Pyrazolones are traditionally synthesized by the reaction of -keto
esters with hydrazine and its derivatives. To date, synthesis of
these compounds have been somewhat limited by the available
chemistry. The methods available in literature to synthesize -keto
esters are suffers by the use of carbon dioxide and carbon monoxide
sources in presence of Pd or transition metal catalysts, long
reaction time, use of excess reagent, inconsistent yield, large
quantity of by products (due to self Claisen condensation) and
require tedious work up procedures to remove the same.
Unfortunately the existing methods not produced the -ketoesters of
heteroaryl compounds from the heteroaryl esters in good yield.
These factors lead us to develop a simple, convenient method to
synthesize -keto esters which in turn converted into their
corresponding pyrazoles. The synthesis of -oxy/thio substituted
-keto esters through cross-Claisen condensation which suffers by
many draw-backs, also been improved by new methodology. The newly
synthesized compounds were subjected to screen their biological
activities and the results discussed."
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