioselective [4 + 2] annulation of 2-ylideneoxindole with malononitrile has been accomplished by cinchonine catalysis under mild conditions. The corresponding enantiomerically enriched 4H-pyrano[3,2-b]indoles were generated in moderate to hig
- Zhou, Jin,Wang, Biao,He, Xiang-Hong,Liu, Li,Wu, Jun,Lu, Jing,Peng, Cheng,Rao, Chao-Long,Han, Bo
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p. 5450 - 5459
(2019/04/25)
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- Practical and Scalable Synthesis of Borylated Heterocycles Using Bench-Stable Precursors of Metal-Free Lewis Pair Catalysts
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A practical and scalable metal-free catalytic method for the borylation and borylative dearomatization of heteroarenes has been developed. This synthetic method uses inexpensive and conveniently synthesizable bench-stable precatalysts of the form 1-NHR2-2-BF3-C6H4, commercially and synthetically accessible heteroarenes as substrates, and pinacolborane as the borylation reagent. The preparation of several borylated heterocycles on 2 and 50 g scales was achieved under solvent-free conditions without the use of Schlenk techniques or a glovebox. A kilogram-scale borylation of one of the heteroarene substrates was also achieved using this cost-effective green methodology to exemplify the fact that our methodology can be conveniently implemented in fine chemical industries.
- Jayaraman, Arumugam,Misal Castro, Luis C.,Fontaine, Frédéric-Georges
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supporting information
p. 1489 - 1499
(2018/10/26)
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- Highly diastereoselective synthesis of cyclopropane-fused spiro-pseudoindoxyl derivatives through [2 + 1] annulation of 2-ylideneoxindoles and sulfonium bromides
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Compared with the intensively studied C3 spirooxindoles, limited reliable approaches are reported for synthesizing structurally analogous C2-spiropseudoindoxyl derivatives. Here, we developed an efficient method for highly diastereoselective synthesis of
- Tang, Xue,Zhu, Hong-Ping,Zhou, Jin,Chen, Yang,Pan, Xiao-Li,Guo, Li,Li, Jun-Long,Peng, Cheng,Huang, Wei
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supporting information
p. 8169 - 8174
(2018/11/23)
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- Heat Versus Basic Conditions: Intramolecular Dehydro-Diels-Alder Reaction of 1-Indolyl-1,6-heptadiynes for the Selective Synthesis of Substituted Carbazoles
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The intramolecular dehydro-Diels-Alder reaction of 1-indolyl-1,6-heptadiynes proceeds smoothly under rather mild heating conditions to give substituted carbazoles in moderate to good yields. The reaction of 7-aryl-1-indolyl-1,6-heptadiynes under heating gives the corresponding carbazoles chemoselectively in high yields, whereas the reaction under basic conditions gives naphthalenes as major products.
- Kudoh, Takayuki,Fujisawa, Syo,Kitamura, Megumi,Sakakura, Akira
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supporting information
p. 2189 - 2193
(2017/09/26)
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- Direct and Selective 3-Amidation of Indoles Using Electrophilic N-[(Benzenesulfonyl)oxy]amides
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Selective C-H amidation of 1H-indoles at the C3 position is reported as a direct entry to biologically important 3-aminoindoles. This transformation is achieved using novel N-[(benzenesulfonyl)oxy]amides as electrophilic nitrogen agents in the presence of ZnCl2. Interestingly, analogous reactions in the absence of ZnCl2 resulted in the formation of indole aminal products.
