In organic synthesis,
multicomponent reactions (MCR) and cascade reactions are frequently used.
Different substituted pyrazoles are accessed using these two synthetic methods.
In the first section, we're interested in learning how to make
aminocyanopyrazoles using a multicomponent process. The current study outlines
a useful protocol for multicomponent reactions (MCRs) involving malononitrile,
an orthoester, and hydrazine derivatives, all of which take place in the
presence of an acid catalyst. The manufacture, isolation, and characterisation
of a series of aminocyanopyrazoles 4 were indeed carried out. Such pyrazoles
reacted with sodium nitrite, secondary amine reagent, and formic
acidpyrazolotriazines 6 and pyrazolopyrimidinones 7 after being exposed to
sodium nitrite. Sulfamoyl chloride was used to convert some of the
aminopyrazoles into the corresponding sulfamides. The human (h) hCA I, II, IX,
and XII isoforms of carbonic anhydrase (CA, EC 4.2.1.1) were tested as
inhibitors of four carbonic anhydrase (CA, EC 4.2.1.1) isoforms. As a result,
many of them revealed that these enzymes were inhibited at low micromolar or
submicromolar concentrations. Low nanomolar CA inhibitors were found in the
matching sulfamides. Acidic hydrolysis of Ugi adducts generated from
-hydrazonocarboxylic acids and amino acetaldehyde dimethyl acetal leads to
fragmentation of aminoacetaldehyde residues and the synthesis of pyrazoles in
the second section. The essential phase of the cascade is proposed to be an
aldol-type reaction of the hydrazone. MCR multicomponent reactions and Ugi
cascade synthesis are efficient and interesting methods for obtaining good to
moderate yields of pyrazoles.
Author(S) Details
Fatma Allouche
Laboratory of Medicinal and Environmental Chemistry, Superior Institute of
Biotechnology of Sfax, University of Sfax, 3018, Sfax, Tunisia.
View Book:- https://stm.bookpi.org/CACS-V6/article/view/4612