Synthesis of 1, 2-Dithiolane Analogues of Leucine for Potential Use in Peptide Chemistry

1,2-Dithiolanes present several points of interest for both peptide and medicinal chem., yet no chiral a-amino acids contg. this five-membered heterocyclic system are available. The authors report here the first synthesis of N- and C-protected deriv. of (S)-2-amino-3-(1,2-dithiolan-4- yl)propionic acid I (Boc-Adp-OBu-t) and its 1,3-dithiolic deriv. II. Dipeptide Cbz-Phe-Adp-OBu-t was also synthesized