Abstract
The reactive intermediate produced in the reaction between alkyl isocyanides and dialkyl acetylenedicarboxylates was trapped by acid N'-(2-oxo-2-phenyl-ethyl)hydrazides in the presence of a catalytic amount of silica sulfuric acid (SiO2-OSO3H2) to yield highly functionalized 2,3-dihydro-1H-pyrazoles in good yields. The reaction is characterized by mild conditions and tolerance to various functional groups such as cyclohexyl, t-butyl isocyanides, and Dimethyl-, diethyl- and di-tert-butyl acetylenedicarboxylates.
Graphical Abstract
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