- C-N Bond forming reactions in the synthesis of substituted 2-aminoimidazole derivatives
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Carbon-nitrogen bond forming reactions oriented to the synthesis of 2-amino-imidazolidines and imidazoles have been investigated. The C-2 amination of imidazolidinones, via the corresponding 2-chlorodihydroimidazoles, led to 2-benzylaminodihydroimidazole or bis(dihydroimidazole)amino derivatives by choosing the adequate experimental conditions. On the other hand, the use of N-acyl-2-methylsulfanyldihydroimidazoles allowed carrying out the reactions with aromatic amines, such as p-anisidine. Finally, palladium catalyzed Buchwald- Hartwig amination was the method of choice for C-N coupling between 2-haloimidazoles and aromatic amines in the synthesis of the corresponding imidazoles.
- Gomez-SanJuan, Asier,Botija, Jose Manuel,Mendez, Almudena,Sotomayor, Nuria,Letea, Esther
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- 2-[(arylmethoxy)imino]imidazolidines with potential biological activities
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A series of 2-[(arylmethoxy)imino]imidazolidines was synthesized by reacting 2-chloro-4,5-dihydroimidazole with corresponding O- arylmethylhydroxylamines and evaluated for their α1-, α2-adrenergic and imidazoline I1, I2 receptor binding affinities. The most potent 2-[(naphthalen-1-ylmethoxy)imino] imidazolidine showed a high selectivity and good affinity for the [ 3H]prazosin-labeled α1-adrenoceptors (Ki = 107 nM). Representative compounds of this series were also tested in vivo for possible circulatory effects in rats after intravenous administration.
- Saczewski, Jaroslaw,Hudson, Alan L.,Rybczynska, Apolonia
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experimental part
p. 671 - 680
(2010/07/04)
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- Efficient synthesis of 2-(N-Substituted)-2-imidazolines and 2-(N-Substituted)-1,4,5, 6-tetrahydropyrimidines
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A general method for the preparation of 2-(N-Substituted)-2-imidazolines and 2-(N-Substituted)-1,4,5,6-tetrahydropyrimidines is described. These heterocycles can be synthesized from their respective anilines with 2-chloro-2-imidazoline or 2-chloro-1,4,5,6-tetrahydropyrimidine, generated in situ from imidazolidin-2-one and tetrahydropyrimidin-2(1H)-one activated by dimethyl chlorophosphate, in good to excellent yields. Copyright Taylor & Francis, Inc.
- Kan, Wai Ming,Lin, Shih-Hsun,Chern, Ching-Yuh
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p. 2633 - 2639
(2007/10/03)
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- COMPOUNDS AND METHODS FOR THE RAPID QUANTITATIVE ANALYSIS OF PROTEINS AND POLYPEPTIDES
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A polypeptide reactive reagent having the formula PRG-Z wherein "PRG" is a polypeptide reactive group which optionally binds to a capture reagent, and wherein "Z" is an aryl, substituted aryl, alkyl, substituted alkyl, lower alkyl or substituted lower alkyl group in which one or more atoms can be differentially labeled with one or more stable isotopes "X", wherein "X" is selected from the group consisting of H and D, is described.
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Page/Page column 29
(2008/06/13)
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- THIOPHENYLAMINOIMIDAZOLINES
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Methods for treatment of IP antagonist mediated diseases or conditions by administration to a subject in need thereof a compound of formula (I) wherein R1, R 2 , A and X are as defined herein. Also disclosed are compounds and related compositions.
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Page/Page column 29-30
(2010/02/10)
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- MODELES DE BIOTINE ACTIVEE PAR PHOSPHORYLATION TRANSFERT DE PHOSPHORYLE
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This work describes the synthesis of the first two O-phosphobiotin models, which mimic the activated form of biotin through a phosphorylation process.In addition, pyrophosphate bond formation is considered through this kind of O-phosphorylated intermediate.Reversible interconversion of the S- and N-phosphorylated urea structures is depicted and implications of the activation process are presented.
- Etemad-Moghadam, G.,Blonski, C.,Gasc, M. B.,Perie, J. J.,Klaebe, A.
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p. 367 - 376
(2007/10/02)
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