5439-83-8Relevant academic research and scientific papers
Dearomative Cycloadditions Utilizing an Organic Photosensitizer: An Alternative to Iridium Catalysis
Rolka, Alessa B.,Koenig, Burkhard
supporting information, p. 5035 - 5040 (2020/07/15)
A highly efficient, cheap, and organic alternative to the commonly used iridium photosensitizer (Ir[dF(CF3)ppy]2(dtbpy))PF6 ([Ir-F]) is presented for visible-light energy transfer catalysis. The organic dye 2CzPN surpasses [Ir-F] in selectivity while at t
Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: Insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity
Ananthan, Subramaniam,Saini, Surendra K.,Zhou, Guangyan,Hobrath, Judith V.,Padmalayam, Indira,Zhai, Ling,Bostwick, J. Robert,Antonio, Tamara,Reith, Maarten E. A.,McDowell, Shea,Cho, Eunie,McAleer, Leah,Taylor, Michelle,Luedtke, Robert R.
, p. 7042 - 7060 (2014/11/07)
Antagonist and partial agonist modulators of the dopamine D3 receptor (D3R) have emerged as promising therapeutics for the treatment of substance abuse and neuropsychiatric disorders. However, development of druglike lead compounds with selectivity for the D3 receptor has been challenging because of the high sequence homology between the D3R and the dopamine D2 receptor (D2R). In this effort, we synthesized a series of acylaminobutylpiperazines incorporating aza-aromatic units and evaluated their binding and functional activities at the D3 and D2 receptors. Docking studies and results from evaluations against a set of chimeric and mutant receptors suggest that interactions at the extracellular end of TM7 contribute to the D3R versus D2R selectivity of these ligands. Molecular insights from this study could potentially enable rational design of potent and selective D3R ligands.
A versatile synthesis of 3-substituted 4-cyano-1,2,3,4-tetrahydro-1-oxo- β-carbolines
Huber, Kilian,Kast, Oliver,Bracher, Franz
scheme or table, p. 3849 - 3854 (2010/12/25)
In a project aimed at the synthesis of analogues of the cytotoxic -carboline alkaloid bauerine C with more advantageous solubility properties, a 3-amino analogue was prepared by treating ethyl 3-(cyanomethyl)indole-2- carboxylate with ammonia. Upon addition of aldehydes or ketones to the reaction mixture, 3-substituted 4-cyano-1,2,3,4-tetrahydro-1-oxo - carbolines were obtained in a one-pot condensation. When cyclic ketones are used, the procedure allows a convenient synthesis of tetracyclic spiro compounds. Georg Thieme Verlag Stuttgart · New York.
Facile Syntheses of Ethyl 2-Alkylindole-3-carboxylates: Reinvestigation of an Earlier Synthesis of Ethyl 3-Methylindole-2-carboxylates
Wadia, M. S.,Mali, R. S.,Tilve, S. G.,Yadav, V. J.
, p. 401 - 404 (2007/10/02)
A convenient, general synthesis of ethyl 2-alkylindole-3-carboxylates has been described from the easily accesible o-nitroarylaldehydes.In an alternate approach the same o-nitroarylaldehydes have been converted to ethyl 3-alkylindole-2-carboxylates.