- Ortiz, Gerardo X.,Hemric, Brett N.,Wang, Qiu
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supporting information
p. 1314 - 1317
(2017/03/23)
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- Facile synthesis of indoles by K2CO3catalyzed cyclization reaction of 2-ethynylanilines in water
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The cyclization reaction of 2-ethynyl-N-sulfonylanilides proceeded efficiently in water with the presence of a catalytic amount of K2CO3under transition metal-free condition to give indoles in high yields. The recovery and reusabilit
- Chen, Zhi,Shi, Xiao-Xiao,Ge, Dong-Qin,Jiang, Zhen-Zhen,Jin, Qi-Qi,Jiang, Hua-Jiang,Wu, Jia-Shou
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supporting information
p. 231 - 234
(2017/01/28)
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- Highly efficient preparation of amides from aminium carboxylates using N-(p-toluenesulfonyl) imidazole
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Treatment of aminium carboxylates with N-(p-toluenesulfonyl)imidazole in the presence of triethylamine in DMF at 100 °C afforded the corresponding amides in good to excellent yields. N-(p-Toluenesulfonyl)imidazole proved to be a highly efficient coupling reagent for the preparation of numerous structurally diverse primary, secondary and tertiary amides.
- Behrouz, Somayeh,Rad, Mohammad Navid Soltani,Forouhari, Elham
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p. 101 - 106
(2016/03/08)
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- ANTI-BACTERIAL PYRUVATE KINASE MODULATOR COMPOUNDS, COMPOSITIONS, USES AND METHODS
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Compounds of general formula I that are capable of inhibiting bacterial pyruvate kinase and/or bacterial growth. The compounds may find use as antibacterial agents in therapeutic and/or non- therapeutic contexts.
- -
-
Paragraph 00235
(2016/04/26)
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- Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators
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Existing CB1 negative allosteric modulators (NAMs) fall into a limited range of structural classes. In spite of the theoretical potential of CB1 NAMs, published in vivo studies have generally not been able to demonstrate the expected therapeutically-relevant CB1-mediated effects. Thus, a greater range of molecular tools are required to allow definitive elucidation of the effects of CB1 allosteric modulation. In this study, we show a novel series of indole sulfonamides. Compounds 5e and 6c (ABD1075) had potencies of 4 and 3?nM respectively, and showed good oral exposure and CNS penetration, making them highly versatile tools for investigating the therapeutic potential of allosteric modulation of the cannabinoid system.
- Greig, Iain R.,Baillie, Gemma L.,Abdelrahman, Mostafa,Trembleau, Laurent,Ross, Ruth A.
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supporting information
p. 4403 - 4407
(2016/08/25)
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- A Palladium(II)-Catalyzed C-H Activation Cascade Sequence for Polyheterocycle Formation
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Polyheterocycles are found in many natural products and are useful moieties in functional materials and drug design. As part of a program towards the synthesis of Stemona alkaloids, a novel palladium(II)-catalyzed C-H activation strategy for the construction of such systems has been developed. Starting from simple 1,3-dienyl-substituted heterocycles, a large range of polycyclic systems containing pyrrole, indole, furan and thiophene moieties can be synthesized in a single step. Don't overdo it: A palladium(II)-catalyzed C-H activation cascade sequence for the synthesis of polyheterocycles is reported. Aromatization of the initially formed dihydro species occurred with a quinone oxidant. In some cases the use of one equivalent of the oxidant enabled isolation of the dihydro species as a single isomer (see scheme; X=NMe, O, S).
- Cooper, Stephen P.,Booker-Milburn, Kevin I.
-
supporting information
p. 6496 - 6500
(2015/06/02)
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- Ruthenium-catalyzed heteroatom-directed regioselective C-H arylation of indoles using a removable tether
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A new approach to C-2 arylated indoles has been developed by utilizing a ruthenium-catalyzed, heteroatom-directed regioselective C-H arylation. The reaction is highly site-selective and results in very good yields. The highlight of the work is the use of a removable directing group and compatibility of the catalytic system with halogen functional groups in the substrates.
