Copper-Catalyzed Direct C(sp3)-H Alkoxylation to Access Quaternary α-Alkoxylated Amino Acid Derivatives. 2020

Qiang Wei, and Yao Ma, and Yi Dong, and Gang Liu
School of Pharmaceutical Sciences, Tsinghua University, Beijing 100084, China.

A copper-catalyzed C(sp3)-H alkoxylation was developed to prepare quaternary α-alkoxylated amino acid derivatives in good yields. This protocol can be applied to a series of α-amino acids bearing a variety of functional group substituents. Facile removal of the auxiliary directing group and tolerance of condensation conditions for amide bond formation enable the potential application of this method in the discovery of new peptide drugs in the future.

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