6323-87-1Relevant articles and documents
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Corey,E.J.,Cane,D.E.
, p. 3405 - 3409 (1970)
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Synthesis of novel triazole-linked mefloquine derivatives: Biological evaluation against Plasmodium falciparum
Hamann, Anton R.,De Kock, Carmen,Smith, Peter J.,Van Otterlo, Willem A.L.,Blackie, Margaret A.L.
supporting information, p. 5466 - 5469 (2015/01/08)
Using 2,8-bis(trifluoromethyl)quinoline, the pharmacophore of mefloquine, as scaffold, eleven novel triazole-linked compounds have been synthesised by the application of CuAAC chemistry. The in vitro biological activity of the compounds on the Plasmodium falciparum chloroquine-sensitive strain NF54 was then determined. The compounds all showed IC50s in the lower μM range with (1R,3S,5R)-N-{[1-(2,8-bis(trifluoromethyl)quinoline-4-yl)-1H-1,2,3-triazol-4-yl]methyl}adamantan-2-amine (29) exhibiting the best activity of 1.00 μM.
Synthesis of functional acetylene derivatives from calcium carbide
Lin, Zhewang,Yu, Dingyi,Sum, Yin Ngai,Zhang, Yugen
scheme or table, p. 625 - 628 (2012/06/04)
AHA Erlebnis: CaC2, used to produce acetylene until several decades ago, is re-emerging as a cheap, sustainable resource synthesized from coal and lignocellulosic biomass. We report efficient catalytic protocols for the synthesis of functional acetylene derivatives from CaC2 through aldehyde, alkyne, and amine (AAA) as well as alkyne, haloalkane, and amine (AHA) couplings, and in addition demonstrate its use in click and Sonogashira chemistry, showing that calcium carbide is a sustainable and cost-efficient carbon source.
