Nickel-catalyzed
asymmetric annulation of oxygenated phenols and
previously challenging 3-aminophenols with β,γ-unsaturated
α-ketoesters is described, leading to rapid access to a variety
of oxygenated and 7-aminated chromans in excellent yields with excellent
diastereoselectivities and enantioselectivities under mild conditions.
This method was readily scaled-up to gram scale and applied for a
concise synthesis of two potential anticancer agents 7-aminated 4-arylchromans