Abstract:1,3‐Difunctionalized cyclobutanes are an emerging scaffold in medicinal chemistry that can confer beneficial pharmacological properties to small‐molecule drug candidates. However, the diastereocontrolled synthesis of these compounds typically requires complicated synthetic routes, indicating a need for novel methods. Here, we report a sequential C−H/C−C functionalization strategy for the stereospecific synthesis of cis‐γ‐functionalized cyclobutyl ketones from readily available cyclobutyl aryl ketones. Specific… Show more
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