1298111-29-1Relevant articles and documents
Efficient formation of C–S bond using heterocyclic thiones and arynes
An, Yu,Xu, Gang,Cai, Menglu,Wang, Shihui,Wang, Xiao zhong,Chen, Yingqi,Dai, Liyan
, (2020/12/23)
Phenylthio heterocyclic compounds are widely used because of their diverse biological activities and medicinal prospects. Here, a facile method was reported. An arylation of 1,3,4-oxa(thia)diazol-2-thiones reacting with arynes to build C(aryl)-S bonds in the presence of CsF had good yields and excellent selectivity. The reaction was completed in short time without using expensive reagents and catalysts. Present reaction system is an efficient procedure to process phenylthio heterocyclic compounds and reveals a sustainable method and better application prospects in future organic synthesis.
Synthetic method of aryl sulfhydryl diazole derivative
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Paragraph 0033-0036; 0049-0050; 0053-0054; 0057-0062, (2020/05/30)
The invention discloses a synthetic method of an aryl sulfhydryl diazole derivative. The preparation method comprises the following steps: with 2,5-disubstituted oxadiazole and thiadiazole as raw materials, dissolving the raw materials in a certain amount of organic solvent, and adding a fluorinating agent to form a raw material system,; sealing the reaction device, fully replacing the gas in thedevice with N2, heating the reactant to reflux, adding a benzyne precursor by using an injector, performing a reaction for 5-6 hours; and after the reaction is finished, carrying out aftertreatment toobtain the aryl sulfhydryl diazole derivative. The reaction method is simple to operate, raw materials and reaction time are saved, the conversion rate and selectivity of the reaction are ideal, andcompared with the prior art, the environmental pollution is small, the operation is safe, and the method is a novel heterocyclic compound sulfydryl arylation reaction method. The method is applied toarylation reaction of sulfydryl on various oxadiazole and thiadiazole rings, but is not limited to preparation of aryl sulfydryl oxadiazole and thiadiazole.