- Synthesis and structure-activity relationship of aminoarylthiazole derivatives as potential potentiators of the chloride transport defect in cystic fibrosis
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Background: Cystic fibrosis (CF) is the autosomal recessive disorder most common in Caucasian populations. It is caused by mutations in the cystic fibrosis transmembrane regulator protein (CFTR). CFTR is predominantly expressed at the apical plasma membra
- Liessi, Nara,Pesce, Emanuela,Salis, Annalisa,Damonte, Gianluca,Tasso, Bruno,Cichero, Elena,Pedemonte, Nicoletta,Millo, Enrico
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p. 646 - 657
(2021/04/02)
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- Assembly of substituted 1H-benzimidazoles and 1,3-dihydrobenzimidazol-2- ones via CuI/L-proline catalyzed coupling of aqueous ammonia with 2-iodoacetanilides and 2-iodophenylcarbamates
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(Chemical Equation Presented) CuI/L-proline catalyzed coupling of aqueous ammonia with 2-iodoacetanilides and 2-iodophenylcarbamates affords the aryl amination products at room temperature, which undergo in situ additive cyclization under acidic conditions or heating to give substituted 1H-benzimidazoles and 1,3-dihydrobenzimidazol-2-ones, respectively. A wide range of functional groups including ketone, nitro, iodo, bromo, and ester are tolerated under these reaction conditions, providing these heterocycles with great diversity.
- Diao, Xiaoqiong,Wang, Yuji,Jiang, Yongwen,Ma, Dawei
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experimental part
p. 7974 - 7977
(2010/02/28)
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- FRIDEL-CRAFTS ACYLATION OF BENZIMIDAZOLIN-2-ONES WITH ALIPHATIC ACID CHLORIDES
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The acylation of benzimidazolin-2-one and its 5,6-disubstituted derivatives with aliphatic acid chlorides in the presence of anhydrous aluminium chloride was studied.The corresponding 5(6)-acyl-, 5-R-6-acyl, and 5,6-dimethyl-4-acylbenzimidazolin-2-ones, the structures of which were confirmed by the results of elementary analysis and IR, PMR, and mass spectroscopy, were obtained.The yields of the acylation products depend on the electronic effects of the substituents in the benzene ring of the benzimidazolin-2-one on steric factors.
- Kadyrov, Ch. Sh.,Khalikov, S. S.
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p. 658 - 661
(2007/10/02)
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