Gold(I)-Catalyzed 2-Deoxy-β-glycosylation via 1,2-Alkyl/Arylthio Migration: Synthesis of Velutinoside A Pentasaccharide.

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Main Authors: Wang, Xianyang, Ding, Han, Guo, Aoxin, Song, Xiaofei, Wang, Peng, Song, Ni, Yu, Biao, Xu, Peng, Liu, Xue-Wei, Li, Ming
Format: Artículo científico
Language:en
Published: Journal of the American Chemical Society 2025
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author Wang, Xianyang
Ding, Han
Guo, Aoxin
Song, Xiaofei
Wang, Peng
Song, Ni
Yu, Biao
Xu, Peng
Liu, Xue-Wei
Li, Ming
author_facet Wang, Xianyang
Ding, Han
Guo, Aoxin
Song, Xiaofei
Wang, Peng
Song, Ni
Yu, Biao
Xu, Peng
Liu, Xue-Wei
Li, Ming
Wang, Xianyang
Ding, Han
Guo, Aoxin
Song, Xiaofei
Wang, Peng
Song, Ni
Yu, Biao
Xu, Peng
Liu, Xue-Wei
Li, Ming
collection PubMed - marine biology
contents Gold(I)-Catalyzed 2-Deoxy-β-glycosylation via 1,2-Alkyl/Arylthio Migration: Synthesis of Velutinoside A Pentasaccharide. Wang, Xianyang Ding, Han Guo, Aoxin Song, Xiaofei Wang, Peng Song, Ni Yu, Biao Xu, Peng Liu, Xue-Wei Li, Ming 2-Deoxy-β-glycosides are essential components of natural products and pharmaceuticals; however, the corresponding 2-deoxy-β-glycosidic bonds are challenging to chemically construct. Herein, we describe an efficient catalytic protocol for synthesizing 2-deoxy-β-glycosides via either IPrAuNTf-catalyzed activation of a unique 1,2--positioned C2--propargyl xanthate (OSPX) leaving group or (PhO)PAuNTf-catalyzed activation of a 1,2--C2--alkynylbenzoate (OABz) substituent of the corresponding thioglycosides. These activation processes trigger 1,2-alkyl/arylthio-migration glycosylation, enabling the synthesis of structurally diverse 2-deoxy-β-glycosides under mild reaction conditions. The power of this strategy is demonstrated by the first synthesis of the pentasaccharide chain corresponding to velutinoside A, which features gold(I)-catalyzed construction of four successive β-l-oleandrosidic bonds in both a convergent and a one-pot glycosylation manner. Mechanistic studies, including control experiments and deuterium-labeling experiments, emphasize the crucial role of the OSPX and the involvement of the gold(I)-activated C≡C triple bond during the glycosylation process. The low-temperature NMR experiments unveiled a unique dual-coordination pattern of the gold(I) catalyst to the thiocarbonyl group and the alkynyl group of the OSPX, initiating a 5--dig cyclization process. Furthermore, density functional theory (DFT) simulations reveal the ligand-induced match-mismatch effect between leaving groups OSPX and OABz and gold catalysts IPrAuNTf and (PhO)PAuNTf. The DFT simulations also suggest that the formation of 2-deoxy-β-glycosidic bonds occurs via the bottom-face attack of the acceptor to the oxocarbenium intermediate, which adopts a half-chair conformation, leading to an energetically favored, -conformed intermediate that is stabilized by a hydrogen bonding interaction.
format Artículo científico
id pubmed_39869845
institution PubMed
language en
publishDate 2025
publisher Journal of the American Chemical Society
record_format pubmed
spellingShingle Gold(I)-Catalyzed 2-Deoxy-β-glycosylation via 1,2-Alkyl/Arylthio Migration: Synthesis of Velutinoside A Pentasaccharide.
Wang, Xianyang
Ding, Han
Guo, Aoxin
Song, Xiaofei
Wang, Peng
Song, Ni
Yu, Biao
Xu, Peng
Liu, Xue-Wei
Li, Ming
Gold(I)-Catalyzed 2-Deoxy-β-glycosylation via 1,2-Alkyl/Arylthio Migration: Synthesis of Velutinoside A Pentasaccharide. Wang, Xianyang Ding, Han Guo, Aoxin Song, Xiaofei Wang, Peng Song, Ni Yu, Biao Xu, Peng Liu, Xue-Wei Li, Ming 2-Deoxy-β-glycosides are essential components of natural products and pharmaceuticals; however, the corresponding 2-deoxy-β-glycosidic bonds are challenging to chemically construct. Herein, we describe an efficient catalytic protocol for synthesizing 2-deoxy-β-glycosides via either IPrAuNTf-catalyzed activation of a unique 1,2--positioned C2--propargyl xanthate (OSPX) leaving group or (PhO)PAuNTf-catalyzed activation of a 1,2--C2--alkynylbenzoate (OABz) substituent of the corresponding thioglycosides. These activation processes trigger 1,2-alkyl/arylthio-migration glycosylation, enabling the synthesis of structurally diverse 2-deoxy-β-glycosides under mild reaction conditions. The power of this strategy is demonstrated by the first synthesis of the pentasaccharide chain corresponding to velutinoside A, which features gold(I)-catalyzed construction of four successive β-l-oleandrosidic bonds in both a convergent and a one-pot glycosylation manner. Mechanistic studies, including control experiments and deuterium-labeling experiments, emphasize the crucial role of the OSPX and the involvement of the gold(I)-activated C≡C triple bond during the glycosylation process. The low-temperature NMR experiments unveiled a unique dual-coordination pattern of the gold(I) catalyst to the thiocarbonyl group and the alkynyl group of the OSPX, initiating a 5--dig cyclization process. Furthermore, density functional theory (DFT) simulations reveal the ligand-induced match-mismatch effect between leaving groups OSPX and OABz and gold catalysts IPrAuNTf and (PhO)PAuNTf. The DFT simulations also suggest that the formation of 2-deoxy-β-glycosidic bonds occurs via the bottom-face attack of the acceptor to the oxocarbenium intermediate, which adopts a half-chair conformation, leading to an energetically favored, -conformed intermediate that is stabilized by a hydrogen bonding interaction.
title Gold(I)-Catalyzed 2-Deoxy-β-glycosylation via 1,2-Alkyl/Arylthio Migration: Synthesis of Velutinoside A Pentasaccharide.
url https://pubmed.ncbi.nlm.nih.gov/39869845/