112717-66-5Relevant academic research and scientific papers
Electrophotocatalytic diamination of vicinal C-H bonds
Shen, Tao,Lambert, Tristan H.
, p. 620 - 626 (2021/02/12)
The conversion of unactivated carbon-hydrogen (C-H) bonds to carbon-nitrogen (C-N) bonds is a highly valued transformation. Existing strategies typically accomplish such reactions at only a single C-H site because the first derivatization diminishes the reactivity of surrounding C-H bonds. Here, we show that alkylated arenes can undergo vicinal C-H diamination reactions to form 1, 2-diamine derivatives through an electrophotocatalytic strategy, using acetonitrile as both solvent and nitrogen source. The reaction is catalyzed by a trisaminocyclopropenium (TAC) ion, which undergoes anodic oxidation to furnish a stable radical dication while the cathodic reaction reduces protons to molecular hydrogen. Irradiation of the TAC radical dication (wavelength of maximum absorption of 450 to 550 nanometers) with a white-light compact fluorescent light generates a strongly oxidizing photoexcited intermediate. Depending on the electrolyte used, either 3, 4- dihydroimidazole or aziridine products are obtained.
Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists
Sato, Nagaaki,Jitsuoka, Makoto,Ishikawa, Shiho,Nagai, Keita,Tsuge, Hiroyasu,Ando, Makoto,Okamoto, Osamu,Iwaasa, Hisashi,Gomori, Akira,Ishihara, Akane,Kanatani, Akio,Fukami, Takehiro
scheme or table, p. 1670 - 1674 (2009/11/30)
Novel imidazoline derivatives were discovered to be potent neuropeptide Y Y5 receptor antagonists. High-throughput screening of Merck sample collections against the human Y5 receptor resulted in the identification of 2,4,4-triphenylimidazoline (1), which had an IC50 of 54 nM. Subsequent optimization led to the identification of several potent derivatives.
