Palladium(II)‐Catalyzed Enantioselective Aminotrifluoromethoxylation of Unactivated Alkenes using CsOCF3 as a Trifluoromethoxide Source

Pd^II‐catalyzed enantioselective intramolecular aminotrifluoromethoxylation of unactivated alkenes using readily accessible and stable CsOCF₃ as a trifluoromethoxide source has been developed, which affords a wide variety of enantiomerically enriched β‐substituted OCF₃‐containing piperidines in good yields. Introducing a sterically bulky group into pyridine‐oxazoline (Pyox) ligands is crucial to increasing both reactivity and enantioselectivity.

Abstract

Asymmetric Pd^II‐catalyzed intramolecular aminotrifluoromethoxylation of unactivated alkenes using readily accessible and stable CsOCF₃ as a trifluoromethoxide source has been developed, which affords a wide variety of enantiomerically enriched β‐substituted OCF₃‐containing piperidines in good yields. Introducing a sterically bulky group into pyridine‐oxazoline (Pyox) ligands is crucial to increasing both reactivity and enantioselectivity for the reaction. Additionally, the reaction features good functional group compatibility and mild reaction conditions.

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