Beilstein J. Org. Chem.2020,16, 1203–1224, doi:10.3762/bjoc.16.105
activity, with IC50 value for the xL3 motility improved to 0.38 µM and for the L4 development to 0.7 nM, with a similar activity for the corresponding fluoropyrazole derivative 24. These latter two compounds 23 and 24 showed high selectivity for the parasite, with low or no cytotoxicity. The authors went
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Graphical Abstract
Figure 1:
Structures of some current front-line anthelmintics discussed in this review. *Denotes the stereoge...
Beilstein J. Org. Chem.2011,7, 1048–1054, doi:10.3762/bjoc.7.120
Research & Development, Ramsgate Road, Sandwich, Kent, CT13 9NJ, UK 10.3762/bjoc.7.120 Abstract 4-Fluoropyrazole systems may be prepared by a single, sequential telescoped two-step continuous gas/liquid–liquid/liquid flow process from diketone, fluorine gas and hydrazine starting materials.
Keywords
: continuous flow reactions; fluorine; fluoropyrazole; gas-liquid flow reactor; selective direct fluorination; Introduction
Organic systems which bear fluorine atoms are used in an ever widening range of applications in the life sciences. Many commercially significant pharmaceutical and agrochemical products
-diketones and hydrazines [23].
However, the synthetic methodology for the preparation of the corresponding fluoropyrazole derivatives has not been developed to any great extent despite the potential use of such systems in life science applications. Recently, we explored direct fluorination of various
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Graphical Abstract
Figure 1:
Sequential gas/liquid–liquid/liquid flow reactor for the synthesis of 4-fluoropyrazole derivatives.