A method for synthesizing the highly potent antimalarial drug artemisinin has been developed by the Southwest Research Institute (SwRI) and the University of Texas at San Antonio (UTSA). This could result in a malaria treatment that is more cost-effective.
The article was recently featured on the cover of Organic Letters.
There were 247 million cases of malaria worldwide in 2021, resulting in 619,000 deaths. Artemisinin, a drug derived from the sweet wormwood plant Artemisia annua, is used in the most effective malaria treatments. However, it takes a long time to isolate artemisinin from the plant, and crop yields are affected by weather, insect pests, and other factors. The most affected nations continue to be burdened by the price of artemisinin, despite scientific advancements in malaria treatment methods.
“We were able to create a novel synthetic method for artemisinin that closely resembles how it occurs in nature,”
Senior Research Scientist Dr. Shawn Blumberg
SwRI Senior Research Scientist Dr. Shawn Blumberg stated, “We were able to develop a novel way of synthesizing artemisinin that mimics how it is made in nature.” Our technique imitates the biosynthetic pathway of how artemisinin is made in the plant where it starts, Artemisia annua. We concentrated on the moderate mixtures along that pathway and afterward utilized science to make those equivalent intermediates and reproduce the pathway.”
Frantz stated, “There was nothing in the public scientific literature suggesting this would work.” We were attempting to accomplish this difficult chemistry, but we let science direct our course. It empowered us to plan a course of taking a typical transitional in the biosynthetic pathway for artemisinin and switching it as far as possible over completely to artemisinic corrosive, which is the immediate antecedent to artemisinin.”
Given the inherent risks of drought, wildfire, and insects that come with relying on a plant that can only grow in certain parts of the world, Blumberg and Frantz hope that pharmaceutical companies will take advantage of their work and offer a malaria treatment that is both more potent and more cost-effective to the impoverished nations that require it the most.
“The inventory of artemisinin is still sort of flighty, which makes costs inconsistent too, and nations managing this endemic need a steady, savvy arrangement,” Blumberg said. “While our new method may not completely replace existing methods, it can complement them and contribute to stabilizing the global supply of artemisinin.”
More information: Nicholas A. Clanton et al, Site-Selective Functionalization of Unactivated Allylic C–H Bonds via Direct Deprotonation with KTMP: Application to the Formal Total Synthesis of (+)-Artemisinin from Amorphadiene, Organic Letters (2023). DOI: 10.1021/acs.orglett.2c04145
