39910-98-0Relevant articles and documents
A soluble polyethyleneglycol-anchored phosphine as a highly active, reusable ligand for Pd-catalyzed couplings of aryl chlorides: comparison with cross and non-cross-linked polystyrene and silica supports
Leyva, Antonio,García, Hermenegildo,Corma, Avelino
, p. 7097 - 7111 (2007)
The so-called SPhos phosphine, an extremely active ligand in the amination and Suzuki coupling of sterically-hindered aryl chlorides, has been anchored on different supports such as non-soluble (cross-linked polystyrene) and soluble (non-cross-linked polystyrene and polyethyleneglycol) polymers, as well as high surface silica. SPhos anchored on polyethyleneglycol (PEG-SPhos) showed the best activity for both amination and Suzuki couplings. The PEG-SPhos ligand can be quantitatively recovered from the reaction mixture through precipitation with diethyl ether and recycled in four consecutive runs without loosing activity. 31P NMR spectra of the reused anchored ligand showed that deactivation of the PEG-SPhos ligand comes from the progressive oxidation of the phosphine-to-phosphine oxide.
Synthesis and antimicrobial evaluation of new 2-pyridinone and 2-iminochromene derivatives containing morpholine moiety
Salem, Mohamed A.,Abbas, Samir Y.,Helal, Mohamed H.,Alzahrani, Abdullah Y.
, p. 2117 - 2123 (2021/07/09)
As trail to overcome on the antimicrobial drug-resistance problems, new functionalized 2-pyridinone and 2-iminochromene derivatives bearing morpholine moiety were designed and synthesized. The 2-pyridinone derivatives were obtained through the cyclization of cyanoacetohydrazone of 4-morpholinylacetophenone with 1,3-dicarbonyl compounds, α,β-unsaturated nitriles or 2-(arylidene)malononitriles. The 2-iminochromene derivatives were synthesized through the ring closure of cyanoacetohydrazonewith salicylaldehyde derivatives. The antibacterial and antifungal activities for the synthesized 2-pyridinone and 2-iminochromene derivatives were investigated. Most of the tested compounds showed moderate activity against P. vulgaris. Compounds 4a,b and 5a,b showed moderate activity against G ?ve bacteria. All iminochromene derivatives showed moderate activity against C. albicans. Compound 8c was the most active compound.
Amination of Aryl Halides Mediated by Electrogenerated Nickel from Sacrificial Anode
Daili, Farah,Sengmany, Stéphane,Léonel, Eric
, p. 2462 - 2469 (2021/06/28)
Electrochemical C(sp2)?N couplings mediated by nickel salts generated from the sacrificial anode has been described for the first time. In this approach, the sacrificial nickel anode is employed as the sole source of nickel and the process, operationally simple to set up, enables the preparation of functionalized arylamine derivatives with moderate to good yields, under mild reaction conditions and without additional ligand. A cooperative process between the two electrodes is involved in the proposed mechanism.
BIOREDUCIBLE N-OXIDE-BASED PROBES FOR IMAGING OF HYPOXIA
-
Paragraph 0220, (2020/03/09)
Hypoxia occurs when limited oxygen supply impairs physiological functions and is a pathological hallmark of many diseases including cancer and ischemia. Thus, detection of hypoxia can guide treatment planning and serve as a predictor of patient prognosis. Current methods suffer from invasiveness, poor resolution and low specificity. To address these limitations, various hypoxia-responsive probes (HyPs) for photoacoustic imaging are disclosed. The emerging modality converts safe, non-ionizing light to ultrasound waves, enabling acquisition of high-resolution 3D images in deep tissue. The HyPs feature an N-oxide trigger that is reduced in the absence of oxygen by haem proteins such as CYP450 enzymes. Reduction of HyPs produce a spectrally distinct product, facilitating identification via photoacoustic imaging. HyPs exhibit selectivity for hypoxic activation in vitro, in living cells and in multiple disease models in vivo. HyPs are also compatible with NIR fluorescence imaging, establishing its versatility as a multimodal imaging agent.
