Tetrahedron Letters p. 1736 - 1740 (2019)
Update date:2022-08-11
Topics:
Huang, Guang
Solano, Claribel Murillo
Su, Yuxin
Ezzat, Nameer
Matsui, Shino
Huang, Liuyu
Chakrabarti, Debopam
Yuan, Yu
A rapid and efficient synthesis of 2-vinylquinolines via trifluoromethanesulfonamide-mediated olefination of 2-methylquinoline and aldehyde under microwave irradiation is reported. Biological evaluation of these scaffolds demonstrates that 2-vinylquinolines 3x-3z possess excellent antimalarial activities against chloroquine-resistant Dd2 strain of Plasmodium falciparum (IC50 < 100 nM).
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