Search results for "DISCOVERY"
showing 10 items of 4119 documents
Synthesis of trifluoromethylated 2-benzoyl- and 2-aminoimidazoles from ring rearrangement of 1,2,4-oxadiazole derivatives
2008
Abstract Fluoroalkylated 2-ylamino-imidazoles have been synthesized by reaction of 3-amino-5-phenyl-1,2,4-oxadiazole with fluorinated β-dicarbonyl compounds and subsequent base-induced Boulton–Katritzky Rearrangement (BKR) of the isolated β-enaminocarbonyl intermediate. Alternatively, one-pot reactions performed in the presence of Montmorillonite K10 favoured the condensation at the 3-amino moiety of the oxadiazole and, in some cases, allowed the direct synthesis of 2-benzoylamino-imidazoles. Hydrolysis of 2-benzoylamino-imidazoles easily yielded fluorinated 2-amino-imidazoles targets.
Die Beeinflussung der Harnstoffsynthese in der Leber durch lokale Gewebssch�den beim Kaninchen
1961
Es wird uber in-vitro-Bestimmungen der Harnstoffsynthese der Lebern von Kaninchen mit einer Crotonolentzundung und einer bakteriellen Entzundung des Kniegelenks und einer mechanischen Kniegelenksentzundung berichtet. Es findet sich eine deutliche Zunahme der Harnstoffbildung gegenuber den bei den Kontrolltieren festgestellten Werten. Die Ergebnisse werden hinsichtlich inrer Bedeutung fur die Pathogenese extrarenaler Azotamien diskutiert.
Fluorescent chemosensors based on cyclohexane: selective sensing of succinate and malonate versus their longer or shorter homologues
2008
The sensing properties towards aliphatic α,ω-dicarboxylates of five cyclohexane-based ligands are described. The studied ligands have been designed following the binding site-signalling unit approach and they all possess thiourea groups as recognition moieties. Ligands 1 and 3 containing naphthalene units can be used as fluorescent sensors as they form intra- or intermolecular excimers in the presence of appropriate dicarboxylates. Selective sensing of succinate and malonate versus their longer or shorter homologues has been observed.
H2-Antihistaminica, 1. Mitt.: 2-Substituierte 4-[[2-(N′-Methyl-thioureido)-äthylmercapto]-methyl]-imidazole
1976
Es wird die Synthese der 2-substituierten 4-[[2-(N′-Methylthioureido)-athylmercapto]-methyl]-imidazole 5a–f als potentielle H2-Antihistaminica beschrieben. Ausgehend von den Imidazol-4-carbinolen 3a–f lassen sich die 2-substituierten 4-[(2-Amino-athylmercapto)-methyl]-imidazole 4a–f durch saurekatalysierte Reaktion mit Cysteamin darstellen und mit Methylisothiocyanat in die entsprechenden Thioharnstoffderivate 5 uberfuhren. 2-Substituted 4-[[2-(N′-Methyl-thioureido)-ethylmercapto]-methyl]-imidazoles The synthesis of 2-substituted 4-[[2-(Ns′-methyl-thioureido)-ethylmercapto]-methyl]-imidazoles 5a–f, as potential H2-antihistaminics, is described. The acid catalyzed reaction of the imidazole-4…
Herbizide, 8. Mitt. Herbicides, VIII. Kernchlorierte und -bromierte Anilinoethentricarbonitrile
1987
In einer Reihe von Herbiziden tritt als gemeinsames Strukturelement die Nitrilgruppe auf, wie in 2,6-Dichlorbenzonitril oder 4-Amino-2,3,5,6-tetrafluorbenzonitril. Als ein weiterer Vertreter dieser Strukturklasse ist in unseren jungsten Untersuchungen das 2-Cyanamino-4,6-diethylpyrimidin durch seine herbizide Wirksamkeit aufgefallen. In Fortfuhrung dieser Forschungsrichtung und in Anlehnung an Herbizide, in denen Kernhalogenierungen eine dominierende Rolle spielen, sind nunmehr entsprechende Partialstrukturen in unsere Untersuchungen einbezogen worden.
1,5,7-Triazabicyclo[4.4.0]dec-1- ene (TBD), 7-Methyl-TBD (MTBD) and the polymer-supported TBD (P-TBD):Three efficient catalysts for the nitroaldol (H…
2000
Abstract The 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) and its 7-methyl derivative (MTBD) have been proven to be of great synthetic utility as catalysts in the nitroaldol (Henry) reaction and for the addition of dialkyl phosphites to a variety of carbonyl compounds. The catalysts were in many cases superior to the parent tetramethylguanidine (TMG). In general the reaction proceeds in a few minutes at 0°C. The polymer-supported-TBD (P-TBD) was also proven to be an efficient promoter of the above cited nucleophilic additions.
The chemistry of [1,2,3]triazolo[1,5- c ]pyrimidine
2001
Abstract Reactions of [1,2,3]triazolo[1,5-c]pyrimidine 2 with some electrophiles and nucleophiles are reported. Triazole ring opening and loss of nitrogen is the principal reaction with electrophiles. With strong acids protonation on N6 competes successfully. Derivatives in which the pyrimidine ring has been opened are obtained in reactions with nucleophiles. No stable simple substitution compounds were found.
Oligopeptide der β-Carbolin-3-carbonsäure - Synthese und Affinität zu Benzodiazepinrezeptoren
1987
Es wurden Oligopeptide der β-Carbolin-3-carbonsaure dargestellt und deren Affinitat zum Benzodiazepinrezeptor in Mausehirn-Membranen bestimmt. Uber Struktur-Affinitatsbeziehungen wird berichtet. Oligopeptides of β-Carboline-3-carboxylic Acid - Synthesis and Benzodiazepine Receptor Affinity Oligopeptides of β-carboline-3-carboxylic acid were prepared and tested with respect to their affinity for the benzodiazepine receptor in mouse brain membranes. Structure-affinity relationships are reported.
Regio- and diastereoselective condensation of resorcarenes with primary amines and formaldehyde
1995
Abstract Mannich reactions of resorcarenes 1 with chiral amines yield single diastereomeric tetrakis-(benzodihydro-1,3-oxazine) derivatives 2 in high yields (80–90%). Epimerisation of these products occurs in the presence of acid.
Über Serotoninderivate mit cyclisierter Seitenkette, 1. Mitt. Darstellung der isomeren 3-(Piperidylmethyl)- und 3-(Piperidylmethyl)-5-hydroxyindole
1975
Es wird die Synthese der drei isomeren 3-(Pyridylmethyl)- und 3-(Piperidylmethyl)-5-hydroxyindole beschrieben. Die 3-(Pyridilmethyl)-5-benzyloxyindole wurden durch Kondensation von 5-Benzyloxyindolylmagnesiumbromid mit den drei isomeren Chlormethyl-pyridinbasen dargestellt. Katalytische Reduktion ihrer quartaren Salze fuhrte zu den entsprechenden Piperidinverbindungen. Die 5-Benzyloxyindole wurden durch hydrierende Debenzylierung in die 5-Hydroxyindolverbindungen ubergefuhrt. 3-(Pyridylmethyl)- and 3-(Piperidylmethyl)-5-hydroxyindoles The synthesis of the three isomeric 3-(pyridylmethyl)- and the 3-(piperidylmethyl)-5-hydroxyindoles is described. To obtain the 3-(pyridylmethyl)-3-benzyloxyi…