Nickel/Copper-Cocatalyzed Asymmetric Benzylation of Aldimine Esters for the Enantioselective Synthesis of α-Quaternary Amino Acids,Angewandte Chemie International Edition

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Nickel/Copper-Cocatalyzed Asymmetric Benzylation of Aldimine Esters for the Enantioselective Synthesis of α-Quaternary Amino Acids
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2022-03-23 , DOI: 10.1002/anie.202203448
Youbin Peng ₁ , Chongyu Han ₁ , Yicong Luo ₁ , Guanlin Li ₁ , Xiaohong Huo ₁ , Wanbin Zhang _{1,

2}

Affiliation

The first Ni/Cu cocatalyzed asymmetric benzylation of aldimine esters has been developed. DFT calculations revealed that the strong electrophilicity of the η³-benzylnickel intermediate enabled the reaction to proceed smoothly under base-free conditions. The method was applied to the synthesis of BIRT-377 analogues, the key intermediate of PD154075 and CI-988.

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