Modern synthetic pathways towards eribulin and its subunits

Area of Science:

• Organic Chemistry
• Medicinal Chemistry
• Oncology

Background:

• Eribulin is a synthetic analog of halichondrin B, a marine natural product.
• It functions as a microtubule dynamics inhibitor, a key mechanism in cancer therapy.
• Eribulin mesylate (Halaven) is approved for metastatic breast cancer and liposarcoma.

Purpose of the Study:

• To review recent advancements in the total synthesis of eribulin.
• To highlight new and efficient synthetic strategies for eribulin assembly.
• To address the ongoing research driven by increasing clinical demand.

Main Methods:

• Focus on recent synthetic procedures for eribulin construction.
• Emphasis on efficient and scalable techniques for assembling key fragments.
• Exploration of novel pathways for total synthesis.

Main Results:

• Summarization of the latest advancements in eribulin synthesis.
• Identification of improved methods for assembling the four key fragments.
• Emergence of new total synthesis pathways in the last decade.

Conclusions:

• Continued innovation in eribulin synthesis is vital for clinical supply.
• Efficient and scalable synthetic routes are crucial for meeting demand.
• Recent synthetic strategies offer promising avenues for eribulin production.