Asymmetric Phase-Transfer Catalytic Alkylation of Imidazoline-4-carboxylates

Significance

α,β-Diamino acids are attractive synthetic targets due to their various biological ­activities. Most of the reported methods for their asymmetric syntheses involve the use of chiral substrates or chiral auxiliaries, which may limit their applications in large-scale industrial productions. The authors report herein a highly efficient and enantioselective method for the synthesis of (S)-α-alkyl-α,β-diaminopropionic acid 4 via asymmetric phase-transfer catalytic (PTC) α-alkylation of imidazoline-4-carboxylates 1.