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Synthesis of protected α-amino acids via decarboxylation amination from malonate derivatives

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Abstract

A general and efficient strategy for the synthesis of protected α-amino acids is reported. The method uses malonate derivatives as the starting materials and Cs2CO3 as a base at 60 degrees, giving α-amino acid derivatives in moderate yields by releasing CO2. This methodology shows broad substrate scope (primary and secondary acids), excellent functional group tolerance and high efficiency to give the desired products under mild reaction conditions. It also allows the construction of β and γ-amino acids and other unnatural products.

Graphical abstract: Synthesis of protected α-amino acids via decarboxylation amination from malonate derivatives

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Article information


Submitted
31 Mar 2020
Accepted
13 May 2020
First published
13 May 2020

Org. Biomol. Chem., 2020, Advance Article
Article type
Paper

Synthesis of protected α-amino acids via decarboxylation amination from malonate derivatives

H. Fu, P. Li, Z. Wang, X. Li, Q. Dai and C. Hu, Org. Biomol. Chem., 2020, Advance Article , DOI: 10.1039/D0OB00677G

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