14429-15-3Relevant academic research and scientific papers
Br?nsted acid catalyzed reductive amination with benzothiazoline as a highly efficient hydrogen donor
Zhu, Chen,Akiyama, Takahiko
, p. 1251 - 1254 (2011)
Reductive amination of aldehyde and amine proceeded smoothly in the presence of benzothiazoline as efficient hydrogen source by means of 20 mol% trifluoroacetic acid to give the corresponding amines in excellent yields. Hydrogen-donor abilities of benzothiazoline, benzimidazoline, and benzoxazoline were compared. Georg Thieme Verlag Stuttgart - New York.
Synthesis and evaluation of N-analogs of 1,2-diarylethane as Helicobacter pylori urease inhibitors
Xiao, Zhu-Ping,Shi, Wei-Kang,Wang, Peng-Fei,Wei, Wei,Zeng, Xiao-Tong,Zhang, Ji-Rong,Zhu, Na,Peng, Miao,Peng, Bin,Lin, Xiao-Yi,Ouyang, Hui,Peng, Xiao-Chun,Wang, Guang-Cheng,Zhu, Hai-Liang
, p. 4508 - 4513 (2015/08/03)
Therapies based on urease inhibition are now seriously considered as the first line of treatment for infections caused by Helicobacter pylori. However, the present inhibitors are ineffective or unstable in highly acidic gastric juice. Here, we report a series of benzylanilines as effective inhibitors of H. pylori urease. Out of the obtained twenty-one compounds, N-(3,4-dihydroxybenzyl)-4-nitroaniline (4) was evaluated in detail and shows promising features for development as anti-H. pylori agent. Excellent potency against urease in both cell-free extract and intact cell was observed at low concentrations of 4 (IC50 = 0.62 ± 0.04 and 1.92 ± 0.09 μM), which showed over 29- and 54-fold increase in potency with respect to the positive control AHA. The SAR analysis revealed that protection of 3,4-dihydroxy group of 4 as methoxy or changes of 4-NO2 will result in a moderate to dramatic decrease in potency.
Molecular iodine catalyzed transfer hydrogenation: Reduction of aldimines, ketimines, and α-imino esters
Bachu, Prabhakar,Zhu, Chen,Akiyama, Takahiko
supporting information, p. 3977 - 3981 (2013/07/25)
An efficient and practical protocol for the reduction of aldimines, ketimines, and α-imino esters in the presence of catalytic amount of molecular iodine with Hantzsch ester at ambient temperature afforded the corresponding amines in excellent yields.
Flow synthesis of organic azides and the multistep synthesis of imines and amines using a new monolithic triphenylphosphine reagent
Smith, Catherine J.,Smith, Christopher D.,Nikbin, Nikzad,Ley, Steven V.,Baxendale, Ian R.
supporting information; experimental part, p. 1927 - 1937 (2011/04/21)
Here we describe general flow processes for the synthesis of alkyl and aryl azides, and the development of a new monolithic triphenylphosphine reagent, which provides a convenient format for the use of this versatile reagent in flow. The utility of these new tools was demonstrated by their application to a flow Staudinger aza-Wittig reaction sequence. Finally, a multistep aza-Wittig, reduction and purification flow process was designed, allowing access to amine products in an automated fashion.
