Modern synthetic pathways towards eribulin and its subunits

• Sebastian Dominik Graf

Beilstein J. Org. Chem. 2026, 22, 495–526, doi:10.3762/bjoc.22.37

• Sebastian Dominik Graf Gertraud-Kaltenecker Straße 24, D-93049 Regensburg, Germany 10.3762/bjoc.22.37 Abstract Eribulin is a synthetic analog of halichondrin B, a natural product derived from marine sponges, and has gained significant importance in oncology (as its commercial mesylate salt

• approaches is rigorously ongoing. Recent procedures mainly focus on more efficient and scalable techniques for the assembly of the 4 key fragments of eribulin. But also new pathways for the total synthesis have emerged in the last decade. In this review the latest advancements towards the construction of

• eribulin are summarized. Keywords: breast cancer; drug manufacturing; eribulin; Halaven; total synthesis; Introduction Eribulin (1) is a truncated derivative of halichondrin B (2), a complex natural product originally isolated from the marine sponge Halichondria okadai (Figure 1) [1][2][3][4][5]. Already

Synthetic study toward the diterpenoid aberrarone

• Liang Shi,
• Zhiyu Gao,
• Yiqing Li,
• Yuanhao Dai,
• Yu Liu,
• Lili Shi and
• Hong-Dong Hao

Beilstein J. Org. Chem. 2022, 18, 1625–1628, doi:10.3762/bjoc.18.173

• products have found myriad use in new drug development, exemplified by ET-743 and eribulin [1]. Back in 1990s, Rodriguez and co-workers isolated a rich array of terpenoid natural products from the Caribbean sea whip, Pseudopterogorgia elisabethae with unprecedented carbon skeleton, most of which showed

Chromium(II)-catalyzed enantioselective arylation of ketones

• Gang Wang,
• Shutao Sun,
• Ying Mao,
• Zhiyu Xie and
• Lei Liu

Beilstein J. Org. Chem. 2016, 12, 2771–2775, doi:10.3762/bjoc.12.275

• pharmaceutical study, finally leading to the discovery of the anticancer drug Eribulin [31][32][33][34][35]. However, to our knowledge, the Cr-catalyzed enantioselective arylation of carbonyl compounds has rarely been explored. On the other hand, most of the reactions focused on aldehyde components, while