- Tiwari, Virendra Kumar,Kamal, Neha,Kapur, Manmohan
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supporting information
p. 1766 - 1769
(2015/04/14)
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- N-SULFONYL INDOLE DERIVATIVE COMPOUND AND USE THEREOF
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PROBLEM TO BE SOLVED: To provide an N-sulfonyl indole derivative compound useful for the treatment of cancer and hypertension. SOLUTION: This invention provides an N-sulfonyl indole derivative compound represented by formula (1) where R1 is an aryl group, cycloalkyl group or heteroaryl group, and R2 is Si(R5)(R6)(R7), C1-C6 alkyl group or acetyl group. COPYRIGHT: (C)2016,JPOandINPIT
- -
-
Paragraph 0038
(2016/10/07)
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- Access to biaryl sulfonamides by palladium-catalyzed intramolecular oxidative coupling and subsequent nucleophilic ring opening of heterobiaryl sultams with amines
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The installation of sulfonamide pharmacophores on heterobiaryls has successfully been executed by a previously unknown palladium-catalyzed intramolecular oxidative coupling in N-arylsulfonyl heterocycles followed by novel ring opening of heterobiaryl sultams with amine nucleophiles. The protocol has a wide scope of substrates warranting broad applications in the synthesis of heterobiaryls containing an o-sulfonyl or carboxyl functional group.
- Laha, Joydev K.,Dayal, Neetu,Jethava, Krupal P.,Prajapati, Dilip V.
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supporting information
p. 1296 - 1299
(2015/03/14)
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- Structural Optimization of Indole Derivatives Acting at Colchicine Binding Site as Potential Anticancer Agents
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A new series of indole analogues based on our earlier lead compound, 2-(1H-indol-5-yl)-4-(3,4,5-trimethoxyphenyl)-1H-imidazo[4,5-c]pyridine (42), was prepared as tubulin inhibitors in an effort to find a molecule with improved cytotoxic potency and metabo
- Hwang, Dong-Jin,Wang, Jin,Li, Wei,Miller, Duane D.
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p. 993 - 997
(2015/09/22)
-
- Synthesis and in vitro antitumor activity of novel 2-alkyl-5- methoxycarbonyl-11-methyl-6H-pyrido[4,3-b]carbazol-2-ium and 2-alkylellipticin-2-ium chloride derivatives
-
Twenty-one types of novel ellipticine derivatives and pyridocarbazoles (5-methoxycarbonyl-11-methyl-6H-pyrido[4,3-b]carbazoles) with a nitrosourea moiety, linked by an oxydiethylene unit at the 2 position, were synthesized, and their cytotoxicity against HeLa S-3 cells was evaluated. Some of these new compounds exhibited potent antitumor activity by comparison with that of ellipticine.
- Mori, Ryota,Kato, Asako,Komenoi, Kousuke,Kurasaki, Haruaki,Iijima, Touru,Kawagoshi, Masashi,Kiran,Takeda, Sho,Sakai, Norio,Konakahara, Takeo
-
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- Rhodium(II)-catalyzed intramolecular annulation of 1-sulfonyl-1,2,3- triazoles with pyrrole and indole rings: Facile synthesis of N-bridgehead azepine skeletons
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A convenient and efficient synthetic method has been developed to construct highly functionalized N-bridgehead azepine skeletons, which are of great importance in biological and pharmaceutical industry. The reaction proceeds through a rhodium(II) azavinyl carbene intermediate, which initiated the intramolecular C-H functionalization with pyrrolyl and indolyl rings. A variety of azepine derivatives were obtained in moderate to good yields under mild reaction conditions with high chemoselectivity. Several interesting derivatizations of the resulting products demonstrate that this method is synthetically valuable and useful. Heads up: A convenient and efficient synthetic method of highly functionalized N-bridgehead azepine skeletons was developed using a rhodium(II)-catalyzed intramolecular annulation of pyrrolyl and indolyl triazoles. Several interesting transformations of the products into poly-heterocyclic products and the reaction mechanism are disclosed. Ts=4-toluenesulfonyl.
- Yang, Jin-Ming,Zhu, Cheng-Zhi,Tang, Xiang-Ying,Shi, Min
-
supporting information
p. 5142 - 5146
(2014/05/20)
-
- Discovery and optimization of a new class of pyruvate kinase inhibitors as potential therapeutics for the treatment of methicillin-resistant Staphylococcus aureus infections
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A novel series of bis-indoles derived from naturally occurring marine alkaloid 4 were synthesized and evaluated as inhibitors of methicillin-resistant Staphylococcus aureus (MRSA) pyruvate kinase (PK). PK is not only critical for bacterial survival which
- Kumar, Nag S.,Dullaghan, Edie M.,Finlay, B. Brett,Gong, Huansheng,Reiner, Neil E.,Jon Paul Selvam,Thorson, Lisa M.,Campbell, Sara,Vitko, Nicholas,Richardson, Anthony R.,Zoraghi, Roya,Young, Robert N.
