Asymmetric synthesis of 3,4,5,6-tetrasubstituted piperidin-2-ones by three-component coupling
Davies SG., Smith AD., Cowley AR.
The asymmetric three-component coupling of α,β-unsaturated esters and alkylidene malonates initiated with a homochiral lithium amide proceeds with high levels of diastereoselectivity, with hydrogenation of the resultant α-substituted β-amino acid derivatives giving a range of differentially protected 3,4,5,6-tetrasubstituted piperidinones with four contiguous stereogenic centres.