1262854-27-2Relevant academic research and scientific papers
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: Structure-activity relationship of P2′ substituents
Truong, Anh P.,Probst, Gary D.,Aquino, Jose,Fang, Larry,Brogley, Louis,Sealy, Jennifer M.,Hom, Roy K.,Tucker, John A.,John, Varghese,Tung, Jay S.,Pleiss, Michael A.,Konradi, Andrei W.,Sham, Hing L.,Dappen, Michael S.,Toth, Gergley,Yao, Nanhua,Brecht, Eric,Pan, Hu,Artis, Dean R.,Ruslim, Lany,Bova, Michael P.,Sinha, Sukanto,Yednock, Ted A.,Zmolek, Wes,Quinn, Kevin P.,Sauer, John-Michael
scheme or table, p. 4789 - 4794 (2010/11/02)
Herein we describe further evolution of hydroxyethylamine inhibitors of BACE-1 with enhanced permeability characteristics necessary for CNS penetration. Variation at the P2′ position of the inhibitor with more polar substituents led to compounds 19 and 32
A concise synthesis of ortho-iodobenzyl alcohols via addition of ortho-Iodophenyl grignard reagent to aldehydes and ketones
Cvengro, Alcohols Jan,Stolz, Daniel,Togni, Antonio
experimental part, p. 2818 - 2824 (2010/01/21)
A wide range of both secondary and tertiary ortho-iodobenzyl alcohols was synthesized via addition of ortho-iodophenyl Grignard reagents to aldehydes and ketones. Significant improvements in terms of yields were observed with ketones upon addition of CeCl3. The potential application of the target compounds as precursors for novel electrophilic trifluoromethylating reagents based on hypervalent iodine derivatives was demonstrated. Georg Thieme Verlag Stuttgart.
