- Pathways in the Degradation of Geminal Diazides
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The degradation of geminal diazides is described. We show that diazido acetates are converted into tetrazoles through the treatment with bases. The reaction of dichloro ketones with azide anions provides acyl azides, through in situ formation of diazido ketones. We present experimental and theoretical evidence that both fragmentations may involve the generation of acyl cyanide intermediates. The controlled degradation of terminal alkynes into amides (by loss of one carbon) or ureas (by loss of two carbons) is also shown.
- Holzschneider, Kristina,H?ring, Andreas P.,Haack, Alexander,Corey, Daniel J.,Benter, Thorsten,Kirsch, Stefan F.
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p. 8242 - 8250
(2017/08/14)
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- CLASS II HMG-COA REDUCTASE INHIBITORS AND METHODS OF USE
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Disclosed are compositions and methods for treating bacterial infections.
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Paragraph 0050
(2014/01/08)
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- Design and synthesis of boronic acid inhibitors of endothelial lipase
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Endothelial lipase (EL) and lipoprotein lipase (LPL) are homologous lipases that act on plasma lipoproteins. EL is predominantly a phospholipase and appears to be a key regulator of plasma HDL-C. LPL is mainly a triglyceride lipase regulating (V)LDL levels. The existing biological data indicate that inhibitors selective for EL over LPL should have anti-atherogenic activity, mainly through increasing plasma HDL-C levels. We report here the synthesis of alkyl, aryl, or acyl-substituted phenylboronic acids that inhibit EL. Many of the inhibitors evaluated proved to be nearly equally potent against both EL and LPL, but several exhibited moderate to good selectivity for EL.
- O'Connell, Daniel P.,Leblanc, Daniel F.,Cromley, Debra,Billheimer, Jeffrey,Rader, Daniel J.,Bachovchin, William W.
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scheme or table
p. 1397 - 1401
(2012/03/26)
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- Liquid-crystalline polymorphism of symmetrical azobananas: Bis(4-(4-alkylphenyl)azophenyl) 2-nitroisophtalates
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In this paper we present a series of novel compounds, bis(4-(4-alkylphenyl) azophenyl) 2-nitroisophtalates, which exhibit nematic and banana-type liquidcrystalline phases. The alkyl chain length varies from 1 to 18 carbons. The first ten members of this series exhibit nematic phase. The last eleven compounds exhibit banana-type liquid crystalline phases. The propyl and pentyl derivatives have extra second type of banana mesophase. Copyright Taylor & Francis Group, LLC.
- Zygadlo,Dardas,Nowicka,Hofmann,Galewski
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p. 283 - 291
(2011/08/02)
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- Novel routes to 4-substituted N,N-dialkylanilines, N-alkylanilines and anilines
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4-(Benzotriazol-1-ylmethyl)-N,N-dialkylanilines, -N-alkylanilines, -anilines and some substituted analogs obtained via lithiation are converted by lithium aluminum hydride or Grignard reagents into 4-substituted N,N-dialkylanilines, N-alkylanilines and anilines, respectively, in good yields.
- Katritzky, Alan R.,Lang, Hengyuan,Lan, Xiangfu
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p. 7445 - 7454
(2007/10/02)
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- Synthesis and evaluation of 4-alkylanilines as mammary tumor inhibiting aromatase inhibitors
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The 4-alkylanilines 1-20 were synthesized to elucidate the importance of the glutarimide moiety for the aromatase inhibiting activity of aminoglutethimide [3-(4-aminophenyl)-3-ethylpiperidine-2,6-dione, AG], the only non-steroidal aromatase inhibitor which is commercially available at present. The most interesting compounds were the (4-aminophenyl)cycloalkanes 4-6 (4, c-pentyl; 5, c-hexyl; 6, c-heptyl) and the 1-alkyl-1-(4-aminophenyl)cyclohexanes 1-3 (1, CH3; 2, C2H5; 3, n-C3H7). Derivatives 1-6 are stronger inhibitors of human placental aromatase than AG exhibiting relative potencies from 1.5 to 2.7 (AG≡1). For selectivity of action, the inhibition of desmolase (cholesterol side chain cleavage enzyme) was determined. Compounds 1-3 showed an inhibition comparable to AG, whereas compounds 4-6 exhibited no effect on desmolase. Being more potent and selective aromatase inhibitors in vitro, compounds 4-6, however, were not superior to AG in vivo, when the reduction of plasma estradiol concentration and the tumor inhibiting activity (PMSG-primed SD rats and DMBA-induced mammary carcinoma of the SD rat, postmenopausal model) were concerned.
- Hartmann,Batzl
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p. 537 - 544
(2007/10/02)
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- LIQUID CRYSTALLINE PROPERTIES OF 4-CHLOROBENZYLIDENE-4-AKYLANILINES
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A new group of Schiff bases containing a polar terminal group was synthesized: .The alkyl was changed from n=1 to n=12.Based on calorimetric (DSC) studies and on observations of textures the phase situation was characterized.
- Galewski, Zbigniew
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p. 233 - 242
(2007/10/02)
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- Mesomorphic Properties of the Homologous Series of 4-n-Propyl-4'-n-alkylazobenzenes and 4-n-Propyl-4'-n-alkylazoxybenzenes
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Two homologous series of compounds: 4-n-propyl-4'-n-alkylazobenzenes and 4-n-propyl-4'-n-alkylazoxybenzenes with 1 to 10 carbon atoms in the alkyl tail have been synthesized and their phase transition temperatures determined.
- Dabrowski, Roman,Kenig, Krystyna
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p. 183 - 189
(2007/10/02)
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- Substituted acetanilidoiminodiacetic acid compounds, diagnostic agents containing such compounds labeled with technetium-99m, and methods for making and using such compounds and agents
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What are disclosed are (2,3,4,5,6-pentafluoroacetanilido)-iminodiacetic acid and a method for its preparation from chloroacetic acid (2,3,4,5,6-pentafluoroanilide); (4-n-pentylacetanilido)-iminodiacetic acid and a method for its preparation from chloroacetic acid (4-n-pentylanilide); diagnostic agents for visualizing the heptobiliary system containing these substituted acetanilidoiminodiacetic acid compounds labeled with technetium-99m; and methods for making and using such diagnostic agents.
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- Study of the Influence of Molecular Length on the Characteristics of the Ordered Smectic Phase.
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Study of DTA and X-rays of p-phenyl-benzylidene-p'-alkylanilines of mesomorphic phases demonstrates the predominant role of the aliphatic chain length. In effect, it governs the appearance of the different phases; the correlation between layers decreases for greater chain lengths. The nonlinear variations of SmB layer thickness for these compounds shows clearly the importance of steric effects coupled with the molecular length with respect to the dipolar effect.
- Benattar,Levelut,Strzelecki
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p. 1233 - 1240
(2007/10/05)
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