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Highly Enantioselective Nickel-Catalyzed Oxa-[3+3]-annulation of Phenols with Benzylidene Pyruvates for Chiral Chromans

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journal contribution
posted on 2018-06-10, 16:13 authored by Hai Ren, Xiang-Yang Song, Sunewang R. Wang, Lijia Wang, Yong Tang
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.