1312716-45-2Relevant academic research and scientific papers
Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates
Bowers, Simeon,Xu, Ying-Zi,Yuan, Shendong,Probst, Gary D.,Hom, Roy K.,Chan, Wayman,Konradi, Andrei W.,Sham, Hing L.,Zhu, Yong L.,Beroza, Paul,Pan, Hu,Brecht, Eric,Yao, Nanhua,Lougheed, Julie,Tam, Danny,Ren, Zhao,Ruslim, Lany,Bova, Michael P.,Artis, Dean R.
, p. 2181 - 2186 (2013/04/23)
The structure-activity relationship of a series of dihydroisoquinoline BACE-1 inhibitors is described. Application of structure-based design to screening hit 1 yielded sub-micromolar inhibitors. Replacement of the carboxylic acid of 1 was guided by X-ray
Synthesis and asymmetric catalytic activity of (1S,1′S)-4,4′- biquinazoline-based primary amines
Cakici, Murat,Catir, Mustafa,Karabuga, Semistan,Ulukanli, Sabri,Kilic, Hamdullah
, p. 300 - 308 (2011/05/17)
A series of (1S,1′S)-4,4′-biquinazoline-based primary amines were prepared from natural amino acids via a six-step reaction sequence of protection and condensation followed by key synthetic steps including chlorination, nickel(0)-mediated homocoupling, and deprotection. These novel amines were screened for the asymmetric ethylation of aryl aldehydes to yield alcohols with an (S)-configuration with enantiomeric excesses (ee) varying from 2% to 95%.
