A Scalable Total Synthesis of Halofuginone

A scalable total synthesis of halofuginone has been accomplished. This synthetic route features a total of 12 steps of highly efficient reactions, without any chromatographic purification. Halofuginone was obtained in 17% overall yield and over 98.5% HPLC purity. All the reaction conditions are mild and reliable. In addition, no hazardous materials are used or produced. All reagents are commercially available and inexpensive. This route is safe, robust, scalable, cost-effective, and environmentally benign.