1298111-54-2Relevant academic research and scientific papers
Synthesis method of aromatic thiol diazole derivatives
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Paragraph 0035; 0036; 0053; 0054, (2020/02/10)
The invention discloses a synthesis method of aromatic thiol diazole derivatives. The method comprises the steps: using multiple thiol-containing 2,5-di-substituted oxadiazole and thiol-containing thiadiazole as raw materials, dissolves the raw materials in a certain amount of an organic solvent, adding a fluorinating agent so as to form a raw material system, closing a reaction device, performingfull replacement with N2, raising the temperature for reflux, adding a benzyne precursor with a syringe, performing a reaction for 5-6 hours, and performing post-treatment after completion of the reaction so as to obtain the aromatic thiol diazole derivatives. The reaction method has simple operation, the raw materials and reaction time are saved, and the conversion rate and selectivity of the reaction are ideal; and compared with the prior art, the synthesis method has little environmental pollution and safe operation, and is a reaction method for thiol arylation of heterocyclic compounds, and the method can be applied to arylation reactions of thiol groups on rings of oxadiazole and thiadiazole, but is not limited to preparation of aromatic thiol oxadiazole and aromatic thiol thiadiazole.
Fabrication of magnetic amino-functionalized nanoparticles for S-arylation of heterocyclic thiols
Liu, Yanhong,Zhou, Lincheng,Hui, Xinping,Dong, Zhenwen,Zhu, Hao,Shao, Yanming,Li, Yanfeng
, p. 49980 - 49985 (2014/12/10)
A series of uniformed mono-disperse magnetic nanoligands (MNLs) (CoFe2O4-NH2 (MNL A), Fe3O4@Si(CH2)3NH2 (MNL B), Fe3O4@Si(CH2)3/
Efficient copper-catalyzed C-S cross-coupling of heterocyclic thiols with aryl iodides
Niu, Liang-Feng,Cai, Yan,Liang, Chao,Hui, Xin-Ping,Xu, Peng-Fei
supporting information; experimental part, p. 2878 - 2881 (2011/05/13)
A copper-catalyzed cross-coupling of heterocyclic thiols with aryl iodides is reported. The reaction was carried out in the presence of CuI (5 mol %), 1,10-phenanthroline (10 mol %) and K2CO3 (1.3 equiv) in DMF at 120 °C. A variety o
Ring opening of pymisyl-protected aziridines with organocuprates
Bornholdt, Jan,Felding, Jakob,Clausen, Rasmus P.,Kristensen, Jesper L.
supporting information; experimental part, p. 12474 - 12480 (2010/12/25)
The pyrimidine-2-sulfonyl (pymisyl) group is introduced as a new protecting group that can be used to activate aziridines towards ring opening. It is readily introduced and removed under mild conditions. Regioselective ring opening of pymisyl-protected 2-methyl-aziridine with organocuprates gives the corresponding sulfonamides in high yields, and the pymisyl group can subsequently be removed upon treatment with a thiolate. The versatility of this new nitrogen protecting group is illustrated with a new synthesis of Selegiline, a monoamine oxidase-B inhibitor marketed for the treatment of Parkinson's disease. Easy on'easy off: The pymisyl group is introduced as a new protecting group for the activation of aziridines towards ring opening with organocuprates (see scheme). It is readily removed under very mild conditions with thiolates. The versatility of the approach is illustrated in a new synthesis of Selegiline, a drug marketed for the treatment of Parkinson's disease.
