- In search of acyclic analogues as universal nucleosides in degenerate probes
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Five acyclic nucleoside analogues with unnatural base moieties have been synthesized of which three successfully were incorporated into oligonucleotides. The acyclic analogue containing the base 5-nitroindazole was the least discriminating and should be further pursued for use as a universal nucleoside analogue.
- Van Aerschot,Hendrix,Schepers,Pillet,Herdewijn
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Read Online
- Self-assembly of 3,5-bis(ethoxycarbonyl)pyrazolate anions and ammonium cations of β-phenylethylamine or homoveratrylamine into hetero-double-stranded helical structures
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Hydrogen-bonded double-stranded hetero-helices are formed when reacting sodium 3,5-bis(ethoxycarbonyl)pyrazolate with β-phenethylammonium or homoveratrylammonium chloride, in which one of the strands is defined by the ammonium cations and the other one by
- Reviriego, Felipe,Sanz, Ana,Navarro, Pilar,Latorre, Julio,Garcia-Espana, Enrique,Liu-Gonzalez, Malva
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Read Online
- FUSED RING PYRIMIDONE DERIVATIVES FOR USE IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
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Provided are compounds according to any of Formula (I-1) to (I-7), pharmaceutical compositions comprising at least one of said compounds, their use as a medicament, and their use in treating chronic hepatitis B virus (HBV) infection. Methods for preparing compounds according to any of Formula (I-1) to (I-7) are also provided.
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Page/Page column 125; 141-142
(2022/04/03)
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- Metal-free C-C, C-O, C-S and C-N bond formation enabled by SBA-15 supported TFMSA
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The construction of intermolecular C-C, C-O, C-S and C-N bonds between diazo compounds and acyclic and cyclic 1,3-dicarbonyl compounds, thiophenol and alkynes was developed by using TFMSA@SBA-15, thus providing a metal-free and eco-friendly platform for f
- Yi, Xiangyan,Feng, Jiajun,Huang, Fei,Baell, Jonathan Bayldon
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supporting information
p. 1243 - 1246
(2020/02/04)
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- Synthetic method for one-step C-N construction C-S of C-C(I), (C) and (C)-(C) bonds (by machine translation)
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An acid load type catalyst is used under the heating C - C condition C - N, C - S and under the heating condition, the α - protonation of the heavy nitrogen ester is carried out, and the construction of the keys is realized in one step, and the method α -
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Paragraph 0042-0044
(2019/11/28)
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- Cyclopentene Annulations of Alkene Radical Cations with Vinyl Diazo Species Using Photocatalysis
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A direct (3+2) cycloaddition between alkenes and vinyl diazo reagents using either Cr or Ru photocatalysis is described. The intermediacy of a radical cation species enables a nucleophilic interception by vinyl diazo compounds, a departure from their trad
- Sarabia, Francisco J.,Li, Qiankun,Ferreira, Eric M.
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supporting information
p. 11015 - 11019
(2018/07/30)
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- [3 + 2] cycloaddition and subsequent oxidative dehydrogenation between alkenes and diazo compounds: A simple and direct approach to pyrazoles using TBAI/TBHP
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A novel Bu4NI-catalyzed pyrazole formation reaction is well described via sequential [3 + 2] cycloaddition and oxidative dehydrogenation reactions using TBHP as the primary oxidant. In comparison with previous cases toward pyrazoles from alkene
- Shao, Ying,Tong, Jingjing,Zhao, Yanwei,Zheng, Hao,Ma, Liang,Ma, Meihua,Wan, Xiaobing
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p. 8486 - 8492
(2016/09/28)
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- Efficient photochemical water oxidation by a dinuclear molecular ruthenium complex
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Herein is described the preparation of a dinuclear molecular Ru catalyst for H2O oxidation. The prepared catalyst mediates the photochemical oxidation of H2O with an efficiency comparable to state-of-the-art catalysts.
- Laine, Tanja M.,K?rk?s, Markus D.,Liao, Rong-Zhen,A?kermark, Torbj?rn,Lee, Bao-Lin,Karlsson, Erik A.,Siegbahn, Per E. M.,A?kermark, Bj?rn
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supporting information
p. 1862 - 1865
(2015/01/30)
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- Effect of configuration of 2-vinyldiazocarbonyl compounds on their reactivity: Experimental and computational study
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Non-fluorinated vinyldiazo compounds with trans-configuration irrespective of the nature of 3-R1-substituent (R1 = H, Me, TBSO) even under ambient conditions easily cyclize to produce pyrazoles, while cis-stereoisomers undergo similar ring closure only at elevated temperatures or decompose to produce vinyloxocarbene reaction products. The 3-CF 3-substituted analogues with cis- or trans-configuration do not produce pyrazoles at all, but on heating furnish only vinylcarbene derived products. DFT calculations of theoretical energy barriers adequately explain the different experimental reactivity found for stereoisomeric vinyldiazocarbonyl compounds, and a new model for their interconversion through the corresponding pyrazoles has been suggested. The Royal Society of Chemistry.
- Supurgibekov, Murat B.,Cantillo, David,Kappe, C. Oliver,Surya Prakash,Nikolaev, Valerij A.
