A convergent approach for the synthesis of C14-C26 fragment of anti-cancer drug eribulin mesylate

Abstract

The stereoselective synthesis of C14-C26 fragment of eribulin is reported in a convergent way by coupling of fragment C14-C19 with fragment C20-C26 that are accessible from commercially available raw materials crotonic acid and 1,4-butanediol. The key steps involved in this practical approach are Hosomi-Sakurai asymmetric alkylation, Maruoka allylation, Noyori reduction, silver catalyzed one pot rearrangement and intramolecular cyclization