Presentation is loading. Please wait.

Presentation is loading. Please wait.

Fig. 1 Reaction rate, efficiency, and substrate scope of the thiol-to-amine macrocyclization reaction. Reaction rate, efficiency, and substrate scope of.

Similar presentations


Presentation on theme: "Fig. 1 Reaction rate, efficiency, and substrate scope of the thiol-to-amine macrocyclization reaction. Reaction rate, efficiency, and substrate scope of."— Presentation transcript:

1 Fig. 1 Reaction rate, efficiency, and substrate scope of the thiol-to-amine macrocyclization reaction. Reaction rate, efficiency, and substrate scope of the thiol-to-amine macrocyclization reaction. (A) Sample reaction of the dipeptide Gly-Cys and bis-electrophile linker 1. The higher thiol reactivity compared to amines enables stepwise reaction in the indicated order, forming a macrocycle as the main product with few side products. (B) Several bis-electrophiles efficiently cyclized the Gly-Cys substrate, adding between three and seven atoms to the macrocyclic backbone. (C to E) The substrate scope was assessed by quantifying the percent of linear substrate converted into the desired macrocycle. The N-terminal amino acid (C), the Cys side-chain length (D), and the number of amino acids were varied (E). R = Gly-Gly-Trp. S. S. Kale et al. Sci Adv 2019;5:eaaw2851 Copyright © 2019 The Authors, some rights reserved; exclusive licensee American Association for the Advancement of Science. No claim to original U.S. Government Works. Distributed under a Creative Commons Attribution NonCommercial License 4.0 (CC BY-NC).


Download ppt "Fig. 1 Reaction rate, efficiency, and substrate scope of the thiol-to-amine macrocyclization reaction. Reaction rate, efficiency, and substrate scope of."

Similar presentations


Ads by Google