| abstract |
The invention discloses a method suitable for industrialized preparation of plecanatide. The solid-phase synthesis of plecanatide is carried out by introducing specially protected amino acids and/or protected dipeptides, such as pseudoproline dipeptide and Dmb dipeptide. , Dmb/Hmb/Fmoc‑Hmb/Hnb/Hmsb/Mmsb/Mmtb protected amino acids, etc., solve the problem that the subsequent amino acid coupling becomes more and more difficult when synthesizing plecanatide by conventional solid-phase methods, thereby improving the purity of crude peptides and yield; especially, the above-mentioned protected amino acid is introduced at the position of Ala 11 , the purity and yield can be improved, the yield of crude peptide can reach 95%, and the purity can reach more than 80%. |