EP 1034154 A1 20000913 - A SOLID-PHASE TECHNOLOGY FOR THE PREPARATION OF COMBINATORIAL LIBRARIES THROUGH AMIDE-BOND ANCHORING
Title (en)
A SOLID-PHASE TECHNOLOGY FOR THE PREPARATION OF COMBINATORIAL LIBRARIES THROUGH AMIDE-BOND ANCHORING
Title (de)
FESTPHASENTECHNOLOGIE ZUR HERSTELLUNG VON KOMBINATORISCHEN BIBLIOTHEKEN DURCH AMIDBINDUNGKNÜPFUNG
Title (fr)
TECHNOLOGIE EN PHASE SOLIDE POUR L'ELABORATION DE BIBLIOTHEQUES COMBINATOIRES PAR VIA ANCRAGE PAR LIAISON AMIDE
Publication
Application
Priority
- GB 9803523 W 19981126
- GB 9724853 A 19971126
- GB 9808744 A 19980425
Abstract (en)
[origin: WO9926902A1] The present invention provides the means to suppress epimerisation of the C alpha terminal amino acid of a protected peptide sequence during coupling by using the protection moiety shown in (1) which is referred to as a "precursor linker". This moiety has a number of features; the functional group R and the 2-hydroxyl function lie in a para position relative to each other while the ether residue lies in a para position relative to the aldehyde residue. R1 is an electron donating alkyl group. The R group is a moiety that may readily be interconverted between electron-withdrawing and electron donating. This is based on the safety catch principle. The principle, that a stable bond is smoothly converted to a labile one at a convenient point during a synthesis, has been applied in peptide chemistry for the development of linkers and protecting groups. One approach has been to exploit the facile reductive conversion of a sulphoxide to sulphide. This approach when applied to the precursor linker (1) provides the functional protection moieties which are referred to as "linker compounds".
IPC 1-7
IPC 8 full level
C07B 61/00 (2006.01); C07C 59/74 (2006.01); C07C 323/22 (2006.01); C07C 323/52 (2006.01); C07K 1/04 (2006.01); C08G 85/00 (2006.01); C40B 40/02 (2006.01); C40B 40/14 (2006.01); C40B 50/00 (2006.01); C40B 50/06 (2006.01)
CPC (source: EP)
C07C 59/74 (2013.01); C07K 1/042 (2013.01); C07K 1/047 (2013.01); C40B 40/00 (2013.01); Y02P 20/55 (2015.11)
Citation (search report)
See references of WO 9926902A1
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU NL PT SE
DOCDB simple family (publication)
WO 9926902 A1 19990603; AU 1342099 A 19990615; AU 734992 B2 20010628; CA 2311490 A1 19990603; EP 1034154 A1 20000913; JP 2001524457 A 20011204
DOCDB simple family (application)
GB 9803523 W 19981126; AU 1342099 A 19981126; CA 2311490 A 19981126; EP 98956988 A 19981126; JP 2000522063 A 19981126