[EN] SUBSTITUTED 3- AND 4- AMINOMETHYLPIPERIDINES FOR USE AS BETA-SECRETASE IN THE TREATMENT OF ALZHEIMER'S DISEASE<br/>[FR] 3- ET 4- AMINOMETHYLPIPERIDINES SUBSTITUEES UTILISEES COMME BETA-SECRETASE DANS LE TRAITEMENT DE LA MALADIE D'ALZHEIMER
申请人:ACTELION PHARMACEUTICALS LTD
公开号:WO2004002483A1
公开(公告)日:2004-01-08
The invention relates to novel compounds, which are substituted chiral or achiral derivatives of 3- or 4- aminomethylpiperidine of the general formula (I). The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula (I) and especially their use as inhibitors of beta-secretases for the treatment of Alzheimer’s disease.
New Hybrid Inorganic−Organic Polymers as Supports for Heterogeneous Catalysis: A Novel Pd(0) Metalated Cyclophosphazene-Containing Polymer as an Efficient Heterogeneous Catalyst for the Heck Reaction
[reaction: see text] A newPd(0) complex of a pendant cyclophosphazene-containing cross-linked polymer is found to be an effective heterogeneouscatalyst for the Heck arylation reaction. The catalyst is robust and can be recycled without significant loss of activity.
Synthesis of biaryl-styrene monomers by microwave-assisted Suzuki coupling
作者:Hazit A. Zayas、Michael C. Bowyer、Christopher P. Gordon、Clovia I. Holdsworth、Adam McCluskey
DOI:10.1016/j.tetlet.2009.07.117
日期:2009.10
Biaryl-styrenic monomers are prepared via Suzukicoupling as functional monomers in the synthesis of molecularly imprinted polymers. Traditional thermal Suzuki approaches are hampered by competition between Suzuki, Heck and homo-coupling reactions. Microwave-assisted approaches facilitated rapid access to the desired Suzuki products whilst suppressing both Heck and homo-couplings of 4-vinylboronic
cross-linked polymer (CPPL) has been utilized for binding Zn(II). The metalatedpolymer (CPPL-Zn) has been found to be very effective catalyst for the hydrolysis of a RNA model phosphodiester substrate [2-(hydroxypropyl)-p-nitrophenyl phosphate, hNPP]. In addition, CPPL-Zn also cleaved supercoiled plasmid DNA pBR322 thus providing a novel structural motif of inorganic-organic hybrid polymers as synthetic
Pd-catalyzed protecting-group-free cross-couplings of iodophenols with atom-economic triarylbismuth reagents
作者:Maddali L.N. Rao、Suresh Meka
DOI:10.1016/j.tetlet.2019.151512
日期:2020.2
An efficient protocol for the protecting-group-free synthesis of unsymmetrical hydroxybiaryls via the Pd-catalyzedcross-couplings of unprotected iodophenols with triarylbismuth reagents is described. The presented protocols exhibits good to high yields of hydroxybiaryls.