- Novel sulfonamidospirobifluorenes as fluorescent sensors for mercury(ii) ion and glutathione
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Novel spirobifluorene derivatives containing two and four sulfonamide groups are successfully synthesized from the commercially available bromo-9,9′-spirobifluorene by Sonogashira couplings. These compounds exhibit an excellent selective fluorescence quen
- Silpcharu, Komthep,Sukwattanasinitt, Mongkol,Rashatasakhon, Paitoon
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Read Online
- A Gold Carbene Manifold to Prepare Fused γ-Lactams by Oxidative Cyclisation of Ynamides
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Gold-catalysed oxidative cyclisation reactions of ynamides offer great promise in γ-lactam synthesis but are limited by preferential over-oxidation to form α-keto imides. Evaluating the factors that might limit N-cyclisation pathways led to effective gold-catalysed conditions that allow access to different fused γ-lactams on changing the ynamide N-substituent and accommodate previously incompatible substitution patterns. New and efficient methods for the synthesis of functionalised 3-aryl indoles and cyclohepta[c]pyrrol-1-one derivatives are presented. These conditions illustrate the complementarity of gold catalysis to other metals.
- Sánchez-Cantalejo, Fernando,Priest, Joshua D.,Davies, Paul W.
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supporting information
p. 17215 - 17219
(2018/11/10)
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- Soft-Hard Acid/Base-Controlled, Oxidative, N-Selective Arylation of Sulfonanilides via a Nitrenium Ion
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In iodine(III)-catalyzed, dehydrogenative arylations of sulfonanilides, the functionalization of C-C bonds is preferred over the functionalization of C-N bonds. Herein, an unprecedented N-selective arylation of sulfonanilides using soft-hard acid-base (SHAB) control by a nitrenium ion over a carbenium ion is reported. Treatment of sulfonanilides with iodine(III) led to the formation of nitrenium ions (soft), which preferentially react with biphenyls (soft) over bimesityl (hard) to generate C-N bonds. The iodine(III) was generated in situ by using PhI and mCPBA at room temperature.
- Maiti, Saikat,Mal, Prasenjit
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p. 1340 - 1347
(2018/02/09)
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- An Organic Intermolecular Dehydrogenative Annulation Reaction
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The discovery of a direct method for the synthesis of three-ring heterocyclic carbazoles from unactivated arenes and anilides by a metal-free (organic) intermolecular dehydrogenative annulation reaction under ambient laboratory conditions is reported. Iodine(III) was used as the sole reagent either stoichiometrically from inexpensive phenyliodine diacetate or organocatalytically by in situ generation from PhI-mCPBA. In a single step, three C(sp2)-H bonds and one N(sp3)-H bond are functionalized from two different arenes for tandem C-C and C-N bond formation reactions.
- Maiti, Saikat,Achar, Tapas Kumar,Mal, Prasenjit
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supporting information
p. 2006 - 2009
(2017/04/28)
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- Palladium-Catalyzed cascade sp2 c?H bond functionalizations allowing one-Pot access to 4?Aryl-1,2,3,4-tetrahydroquinolines from n?Allyl?N?arylsulfonamides
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We have developed a palladium-catalyzed cascade reaction allowing an efficient synthesis of 4-aryl-1,2,3,4-tetrahydroquinolines from N-allyl-N-arylsulfonamides and benzenesulfonyl chlorides. In this transformation, two C(sp2)?C(sp3) bonds were formed via activation of C(sp2)?H bonds. The reaction proceeds using the easily accessible catalyst PdCl2, with Li2CO3 as inexpensive base and CuBr as additive, and tolerates a wide variety of substituents on both reaction partners.
