POLYMERIC 2‐MERCAPTOPYRIDINE AND 2‐MERCAPTO‐NITROBENZENE DERIVATIVES: New Reagents for Peptide Synthesis

Authors:
Publisher website
Google Scholar
Abstract
Insoluble 2‐mercaptopyridine and 2‐mercapto‐nitrobenzene derivatives were prepared by modification of commercially available polystyrene. Applicability of these polymers as reagents for the thiolytic removal of the 2‐nitrophenyl‐sulphenyl amino‐protecting group and as supports for preparation of polymeric active esters was evaluated. Polymeric 2‐mercaptopyridine (PMP) was found efficient for both purposes. It was used in the stepwise synthesis of Leu‐enkephalin via the polymeric reagent approach, serving as an Nps‐cleaver. Polymeric esters derived from PMP and Boc‐amino acids proved to be excellent acylators. Their usefulness is exemplified in the preparation of two dipeptides, which were produced rapidly and in high yields and purity.

This publication has 16 references indexed in Scilit: