Co-Catalyzed Direct Regio- and Enantioselective Intermolecular γ-Amination of N-Acylpyrazoles

A cobalt-catalyzed regio- and enantioselective gamma-amination of beta,gamma-unsaturated N-acylpyrazoles that delivers the corresponding gamma-amination products in good regio- and enantioselectivity has been established. Moreover, the nitrogen-containing compounds could be easily synthesized. DFT calculations have been provided to explain regio- and enantioselectivity for this gamma-amination. The chiral gamma-amination products were readily converted into the chiral gamma-amino acid derivatives.

Automated summary

The cobalt-catalyzed regio- and enantioselective gamma-amination of beta,gamma-unsaturated N-acylpyrazoles has been achieved, delivering the corresponding products with good regio- and enantioselectivity. DFT calculations were used to explain the selectivity of this gamma-amination, and the chiral products were easily converted into chiral gamma-amino acid derivatives.