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Enantioselective Construction of Tertiary α‑Alkyl Fluoride via BTM-Catalyzed Fluorination of α‑Alkynyl-Substituted Acetic Acids

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journal contribution
posted on 20.12.2021, 11:43 authored by Shiru Yuan, Wen-Hua Zheng
The isothiourea-catalyzed enantioselective construction of tertiary α-fluoro stereogenic centers has been demonstrated by using branched alkynyl-substituted acetic acids as starting materials, providing a broad range of optically active tertiary α-alkyl fluorides in high enantioselectivity (up to 97% ee). Furthermore, this methodology was proven to be scaled up to a Gram scale without loss of enantioselectivity.