- Determination of inter-ionic and intra-ionic interactions in a monofluorinated imidazolium ionic liquid by a combination of X-ray crystallography and NOE NMR spectroscopy
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We report the very first application of a Transient 1D 1H{19F} NOE NMR experiment in neat ionic liquids. In comparison with classical 2D HOESY NMR spectroscopy, a substantial reduction in measurement time is gained with comparable quality and information content of the spectra. In combination with classical X-ray crystallography, we have applied this technique for the determination of inter-ionic distances (i.e. probabilities of presence) utilizing an ionic liquid containing a monofluorinated imidazolium cation. Copyright
- Lingscheid, Yves,Paul, Mathias,Br?hl, Andreas,Neud?rfl, J?rg-Martin,Giernoth, Ralf
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- Synthesis of 4,5-difluoroimidazole
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5-Fluoroimidazole-4-carboxylic acid ethyl ester was converted to the corresponding hydrazide. Oxidation of the hydrazide to the carbonyl azide and Curtius rearrangement in t-butyl alcohol produced 4-t-butyloxycarbonylamino-5-fluoroimidazole. Dissolution o
- Dolensky, Bohumil,Takeuchi, Yoshio,Cohen, Louis A.,Kirk, Kenneth L.
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- Novel imidazobenzazepine derivatives as dual H1/5-HT 2A antagonists for the treatment of sleep disorders
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A novel imidazobenzazepine template (5a) with potent dual H 1/5-HT2A antagonist activity was identified. Application of a zwitterionic approach to this poorly selective and poorly developable starting point successfully delivered a class of high quality leads, 3-[4-(3-R1-2-R-5H-imidazo[1,2-b][2]benzazepin-11-yl)-1-piperazinyl]- 2,2-dimethylpropanoic acids (e.g., 9, 19, 20, and 21), characterized by potent and balanced H1/5-HT2A receptor antagonist activities and good developability profiles.
- Gianotti, Massimo,Corti, Corrado,Fratte, Sonia Delle,Di Fabio, Romano,Leslie, Colin P.,Pavone, Francesca,Piccoli, Laura,Stasi, Luigi,Wigglesworth, Mark J.
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supporting information; experimental part
p. 5069 - 5073
(2010/10/20)
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- NOVEL COMPOUNDS
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Disclosed are N-{[(1R,4S,6R)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.
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Page/Page column 47; 48
(2010/06/19)
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- IMIDAZOBENZAZEPINE COMPOUNDS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM (CNS) DISEASES
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This invention relates to novel novel imidazobenzazepine derivatives of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.
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Page/Page column 44-45
(2010/12/29)
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- Regio- and stereoselective glycosylation: Synthesis of 5-haloimidazole α-ribonucleosides
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We describe the synthesis of novel 5-haloimidazole ribonucleosides as precursors of modified cobalamins. A regio- and stereoselective glycosylation of protected ribose with silylated 4(5)-haloimidazoles produces 5-haloimidazole ribonucleosides predominant
- Chandra, Tilak,Zou, Xiang,Valente, Edward J.,Brown, Kenneth L.
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p. 5000 - 5003
(2007/10/03)
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