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p. 1708 - 1725
(2014/03/21)
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- Synthesis and quantitative structure-activity relationship (QSAR) study of novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives as nematicidal agents
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In continuation of our program aimed at the discovery and development of natural-product-based pesticidal agents, 54 novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives were prepared, and their structures were well characterized by 1
- Che, Zhiping,Zhang, Shaoyong,Shao, Yonghua,Fan, Lingling,Xu, Hui,Yu, Xiang,Zhi, Xiaoyan,Yao, Xiaojun,Zhang, Rui
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p. 5696 - 5705
(2013/07/26)
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- Total synthesis of bouchardatine
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Two new, efficient and simple routes using Heck-type reaction and intramolecular cyclization were developed for the synthesis of the naturally occurring cytotoxic alkaloid 2-(4-oxo-3,4-dihydroquinazolin-2-yl)-1H-indole-3- carbaldehyde (bouchardatine).
- Naik, Nilesh H.,Urmode, Tukaram D.,Sikder, Arun K.,Kusurkar, Radhika S.
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p. 1112 - 1114
(2013/09/24)
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- HEPATITIS C INHIBITOR COMPOUNDS
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Compounds of Formula (I) wherein n, X1, X2, R1, R2, Y1, Y2 and RA are defined herein, are useful for the treatment of hepatitis C viral infection.
- -
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Page/Page column 45
(2013/03/26)
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- HEPATITIS C INHIBITOR COMPOUNDS
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A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6/sub
- -
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Page/Page column 69-70
(2013/03/26)
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- HETEROCYCLIC COMPOUNDS AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
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The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
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Page/Page column 129
(2013/04/13)
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- Azaindole-1,2,3-triazole conjugate as selective fluorometric sensor for dihydrogenphosphate
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A new receptor 1 has been designed and synthesized. The open cavity of 1 selectively recognizes H2PO4- over a series of other anions in CH3CN containing 0.01% DMSO by exhibiting a ratiometric change in emission.
- Ghosh, Kumaresh,Kar, Debasis,Joardar, Soumen,Sahu, Debashis,Ganguly, Bishwajit
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p. 16144 - 16151
(2013/09/12)
-
- Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H- pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4- (phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones
-
Several members of the quinazoline class of known tyrosine kinase inhibitors are approved anticancer agents, often showing selectivity for receptors of the HER/ErbB-family. Combining structural elements of this class with the bisindolylmethanone-structure
- Beckers, Thomas,Sellmer, Andreas,Eichhorn, Emerich,Pongratz, Herwig,Sch?chtele, Christoph,Totzke, Frank,Kelter, Gerhard,Krumbach, Rebekka,Fiebig, Heinz-Herbert,B?hmer, Frank-D.,Mahboobi, Siavosh
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experimental part
p. 125 - 136
(2012/02/16)
-
- NOVEL COMPOUNDS
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The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as in the description, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.
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Page/Page column 48
(2011/02/18)
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- Synthesis of a pentalene centered polycyclic fused system
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A novel pentalene-centered polycyclic 24π-electron system, IB1, was synthesized via a Pd-catalyzed homocoupling reaction. The geometry structure was studied by X-ray diffraction and theoretical method. The HOMO level of IB1 was studied by electrochemical
- Li, Yuliang,Yin, Xiaodong,Li, Yongjun,Zhu, Yulan,Kan, Yuhe,Zhu, Daoben
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scheme or table
p. 1520 - 1523
(2011/05/02)
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- Synthesis of 2-and 3-indolylpyrroles via 1,3-dipolar cycloadditions of muenchnones and nitroalkenes
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A series of 2-and 3-indolylpyrroles were generated via 1,3-dipolar cycloadditions between (2-nitrovinyl)indoles and symmetrical and unsymmetrical 1,3-oxazolium-5-olates (muenchnones). The Japan Institute of Heterocyclic Chemistry.
