Department of Chemistry, University of Texas , 1 University Station A1590, Austin, Texas 78712, United States.
Org Lett. 2017 Apr 7;19(7):1654-1657. doi: 10.1021/acs.orglett.7b00451. Epub 2017 Mar 10.
Macrocyclic peptides are an increasingly important class of biopharmaceuticals. A new method of macrocyclization is reported that involves reaction of the N-terminal amine and thiol side chain of cysteine with a Meldrum's acid derived conjugate acceptor. This reaction, which utilizes naturally occurring amino acids and requires no orthogonal protection of side chains, can also be reversed to yield the original linear peptide as desired.
大环肽是一类日益重要的生物制药。本文报道了一种新的大环化方法，涉及 N-末端胺和半胱氨酸的巯基侧链与梅尔杜姆酸衍生的共轭接受体的反应。该反应利用天然存在的氨基酸，并且不需要侧链的正交保护，也可以根据需要反转生成原始的线性肽。
