17223-85-7Relevant articles and documents
Carbazolyl nitrenium cations: Generation and reactions
Bogdal, Dariusz
, p. 2679 - 2688 (2000)
Carbazolyl nitrenium cations were generated during the thermolysis and photolysis of 1-carbazol-9-yl-2,4,6-triphenylpyridinium (Py+-Cz) tetrafluoroborate in 2,2,2-trifluoroethanol- and TFA - mesitylene mixtures. The thermolysis of Py+-Cz in TFA-mesitylene mixture gave 9-mesitylcarbazole in good yield along with carbazole, non-symmetrical mesitylene dimer, 2,4,6-triphenylpyridine, and a small amount of 9-(3,5-dimethylbenzyl)carbazole, whereas the thermolysis in trifluoroethanol - mesitylene mixture gave 9-mesitylcarbazole as the main product along with carbazole and 2,4,6-triphenylpyridine. The product distributions lead to two major conclusions. First, photolysis and thermolysis of Py+-Cz salt produce nitrenium ions that can be in singlet or triplet state dependant on the reaction conditions. Second, the carbazolyl nitrenium ion exhibits singlet state in the ground state.
SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME
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Page/Page column 102-103, (2017/09/08)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof: Formula (I) wherein Q is selected from O, S and Se; J is S or Se; W1 and W2, when present, are independe
Synthesis and structure-activity relationships of N-propyl-N-(4- pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease
Klein,Davis,Olsen,Wong,Huger,Smith,Petko,Cornfeldt,Wilker,Blitzer,Landau,Haroutunian,Martin,Effland
, p. 570 - 581 (2007/10/03)
A series of novel N-(4-pyridinyl)-1H-indol-1-amines and other heteroaryl analogs was synthesized and evaluated in tests to determine potential utility for the treatment of Alzheimer's disease. From these compounds, N-propyl-N- (4-pyridinyl)-1H-indol-1-amine (besipirdine, 4c) was selected for clinical development based on in-depth biological evaluation. In addition to cholinomimetic properties based initially on in vitro inhibition of [3H]quinuclidinyl benzilate binding, in vivo reversal of scopolamine- induced behavioral deficits, and subsequently on other results, 4c also displayed enhancement of adrenergic mechanisms as evidenced in vitro by inhibition of [3H]clonidine binding and synaptosomal biogenic amine uptake, and in vivo by reversal of tetrabenazine-induced ptosis. The synthesis, structure-activity relationships for this series, and the biological profile of 4c are reported.