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p. 682 - 689
(2014/01/06)
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- A facile synthesis of pyrazoles with multi-point structural diversity by 1,3-dipolar cycloaddition
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We describe the synthesis of diverse pyrazoles by 1,3-dipolar cycloaddition of ethyl diazoacetate with various acetylenes in refluxing toluene. The product pyrazoles are useful starting points for preparing a diverse collection of trisubstituted pyrazole
- Cheung, Kwai Ming J.,Reynisson, Jóhannes,McDonald, Edward
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supporting information; experimental part
p. 5915 - 5918
(2010/11/18)
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- Synthesis of pyrazoles through catalyst-free cycloaddition of diazo compounds to alkynes
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The synthesis of pyrazoles via 1,3-dipolar cycloaddition of diazo compounds to alkynes proceeds easily by heating. With α-diazocarbonyl substrates the reactions are conducted under solvent-free conditions affording the pyrazole products in high yields wit
- Vuluga, Daniela,Legros, Julien,Crousse, Benoit,Bonnet-Delpon, Daniele
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scheme or table
p. 156 - 159
(2010/04/22)
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- Lewis acid- and/or Lewis base-catalyzed [3+2] cycloaddition reaction: synthesis of pyrazoles and pyrazolines
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A facile, InCl3 and/or DABCO mediated 1, 3-dipolar cycloaddition of ethyl diazoacetate (EDA) with various activated olefins under solvent-free conditions at ambient temperature to afford 3, 5-disubstituted pyrazolines and pyrazoles in moderate
- Krishna, Palakodety Radha,Sekhar, Empati Raja,Mongin, Florence
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scheme or table
p. 6768 - 6772
(2009/04/11)
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- 1,3-dipolar cycloaddition of ethyl diazoacetate to alkynes in the pores of zeolite NaY
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Zeolite NaY promotes 1,3-dipolar cycloaddition of ethyl diazoacetate to alkynes having an electron-withdrawing group to afford the corresponding functionalized pyrazoles in high yields. The activation of the dipolarophile inside the pores of NaY is proposed based on the 13CMASNMR analysis. Copyright
- Kobayashi, Keijiro,Igura, Yuta,Imachi, Shouhei,Masui, Yoichi,Onaka, Makoto
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- Novel 1,3-dipolar cycloaddition of diazocarbonyl compounds to alkynes catalyzed by InCl3 in water
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The first intermolecular 1,3-dipolar cycloaddition of diazocarbonyl compounds with alkynes was developed by using an InCl3 catalyzed cycloaddition in water. The reaction was found to proceed by a domino 1,3-dipolar cycloaddition-hydrogen (alkyl or aryl) migration.
- Jiang, Nan,Li, Chao-Jun
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p. 394 - 395
(2007/10/03)
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- Chemoselective radical cleavage of Cbz-protected nitrogen compounds
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(Matrix presented) Tributylstannyl radicals promote the deprotection of N-Cbz derivatives of amides and nitrogen-containing heteroaromatic rings. These radical conditions do not affect N-Cbz derivatives of basic amines.
- Bennasar, M.-Lluisa,Roca, Tomas,Padulles, Ariadna
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p. 569 - 572
(2007/10/03)
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- Synthesis and Protonation Behavior of 26-Membered Oxaaza and Polyaza Macrocycles Containing Two Heteroaromatic Units of 3,5-Disubstituted Pyrazole or 1-Benzylpyrazole. A Potentiometric and 1H and 13C NMR Study
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The synthesis and acid-base behavior of two series of 26-membered dioxatetraamine and hexaamine heterocyclophanes containing two nuclei of either pyrazole (4a and 6a) or 1-benzylpyrazole (4b and 6b), respectively, are reported. Dipodal (2 + 2) condensations of 3,5-pyrazoledicarbaldehyde 2a or its 1-benzyl derivative 2b with 1,5-diamino-3-oxapentane afford in both cases the stable Schiff bases 3a,b in 90% yield, which after reduction with NaBH4 gave 4a,b in 75% and 84% yield, respectively. Condensation of 2a with diethylenetriamine leads to a complex mixture containing imidazolidine isomers, which was reduced in situ to afford 6a in 30% yield. Condensation of 2b with the same amine gave the stable diimidazolidine derivative 5b, which after crystallization was isolated as a pure compound in 80% yield and fully identified from analytical and 1H and 13C NMR data as a constitutional isomer with both imidazolidine rings located at the side of the pyrazole closer to the benzylic substituents. Reduction of 5b with NaBH4 afforded the polyamine 6b in 86% yield. Protonation constants of 4a,b and 6a,b have been determined by potentiometric methods in the pH 2-11 range, and their protonation sequences were established by a 1H and 13C NMR study in D2O at variable pH. For each compound, the number of protonation constants equals the number of nitrogens in the side chains. In the pH range studied, the pyrazole rings are not involved in protonation or deprotonation processes.
- Aran, Vicente J.,Kumar, Manoj,Molina, Jose,Lamarque, Laurent,Navarro, Pilar,Garcia-Espana, Enrique,Ramirez, Jose A.,Luis, Santiago V.,Escuder, Beatriz
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p. 6135 - 6146
(2007/10/03)
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- Substituted pyrazolyl compounds and methods employing such compounds
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This invention pertains to novel substituted pyrazolyl compounds useful as intravenous anesthetics represented by the Formula: STR1 including geometric and optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein: one of Y and Z is nitrogen, and the other is CH; R1 is hydrogen or lower-alkyl; R2 and R3 are selected from the group consisting of hydrogen, --CHO, lower-alkylcarbonyl, lower-alkoxy carbonyl, lower-alkylaminocarbonyl, lower-alkyl, lower-alkenyl, lower-alkoxy-lower-alkenyl, lower-alkylcarbonyloxymethyl, substituted and unsubstituted heterocyclic rings, and substituted or unsubstituted aryl groups, wherein the symbol * represents a carbon atom which may be asymmetric and at least one of R2 and R3 is other than hydrogen.
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