651326-28-2Relevant articles and documents
Iodine-mediated aminohalogenation-oxidation to synthesize 2-fluoroalkyl imidazole derivatives
Li, Shan,Liang, Jian,Liu, Xiaofeng,Xian, Liqing,Du, Mingxu
, p. 1041 - 1053 (2020/10/02)
A simple and efficient method of iodine-mediated aminohalogenation-oxidation of fluorinated N’-propargyl amidines to synthesize 2-fluoroalkyl imidazole-5-carbaldehydes was developed. This method showed good functional group compatibility and wide substrat
Copper-catalyzed direct C-H oxidative trifluoromethylation of heteroarenes
Chu, Lingling,Qing, Feng-Ling
supporting information; experimental part, p. 1298 - 1304 (2012/02/16)
This article describes the copper-catalyzed oxidative trifluoromethylation of heteroarenes and highly electron-deficient arenes with CF 3SiMe3 through direct C-H activation. In the presence of catalyst Cu(OAc)2, ligand 1,10-phenanthroline and cobases tert-BuONa/NaOAc, oxidative trifluoromethylation of 1,3,4-oxadiazoles with CF3SiMe3 proceeded smoothly using either air or di-tert-butyl peroxide as an oxidant to give the corresponding trifluoromethylated 1,3,4-oxadiazoles in high yields. Di-tert-butyl peroxide was chosen as the suitable oxidant for oxidative trifluoromethylation of 1,3-azoles and perfluoroarenes. Cu(OH)2 and Ag2CO3 were the best catalyst and oxidant for direct oxidative trifluoromethyaltion of indoles. The optimum reaction conditions enable oxidative trifluoromethylation of a range of heteroarenes that bear numerous functional groups. The prepared trifluoromethylated heteroarenes are of importance in the areas of pharmaceuticals and agrochemicals. The preliminary mechanistic studies of these oxidative trifluoromethylations are also reported.
Novel imidazole compounds as a new series of potent, orally active inhibitors of 5-lipoxygenase
Mano, Takashi,Stevens, Rodney W.,Ando, Kazuo,Nakao, Kazunari,Okumura, Yoshiyuki,Sakakibara, Minoru,Okumura, Takako,Tamura, Tetsuya,Miyamoto, Kimitaka
, p. 3879 - 3887 (2007/10/03)
Replacement of the dihydroquinolinone pharmacophore of Zeneca's ZD2138 by ionizable imidazolylphenyl moiety has lead to the discovery of a novel series of potent and orally active 5-lipoxygenase (5-LO) inhibitors. The synthesis and structure-activity relationship (SAR) of this series of compounds are described herein.
