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Abstract

Described herein are methods for preparing chiral α-amino acids using chiral phosphoric acids as catalysts. The disclosed methods can use amino-malonic acids as substrates to generate chiral amino acids with a variety of side chains in high optional purity (such as an ee value of at least 70%) and with a high yield (i.e., a yield of at least 80%, such as in a range from about 80% to about 99%), via an asymmetric decarboxylation reaction. The decarboxylation reaction of the methods is catalyzed by chiral phosphoric acids that can achieve a selective protonation during decarboxylation, which is considered one of the most difficult processes in asymmetric catalysis.

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First Claim