OKAYAMA UNIVERSITY Develops Innovative Macrolactonization Reaction Using Light Energy for Drug Synthesis

New Macrolactonization Reaction Developed Using Light Energy at Okayama University

In a significant breakthrough, researchers at Okayama University have successfully developed a novel macrolactonization reaction that harnesses light energy. This approach is based on generating radicals and utilizes previously underexplored hydroxyaldehydes as starting materials. This innovative reaction method holds promise for enhancing the efficiency of synthesizing macrolactones, which are pivotal in various pharmaceuticals due to their diverse physiological activities.

Importance of Macrolactones

Macrolactones are vital chemical compounds found in many pharmaceuticals owing to their biological functions. However, efficient synthesis methods for these compounds have remained a challenge. Recognizing this need, the research team, comprised of Assistant Professor Kenta Tanaka, graduate students Sakura Kodaki and Haru Ando, and other esteemed faculty members, successfully optimized a new macrolactonization reaction using radical generation through light energy.

Research Methodology

The team's reaction involves the use of LED light coupled with bromination agents to synthesize macrolactones ranging from 7 to 21 membered rings. By adapting the reaction conditions for various substrates, the team overcame difficulties in achieving broad applicability. This not only highlights the versatility of the developed method but also emphasizes its potential in the efficient total synthesis of macrolide-type natural products that exhibit significant physiological effects.

Publication and Future Applications

The findings of this pioneering study were published online on November 14, 2025, in the journal Precision Chemistry. Given the potential for this method to facilitate the total synthesis of diverse biologically active natural products, researchers anticipate that it will accelerate advancements in pharmaceutical development and innovation.

Macrolactonization Reaction Example

Figure: Example of the macrolactonization reaction.

Researchers' Insights

The research team expressed their excitement regarding the success of the new macrolactonization reaction. They acknowledged the challenges faced in optimizing the reaction conditions to apply to various substrates but are thrilled about the diverse macrolactones synthesized through this novel approach. They hope this achievement will support the efficient synthesis of pharmaceuticals and natural products, contributing to health and well-being globally.

Funding and Further Information

This research project received funding from JSPS KAKENHI Grant Number JP25K18038 and was supported by the Wesco Academic Promotion Foundation. For more details about this innovative research, you can access the full press release here.

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In conclusion, Okayama University continues to lead and innovate in various scientific fields while contributing to the realization of the UN’s Sustainable Development Goals. Their proactive approach in research and development is paving the way for a sustainable and innovative future in health and beyond.