Fragment synthesis of disulfide-containing peptides

Yuxuan Dai,Na Yue,Wenlong Huang,Hai Qian

doi:10.1016/j.mex.2020.100945

Abstract

A new strategy for solid phase peptide synthesis in the fragment synthesis based on the use of 2-Cl-trityl resin as carrier to obtain protected peptide-resin and Rink Amide Resin, HOBT/HBTU or PyBOP/DIPEA or HATU/DIPEA as the coupling method is described. The highlights of this method are:•Simple.•Low cost.•Solid phase based.

Highlights

A Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China b Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China abstractA new strategy for solid phase peptide synthesis in the fragment synthesis based on the use of 2-Cl-trityl resin as carrier to obtain protected peptide-resin and Rink Amide Resin, HOBT/HBTU or PyBOP/diisopropylethyl amine (DIPEA) or HATU/DIPEA as the coupling method is described
Peptide synthesis is a process of repeating the addition of amino acids[1]
We introduced a fragment synthesis method of target conjugate (Fig. 1)

Summary

Method Article

A Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China b Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China abstractA new strategy for solid phase peptide synthesis in the fragment synthesis based on the use of 2-Cl-trityl resin as carrier to obtain protected peptide-resin and Rink Amide Resin, HOBT/HBTU or PyBOP/DIPEA or HATU/DIPEA as the coupling method is described. Unless otherwise indicated, were obtained from Sigma-Aldrich Co. (Saint Louis, MO)

Method overview

Method description