主催: 日本薬学会化学系薬学部会
We will present a Cu(I)-catalyzed migratory oxidative coupling between nitrones and heterocycles or a methylamine as a new entry of Cross-dehydrogenative coupling (CDC) reaction. The mild conditions allow for broad substrate scope with excellent functional group tolerance and chemoselectivity compared with any previously reported CDCs. Several conversions of the products afforded valuable and densely functionalized unnatural α-amino acid surrogates, which are common in bioactive molecules and important for medicinal chemistry. Radical clock studies suggest that the nucleophilic addition of nitrones to an oxidatively generated carbocation is a key step.