1186403-41-7Relevant academic research and scientific papers
Regioselective deoxygenative chalcogenation of 7-Azindole: N-oxides promoted by I2/PEG-200
Liu, Shanshan,Yang, Heng,Jiao, Lin-Yu,Zhang, Jian-Hua,Zhao, Chen,Ma, Yangmin,Yang, Xiufang
, p. 10073 - 10087 (2019)
We developed a general and sustainable approach for the regioselective deoxygenative chalcogenation of 7-Azindole N-oxides; the combination of an internal oxidant and a green solvent has been used successfully for the synthesis of mono-and dichalcogenyl 7-Azaindoles which are of pharmaceutical interest. The regioselectivity is tunable by the variation of the reaction conditions. I2/PEG was established as an efficient and reusable catalytic system for C-H chalcogenation. This developed methodology has great potential for practical utility, with a broad substrate scope, green reaction conditions, and operational simplicity.
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT6 agonists
Bernotas, Ronald C.,Lenicek, Steven,Antane, Schuyler,Cole, Derek C.,Harrison, Boyd L.,Robichaud, Albert J.,Zhang, Guo Ming,Smith, Deborah,Platt, Brian,Lin, Qian,Li, Ping,Coupet, Joseph,Rosenzweig-Lipson, Sharon,Beyer, Chad E.,Schechter, Lee E.
experimental part, p. 5153 - 5163 (2009/12/09)
A series of 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines 10a-z was prepared as novel 5-HT6 ligands. The best compounds were high affinity, full agonists at 5-HT6 receptors. Several agonists demonstrated good selectivity over other serotonergic and dopaminergic receptors. Acute administration of selective agonist 10e significantly increased extracellular GABA concentrations in rat frontal cortex. This compound also reduced adjunctive drinking behavior in the rat schedule-induced polydipsia assay, possibly predictive of efficacy in obsessive compulsive disorder and other anxiety related disorders.
