A two-step metal−halogen exchange and diastereoselective copper-mediated Michael addition onto a complex α,β-unsaturated system has been developed and applied toward the synthesis of bisaryl Nrf2 activators. Optimization of metal−halogen exchange using (n-Bu)<sub>3</sub>MgLi allowed for the preparation of custom aryl-functionalized magnesiate reagents at noncryogenic temperatures. Following transmetalation, these reagents were used in highly diastereoselective Michael addition reactions.

Diastereoselective copper-mediated conjugate addition of functionalized magnesiates for the preparation of bisaryl Nrf2 activators

ACS Fall 2021

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