Due to widespread biological activities of pyrazoles/isoxazoles in medicinal chemistry as well as in agrochemical industry [1], their efficient synthesis remains an ongoing challenge for synthetic chemists. Traditionally, synthesis of 1,2-azoles involves the condensation of a 1,3-dicarbonyl compounds or their equivalents with a hydrazine derivative or hydroxylamine. Our goal has been to introduce alternative paths toward fully substituted azoles via a cascade of addition-ring closure-ring opening.
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