An efficient TfNH-catalyzed [2 + 2] cycloaddition of ynamides under mild conditions has been developed. Within short reaction times, various ynamides are transformed into the corresponding 3-aminocyclobutenones in good to excellent yields. This is the first example for the metal-free intermolecular [2 + 2] self-cycloaddition of ynamides. Meanwhile, the desired cycloaddition products can be easily transformed into aminonaphthol derivatives.
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| http://dx.doi.org/10.1021/acs.orglett.2c01825 | DOI Listing |
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