4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors
Novel 4-phenyl tetrahydroisoquinolines that inhibit both dopamine and norepinephrine transporters were designed and prepared. In this Letter, we describe the synthesis, in vitro activity and associated structure-activity relationships of this series. We also report the ex vivo NET occupancy of a representative compound, 41.
Pechulis, Anthony D.,Beck, James P.,Curry, Matt A.,Wolf, Mark A.,Harms, Arthur E.,Xi, Ning,Opalka, Chet,Sweet, Mark P.,Yang, Zhicai,Vellekoop, A. Samuel,Klos, Andrew M.,Crocker, Peter J.,Hassler, Carla,Laws, Mia,Kitchen, Douglas B.,Smith, Mark A.,Olson, Richard E.,Liu, Shuang,Molino, Bruce F.
p. 7219 - 7222
(2013/01/15)
Nucleophilic addition of β-amino carbanions to arynes: One-pot synthesis of 4-aryl-N-methyl-1,2,3,4-tetrahydroisoquinolines
A novel approach for the direct C-4 arylation of N-methyl-1,2,3,4- tetrahydroisoquinolines by nucleophilic addition of β-aminocarbanions to benzynes is described which provides a one-pot procedure for synthesis of the title compounds.
Singh, Kamal Nain,Singh, Paramjit,Singh, Pushpinder,Deol, Yadwinder Singh
supporting information; experimental part
p. 2202 - 2205
(2012/06/18)
A New Synthesis of 1,2,3,4-Tetrahydro-2-methyl-4-phenylisoquinolines
1,2,3,4-Tetrahydro-2-methyl-4-phenylisoquinolines 6 are obtained from aromatic aldehydes 1, methyl amine and α-haloacetophenones 2 in the presence of sodium borohydride followed by cyclization with sulfuric acid and zinc in methanol.
Venkov, Atanas P.,Vodenicharov, Daniel M.
p. 253 - 255
(2007/10/02)
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