An Update on the Total Synthesis of (S)-Quisqualic Acid and Its Derivatives

Abstract (S)-Quisqualic acid and its structural analogues show potent activity across various fields of medicine. The growing interest in this amino acid family creates a pressing need for detailed synthetic procedures. Here, we present a comprehensive synthesis of N-Boc-(S)-quisqualic acid from l-serine with an overall yield of 58% over six steps. Further transformation into the C-protected (S)-quisqualic acid and the unprotected (S)-quisqualic acid HCl salt is also feasible with good yields. The complete characterization (NMR, HRMS, IR) of the intermediates and target molecules allows the reliable utilization of this synthetic work.