Search results for "Cyclic compound"
showing 10 items of 819 documents
ChemInform Abstract: Selective Formal Transesterification of Fluorinated 2-(Trimethylsilyl)ethyl α-Imino Esters Mediated by TBAF.
2008
The scope of the transesterification reaction between β-fluorinated α-imino esters and various electrophiles in the presence of TBAF as fluorine source is described. The reaction is highly selective for alkyl iodides, bromides, and mesylates, while alkyl chlorides react at a significantly slower rate and tosylates do not react under the reaction conditions. This methodology represents a simple and useful alternative for the preparation of a wide variety of fluorinated α-imino esters.
Synthesis of [18F]-Fluoroethylfenoterol for imaging β2 receptor status in lung in vivo
2001
5-(-{2-[4-(2-[18F]Fluoroethoxy)-phenyl]-l-methyl-ethylamino}-l-hydroxy-ethyl)-benzene-1, 3-diol ([18F]fluoroethylfenoterol) was synthesised from 4-(2-{benzyl-[2-(3,5-bis-benzyloxy-phenyl)-2-hydroxy-ethyl]-amino}-propyl)-phenol using 2-[18F]fluoroethyltosylate (92% RCY) followed by reductive cleavage of the benzyl protecting groups. Preliminary in vitro tests showed [19F]fluoroethylfenoterol to be as potent in relaxation of lung tissue as fenoterol itself.
Inhibition of GABA and benzodiazepine receptor binding by penicillins.
1980
Penicillins are thought to be GABA receptor antagonists. In order to determine the affinities of various penicillin derivatives for the GABA receptor, their potencies as inhibitors of specific [3H]GABA binding to rat brain membranes were investigated. All investigated penicillins inhibit specific [3H]GABA binding, with IC50 values ranging from 2 to 60 mM. The results are consistent with the assumption that penicillins are weak GABA receptor antagonists.
Palladium-Catalyzed Alkoxy- and Aminocarbonylation of α-Halomethyl Oxime Ethers: Synthesis of 1,3-Alkoxyimino Esters and 1,3-Alkoxyimino Amides
2014
The three component reactions of α-bromomethyl oxime ethers, carbon monoxide, and alcohols or aromatic amines give imino esters and amides, respectively.
Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs
2008
Graphical abstract Several bisnoradamantylamines and noradamantylamines have been synthesized and their antiviral, trypanocidal, NMDA receptor antagonist, and dopamine reuptake inhibitory activities have been studied.
CuCl catalyzed radical cyclisation of N-alpha-perchloroacyl-ketene-N,S-acetals: a new way to prepare disubstituted maleic anhydrides
2012
The discovery that cycloalkanes can form thermomorphic systems with typical polar organic solvents has led to the development of less-polar electrolyte solutions. Their mixing and separation can be regulated reversibly at a moderate temperature range. The phase switching temperature can be controlled by changing the solvent compositions. While biphasic conditions are maintained below the phase switching temperature, conductive monophasic conditions as less-polar electrolyte solutions are obtained above the phase switching temperature. After the electrochemical transformations, biphasic conditions are reconstructed below the phase switching temperature, facilitating the separation of cycloal…
Degradation of heterocyclic aromatic amines in oil under storage and frying conditions and reduction of their mutagenic potential.
2007
Heterocyclic aromatic amines (HAA) were systematically studied concerning their partition behavior in water/oil-systems and their thermostability in different animal derived fats and vegetable oils. Partitioning of IQx-compounds and PhIP in water/oil systems was found to depend on the polarity defined by the molecular structure and on the pH-value of the aqueous phase. In particular, beta-carbolines norharman and harman showed a significant strong lipophilic character at alkaline pH. After heating in frying fats at 130 degrees C, contents of IQx compounds and PhIP were reduced by more than 40% and after heating at 180 degrees C less than 10% of the HAA initial concentration was recovered. B…
Novel bioactive bromopyrrole alkaloids from the Mediterranean sponge Axinella verrucosa
2005
The Mediterranean sponge Axinella verrucosa has been investigated for its alkaloid composition and has been found to produce a complex mixture of bromopyrrole alkaloids. Along with the previously isolated compounds 5-18, four novel alkaloids of this class, compounds 1-4, have been isolated, and their structures established through spectroscopic methods. Compounds 1-4 were found to display neuroprotective activity against the agonists serotonin and glutamate in vitro.
The critical concentration of C1-esterase inhibitor (C1-INH) in human serum preventing auto-activation of the first component of complement (C1)
2005
C1-esterase inhibitor (C1-INH) was depleted from normal human serum (NHS) at 4 degrees C by affinity chromatography with a monoclonal anti-C1-INH antibody (mAb 13 E1) coupled to CNBr-activated Sepharose 4B. The C1-INH-depleted serum (C1-INH-depl-HS) had normal levels of C1, C4, and CH 50 and C1-INH concentration was less than 10% of normal (15 microg/ml in C1-INH-depl-HS compared to 230 microg/ml in NHS). C1-auto-activation in C1-INH-depl-HS was followed by measuring C4-consumption in a haemolytic assay and by detection of activated C1s in a C1s-ELISA. After a lag phase of 10-20 min, C1-auto-activation in C1-INH depl-HS occurred and reached its maximum after 40 min at 37 degrees C. In contr…
Fluoreszierende silane als OH-selektive schutzgruppen
1985
Abstract Fluorescent tertiary silanes are synthesized which, under cesium fluoride/ imidazole activation, discriminate between primary and secondary OH groups. Serine n-butylamide reacts with [5-dimethylamino(1-naphthyl)]dimethylsilane ( 1 ) and diisopropyl[5-dimethylamino(1-naphthyl)]silane ( 2 ) to form the silyl ethers (−)- l -3-[5-dimethylamino(1-naphthyl)]-dimethylsilyloxy]serine n-butylamid ( 14 ) and (−)- l -3-[diisopropyl[5-dimethylamino(1-naphthyl)]silyloxy]serine n-butylamid ( 15 ) exclusively. The silyl ethers are cleaved on treatment with H 2 F 2 , forming the corresponding fluorescent silyl fluorides. Absorption and fluorescence data as well as stability data for the hydrolysis…