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Total Synthesis of Paliurine E by a Highly Convergent Block Approach
Jianjun Wang1,2, Damien F Dewez1, Gwilherm Evano1,3
1Laboratoire de Chimie Organique, Service de Chimie et PhysicoChimie Organiques, Université libre De Bruxelles (ULB), Brussels, Belgium.
Chemistry (Weinheim an Der Bergstrasse, Germany)
|August 13, 2026
Summary
This study introduces a novel "block" strategy for synthesizing macrocycles, enabling direct, convergent assembly of unprotected building blocks. This efficient method simplifies the creation of complex macrocyclic structures, including natural products.
Area of Science:
- Organic Chemistry
- Synthetic Chemistry
- Medicinal Chemistry
Background:
- Macrocycles are crucial in chemistry, biology, and medicine, but their synthesis is challenging.
- Existing methods like linear assembly and fragment coupling are inefficient and limit structural diversity.
- Protecting groups and symmetry restrictions further complicate current macrocycle construction.
Purpose of the Study:
- To develop a general and efficient synthetic strategy for macrocycles.
- To enable the straightforward synthesis of unsymmetrical macrocyclic architectures.
- To minimize step count and optimize time economy in macrocycle synthesis.
Main Methods:
- A new conceptual framework based on direct, convergent assembly of two different bifunctional, unprotected building blocks.
- Implementation of a "block" strategy to circumvent protecting-group manipulations.
- Demonstration of viability despite challenges like oligomerization and regioselectivity.
Main Results:
- Successful development of a direct, convergent macrocycle synthesis strategy.
- The "block" strategy provides the most straightforward entry to unsymmetrical macrocyclic architectures.
- Achieved an unusually concise total synthesis of the macrocyclic natural product paliurine E, showcasing efficiency.
Conclusions:
- The novel "block" strategy offers a significant advancement in macrocycle synthesis.
- This approach enhances efficiency, convergence, and structural diversity in creating macrocyclic compounds.
- The method holds promise for broader exploitation of macrocycles in various scientific fields.
