65577-55-1Relevant academic research and scientific papers
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human β-secretase (BACE1)
Manzenrieder, Florian,Frank, Andreas O.,Huber, Timo,Dorner-Ciossek, Cornelia,Kessler, Horst
, p. 4136 - 4143 (2007)
Phosphino dipeptide (PDP) isosteres are known to be useful analogues of the transition state of metalloprotease substrates. Here we describe the use of this unit for the design of aspartic protease inhibitors. A PDP analogue of OM00-3, a potent BACE1 inhibitor, was synthesized and exhibited high biological activity (IC50 ～ 12 nM).
Method of synthesis of phosphinic acids based on hypophosphites: VIII.1 synthesis of α-aminoalkylphenethylphosphinic acids
Dmitriev,Ragulin
experimental part, p. 1786 - 1791 (2012/01/12)
Development of methodology of double Arbuzov rearrangement based on hypophosphites allows a one-pot formation of two unsymmetrical phosphorus-carbon bonds by the Michael-Pudovik type reaction of stepwise addition of the intermediately forming silyl esters of trivalent phosphorus to different unsaturated compounds. A procedure was developed of the synthesis of α-aminoalkylphenethylphosphinic acids. Bis-(trimethylsilyl) phenethylphosphonite formed as a result of the addition of bis(trimethylsilyl) hypophosphite to styrene in situ was added without isolation from the reaction mixture to Schiff bases obtained preliminary from benzylamine or diphenylmethylamine and various aldehydes. The subsequent removal of N-protecting groups by hydrogenation or acidic hydrolysis gave a number of new α-aminoalkylphenethylphosphinic acids.
Synthesis of an optically active al(salalen) complex and its application to catalytic hydrophosphonylation of aldehydes and aldimines
Saito, Bunnai,Egami, Hiromichi,Katsuki, Tsutomu
, p. 1978 - 1986 (2007/10/03)
Optically active aluminum(salalen) complex 2 was newly synthesized in a modular synthetic manner, and it was found to serve as an efficient catalyst for hydrophosphonylation of aldehydes and aldimines, giving the corresponding α-hydroxy and α-amino phosph
