160844-75-7Relevant articles and documents
Synthesis, structural elucidation and larvicidal activity of novel arylhydrazones
P, Nefisath,Dasappa, Jagadeesh Prasad,B, Haripriya,Chopra, Deepak,Venugopala, Katharigatta N.,Deb, Pran Kishore,Gleiser, Raquel M.,Mohanlall, Viresh,Maharaj, Rajendra,Shashiprabha,Poojary, Vishwanatha
, (2021)
The present study focuses on a series of novel hydrazones of 2- [3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carbohydrazide (5a-l) for their larvicidal activity against Anopheles arabiensis. The synthesis of the title compounds was achieved by the conventional reflux method, and structures of the novel compounds were ascertained by FT-IR, NMR (1H &13C), LC-MS, and elemental analysis. Compound (5l) was studied by single crystal X-ray diffraction for intra and intermolecular interactions. Title compounds (E)-2-(3-cyano-4-isobutoxyphenyl)-N'-(4-fluoro-3-phenoxybenzylidene)-4-methylthiazole-5-carbohydrazide (5a) and (E)-N'-(4-Chlorobenzylidene)-2-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carbohydrazide (5g) emerged as promising larvicidal agents against Anopheles arabiensis.
Pd/Cu-Catalyzed C-H/C-H Cross Coupling of (Hetero)Arenes with Azoles through Arylsulfonium Intermediates
Lin, Zeng-Hui,Tian, Ze-Yu,Zhang, Cheng-Pan
supporting information, p. 4400 - 4405 (2021/06/27)
A highly efficient method for the selective formal C-H/C-H cross-coupling of azoles and (hetero)arenes was established through arylsulfonium intermediates under transition-metal catalysis, which produced a variety of 2-(hetero)aryl azoles in good to excellent yields. Advantages of the reaction included mildness, a good functional group tolerance, a wide range of substrates, a high regio- and chemoselectivity, one-pot procedures, and the late-stage functionalization of complex molecules without the use of oxidants, offering a promising strategy for the transition-metal-catalyzed C-H arylation of azoles.
Method for synthesizing febuxostat and intermediate thereof
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, (2020/05/02)
The invention relates to a method for synthesizing febuxostat and an intermediate thereof, specifically a method for synthesizing 2-(3-formyl-4-isobutoxy-phenyl)-4-methyl-thiazole-5-carboxylic acid ethyl ester. The method comprises the following steps: preparing 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate; enabling the product obtained in the step (a) to react in DMF (Dimethyl Formamide) in the presence of potassium carbonate and bromo-isobutane, adding water and ethyl acetate for extraction, concentrating to obtain an organic layer, and recrystallizing with DMF to obtain 2-(3-formyl-4-isobutoxy-phenyl)-4-methyl-thiazole-5-carboxylic acid ethyl ester. The invention also relates to 2-(3-formyl-4-isobutoxy-phenyl)-4-methyl-thiazole-5-carboxylic acid ethyl ester and 2-(3-formyl-4-hydroxyphenyl)-4-methyl-5-thiazoleethyl formate and application thereof to the preparation of febuxostat. The method of the invention has excellent performance.