Heterogeneous Catalytic Reductive Amination of Carbonyl Compounds with Ni-Al Alloy in Water as Solvent and Hydrogen Source
The heterogeneous catalytic reductive amination of carbonyl compounds has been achieved by reactions of ammonium hydroxide and various amines with ketones and aldehydes. The process is based on the application of Raney type Ni-Al alloy in an aqueous medium. The reaction of the carbonyl compounds with the amine provided the corresponding Schiff bases that immediately underwent a reduction to provide primary and secondary amines as products. The controlled reaction of the Al content of the alloy with the solvent water generates hydrogen, and the in situ formed Raney Ni serves as a hydrogenation catalyst. The method is a simple and efficient way of preparing a broad variety of primary and secondary amines.
Sch?fer, Christian,Ni?anci, Bilal,Bere, Matthew P.,Da?tan, Arif,T?r?k, Béla
p. 3127 - 3133
(2016/09/09)
Synthesis and spectroscopic properties of a series of novel 2-aryl-3-phenyl-2,3-dihydro-4H-1,3-benzothiazin-4-ones
A series of thirteen novel 2-aryl-3-phenyl-2,3-dihydro-4H-1,3-benzothiazin-4-ones was prepared at room temperature by T3P-mediated cyclization of N-phenyl-C-aryl imines with thiosalicylic acid. The spectroscopic and physical properties are reported and discussed. 1H-19F and 13C-19F couplings were observed in the NMR spectra of fluorinated compounds. Through-space interactions were observed in the 1H and 13C NMR spectra of the ortho-nitro compound. Trends were observed in the IR and UV absorptions of the ortho/meta/para-nitro series.
Silverberg, Lee J.,Pacheco, Carlos,Lagalante, Anthony,Tierney, John,Bachert, Joshua T.,Bayliff, J. Austin,Bendinsky, Ryan V.,Cali, Aaron S.,Chen, Liuxi,Cooper, Avril D.,Minehan, Michael J.,Mroz, Caitlin R.,Noble, Duncan J.,Weisbeck, Alexander K.,Xie, Yiwen,Yang, Ziwei
p. 122 - 143
(2018/05/09)
New insights into the bacterial RNA polymerase inhibitor CBR703 as a starting point for optimization as an anti-infective agent
CBR703 was reported to inhibit bacterial RNA polymerase (RNAP) and biofilm formation, considering it to be a good candidate for further optimization. While synthesized derivatives of CBR703 did not result in more-active RNAP inhibitors, we observed promising antibacterial activities. These again correlated with a significant cytotoxicity toward mammalian cells. Furthermore, we suspect the promising effects on biofilm formation to be artifacts. Consequently, this class of compounds can be considered unattractive as antibacterial agents. Copyright
Zhu, Weixing,Haupenthal, J?rgm,Groh, Matthias,Fountain, Michelle,Hartmann, Rolf W.
supporting information
p. 4242 - 4245
(2014/07/08)
Discovery of chiral N,N-disubstituted trifluoro-3-amino-2-propanols as potent inhibitors of cholesteryl ester transfer protein [1]