- Hydroxy Group Directed Catalytic Hydrosilylation of Amides
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Chemo- and site-selective hydrosilylation of α- or β-hydroxy amides using organocatalyst B(C6F5)3 and commercially available hydrosilanes is described. This transformation is operative under mild conditions and tolerates a wide range of functional groups. The reaction was applied for selective reduction of a specific amide group of the therapeutically important cyclic peptide cyclosporin A, demonstrating the potential usefulness of this catalytic method in late-stage structural transformations of drug lead molecules.
- Ni, Jizhi,Oguro, Tsubasa,Sawazaki, Taka,Sohma, Youhei,Kanai, Motomu
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supporting information
p. 7371 - 7374
(2018/11/25)
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- A preparing method of rafoxanide
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A preparing method of rafoxanide is provided. The method includes preparing 2-chloro-4-nitrophenyl tert-chlorophenyl ether by adopting p-chlorophenol and 3,4-dichloronitrobenzene as raw materials and adopting DMF as a solvent under catalysis of a catalyst that is cuprous chloride, preparing 4-amino-2-chlorophenyl tert-chlorophenyl ether by hydrogenating under catalysis of a 10% Pd/C catalyst, reacting 3,5-diiodosalicylic acid that is adopted as a raw material with an acyl chlorination reagent that is BTC/C2H4Cl2 to prepare 3,5-diiodosalicyloyl chloride, and subjecting the 4-amino-2-chlorophenyl tert-chlorophenyl ether and the 3,5-diiodosalicyloyl chloride to condensation to prepare the rafoxanide. The method is mild in reaction conditions, simple in process and easy in operation. A product of the method is high in purity and high in yield. The method is suitable for industrial production.
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- Compositions and methods for the treatment of helminthiasis
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Compositions and methods for the treatment of helminthiasis are disclosed which utilize 5-isopropoxycarbonylamino-2-(4'-thiazolyl)-benzimidazole and 3'-chloro-4'-(p-chlorophenoxy)-3,5-diiodosalicylanilide as the active ingredients.
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