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A Direct, Early Stage Guanidinylation Protocol for the Synthesis of Complex Aminoguanidine-containing Natural Products
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A simplified and scalable synthesis of artesunate
Armin Presser1, Andrea Feichtinger1, Silke Buzzi1
1Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria.
Monatshefte Fur Chemie
|January 28, 2017
Abstract:
An efficient and economically viable approach for the large-scale conversion of artemisinin into the antimalarial frontline drug artesunate was developed. This advanced synthesis includes an NaBH4-induced reduction, followed by an esterification with succinic anhydride under basic conditions. The entire conversion follows the principles of green chemistry, i.e., application of reusable solvents.