- Yuan, Kedong,Soule, Jean-Francois,Dorcet, Vincent,Doucet, Henri
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p. 8121 - 8126
(2018/05/23)
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- COMPOUNDS AS HEPATITIS C VIRUS (HCV) INHIBITORS AND USES THEREOF IN MEDICINE
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Provided herein are compounds of Formula (I), or a stereoisomer, a geometric isomer, an enantiomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which are used in the treatment of HCV
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Paragraph 00153; 00184
(2016/01/25)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 132
(2014/08/07)
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- Desulfonylative radical ring closure onto aromatics. A modular route to benzazepin-2-ones and 5-arylpiperidin-2-ones
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Adducts from the intermolecular radical addition of N-xanthylacetyl-N- methanesulfanilides to Boc-protected allylamine undergo ring closure with loss of a methanesulfonyl radical to give benzazepin-2-ones. Upon deprotection and exposure to triethylamine,
- Charrier, Nicolas,Liu, Zhibo,Zard, Samir Z.
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supporting information; experimental part
p. 2018 - 2021
(2012/06/01)
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- 3,5-Disubstituted-thiazolidine-2,4-dione analogs as anticancer agents: Design, synthesis and biological characterization
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A series of 2,5-disubstituted-thiazolidine-2,4-dione analogs based on the newly identified lead 1, a potential anticancer agent via the inhibition of the Raf/MEK/extracellular signal regulated kinase (ERK) and phosphatidylinositol 3-kinase (PI3K)/Akt signaling cascades, were synthesized and biologically characterized. A new lead structure, 15, was identified to have improved anti-proliferative activities in U937 cells, to induce apoptosis in U937, M12 and DU145 cancer cells, and to arrest U937 cells at the S-phase. Furthermore, Western blot analysis demonstrated a correlation of the anti-proliferative activity and blockade of the Raf/MEK/ERK and PI3K/Akt signaling pathways. Collectively, these results strongly encourage further optimization of 15 as a new lead with multi-target properties to develop more potent compounds as anticancer agents.
- Liu, Kai,Rao, Wei,Parikh, Hardik,Li, Qianbin,Guo, Tai L.,Grant, Steven,Kellogg, Glen E.,Zhang, Shijun
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experimental part
p. 125 - 137
(2012/03/08)
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- HETEROCYCLIC DERIVED METALLOPROTEASE INHIBITORS
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This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
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Page/Page column 51
(2008/06/13)
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- β-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: Part 1. Design, synthesis, and lead identification
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A new series of β-N-biaryl ether sulfonamide hydroxamates as novel gelatinase inhibitors is described. These compounds exhibit good potency for MMP-2 and MMP-9 without inhibiting MMP-1. The structure-activity relationships (SAR) reveal the biaryl ether ty
- Yang, Shyh-Ming,Scannevin, Robert H.,Wang, Bingbing,Burke, Sharon L.,Wilson, Lawrence J.,Karnachi, Prabha,Rhodes, Kenneth J.,Lagu, Bharat,Murray, William V.
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p. 1135 - 1139
(2008/12/22)
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- Phenylpyridylpiperazine compounds
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A compound selected from those of formula (I): wherein: R1 represents an NR3SO2R4 group wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents an alkyl group, aryl group or
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Page/Page column 4
(2008/06/13)
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- Novel thiocarbamic acid derivatives and the pharmaceutical compositions containing the same
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The present invention relates to an antagonist against vanilloid receptor and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-opera
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- SULPHONAMIDE DERIVATIVES
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The invention concerns sulphonamide derivatives of the formula I wherein R1 includes (1-4C)alkyl; R2 and R3 together form ?A2 ?X2 ?A3? which defines a ring having 5 to 7 ring atoms, wherein A2 and A3 each is (1-3 C)alkylene and X2 is oxy, thio, sulphinyl or sulphonyl; A1 is a direct link to X1 or is (1-3 C)alkylene; X1 is oxy, thio, sulphinyl, sulphonyl or imino; Ar is optionally substituted phenylene or Ar is pyridylene; Q is nitrogen or of the formula CR7, wherein R7 includes hydrogen, halogeno, (1-4 C)alkyl and (1-4 C)alkoxy; each of R4 and R5 is (1-4 C)alkyl, (3-4 C)alkenyl, (3-4 C)alkynyl or optionally substituted phenyl, benzyl or pyridyl, or R5 may be hydrogen; and R6 has any of the meanings defined for R7; or a pharmaceutically-acceptable salt thereof; processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors
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