- HAPTENS, HAPTEN CONJUGATES, COMPOSITIONS THEREOF AND METHOD FOR THEIR PREPARATION AND USE
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A method for performing a multiplexed diagnostic assay, such as for two or more different targets in a sample, is described. One embodiment comprised contacting the sample with two or more specific binding moieties that bind specifically to two or more di
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Paragraph 0247; 0248
(2016/07/27)
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- TLR-AGONIST-CONJUGATED ANTIBODY RECRUITING MOLECULES (TLR_ARMS)
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The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) and Toll-like receptor agonist (TLR) through a linker and a multifunctional connector group or molecule.
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- An all-organic steroid-D-π-A modular design drives ferroelectricity in supramolecular solids and nano-architectures at RT
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Confluence of a modular design approach and self-assembly with a 'steroid-D-π-A' module generates spontaneous polarization in solids and for the first time in nano-architectures constituted from organogels, at room temperature (RT).
- Asthana, Deepak,Kumar, Anil,Pathak, Abhishek,Sukul, Pradip Kumar,Malik, Sudip,Chatterjee, Ratnamala,Patnaik, Satyabrata,Rissanen, Kari,Mukhopadhyay, Pritam
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supporting information; experimental part
p. 8928 - 8930
(2011/10/01)
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- The "dimer nucleophile mechanism" for reactions with rate-determining first step: Derivation of the whole kinetic law and further treatment of kinetic results
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Overwhelming evidence has been previously reported for the existence of the so-called "dimer nucleophile mechanism" in aromatic nucleophilic substitutions by amines in aprotic solvents, for which the most prominent feature is the fourth-order kinetics (third order in amine) that has been observed with many different substrate-nucleophile systems, especially those in which departure of the nucleofuge is the rate-determining step. The mechanism has been confirmed by several other features, although other alternative mechanisms were suggested to explain the fourth-order kinetics, no one has been able to explain the other above-mentioned features. The present paper affords additional experimental evidence and derivation of the kinetic expressions for reactions with good nucleofugues, where the first step is rate determining. The work involves studies of the reactions of 2,4-dinitrofluorobenzene and 2,4-dinitrochlorobenzene with aniline and with alkyldiamines in toluene. The novelty of this work lies in the selection of substrate-nucleophile systems exhibiting kinetic behavior that allows estimations of the different k's involved. The satisfactory agreement between the quotients of k's calculated from sets of data obtained under different reaction conditions hereby reported indicates that the assumptions made are correct and that the whole treatment applied to the kinetic data is justified. All together, the results fit well with the reaction scheme involving the dimer nucleophile mechanism, adding new evidence to this mechanism that it is well established in the current literature.
- Alvaro, Cecilia E. Silvana,Nudelman, Norma Sbarbati
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scheme or table
p. 735 - 742
(2011/07/29)
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- Nucleotides. Part LXXVIII: Double labeling of nucleosides and nucleotides
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Several N(-hydroxyalkyl)-2,4-dinitroanilines were transformed into their phosphoramidites (see 5 and 6 in Scheme 1) in view of their use as fluorescence quenchers, and modified 2-aminobenzamides (see 9, 10, 18, and 19 in Scheme 1) were applied in model re
- Maier, Thomas,Pfleiderer, Wolfgang
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experimental part
p. 2365 - 2392
(2011/02/18)
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- Facile solid-phase synthesis of AICAR 5-monophosphate (ZMP) and its 4-N-Alkyl derivatives
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We report herein a facile, solid-phase synthesis of 5-aminol-β-D- ribofuranosylimidazole-4-carboxamide-5'-monophosphate (ZMP), a biosynthetic precursor of purine nucleotides, as well as a small collection of its 4-N-alkyl derivatives. The very difficult, direct, chemical phosphorylation of 5-amino-lβ-D-ribofuranosylimidazole-4-carboxamide (AICAR) was circumvented by installing a suitable, fully protected, phos phate group on the 5'-position of A-l-(2,4-dinitrophenyl)inosine, connected to the solid support through the 2',3'-positions, prior to the purine degradation, which led to the 5amino-imidazole-4-ca:rboxamide moiety. A plausible reaction mechanism for the formation of the ZMP imidazole was also reported.
- Oliviero, Giorgia,D'Errico, Stefano,Borbone, Nicola,Amato, Jussara,Piccialli, Vincenzo,Piccialli, Gennaro,Luciano, Mayoi
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experimental part
p. 1517 - 1524
(2010/06/16)
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- A highly selective and colorimetric naked-eye chemosensor for Cu2+
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A sample and practical colorimetric naked-eye chemosensor 3-nitro-4-ethylenediamido-nitrobenzene (2) for metal cations was designed and synthesized. It displays high selectivity and sensitivity for Cu2+ by the UV absorption which appeared a new peak at 525 nm and color change from yellow to red by naked-eye in CH3OH/H2O pH 7.6.
- Wang, Zhijun,Fan, Xiaojun,Li, Donghong,Feng, Liheng
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experimental part
p. 1224 - 1227
(2009/02/07)
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- A new leaving group in nucleophilic aromatic substitution reactions (S NAr)
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Nucleophilic aromatic substitution of a 2,4-dinitrophenyl substituted pyrazole 1 with primary amines leads to substitution of the pyrazolo substituent. In these nucleophilic aromatic substitution reactions (S NAr), 5-amino-1H-4- pyrazolecarbonitrile (3) acts as a new leaving group.
