Visible-light-promoted direct desulfurization of glycosyl thiols to access C-glycosides

Abstract C-Glycosides are essential for the study of biological processes and the development of carbohydrate-based drugs. Despite the tremendous hurdles, glycochemists have often fantasized about the efficient, highly stereoselective synthesis of C-glycosides with the shortest steps under mild cond...

Full description

Saved in:
Bibliographic Details
Main Authors: Demeng Xie, Wei Zeng, Jian Yang, Xiaofeng Ma
Format: Article
Language:English
Published: Nature Portfolio 2024-10-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-024-53563-0
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850204005696798720
author Demeng Xie
Wei Zeng
Jian Yang
Xiaofeng Ma
author_facet Demeng Xie
Wei Zeng
Jian Yang
Xiaofeng Ma
author_sort Demeng Xie
collection DOAJ
description Abstract C-Glycosides are essential for the study of biological processes and the development of carbohydrate-based drugs. Despite the tremendous hurdles, glycochemists have often fantasized about the efficient, highly stereoselective synthesis of C-glycosides with the shortest steps under mild conditions. Herein, we report a desulfurative radical protocol to synthesize C-alkyl glycosides and coumarin C-glycosides under visible-light induced conditions without the need of an extra photocatalyst, in which stable and readily available glycosyl thiols that could be readily obtained from native sugars are activated in situ by pentafluoropyridine. The benefits of this procedure include high stereoselectivity, broad substrate scope, and easy handling. Mechanistic studies indicate that the in situ produced tetrafluoropyridyl S-glycosides form key electron donor–acceptor (EDA) complexes with Hantzsch ester (for C-alkyl glycosides) or Et3N (for coumarin C-glycosides), which, upon irradiation with visible light, trigger a cascade of glycosyl radical processes to access C-glycosides smoothly.
format Article
id doaj-art-a648cbc5e8ee453599076151d4c4190e
institution OA Journals
issn 2041-1723
language English
publishDate 2024-10-01
publisher Nature Portfolio
record_format Article
series Nature Communications
spelling doaj-art-a648cbc5e8ee453599076151d4c4190e2025-08-20T02:11:22ZengNature PortfolioNature Communications2041-17232024-10-0115111010.1038/s41467-024-53563-0Visible-light-promoted direct desulfurization of glycosyl thiols to access C-glycosidesDemeng Xie0Wei Zeng1Jian Yang2Xiaofeng Ma3Natural Products Research Center, Chengdu Institute of Biology, Chinese Academy of SciencesNatural Products Research Center, Chengdu Institute of Biology, Chinese Academy of SciencesNatural Products Research Center, Chengdu Institute of Biology, Chinese Academy of SciencesNatural Products Research Center, Chengdu Institute of Biology, Chinese Academy of SciencesAbstract C-Glycosides are essential for the study of biological processes and the development of carbohydrate-based drugs. Despite the tremendous hurdles, glycochemists have often fantasized about the efficient, highly stereoselective synthesis of C-glycosides with the shortest steps under mild conditions. Herein, we report a desulfurative radical protocol to synthesize C-alkyl glycosides and coumarin C-glycosides under visible-light induced conditions without the need of an extra photocatalyst, in which stable and readily available glycosyl thiols that could be readily obtained from native sugars are activated in situ by pentafluoropyridine. The benefits of this procedure include high stereoselectivity, broad substrate scope, and easy handling. Mechanistic studies indicate that the in situ produced tetrafluoropyridyl S-glycosides form key electron donor–acceptor (EDA) complexes with Hantzsch ester (for C-alkyl glycosides) or Et3N (for coumarin C-glycosides), which, upon irradiation with visible light, trigger a cascade of glycosyl radical processes to access C-glycosides smoothly.https://doi.org/10.1038/s41467-024-53563-0
spellingShingle Demeng Xie
Wei Zeng
Jian Yang
Xiaofeng Ma
Visible-light-promoted direct desulfurization of glycosyl thiols to access C-glycosides
Nature Communications
title Visible-light-promoted direct desulfurization of glycosyl thiols to access C-glycosides
title_full Visible-light-promoted direct desulfurization of glycosyl thiols to access C-glycosides
title_fullStr Visible-light-promoted direct desulfurization of glycosyl thiols to access C-glycosides
title_full_unstemmed Visible-light-promoted direct desulfurization of glycosyl thiols to access C-glycosides
title_short Visible-light-promoted direct desulfurization of glycosyl thiols to access C-glycosides
title_sort visible light promoted direct desulfurization of glycosyl thiols to access c glycosides
url https://doi.org/10.1038/s41467-024-53563-0
work_keys_str_mv AT demengxie visiblelightpromoteddirectdesulfurizationofglycosylthiolstoaccesscglycosides
AT weizeng visiblelightpromoteddirectdesulfurizationofglycosylthiolstoaccesscglycosides
AT jianyang visiblelightpromoteddirectdesulfurizationofglycosylthiolstoaccesscglycosides
AT xiaofengma visiblelightpromoteddirectdesulfurizationofglycosylthiolstoaccesscglycosides