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Beilstein J. Org. Chem. 2018, 14, 583–592, doi:10.3762/bjoc.14.45
Graphical Abstract
Figure 1: Commercially available antimalarial drugs.
Scheme 1: Current batch syntheses of the key intermediate 5-(ethyl(2-hydroxyethyl)amino)pentan-2-one (6).
Scheme 2: Retrosynthetic strategy to hydroxychloroquine (1).
Scheme 3: Schematic representation for continuous in-line extraction of 10.
Scheme 4: Optimization of the flow process for the synthesis of 12.
Beilstein J. Org. Chem. 2013, 9, 2570–2578, doi:10.3762/bjoc.9.292
Figure 1: The estimated demand of for nevirapine until 2015 [6].
Scheme 1: Commercial building blocks to nevirapine.
Scheme 2: a) Current commercial process to CAPIC and b) newly developed batch synthesis to CAPIC and its brom...
Scheme 3: Proposed synthesis to 2-bromo-4-methylnicotinonitrile using a continuous approach with the consider...
Figure 2: a) Flow scheme to produce the enamine intermediate 5 from isopropylidenemalononitrile (4) (see Supporting Information File 1 for...
Scheme 4: Flow scheme to produce the enamine 5 starting from acetone and malononitrile (See Supporting Information File 1 for details).
Figure 3: Comparing the long-term stability of the Al2O3 and 3 Å MS columns when the Al2O3 column temperature...
Scheme 5: Several byproducts were observed when producing 5 starting from acetone and malononitrile. 7 is for...
Scheme 6: Flow scheme to produce 2-bromo-4-methylnicotinonitrile (6b) in 81% yield from 4 with a 1 M concentr...
Scheme 7: Reactor scheme for the continuous synthesis of 2-bromo-4-methylnicotinonitrile (6b) with an average...