Herein we report a Pd-catalyzed regio- and diastereoselective hydro(hetero)arylation of inactivated alkylidenecyclobutanes. This protocol provides a rapid and atom-economical route to access 3-cyclobutyl (hetero)arenes with good functionalities toleration. With the… Click to show full abstract
Herein we report a Pd-catalyzed regio- and diastereoselective hydro(hetero)arylation of inactivated alkylidenecyclobutanes. This protocol provides a rapid and atom-economical route to access 3-cyclobutyl (hetero)arenes with good functionalities toleration. With the assistance of the directing group, nucleophilic attack happened on the bulkier γ-position to form the quaternary carbon center. Furthermore, the selected products exhibited antitumor bioactivities.
Journal Title: Organic letters
Year Published: 2024
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