473567-47-4Relevant articles and documents
MaxPHOS ligand: PH/NH tautomerism and rhodium-catalyzed asymmetric hydrogenations
Cristobal-Lecina, Edgar,Etayo, Pablo,Doran, Sean,Reves, Marc,Martin-Gago, Pablo,Grabulosa, Arnald,Costantino, Andrea R.,Vidal-Ferran, Anton,Riera, Antoni,Verdaguer, Xavier
, p. 795 - 804 (2014/04/03)
MaxPHOS is an active and robust P-stereogenic ligand for asymmetric catalysis. The presence of an -NH- bridge between the two phosphine moieties allows the NH/PH tautomerism to take place. The neutral ligand, in which the NH form predominates, is an air-sensitive compound. However, protonation of MaxPHOS leads to the stable PH form of the ligand, in which the overall positive charge is distributed on both P centers. This protonation turns the MaxPHOS×HBF4 salt 3 into an air-stable compound both in the solid state and in solution. The salt 3 is also a convenient precursor for the preparation of rhodium(I) complexes by direct ligand exchange with the complex [Rh(acac)(cod)]. Finally, the corresponding rhodium(I)-MaxPHOS complex was tested in the asymmetric hydrogenation of a wide range of substrates. The complex proved to be a highly selective and robust system in these reactions.
BETA-SECRETASE INHIBITING COMPOUNDS HAVING OXO-DIHYDRO-PYRAZOLE MOIETY
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Page/Page column 35, (2009/04/25)
Disclosed are compounds represented by Formula (I) as defined in the specification, or pharmaceutically acceptable salts or isomers thereof, and a pharmaceutical composition for inhibiting beta-secretase activity comprising a therapeutically effective amo
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives
Park, Heuisul,Min, Kyeongsik,Kwak, Hyo-Shin,Koo, Ki Dong,Lim, Dongchul,Seo, Sang-Won,Choi, Jae-Ung,Platt, Bettina,Choi, Deog-Young
, p. 2900 - 2904 (2008/12/22)
We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modification of P3, P1, and P2′ and combination of SAR display a >100-fold increase in potency with good cellular activity (IC50 = 0.1