60694-67-9Relevant academic research and scientific papers
Synthesis of biaryl ketones by arylation of Weinreb amides with functionalized Grignard reagents under thermodynamic controlvs.kinetic control ofN,N-Boc2-amides
Li, Guangchen,Szostak, Michal
supporting information, p. 3827 - 3831 (2020/06/03)
A highly efficient method for chemoselective synthesis of biaryl ketones by arylation of Weinreb amides (N-methoxy-N-methylamides) with functionalized Grignard reagents is reported. This protocol offers rapid entry to functionalized biaryl ketones after Mg/halide exchange with i-PrMgCl·LiCl under operationally-simple and practical reaction conditions. The scope of the method is highlighted in >40 examples, including bioactive compounds and pharmaceutical derivatives. Collectively, this transition-metal-free approach offers a major advantage over the recently established cross-coupling of amides by oxidative addition of N-C(O) bonds. Considering the utility of amide acylation reactions in modern synthesis, we expect that this method will be of broad interest.
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents
Hayashi, Yoshio,Yamazaki, Yuri,Sumikura, Makiko,Masuda, Yurika,Hayashi, Yoshiki,Yasui, Hiroyuki,Kiso, Yoshiaki,Chinen, Takumi,Usui, Takeo,Yakushiji, Fumika,Potts, Barbara,Neuteboom, Saskia,Palladino, Michael,Lloyd, George Kenneth
experimental part, p. 4279 - 4289 (2012/09/08)
KPU-105 (4), a potent anti-microtubule agent that contains a benzophenone was derived from the diketopiperazine-type vascular disrupting agent (VDA) plinabulin 3, which displays colchicine-like tubulin depolymerization activity. To develop derivatives wit
Leukotriene antagonists and use thereas
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, (2008/06/13)
This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Merostabilization in radical ions, triplets, and biradicals. 4. Substituent effects on the half-wave reduction potentials and n, ?* triplet energies of aromatic ketones
Leigh, William J.,Arnold, Donald R.,Humphreys, Robert W. R.,Wong, Po Cheong
, p. 2537 - 2549 (2007/10/02)
The half-wave reduction potentials, measured by cyclic voltammetry, and n, ?* triplet energies, measured by phosphorescence spectroscopy, were determined for a series of eighteen symmetrically and unsymmetrically substituted benzophenones.Attempts are made to correlate the results with Hammett substituent constants.Better correlations are observed when the data are correlated with a two-parameter function consisting of Hammett substituent constants and a set of substituent parameters describing variations in free radical stability.Significant deviations from "normal" behaviour are observed for benzophenones substituted by both electron-donating and electron-withdrawing substituents.These deviations are attributed to merostabilization of the radical-like species, and an empirical approach designed to evaluate the importance of this effect is developed.Ab initio calculations of molecular orbital energies in meta- and para-substituted benzaldehydes are used to evaluate the substituent effects on E1/2red and ETn,?* in terms of the effect on the energies of the n- and ?*-orbitals.
Synthesis and anthelminthic acitivity of alkyl-(5-acyl-1-benzimidazol-2-yl) carbamates
Raeymackers,Van Gelder,Roevens,Janssen
, p. 586 - 594 (2007/10/05)
A series of alkyl-(5-acyl-l-H-benzimidazol-2-yl)-carbamates were prepared and screened for anthelminthic activity. Some of them were found to be fully active at low, atoxic oral dose levels against gastro-intestinal nematodes. The activity against Syphacia muris and Strongyloides ratta is indicated. From these studies methyl (5-benzoyl-1-H-benzimidazol-2-yl) carbamate (mebendazole) and methyl [5-(4-fluorobenzoyl)-1-H-benzimidazol-2-yl]carbamate (flubendazole) were selected for detailed investigation.