- Lopchuk, Justin M.,Gribble, Gordon W.
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scheme or table
p. 1617 - 1631
(2011/05/04)
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- Total synthesis of tryprostatins A and B
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Three distinct synthetic routes to the 2-prenyl tryptophan core skeleton of tryprostatins and their total syntheses are described. The strategies include a traditional gramine-mediated coupling reaction, Fuerstner indole synthesis, and our radical-mediated indole synthesis from o-alkenylphenyl isocyanide. The establishment of reliable conditions for the radical-mediated construction of indoles via a low-temperature radical initiator V-70 (2,2′-azobis(4- methoxy-2,4-dimethylvaleronitrile)) led to the highly efficient syntheses of tryprostatins A and B.
- Yamakawa, Takayuki,Ideue, Eiji,Iwaki, Yuzo,Sato, Ayumu,Tokuyama, Hidetoshi,Shimokawa, Jun,Fukuyama, Tohru
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scheme or table
p. 6547 - 6560
(2011/09/20)
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- Construction of carbocyclic ring of indoles using ruthenium-catalyzed ring-closing olefin metathesis
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The selective synthesis of substituted indoles was achieved by the ring-closing olefin metathesis (RCM)/elimination sequence or the RCM/tautomerization sequence of functionalized pyrrole precursors. The RCM/elimination sequence was also applied to double
- Yoshida, Kazuhiro,Hayashi, Kazushi,Yanagisawa, Akira
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supporting information; experimental part
p. 4762 - 4765
(2011/11/13)
-
- An efficient synthesis of N-arylsulfonylindoles from indoles and arylsulfonyl chlorides in the presence of triethylbenzylammonium chloride (TEBA) and NaOH
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An efficient synthesis of N-arylsulfonylindoles from indoles and arylsulfonyl chlorides in the presence of triethylbenzylammonium chloride (TEBA) and NaOH at room temperature is described.
- Xu, Hui,Wang, Yangyang
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scheme or table
p. 125 - 127
(2010/09/15)
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- NOVEL INDOLIC DERIVATIVES, THEIR PREPARATION PROCESSES AND THEIR USES IN PARTICULAR AS ANTIBACTERIALS
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The invention relates to the use of at least one compound of the formula (I), in which R and R3 are particularly a hydrogen atom, R1 is particularly a hydrogen atom or a methyl, ethyl or isobutyl mi group, R4, R5, R6 and R7 are independently a hydrogen atony, an alkoxyl group with 1 to 7 carbon atoms or a halogen atom, R2 is a hydrogen atom, an O? group or an OH group, B is an N-GP1 or NRc, group, GP1 being a Boc or Cbz group, and Rc is a hydrogen atom or a methyl or t-butyl group, for preparing a drug for treating conditions associated with bacterial infections, in particular for treating bacterial diseases.
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Page/Page column 45
(2010/06/19)
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- Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro
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In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-
- Ran, Jun-Qiang,Huang, Ning,Xu, Hui,Yang, Liu-Meng,Lv, Min,Zheng, Yong-Tang
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supporting information; experimental part
p. 3534 - 3536
(2010/08/21)
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- Antifungal agents. Part 5: Synthesis and antifungal activities of aminoguanidine derivatives of N-arylsulfonyl-3-acylindoles
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In order to discover more promising antifungal agents, a series of aminoguanidine derivatives of N-arylsulfonyl-3-acylindoles (5a-r) were prepared and evaluated in vitro for their antifungal activities against seven phytopathogenic fungi. Especially compo
- Xu, Hui,Wang, Yang-Yang
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scheme or table
p. 7274 - 7277
(2011/01/12)
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- Anti human immunodeficiency virus-1 (HIV-1) agents 3. Synthesis and in vitro anti-HIV-1 activity of some N-arylsulfonylindoles
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In order to find compounds with superior anti human immunodeficiency virus type 1 (HIV-1) activity, twelve simple N-arylsulfonylindoles (3a-l) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Several compounds demonstrated significant anti-HIV-1 activity, especially N-(3-nitrobenzene) sulfonyl-6-methylindole (3h) and N-(3-nitrobenzene)sulfonylindole (3i) showed the highest anti-HIV-1 activity with EC50 values of 0.26 and 0.74 μg/ml, and TI values of 543.78 and >270.27, respectively.