- Bakavoli, Mehdi,Pordel, Mehdi,Rahimizadeh, Mohammad,Jahandari, Pooneh
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experimental part
p. 432 - 433
(2009/06/30)
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- Effect of substituent on regioselectivity and reaction mechanism in aminolysis of 2,4-dinitrophenyl X-substituted benzenesulfonates
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(Chemical Equation Presented) We report on a kinetic study for the nucleophilic substitution reactions of 2,4-dinitrophenyl X-substituted benzensulfonates (X = 4-MeO, 1a, and X = 4-NO2, 1c) with a series of primary amines in 80 mol % H2O/20 mol % DMSO at 25.0 °C. The reactions proceed through S-O and C-O bond fission pathways competitively. The fraction of the S-O bond fission increases as the attaching amine becomes more basic and the substituent X changes from 4-MeO to 4-NO2, indicating that the regioselectivity is governed by the electronic nature of the substituent X as well as the basicity of amines. The S-O bond fission has been suggested to proceed through an addition intermediate with a change in the rate-determining step (RDS) at pK°a = 8.9 ± 0.1. The electronic nature of the substituent X influences kNS-O and k1 values, but not the k2/k-1 ratios and the pK°a value significantly. Stabilization of the ground state (GS) through resonance interaction between the electron-donating substituent and the electrophilic center has been suggested to be responsible for the decreased reactivity of 1a compared to 1c. The second-order rate constants for the C-O bond fission exhibit no correlation with the electronic nature of the substituent X. The distance effect and the nature of the reaction mechanism have been suggested to be responsible for the absence of the correlation.
- Um, Ik-Hwan,Hong, Jin-Young,Seok, Jin-Ah
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p. 1438 - 1444
(2007/10/03)
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- Role of hydrogen-bonded nucleophiles in aromatic nucleophilic substitutions in aprotic solvents. Reactions of halonitrobenzenes with ethylenediamine, 3-dimethylamino-1-propylamine and histamine in toluene
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The kinetics of the reactions between 1-halogeno-2,4-dinitrobenzene (halogen = F, C1) and the amines ethylenediamine (EDA) and 3-dimethylamino-1- propylamine (DMPA) were studied in toluene at 25° ±0.2C under pseudo-first-order conditions using varying amounts of amine. Even with C1 as the nucleofugue (where usually the first step is rate-determining), a third-order-in-amine kinetic law was observed: these results can be interpreted within the 'dimer nucleophile' mechanism where the amine homo-aggregates are better nucleophiles than the amine monomers. To confirm this interpretation, the reaction of 2,4-dinitrofluorobenzene with histamine was studied in the same solvent. Because of the rigid geometry, an intramolecular hydrogen bond is easily established, which prevents the formation of self-aggregates. Consequently, the plot of kA vs. [histamine] is a straight line, as expected for a classical mechanism of base-catalysed decomposition of the zwitterionic intermediate. All these results are well explained in the frame of the 'dimer nucleophile' mechanism. Copyright
- Alvaro, Cecilia E. Silvana,Nudelman, Norma Sbarbati
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p. 880 - 885
(2007/10/03)
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- ETUDE DE LA REACTIVE DE LA 7-PHENYL-1,4-DIAZEPINE-5-ONE
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The reactivity of 7-phenyl-1,4-diazepin-5-one has been described.The new compounds obtained have been characterized by 1H NMR, IR, MS and microanalysis.
- Chammache, M.,Essassi, E. M.,Salem, M.,Zniber, R.
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- Chromatographic approach to the measurement of the interstrand distance for some chiral bonded phases
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A series of homologous N,N′-bis(2,4-dinitrophenyl)-α,ω-diaminoalkanes (bis-DNP's) was chromatographed at various temperatures on π-basic chiral stationary phases derived from N-(2-naphthyl)alanine in order to determine the enthalpy and entropy of adsorption. The number of methylene groups in the bis-DNP's influences the ability of the terminal π-acidic groups to interact simultaneously with neighboring strands of stationary phase, a process termed "bridging". When the number of methylene groups is optimal for bridging, the enthalpy of adsorption is most exothermic. The length of the bis-derivative required for optimal bridging is related to the interstrand distance. Optimal bridging occurs for the bis-DNP's having five methylene groups regardless of the extent of surface coverage of the silica for the surface coverage range investigated. This suggests that the strands are not randomly spaced on the silica, with interstrand distance being influenced only by surface coverage, but are instead clustered, the clusters having similar distributions of interstrand distances. Adsorption is more exothermic for phases of high surface coverages than for low. If Interstrand spacing is independent of surface coverage but surface coverage affects the enthalpy of adsorption, then surface coverage must influence the cluster size, which then influences the average extent of solvation of a strand of bonded phase.
- Pirkle, William H.,Readnour, Robin S.
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- Intramolecular Catalysis in the Reaction of 1-Fluoro-2,4-dinitrobenzene with Diamines in Benzene
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A kinetic investigation of the reaction of 1-fluoro-2,4-dinitrobenzene (FDNB) with saturated diamines in benzene shows that, when the two amino groups are suitable placed with respect to each other, catalysis by a second diamine molecule is kinetically insignificant throughout the diamine concentration range examined.A comparison with the reactivity of the same diamines towards 1-chloro-2,4-dinitrobenzene (CNDB) suggests that the rate-determining step is nucleophilic attack also for the FDNB system.This behaviour is attributed to efficient intramolecular assistance of the second amino group of a diamine molecule to decomposition of the tetrahedral reaction intermediate.
- Guanti, Giuseppe,Petrillo, Giovanni,Thea, Sergio,Pero, Francesca
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p. 2764 - 2771
(2007/10/02)
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