Reductive sulfinylation by nucleophilic chain isomerization of sulfonylpyridinium

Abstract Sulfur-containing units are fundamental components widely found in bioactive compounds, prompting notable efforts toward developing synthetic methodologies for incorporating sulfur functionality into organic precursors. The synthesis of sulfinate esters and sulfinamides has garnered signifi...

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Main Authors: Yifan Li, Weigang Zhang, Jeonguk Kweon, Yi Pan, Qing Wang, Sukbok Chang, Yi Wang
Format: Article
Language:English
Published: Nature Portfolio 2025-01-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-024-55786-7
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author Yifan Li
Weigang Zhang
Jeonguk Kweon
Yi Pan
Qing Wang
Sukbok Chang
Yi Wang
author_facet Yifan Li
Weigang Zhang
Jeonguk Kweon
Yi Pan
Qing Wang
Sukbok Chang
Yi Wang
author_sort Yifan Li
collection DOAJ
description Abstract Sulfur-containing units are fundamental components widely found in bioactive compounds, prompting notable efforts toward developing synthetic methodologies for incorporating sulfur functionality into organic precursors. The synthesis of sulfinate esters and sulfinamides has garnered significant interest owing to their immense potential for applications, especially in drug development. However, most existing synthetic protocols suffer from some limitations. To address these challenges, we herein present a practical and efficient approach for the reductive sulfinylation of diverse nucleophiles with sulfonylpyridinium salts (SulPy) through the nucleophilic chain substitution, namely SNC reaction, which involves S(VI) to S(IV) nucleophilic chain isomerization process. These versatile sulfinylation reagents can be readily accessed from diverse commercially available resourses. The late-stage modification of complex molecules and the ability to rapidly synthesize numerous sulfinyl bioisosteres of various drugs highlights the utility of this protocol.
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publisher Nature Portfolio
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spelling doaj-art-3a411cf8821741d79d7e29c30b37c18b2025-08-20T02:53:57ZengNature PortfolioNature Communications2041-17232025-01-0116111210.1038/s41467-024-55786-7Reductive sulfinylation by nucleophilic chain isomerization of sulfonylpyridiniumYifan Li0Weigang Zhang1Jeonguk Kweon2Yi Pan3Qing Wang4Sukbok Chang5Yi Wang6Jiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry and Chemical Engineering, Nanjing UniversityJiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry and Chemical Engineering, Nanjing UniversityCenter for Catalytic Hydrocarbon Functionalizations, Institute for Basic Science (IBS)Jiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry and Chemical Engineering, Nanjing UniversityCenter for Catalytic Hydrocarbon Functionalizations, Institute for Basic Science (IBS)Center for Catalytic Hydrocarbon Functionalizations, Institute for Basic Science (IBS)Jiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry and Chemical Engineering, Nanjing UniversityAbstract Sulfur-containing units are fundamental components widely found in bioactive compounds, prompting notable efforts toward developing synthetic methodologies for incorporating sulfur functionality into organic precursors. The synthesis of sulfinate esters and sulfinamides has garnered significant interest owing to their immense potential for applications, especially in drug development. However, most existing synthetic protocols suffer from some limitations. To address these challenges, we herein present a practical and efficient approach for the reductive sulfinylation of diverse nucleophiles with sulfonylpyridinium salts (SulPy) through the nucleophilic chain substitution, namely SNC reaction, which involves S(VI) to S(IV) nucleophilic chain isomerization process. These versatile sulfinylation reagents can be readily accessed from diverse commercially available resourses. The late-stage modification of complex molecules and the ability to rapidly synthesize numerous sulfinyl bioisosteres of various drugs highlights the utility of this protocol.https://doi.org/10.1038/s41467-024-55786-7
spellingShingle Yifan Li
Weigang Zhang
Jeonguk Kweon
Yi Pan
Qing Wang
Sukbok Chang
Yi Wang
Reductive sulfinylation by nucleophilic chain isomerization of sulfonylpyridinium
Nature Communications
title Reductive sulfinylation by nucleophilic chain isomerization of sulfonylpyridinium
title_full Reductive sulfinylation by nucleophilic chain isomerization of sulfonylpyridinium
title_fullStr Reductive sulfinylation by nucleophilic chain isomerization of sulfonylpyridinium
title_full_unstemmed Reductive sulfinylation by nucleophilic chain isomerization of sulfonylpyridinium
title_short Reductive sulfinylation by nucleophilic chain isomerization of sulfonylpyridinium
title_sort reductive sulfinylation by nucleophilic chain isomerization of sulfonylpyridinium
url https://doi.org/10.1038/s41467-024-55786-7
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AT yipan reductivesulfinylationbynucleophilicchainisomerizationofsulfonylpyridinium
AT qingwang reductivesulfinylationbynucleophilicchainisomerizationofsulfonylpyridinium
AT sukbokchang reductivesulfinylationbynucleophilicchainisomerizationofsulfonylpyridinium
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