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Abstract A copper-catalyzed formal propargylic [3 + 2] cycloaddition between propargylic acetates and 3-(2-tosylhydrazono)propanoates for the synthesis of (E)-β-substituted-β-pyrazolylacrylates has been realized. The reaction showed broad substrate scope and excellent stereoselectivities, thus… Click to show full abstract
Abstract A copper-catalyzed formal propargylic [3 + 2] cycloaddition between propargylic acetates and 3-(2-tosylhydrazono)propanoates for the synthesis of (E)-β-substituted-β-pyrazolylacrylates has been realized. The reaction showed broad substrate scope and excellent stereoselectivities, thus leading to a variety of (E)-β-substituted-β-pyrazolylacrylates in moderate to good yields. The employment of a tridentate diPh-pybox ligand proved to be crucial for the success of the reaction.
Journal Title: Tetrahedron Letters
Year Published: 2020
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