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Synthesis 2024; 56(03): 462-468
DOI: 10.1055/a-2202-5597
DOI: 10.1055/a-2202-5597
paper
A Convergent Approach for the Synthesis of C14–C26 Fragment of Anticancer Drug Eribulin Mesylate
The authors thanks CSIR, New Delhi for funding this project under mission INPROTICS.

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.
Supporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/a-2202-5597.
- Supporting Information
Publication History
Received: 01 August 2023
Accepted after revision: 02 November 2023
Accepted Manuscript online:
02 November 2023
Article published online:
29 November 2023
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The diastereomeric mixture was inseparable at this stage and was used further as such.