- Fan, Ling-Ling,Liu, Wu-Qing,Xu, Hui,Yang, Liu-Meng,Lv, Min,Zheng, Yong-Tang
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experimental part
p. 797 - 800
(2010/02/27)
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- Novel furanylarylene arylsulfonylindolesulfonamides: Synthesis and their antibacterial evaluation
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An array of furanylarylene arylsulfonylindolesulfonamides was synthesized through multi-step synthetic protocols involving bromination, stannylation, Stille cross coupling, reduction, arylsulfonylation, chlorosulfonylation, and condensation reactions. As
- Ramalingan, Chennan,Lee, In-Sook,Kwak, Young-Woo
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experimental part
p. 591 - 596
(2009/12/27)
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- Enhancement of chemically-induced HL-60 cell differentiation by 3,3′-diindolylmethane derivatives
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3,3′-Diindolylmethane (DIM, 1) and its derivatives have been prepared, and their enhancing effects on chemically-induced HL-60 cell differentiation were analyzed. Among the prepared compounds, IndDIM (12) showed the most potent enhancing effect on HL-60 cell differentiation induced by chemicals, including retinoids, 1,25-dihydroxyvitamin D3, 12-O-tetradecanoyl phorbol-13-acetate and dimethyl sulfoxide.
- Noguchi-Yachide, Tomomi,Tetsuhashi, Masashi,Aoyama, Hiroshi,Hashimoto, Yuichi
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experimental part
p. 536 - 540
(2009/12/27)
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- Reduction of arenediazonium salts by tetrakis(dimethylamino)ethylene (TDAE): Efficient formation of products derived from aryl radicals
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Tetrakis(dimethylamino)ethylene (TDAE 1), has been exploited for the first time as a mild reagent for the reduction of arenediazonium salts to aryl radical intermediates through a single electron transfer (SET) pathway. Cyclization of the aryl radicals produced in this way led, in appropriate substrates, to syntheses of indolines and indoles. Cascade radical cyclizations of aryl radicals derived from arenediazonium salts are also reported. The relative ease of removal of the oxidized by-products of TDAE from the reaction mixture makes the methodology synthetically attractive.
- Mahesh, Mohan,Murphy, John A.,Lestrat, Franck,Wessel, Hans Peter
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supporting information; experimental part
(2010/04/22)
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- A new family of tunable indolylphosphine ligands by one-pot assembly and their applications in Suzuki-Miyaura coupling of aryl chlorides
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(Chemical Equation Presented) This study describes a new class of indolylphosphine ligands, which can be easily accessed by a simple one-pot assembly from commercially available indoles, acid chlorides, and chlorophosphines. A combination of these three starting materials provides a high diversification of the ligand structure. The application of this ligand array in palladium-catalyzed Suzuki-Miyaura coupling reaction of aryl chlorides with arylboronic acids is described. A catalyst loading down to 0.01 mol % of Pd can be achieved.
- Chau, Ming So,Chung, Chiu Yeung,Chak, Po Lau,Fuk, Yee Kwong
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p. 7803 - 7806
(2008/12/22)
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- One-pot synthesis of bicyclic β-alkoxy amides from cyanohydrin ethers
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In this manuscript we report that Intramolecular Friedel-Crafts alkylation reactions of aryl-substituted a-alkoxy acylimines proceed in the presence of mild Lewis acids to afford bicyclic β-alkoxy amides. The intermediate acylimines are prepared through c
- Xiao, Qing,Floreancig, Paul E.
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supporting information; experimental part
p. 1139 - 1142
(2009/04/06)
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