Efficient Synthesis of Eight-Membered Cyclic Diaryl Sulfides via an Aryne Reaction with 2-Methylenebenzothiophene-3-Ones

In this study, we develop a concise and efficient synthetic strategy for the construction of eight-membered cyclic diaryl sulfides by undertaking [3+2] cycloaddition, 1,2-hydrogen shift, and C(sp<sup>2</sup>)-S bond cleavage steps on 2-methylenebenzothiophene-3-ones with aryne, using TBA...

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Main Authors: Juhua Feng, Wenjie Zou, Haokun Zhang, Qilin Huang, Ailin Huang, Kuan Liu, Guizhou Yue
Format: Article
Language:English
Published: MDPI AG 2025-05-01
Series:Reactions
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Online Access:https://www.mdpi.com/2624-781X/6/2/35
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author Juhua Feng
Wenjie Zou
Haokun Zhang
Qilin Huang
Ailin Huang
Kuan Liu
Guizhou Yue
author_facet Juhua Feng
Wenjie Zou
Haokun Zhang
Qilin Huang
Ailin Huang
Kuan Liu
Guizhou Yue
author_sort Juhua Feng
collection DOAJ
description In this study, we develop a concise and efficient synthetic strategy for the construction of eight-membered cyclic diaryl sulfides by undertaking [3+2] cycloaddition, 1,2-hydrogen shift, and C(sp<sup>2</sup>)-S bond cleavage steps on 2-methylenebenzothiophene-3-ones with aryne, using TBAT as the fluorine source. This transformation proceeds well under mild conditions and affords the target products in high to excellent yields (up to 93% yields). The process provides a practical route to achieving sulfur-containing medium-sized heterocycles.
format Article
id doaj-art-4f783260bc444b1f9a4110e5c230fa17
institution DOAJ
issn 2624-781X
language English
publishDate 2025-05-01
publisher MDPI AG
record_format Article
series Reactions
spelling doaj-art-4f783260bc444b1f9a4110e5c230fa172025-08-20T03:16:38ZengMDPI AGReactions2624-781X2025-05-01623510.3390/reactions6020035Efficient Synthesis of Eight-Membered Cyclic Diaryl Sulfides via an Aryne Reaction with 2-Methylenebenzothiophene-3-OnesJuhua Feng0Wenjie Zou1Haokun Zhang2Qilin Huang3Ailin Huang4Kuan Liu5Guizhou Yue6College of Science, Sichuan Agricultural University, Xinkang Road 46, Ya’an 625014, ChinaCollege of Science, Sichuan Agricultural University, Xinkang Road 46, Ya’an 625014, ChinaCollege of Science, Sichuan Agricultural University, Xinkang Road 46, Ya’an 625014, ChinaCollege of Science, Sichuan Agricultural University, Xinkang Road 46, Ya’an 625014, ChinaCollege of Science, Sichuan Agricultural University, Xinkang Road 46, Ya’an 625014, ChinaCollege of Science, Sichuan Agricultural University, Xinkang Road 46, Ya’an 625014, ChinaCollege of Science, Sichuan Agricultural University, Xinkang Road 46, Ya’an 625014, ChinaIn this study, we develop a concise and efficient synthetic strategy for the construction of eight-membered cyclic diaryl sulfides by undertaking [3+2] cycloaddition, 1,2-hydrogen shift, and C(sp<sup>2</sup>)-S bond cleavage steps on 2-methylenebenzothiophene-3-ones with aryne, using TBAT as the fluorine source. This transformation proceeds well under mild conditions and affords the target products in high to excellent yields (up to 93% yields). The process provides a practical route to achieving sulfur-containing medium-sized heterocycles.https://www.mdpi.com/2624-781X/6/2/35aryne[3+2] cycloadditioneight-membered cyclic diaryl sulfides2-methylenebenzothiophene-3-ones
spellingShingle Juhua Feng
Wenjie Zou
Haokun Zhang
Qilin Huang
Ailin Huang
Kuan Liu
Guizhou Yue
Efficient Synthesis of Eight-Membered Cyclic Diaryl Sulfides via an Aryne Reaction with 2-Methylenebenzothiophene-3-Ones
Reactions
aryne
[3+2] cycloaddition
eight-membered cyclic diaryl sulfides
2-methylenebenzothiophene-3-ones
title Efficient Synthesis of Eight-Membered Cyclic Diaryl Sulfides via an Aryne Reaction with 2-Methylenebenzothiophene-3-Ones
title_full Efficient Synthesis of Eight-Membered Cyclic Diaryl Sulfides via an Aryne Reaction with 2-Methylenebenzothiophene-3-Ones
title_fullStr Efficient Synthesis of Eight-Membered Cyclic Diaryl Sulfides via an Aryne Reaction with 2-Methylenebenzothiophene-3-Ones
title_full_unstemmed Efficient Synthesis of Eight-Membered Cyclic Diaryl Sulfides via an Aryne Reaction with 2-Methylenebenzothiophene-3-Ones
title_short Efficient Synthesis of Eight-Membered Cyclic Diaryl Sulfides via an Aryne Reaction with 2-Methylenebenzothiophene-3-Ones
title_sort efficient synthesis of eight membered cyclic diaryl sulfides via an aryne reaction with 2 methylenebenzothiophene 3 ones
topic aryne
[3+2] cycloaddition
eight-membered cyclic diaryl sulfides
2-methylenebenzothiophene-3-ones
url https://www.mdpi.com/2624-781X/6/2/35
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