NDTP 介导的直接快速酰胺和肽合成，无差向异构化。

NDTP Mediated Direct Rapid Amide and Peptide Synthesis without Epimerization.

机构信息

Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences & Research Unit of Peptide Science, Chinese Academy of Medical Sciences, 2019RU066, Lanzhou University, 199 West Donggang Rd, Lanzhou 730000, Gansu, P. R. China.

Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, P. R. China.

出版信息

Org Lett. 2022 Feb 11;24(5):1169-1174. doi: 10.1021/acs.orglett.1c04258. Epub 2022 Jan 7.

DOI:10.1021/acs.orglett.1c04258

PMID:34994572

Abstract

Herein, we explored an unprecedented mild, nonirritating, conveniently available, and recyclable coupling reagent , which could activate the carboxylic acids via acyl thiocyanide and enable the rapid amide and peptide synthesis at very mild conditions. In addition, the methodology was compatible with Fmoc-SPPS, which may provide an alternative to peptide manufacturing.

摘要

在此，我们探索了一种前所未有的温和、无刺激性、方便易得且可回收的偶联试剂，它可以通过硫氰酸酯酰基激活羧酸，使酰胺和肽在非常温和的条件下快速合成。此外，该方法与 Fmoc-SPPS 兼容，可为肽生产提供替代方案。