Palladium-Catalyzed\nRegio- and Diastereoselective\nHydro(hetero)arylation for Rapid Construction of Quaternary Center\nContaining Cyclobutanes

Herein we report a Pd-catalyzed regio- and diastereoselective\nhydro(hetero)arylation\nof inactivated alkylidenecyclobutanes. This protocol provides a rapid\nand atom-economical route to access 3-cyclobutyl (hetero)arenes with\ngood functionalities toleration. With the assistance of the directing\ngroup, nucleophilic attack happened on the bulkier γ-position\nto form the quaternary carbon center. Furthermore, the selected products\nexhibited antitumor bioactivities.

Publication Details

Journal
Figshare
Published
2024-08-19
DOI
https://doi.org/10.1021/acs.orglett.4c02645.s001
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
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article

Palladium-Catalyzed\nRegio- and Diastereoselective\nHydro(hetero)arylation for Rapid Construction of Quaternary Center\nContaining Cyclobutanes

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Catalytic C–H Functionalization Methods
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Palladium-Catalyzed\nRegio- and Diastereoselective\nHydro(hetero)arylation for Rapid Construction of Quaternary Center\nContaining Cyclobutanes

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Abstract

Herein we report a Pd-catalyzed regio- and diastereoselective\nhydro(hetero)arylation\nof inactivated alkylidenecyclobutanes. This protocol provides a rapid\nand atom-economical route to access 3-cyclobutyl (hetero)arenes with\ngood functionalities toleration. With the assistance of the directing\ngroup, nucleophilic attack happened on the bulkier γ-position\nto form the quaternary carbon center. Furthermore, the selected products\nexhibited antitumor bioactivities.

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Catalytic C–H Functionalization Methods
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Palladium-Catalyzed\nRegio- and Diastereoselective\nHydro(hetero)arylation for Rapid Construction of Quaternary Center\nContaining Cyclobutanes · Figshare (2024) | TGRS Research Map | TGRS