In 2010 malaria caused an estimated 665,000 deaths, mostly among African children. Now, chemists at Indiana University have developed a new synthesis for the world's most useful antimalarial drug, artemisinin, giving hope that fully synthetic artemisinin might help reduce the cost of the live-saving drug in the future.
Effective deployment of ACT, or artemisinin-based combination therapy, has been slow due to high production costs of artemisinin. The World Health Organization has set a target "per gram" cost for artemisinin of 25 cents or less, but the current cost is about $2.40 per gram, and production of low-cost semi-synthetic artemisinin has yet to materialize.
"In 2005, the WHO claimed that the structure of artemisinin was too complex for cost-effective synthesis," said IU Bloomington College of Arts and Sciences chemistry professor Silas Cook. "We saw this as a natural challenge to the creativity and tenacity of organic chemists."
Published recently in the Journal of the American Chemical Society as "A Concise Synthesis of Artemisinin," Cook and postdoctoral co-author Chunyin Zhu report a succinct five-part process beginning with inexpensive cyclohexenone, an ideal feedstock available on metric-ton scale. Subsequent chemistry highlights several new reactions developed in the Cook group to enable this short, low-cost synthesis.
The result was the production of fully synthetic artemisinin on gram scale, greater than all previous total syntheses combined.