EP 2235032 A2 20101006 - CHEMICAL-CATALYTIC METHOD FOR THE PERACYLATION OF OLEUROPEIN AND ITS PRODUCTS OF HYDROLYSIS
Title (en)
CHEMICAL-CATALYTIC METHOD FOR THE PERACYLATION OF OLEUROPEIN AND ITS PRODUCTS OF HYDROLYSIS
Title (de)
CHEMISCH-KATALYTISCHES VERFAHREN ZUR PERACETYLIERUNG VON OLEUROPEIN UND SEINE HYDROLYSEPRODUKTE
Title (fr)
PROCÉDÉ CHIMICO-CATALYTIQUE POUR LA PÉRACYLATION DE L'OLÉUROPÉINE ET DE SES PRODUITS D'HYDROLYSE
Publication
Application
Priority
- IT 2008000303 W 20080505
- IT MI20070903 A 20070504
- IT MI20070904 A 20070504
Abstract (en)
[origin: WO2008136037A2] The method, object of the present invention, concerns the peracylation of oleuropein and its products of hydrolysis: The method makes use of the excellent properties as Lewis acid catalysts of halides and tryphilates of lanthanides (III). The component is placed to react, in the presence of catalytic quantities of Lewis acid, directly with an acylating agent containing at least one acylic group R, where R is H, an alkylic radical of 1-31 atoms of linear or branched carbon, an alkenylic radical containing up to 31 atoms of carbon or an arylic group. The procedures for the extraction and the successive hydrolysis of the oleuropein for the synthesis of its aglycon and the hydroxytyrosol, resolve the problems tied to the quantitative yield of the products and to the use of highly-toxic and expensive catalysts. Furthermore, the innovative and inventive contribution is given by the peracylation of the oleuropein and its products of synthesis, aglycon and hydroxytyrosol, that supply a new class of molecule, biologically active as anti-oxidants and anti-inflammatory ones. The proven anti-oxidant activity of oleuropein and its derivates leads to the hypothesis that they could also act as protectors against oxidative stress at the level of the central nervous system, one of the causal factors of Parkinson's disease. The molecules examined are all good protectors against oxidative stress and the greater efficiency of the peracylated derivatives is presumably due to their greater lipophilicity and the possibility of penetrating the cellular membrane.
IPC 8 full level
C07H 17/04 (2006.01); A61K 31/7048 (2006.01); A61P 9/10 (2006.01)
CPC (source: EP)
A61P 9/10 (2017.12); C07H 17/04 (2013.01)
Citation (search report)
See references of WO 2008136037A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA MK RS
DOCDB simple family (publication)
WO 2008136037 A2 20081113; WO 2008136037 A3 20081224; EP 2235032 A2 20101006
DOCDB simple family (application)
IT 2008000303 W 20080505; EP 08763854 A 20080505