408521-57-3Relevant academic research and scientific papers
Bf3-oet2 catalyzed c3-alkylation of indole: Synthesis of indolylsuccinimidesand their cytotoxicity studies
Shaikh, Iqbal N.,Rahim, Abdul,Faazil, Shaikh,Adil, Syed Farooq,Assal, Mohamed E.,Hatshan, Mohammad Rafe
, (2021/05/26)
A simple and efficient BF3-OEt2 promoted C3-alkylation of indole has been developed to obtain3-indolylsuccinimidesfrom commercially available indoles and maleimides, with excellent yields under mild reaction conditions. Furthermore,
Highly efficient aluminum trichloride catalyzed michael addition of indoles and pyrroles to maleimides
An, Yu-Long,Shao, Zhi-Yu,Cheng, Jian,Zhao, Sheng-Yin
, p. 2719 - 2726 (2013/10/21)
A highly efficient synthetic strategy for Michael addition of indoles and pyrroles to maleimides has been developed using the Lewis acids zinc chloride or aluminum trichloride as the catalyst. The reactions generated 3-substituted indoles and 2-substitute
Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors
Bannwart, Linda M.,Carter, David S.,Cai, Hai-Ying,Choy, Jason C.,Greenhouse, Robert,Jaime-Figueroa, Saul,Iyer, Pravin S.,Lin, Clara J.,Lee, Eun Kyung,Lucas, Matthew C.,Lynch, Stephen M.,Madera, Ann Marie,Moore, Amy,Ozboya, Kerem,Raptova, Lubica,Roetz, Ralf,Schoenfeld, Ryan C.,Stein, Karin Ann,Steiner, Sandra,Villa, Marzia,Weikert, Robert J.,Zhai, Yansheng
scheme or table, p. 6062 - 6066 (2009/06/30)
A series of 3,3-disubstituted pyrrolidine monoamine triple reuptake inhibitors were discovered. Analogues with low nanomolar potency, good human in vitro microsomal stability and in vitro permeability, and low drug-drug interaction potential are described. One example showed in vivo anti-depressant-like effects in the mouse tail suspension assay with a minimum effective dose of 30 mg/kg ip.
Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists
Cole, Derek C.,Lennox, William J.,Stock, Joseph R.,Ellingboe, John W.,Mazandarani, Hossein,Smith, Deborah L.,Zhang, Guoming,Tawa, Gregory J.,Schechter, Lee E.
, p. 4780 - 4785 (2007/10/03)
Several series of conformationally constrained N1- arylsulfonyltryptamine derivatives were prepared and tested for 5-HT6 receptor binding affinity and ability to modulate cAMP production in a cyclase assay. The 3-piperidin-3-yl-, 3-(1-methylpyrrolidin-2-ylmethyl)-, and 3-pyrrolidin-3-yl-1H-indole arrays (8-13) appear to be able to adopt a conformation that allows high affinity 5-HT6 receptor binding, while the β-carboline array 14 binds with a significantly weaker (10- to 100-fold) affinity. N1-Benzenesulfonyl-3-piperidin-3-yl-1H-indole 9a is a high affinity full agonist with EC50 = 24 nM. Several of the N1-arylsulfonyl-3-(1-methylpyrrolidin-2-ylmethyl)-1H-indole derivatives behave as very potent antagonists ((S)-11r, (S)-11t; IC50 = 0.8, 1.0 nM).
