A sustainable, efficient, and potentially cost-effective approach to the antimalarial drug candidate MMV688533

Autor:	Rahul D. Kavthe, Karthik S. Iyer, Juan C. Caravez, Bruce H. Lipshutz
Rok vydání:	2023
Předmět:	Orphan Drug Infectious Diseases Rare Diseases Chemical Sciences General Chemistry
Zdroj:	Chemical science, vol 14, iss 23
ISSN:	2041-6539 2041-6520
DOI:	10.1039/d3sc01699d
Popis:	A 6-step synthesis of the antimalarial drug candidate MMV688533 is reported. Key transformations carried out under aqueous micellar conditions include two Sonogashira couplings and amide bond formation. Compared with the first-generation manufacturing process reported by Sanofi, the current route featuresppm levels of palladium loading, less material input, less organic solvent, and no traditional amide coupling reagents. The overall yield is improved ten-fold, from 6.4% to 67%.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9ab3bc2a2234cc0bdabdf287795062b https://doi.org/10.1039/d3sc01699d Zobrazit plný text záznamu