1186403-43-9Relevant academic research and scientific papers
Regioselective C-H sulfenylation ofN-sulfonyl protected 7-azaindoles promoted by TBAI: a rapid synthesis of 3-thio-7-azaindoles
Hao, Shuai,Hu, Jingyan,Ji, Xiaoming,Lai, Miao,Ren, Tianbao,Wang, Erbin,Wang, Juanjuan,Wu, Zhiyong,Xi, Gaolei,Zhao, Mingqin
, p. 31819 - 31823 (2020)
This paper describes the regioselective C-3 sulfenylation ofN-sulfonyl protected 7-azaindoles with sulfonyl chlorides. In this transformation, dual roles of TBAI serving as both promoter and desulfonylation reagent have been demonstrated. The reaction proceeded smoothly under simple conditions to afford 3-thio-7-azaindoles in moderate to good yields with broad substrate scopes. This protocol refrains from using transition-metal catalysts, strong oxidants or bases, and shows its practical synthetic value in organic synthesis.
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.
