Organocatalytic, enantioselective synthesis of VNI: a robust therapeutic development platform for Chagas, a neglected tropical disease

VNI is a potent inhibitor of CYP51 and was recently shown to achieve a parasitological cure of mice infected with T. cruzi in both acute and chronic stages of Infection. T. cruzi is the causative Parasite of Chagas disease, a neglected tropical disease. The first enantioselective chemical synthesis of VNI (at a Materials cost of less than $0.10/mg) is described. Furthermore, the key enantioselective step is performed at the 10 g scale.