EP 1021407 A1 20000726 - SYNTHESIS OF CLASTO-LACTACYSTIN BETA-LACTONE AND ANALOGS THEREOF
Title (en)
SYNTHESIS OF CLASTO-LACTACYSTIN BETA-LACTONE AND ANALOGS THEREOF
Title (de)
HERSTELLUNG VON CLASTO-LACTACYSTIN-BETA-LACTON UND ANALOGA DAVON
Title (fr)
SYNTHESE DE CLASTO-LACTACYSTINE BETA-LACTONE ET DE SES ANALOGUES
Publication
Application
Priority
- US 9816858 W 19980814
- US 5584897 P 19970815
- US 91211197 A 19970815
- US 6735297 P 19971203
Abstract (en)
[origin: WO9909006A1] The present invention is directed to an improved synthesis of clasto-lactacystin- beta -lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin- beta -lactones, and analogs thereof and their use as proteosome inhibitors.
IPC 1-7
IPC 8 full level
A61K 31/40 (2006.01); A61K 31/4015 (2006.01); C07D 207/46 (2006.01); A61K 31/407 (2006.01); C07D 491/044 (2006.01); A61K 31/421 (2006.01); A61P 9/10 (2006.01); A61P 29/00 (2006.01); A61P 35/00 (2006.01); A61P 35/04 (2006.01); A61P 43/00 (2006.01); C07B 61/00 (2006.01); C07C 69/675 (2006.01); C07C 231/10 (2006.01); C07C 231/14 (2006.01); C07C 233/82 (2006.01); C07C 235/80 (2006.01); C07C 237/06 (2006.01); C07C 247/04 (2006.01); C07D 207/28 (2006.01); C07D 263/14 (2006.01); C07D 263/16 (2006.01); C07D 491/04 (2006.01); C07C 233/83 (2006.01)
CPC (source: EP KR)
A61K 31/4015 (2013.01 - KR); A61P 9/10 (2018.01 - EP); A61P 29/00 (2018.01 - EP); A61P 35/00 (2018.01 - EP); A61P 35/04 (2018.01 - EP); A61P 43/00 (2018.01 - EP); C07C 69/675 (2013.01 - EP KR); C07C 231/14 (2013.01 - EP KR); C07C 235/80 (2013.01 - EP KR); C07C 237/06 (2013.01 - EP KR); C07C 247/04 (2013.01 - EP KR); C07D 207/28 (2013.01 - EP KR); C07D 263/16 (2013.01 - EP KR); C07D 491/04 (2013.01 - EP KR); C07B 2200/07 (2013.01 - EP)
C-Set (source: EP)
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9909006 A1 19990225; AU 749857 B2 20020704; AU 8906298 A 19990308; BR 9811304 A 20011113; CA 2301054 A1 19990225; CN 1271342 A 20001025; EP 1021407 A1 20000726; EP 1021407 A4 20010704; HU P0002724 A2 20010228; HU P0002724 A3 20010428; IL 134538 A0 20010430; IL 134538 A 20051120; JP 2001515064 A 20010918; KR 20010022950 A 20010326; NZ 503169 A 20011221
DOCDB simple family (application)
US 9816858 W 19980814; AU 8906298 A 19980814; BR 9811304 A 19980814; CA 2301054 A 19980814; CN 98809526 A 19980814; EP 98940885 A 19980814; HU P0002724 A 19980814; IL 13453898 A 19980814; JP 2000509690 A 19980814; KR 20007001558 A 20000215; NZ 50316998 A 19980814