20637-04-1Relevant articles and documents
Copper-Catalyzed Conjugate Addition of Carbonyls as Carbanion Equivalent via Hydrazones
Luo, Siyi,Peng, Marie,Querard, Pierre,Li, Chen-Chen,Li, Chao-Jun
, p. 13111 - 13117 (2021/09/18)
Copper-catalyzed conjugate addition is a classic method for forming new carbon-carbon bonds. However, copper has never showed catalytic activity for umpolung carbanions in hydrazone chemistry. Herein, we report a facile conjugate addition of hydrazone catalyzed by readily available copper complexes at room temperature. The employment of mesitylcopper(I) and electron-rich phosphine bidentate ligand is a key factor affecting reactivity. The reaction allows various aromatic hydrazones to react with diverse conjugated compounds to produce 1,4-adducts in yields of about 20 to 99%.
Reductive C-C Coupling by Desulfurizing Gold-Catalyzed Photoreactions
Zhang, Lumin,Si, Xiaojia,Yang, Yangyang,Witzel, Sina,Sekine, Kohei,Rudolph, Matthias,Rominger, Frank,Hashmi, A. Stephen K.
, p. 6118 - 6123 (2019/07/03)
[Au2(μ-dppm)2]Cl2-mediated photocatalysis reactions are usually initiated by ultraviolet A (UVA) light; herein, an unreported system using blue light-emitting diodes (LEDs) as excitation light source was found. The red shift of the absorption wavelength originates from the combination of [Au2(μ-dppm)2]Cl2 and ligand (Ph3P or mercaptan). On the basis of this finding, a gold-catalyzed reductive desulfurizing C-C coupling of electrophilic radicals and styrenes mediated by blue LEDs is presented, a coupling which cannot be efficiently accessed by previously reported methods. This mild and highly efficient C-C bond formation strategy uses mercaptans both as electron-deficient alkyl radical precursor as well as the hydrogen source. Two examples of amino acids have also been modified by using this strategy. Moreover, this methodology could be applied in polymer synthesis. Gram-scale synthesis and mechanistic insights into this transformation are also presented.
Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: A case of clofilium analogues
Louvel, Julien,Carvalho, Jo?o F.S.,Yu, Zhiyi,Soethoudt, Marjolein,Lenselink, Eelke B.,Klaasse, Elisabeth,Brussee, Johannes,Ijzerman, Adriaan P.
supporting information, p. 9427 - 9440 (2014/01/06)
Cardiotoxicity is a side effect that plagues modern drug design and is very often due to the off-target blockade of the human ether-à-go-go related gene (hERG) potassium channel. To better understand the structural determinants of this blockade, we design