Scalable synthesis of the C14–C23 fragment of Eribulin and Halichondrin B

Abstract

AbstractA novel, scalable approach to the C14–C23 fragment of eribulin mesylate is disclosed. Key 2,3‐Wittig rearrangement is strategically effected via [Rh] mediated decomposition of 1,2,3‐triazole intermediate to derive the 2,5‐trans‐tetrahydrofuran motif, enabling multi‐kilogram access to the desired C14–C23 fragment.