The feasibility of peptide synthesis by four component condensation (4CC) [1] has been demonstrated [2]. In particular the advantages of peptide synthesis by 4CC, namely coupling without carboxyl activation, the possibility of reaction in highly polar media, and the effectively unimolecular nature of the coupling step in such coupling of peptide fragments are being recognized [3]. The unique fe...

Amidation is the predominant reaction within pharmaceutical setting, and it attracting greater attention due to increased demand for therapeutic peptides. The high efficacy safety profile of peptides have placed these molecules in prime position arena, which reflected by receiving several approvals from various regulatory agencies each year. In this context, developing efficient strategies pept...

The design and solid-phase synthesis of tetrahydropyridazine-3,6-dione (Tpd) peptidomimetics derived from backbone-aminated peptides is reported. The described protocol features the synthesis of chiral α-hydrazino acids suitable for chemoselective incorporation into growing peptide chains. Acid-catalyzed cyclization to form the Tpd ring during cleavage affords the target peptidomimetics in good...