Global Patent Index - EP 1021407 A1

EP 1021407 A1 2000-07-26 - 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

EP 1021407 A1 (EN)

Application

EP 98940885 A

Priority

  • US 9816858 W
  • US 5584897 P
  • US 91211197 A
  • US 6735297 P

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 (main, further and additional classification)

C07D 207/46; C07D 263/14

IPC 8 full level (invention and additional information)

C07D 207/46 (2006.01); C07D 491/044 (2006.01); A61K 31/40 (2006.01); A61K 31/4015 (2006.01); A61K 31/407 (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 (invention and additional information)

C07D 263/16 (2013.01); C07C 69/675 (2013.01); C07C 231/14 (2013.01); C07C 235/80 (2013.01); C07C 237/06 (2013.01); C07C 247/04 (2013.01); C07D 207/28 (2013.01); C07D 491/04 (2013.01); C07B 2200/07 (2013.01)

Combination set (CPC)

C07C 231/14 + C07C 233/83

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

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 0002724 A2 20010228; HU 0002724 A3 20010428; IL 134538 A 20051120; IL 134538 D0 20010430; JP 2001515064 A 20010918; NZ 503169 A 20011221