31675-43-1Relevant academic research and scientific papers
Design and synthesis of 5,5′-disubstituted aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors
Malamas, Michael S.,Erdei, Jim,Gunawan, Iwan,Turner, Jim,Hu, Yun,Wagner, Erik,Fan, Kristi,Chopra, Rajiv,Olland, Andrea,Bard, Jonathan,Jacobsen, Steve,Magolda, Ronald L.,Pangalos, Menelas,Robichaud, Albert J.
experimental part, p. 1146 - 1158 (2010/07/02)
The identification of small molecule aminohydantoins as potent and selective human β-secretase inhibitors is reported. These analogues exhibit low nannomolar potency for BACE1, show comparable activity in a cell-based (ELISA) assay, and demonstrate 50 value for BACE1 of 10 nM and exhibited comparable cellular activity (EC 50 = 20 nM) in the ELISA assay. Acute oral administration of (S)-55 at 100 mg/kg resulted in a 69% reduction of plasma Aβ40 at 8 h in a Tg2576 mouse (p 0.001).
One-pot synthesis of primary 1-aminophosphonates: Coupling reaction of carbonyl compounds, hexamethyldisilazane, and diethyl phosphite catalyzed by al(otf)3
Sobhani, Sara,Tashrifi, Zahra
experimental part, p. 109 - 115 (2009/09/29)
Al(OTf)3 has been utilized as a new and efficient catalyst for the selective synthesis of primary 1-aminophosphonates by a one-pot coupling reaction of various types of aldehydes/ketones, hexamethyldisilazane, and diethyl phosphite under solvent-free cond
Highly efficient chemo- and regioselective silylation of -OH groups and cyanosilylation of aldehydes promoted by TiCl2(OTf)-SiO2 as a new recyclable catalyst
Firouzabadi, Habib,Iranpoor, Nasser,Farahi, Soghra
scheme or table, p. 3923 - 3928 (2010/02/28)
TiCl2(OTf)-SiO2 as an easy handling recyclable catalyst was applied for trimethylsilylation of diethyl α-hydroxyphosphonates, alcohols and phenols with high selectivity using HMDS as a silylating agent. Cyanotrimethylsilyl ethers were also obtained in excellent yields from treatment of aldehydes with TMSCN in the presence of this catalyst.
Synthesis of functionalized 1-trimethylsiloxy-substituted O-trimethylsilyl alkylphosphonites and their derivatives
Prishchenko, Andrey A.,Livantsov, Mikhail V.,Novikova, Olga P.,Livantsova, Ludmila I.,Petrosyan, Valery S.
, p. 352 - 359 (2008/09/20)
Nucleophilic addition of trimethylsilyl esters of tricoordinate organophosphorus acids to various functionalized aldehydes with vinyl, aryl, and heterocyclic fragments is proposed as a convenient method for the synthesis of new 1-trimethylsiloxysubstituted alkylphosphonites and their derivatives at mild conditions. Also the new functionalized derivatives of these phosphonites, including amino groups as well as certain properties of these compounds as important precursors of new functionalized 1-hydroxyalkylorganophosphorus acids, are presented.
Iron(III) trifluoroacetate [Fe(F3CCO2)3] as an easily available, non-hygroscopic, non-corrosive, highly stable and a reusable Lewis Acid catalyst: Efficient O-silylation of α-hydroxyphosphonates, alcohols and phenols by he
Firouzabadi, Habib,Iranpoor, Nasser,Jafari, Abbas Ali,Jafari, Mohammad Reza
, p. 2711 - 2714 (2008/12/20)
O-Silylation of hydroxyl groups of α-hydroxyphosphonates, primary, secondary tertiary-alcohols and phenols with HMDS was achieved in high to excellent yields using iron(III) trifluoroacetate [Fe(F3CCO2)3] as an easily avai
CYCLOALKYL AMINO-HYDANTOIN COMPOUNDS AND USE THEREOF FOR BETA-SECRETASE MODULATION
-
Page/Page column 16, (2010/11/25)
The present invention provides a 2-amino-5-cycloalkyl-hydantoin compound of formula I The present invention also provides methods and compositions for the inhibition of β-secretase (BACE) and the treatment of β-amyloid deposits and neurofibrillary tangles.
Aluminium triflate [Al(OTf)3] as a recyclable catalyst for the conversion of α-hydroxyphosphonates, alcohols and phenols to their corresponding O-silylated products with hexamethyldisilazane (HMDS)
Firouzabadi, Habib,Iranpoor, Nasser,Sobhani, Sara,Ghassamipour, Soheila
, p. 595 - 599 (2007/10/03)
Al(OTf)3 as a recyclable catalyst conducts the efficient conversion of various types of α-hydroxyphosphonates to their corresponding α-trimethysilyloxyphosphonates with HMDS in the absence of solvent at room temperature. The general applicabili
Magnesium triflate [Mg(OTf)2] a highly stable, non-hygroscopic and a recyclable catalyst for the high yielding preparation of diethyl α-trimethylsilyloxyphosphonates from diethyl α-hydroxyphosphonates by HMDS under solventless conditions
Firouzabadi, Habib,Iranpoor, Nasser,Sobhani, Sara,Ghassamipour, Soheila
, p. 3197 - 3202 (2007/10/03)
A broad, adaptable, high yielding and convenient procedure for the easy conversion of various α-hydroxyphosphonates to α-trimethylsilyloxyphosphonates under mild conditions with HMDS in the presence of a catalytic amount of magnesium triflate as a highly stable and a non-hygroscopic recyclable catalyst in neat conditions is described. In order to show the general applicability of this method, we have also applied this procedure successfully for the silylation of ordinary alcohols and phenols.
Copper triflate [Cu(OTf)2] is an efficient and mild catalyst for the silylation of α-hydroxyphosphonates to α-trimethylsilyloxyphosphonates with HMDS at room temperature
Firouzabadi, Habib,Iranpoor, Nasser,Sobhani, Sara,Ghassamipour, Soheila,Amoozgar, Zohreh
, p. 891 - 893 (2007/10/03)
A broad, adaptable, high yielding and convenient procedure for the fast conversion of various α-hydroxyphosphonates to α-trimethylsilyloxyphosphonates under mild conditions with HMDS in the presence of a catalytic amount of copper triflate is described. T
A high yielding preparation of α-trimethylsilyloxyphosphonates by silylation of α-hydroxyphosphonates with HMDS catalyzed by iodine
Firouzabadi, Habib,Iranpoor, Nasser,Sobhani, Sara
, p. 3653 - 3655 (2007/10/03)
A general, versatile, high yielding and convenient procedure for the immediate conversion of various α-hydroxyphosphonates to α-trimethylsilyloxyphosphonates under neutral conditions using HMDS in the presence of a catalytic amount of iodine is described.
