Arzneimittelforschung 2007; 57(3): 155-163
DOI: 10.1055/s-0031-1296599
poAntibiotics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

Large-scale Synthesis of GMP Grade α-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl) propenamide (LFM-A13), a New Anti-cancer Drug Candidate

Darin DuMez
1   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
,
Taracad K. Venkatachalam
1   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
,
Fatih M. Uckun
1   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
› Author Affiliations
Further Information

Publication History

Publication Date:
21 December 2011 (online)

Abstract

The leflunomide (CAS 75706-12-6) metabolite (LFM) analog α-cyano-β-hydro-xy-β-methyl-N- (2,5-dibromophenyl) -propenamide (LFM-A13, DDE-28, CAS 244240-24-2), is a rationally designed inhibitor of the anti-apoptotic enzyme Bruton's tyrosine kinase (BTK). LFM-A13 is being developed as a novel dual-function anti-cancer drug with apoptosis-promoting and anti-thrombotic properties. LFM-A13 was prepared under current Good Manufacturing Practice (cGMP) conditions on the scale of kilograms.