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.