EP 2616549 A1 20130724 - CHEMICAL MODIFICATION OF RNA AT THE 2'-POSITION OF THE RIBOSE RING VIA AAA COUPLING
Title (en)
CHEMICAL MODIFICATION OF RNA AT THE 2'-POSITION OF THE RIBOSE RING VIA AAA COUPLING
Title (de)
CHEMISCHE MODIFIKATION VON RNA AN DER 2'-POSITION DES RIBOSERINGS MITTELS AAA-KOPPLUNG
Title (fr)
MODIFICATION CHIMIQUE D'ARN EN POSITION 2' SUR LE CYCLE RIBOSE PAR COUPLAGE AAA
Publication
Application
Priority
- US 38377910 P 20100917
- US 2011050903 W 20110909
Abstract (en)
[origin: WO2012036972A1] A method that relates to the post-synthetic chemical modification of RNA at the 2'-position on the ribose ring via a silver catalyzed alkyne, aldehyde, amine coupling ("AAA or A3 or AA3 coupling") chemistry is disclosed. The method 1) avoids complex, tedious multi-step syntheses of each desired modified ribonucleoside; 2) allows diverse chemical modifications using high-fidelity chemistry that is completely orthogonal to commonly used alkylamino, carboxylate and disulfide linker reactivities; 3) allows introduction of functional groups that are incompatible with modern automated solid-phase synthesis of RNA and subsequent cleavage-deprotection steps; 4) allows introduction of functional groups useful as targeting ligands; and 5) enables high-throughput structure-activity relationship studies on chemically modified RNA in 96-well format.
IPC 8 full level
C12P 19/34 (2006.01); C07H 21/02 (2006.01); C07H 21/04 (2006.01)
CPC (source: EP)
C07H 21/02 (2013.01)
Citation (search report)
See references of WO 2012036972A1
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
DOCDB simple family (publication)
DOCDB simple family (application)
US 2011050903 W 20110909; EP 11825711 A 20110909