155570-08-4Relevant academic research and scientific papers
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with α2- adrenoceptor blocking activity
Andrés, J. Ignacio,Alcázar, Jesús,Alonso, José M.,Alvarez, Rosa M.,Bakker, Margot H.,Biesmans, Ilse,Cid, José M.,De Lucas, Ana I.,Fernández, Javier,Font, Luis M.,Hens, Koen A.,Iturrino, Laura,Lenaerts, Ilse,Martínez, Sonia,Megens, Anton A.,Pastor, Joaquín,Vermote, Patrick C. M.,Steckler, Thomas
, p. 2054 - 2071 (2005)
The synthesis and pharmacology of a new series of 3-piperazinylmethyl-3a,4- dihydro-3H-[1]-benzopyrano[4,3-c]isoxazoles that combine central serotonin (5-HT) reuptake inhibition with α2-adrenoceptor blocking activity is described as potential antidepressants. Four compounds were selected for further evaluation, and the combination of both activities was found to be stereoselective, residing mainly in one enantiomer. Reversal of the loss of righting induced by the α2-agonist medetomidine in rats confirmed the α2-adrenoceptor blocking activity in vivo and also demonstrated CNS penetration. Antagonism of p-chloroamphetamine (pCA)-induced excitation as well as blockade of the neuronal 5-HT depletion induced by p-CA administration in rats confirmed their ability to block the central 5-HTT, even after oral administration. Replacement of the oxygen atom at the 5-position of the tricyclic scaffold by a nitrogen or a carbon atom, as well as O-substitution at position 7, led also to active compounds, both in vitro and in vivo.
Rhenium-catalyzed formation of indene frameworks via C-H bond activation: [3+2] Annulation of aromatic aldimines and acetylenes
Kuninobu, Yoichiro,Kawata, Atsushi,Takai, Kazuhiko
, p. 13498 - 13499 (2007/10/03)
A rhenium complex, [ReBr(CO)3(thf)]2, catalyzes the reaction of an aromatic aldimine with an acetylene to give an indene derivative in a quantitative yield. The reaction proceeds via C-H bond activation, insertion of the acetylene, intramolecular nucleophilic cyclization, and reductive elimination. In contrast to ruthenium and rhodium catalysts, which are usually employed in this type of reaction, the rhenium catalyst promotes the intramolecular nucleophilic cyclization of the alkenylmetal species generated by insertion of the acetylene. Copyright
Processes and intermediates for the preparation of 2-substituted benzaldehydes
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, (2008/06/13)
Processes for preparing 2-substituted benzaldehydes of general formula (I), wherein: R1 is CH2 CH2 --(L1)p --(CH2)q --(L2)r --CH2 --(T)2/su
