Supporting InformationThe supporting information is available free of charge on the ACS Publications website at DOI: Synthetic methods, characterization, crystallographic and computational modeling data.
Chagas disease also know as AmericanT rypanosomiasis (AT) is at ropical parasitic disease endemici nS outh America, is caused by Trypanosoma cruzi,w hichi st ransmitted by the blood-sucking insect vectors called triatomine bugs. Quinoline alkaloids from the root extract of Waltheria indica are known to possess antitrypanosomal activity. Waltherione F, one of those alkaloids, was synthesised in 5steps in 11 %o verall yield. We report here the first X-ray crystallographic confirmation of the structureo fW altherione F 3.Akey step in the sequence utilisedt he Conrad-Limpach synthesis for the formation of the quinolin-4(1H)-oner ing system. Our synthetic strategy was designed to enablet he modification of the 2-and 3-positions of the scaffold, allowing the generation of ad iverse libraryo fa nalogues to support our on-going medicinal chemistry program that is looking for new agents to tackle this devastating disease.
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