AI Article Synopsis
- The study presents a new method for selectively adding (hetero)aryl groups to inactivated alkylidenecyclobutanes using a palladium catalyst.
- This process allows for the efficient synthesis of 3-cyclobutyl (hetero)arenes while accommodating various functional groups.
- The resulting compounds show potential anti-tumor activity, highlighting their significance in medicinal chemistry.
Article 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.
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| http://dx.doi.org/10.1021/acs.orglett.4c02645 | DOI Listing |
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