- Visible-light-promotedE-selective synthesis of α-fluoro-β-arylalkenyl sulfidesviathe deoxygenation/isomerization process
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Regioselective synthesis of α-fluoro-β-arylalkenyl sulfides has been established withgem-difluoroalkenes and sodium sulfinates in a transition-metal-free manner. A series of control experiments were executed to demonstrate thiol radicals and anions as the proposed intermediates. Notably, regioselectiveZ→Eisomerization was achieved under green light irradiation in the absence of a photoinitiator.
- Li, Yuxiu,Li, Xiangqian,Li, Xiaowei,Shi, Dayong
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supporting information
p. 2152 - 2155
(2021/03/06)
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- Base-Catalyzed Intramolecular Defluorination/O-Arylation Reaction for the Synthesis of 3-Fluoro-1,4-oxathiine 4,4-Dioxide
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A novel process involving base-catalyzed intramolecular defluorination/O-arylation of readily available α-fluoro-β-one-sulfones was realized and provided a series of 3-fluoro-1,4-oxathiine 4,4-dioxide derivatives in good to excellent yields. Unlike traditional defluorination reactions with stoichiometric base as the deacid reagent, this process is triggered by a catalytic amount of base (TMG: tetramethylguanidine) and molecular sieves serve as both an adsorbent to remove HF acid and an activator to assist C-F bond cleavage.
- Kang, Lei,Zhang, Jinlong,Yang, Huameng,Qian, Jinlong,Jiang, Gaoxi
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supporting information
p. 785 - 789
(2021/04/09)
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- Enhancing the Potential of Miniature-Scale DNA-Compatible Radical Reactions via an Electron Donor-Acceptor Complex and a Reversible Adsorption to Solid Support Strategy
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DNA-encoded library (DEL) technology is a powerful tool in the discovery of bioactive probe molecules and drug leads. Mostly, the success in DEL technology stems from the molecular diversity of the chemical libraries. However, the construction of DELs has been restricted by the idiosyncratic needs and the required low concentration (~1 mM or less) of the library intermediate. Here, we report visible-light-promoted on-DNA radical coupling reactions via an electron donor-acceptor (EDA) complex and a reversible adsorption to solid support (RASS) strategy. This protocol provides a unique solution to the challenges of increasing the reactivity of highly diluted DNA substrates and reducing the residues of heavy metals from photocatalysts. A series of on-DNA indole sulfone and selenide derivatives were obtained with good to quantitative conversions. It is anticipated that these mild-condition on-DNA radical reactions will significantly improve the chemical diversity of DELs and find widespread utility to DEL construction.
- Lin, Bizhen,Lu, Weiwei,Chen, Zhen-Yu,Zhang, Yue,Duan, Yin-Zhe,Lu, Xiaojie,Yan, Ming,Zhang, Xue-Jing
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supporting information
p. 7381 - 7385
(2021/10/12)
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- Sulfonyl pyridine amide derivatives and preparation method thereof
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The invention relates to a Sulfonyl pyridine amide derivatives and a preparation method thereof; the preparation method comprises the following steps: adding a compound as shown in a structural formula (II), a compound as shown in a structural formula (III), an oxidant, an additive and a heterogeneous biomass supported copper catalyst into a reaction container, adding a solvent, and carrying out astirring reaction at room temperature; and after the reaction is finished, filtering, extracting, concentrating, separating and purifying to obtain the sulfonyl pyridine amide derivative with the structural formula shown in the formula (I). The synthesis method of the sulfonyl pyridine amide derivatives is scientific and reasonable, and a series of sulfonyl pyridine amide derivatives are synthesized by a green and efficient synthesis method by adopting a heterogeneous biomass copper-loaded catalyst for catalytic reaction.
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Paragraph 0068-0070
(2021/01/15)
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- Diastereoselective Monofluorocyclopropanation Using Fluoromethylsulfonium Salts
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Diarylfluoromethylsulfonium salts, alternatives to freons or advanced fluorinated building blocks, are bench stable and easy-to-use sources of direct fluoromethylene (:CHF) transfer to alkenes. These salts enabled development of a trans-selective monofluorinated Johnson-Corey-Chaykovsky reaction with vinyl sulfones or vinyl sulfonamides to access synthetically challenging monofluorocyclopropane scaffolds. The described method offers rapid access to monofluorinated cyclopropane building blocks with further functionalization opportunities to deliver more complex synthetic targets diastereoselectively.
- Melngaile, Renate,Sperga, Arturs,Baldridge, Kim K.,Veliks, Janis
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supporting information
p. 7174 - 7178
(2019/09/12)
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- Sulfonamide formation from sodium sulfinates and amines or ammonia under metal-free conditions at ambient temperature
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A novel, practical and highly efficient method for the construction of a variety of sulfonamides mediated by I2 was demonstrated. The reaction proceeds readily at room temperature using a variety of sodium sulfinates and amines or ammonia in water in a metal-, base-, ligand-, or additive-free protocol. Primary, secondary and tertiary sulfonamides were obtained in good to excellent yields with a broad range of functional group tolerability. This journal is
- Yang, Kai,Ke, Miaolin,Lin, Yuanguang,Song, Qiuling
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supporting information
p. 1395 - 1399
(2015/03/18)
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- Expedient synthesis of biologically important sulfonylmethyl pyrimidines
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Two novel synthetic strategies that allow rapid diversification of the sulfone moiety in sulfonylmethyl pyrimidines, a class of compounds with a wide range of biological activity, which are of interest in a wide variety of drug discovery programmes, are described.
- Blades, Kevin,Demeritt, Julie,Fillery, Shaun,Foote, Kevin M.,Greenwood, Ryan,Gregson, Clare,Hassall, Lorraine A.,McGuire, Thomas M.,Pike, Kurt G.,Williams, Emma
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supporting information
p. 3851 - 3855
(2014/07/08)
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- Copper-catalysed coupling of aryl tosylates with sodium arylsulfinates
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Diaryl sulfones derivatives were easily synthesised from aryl tosylates and sodium arylsulfinates in high yields using [Cu(CH3CN)4]PF6 as catalyst. The transformation is efficient, simple and the starting materials are readily available.
- Wang, Chunjie,Zhang, Hui,Li, Zhiwei,Wang, Ziyun
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p. 639 - 642
(2015/02/02)
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- Herbicidal compounds and compositions containing them
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Herbicides of formula: STR1 in which: n=0,1, 2 f=0,1 A is chosen from the groups STR2 in which: Ar is chosen from the groups STR3 B is chosen from optionally substituted C1 -C10 alkyl and C3 -C10 cycloalkyl grou
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