Toward Continuous-Flow Synthesis of Biologically Interesting Pyrazole Derivatives
A two-step continuous-flow synthesis of substituted pyrazole derivatives has been developed via the formation of vinylidene keto esters as key intermediates. Heterogeneous Ni2+-montmorillonite was found to be an efficient catalyst for orthoester condensation of 1,3-dicarbonyls under flow conditions. The intermediate reacted with methylhydrazine to afford pyrazole derivatives, for which suitable selection of a solvent played a key role in achieving high yields and excellent regioselectivities of the desired products. An application of this protocol has been demonstrated by the synthesis of a key intermediate for biologically active pyrazoles such as Bixafen. (Figure presented.).
Das, Amrita,Ishitani, Haruro,Kobayashi, Shū
supporting information
p. 5127 - 5132
(2019/11/13)
CONDENSATION OF IODO-N-METHYLPYRAZOLE-4-CARBOXYLIC ACIDS WITH COPPER ACETYLIDES
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Vasilevskii, S. F.,Gerasimov, V. A.,Shvartsberg, M. S.
p. 683 - 685
(2007/10/02)
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