Atroposelective Synthesis of Biheteroaryl Isoquinolines via Palladium Catalysis

Keywords

palladium - Larock reaction - atroposelective - isoquinolines

Significance

Luo, Ye and co-workers report an axially chiral synthesis of isoquinolines via an asymmetric Larock reaction. The reaction is amenable to a wide range of functionalities in yields up to 99 % and high enantioselectivities. The products of the reaction could be easily derivatized to a series of biologically relevant scaffolds.

 

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Comment

The reported reaction yields diverse axially chiral isoquinolines. The high enantioselectivity is reliant on ortho-substituents and diminished results are observed in their absence. The authors also rule out an oxidative addition, C–H activation pathway, suggesting that nucleopalladation is the dominant pathway.

 

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Publication History

Article published online:
21 November 2024