Department of Chemistry, New York University , 100 Washington Square East, New York, New York 10003, United States.
Org Lett. 2017 Oct 6;19(19):5122-5125. doi: 10.1021/acs.orglett.7b02412. Epub 2017 Sep 11.
Herein, the design of a catalyst that combines lessons learned from peptide biosynthesis, enzymes, and organocatalysts is described. The catalyst features a urea scaffold for carbonyl recognition and elements of nucleophilic catalysis. In the presence of 10 mol % of the organocatalyst, the rate of peptide bond formation is accelerated by 10000-fold over the uncatalyzed reaction between Fmoc-amino acid thioesters and amino acid methyl esters.
本文描述了一种催化剂的设计,该催化剂结合了肽生物合成、酶和有机催化剂的经验教训。该催化剂具有用于羰基识别的尿素支架和亲核催化元件。在 10 mol%的有机催化剂存在下,Fmoc-氨基酸硫酯和氨基酸甲酯之间的无催化剂反应的肽键形成速率被加速了 10000 倍。