- Beta receptor blocker Acebutolol intermediate synthesized by photochemical Fries rearrangement
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The invention belongs to the field of organic photochemistry and medicinal chemistry, and particularly relates to a beta receptor blocker Acebutolol intermediate synthesized by photochemical Fries rearrangement. An efficient continuous acetylation synthesis method is adopted, raw materials including p-aminophenol and n-butyric anhydride are mixed and subjected to a water diversion reaction with a water-carrying agent, then the water-carrying agent is removed through distillation, reactants are cooled, water is added as a dispersing agent, then liquid caustic soda is added for a reaction, phenate is generated, acetic anhydride is dropwise added, the mixture is stirred for a reaction, ester is generated, recrystallizing is carried out to generate a first-step product N-(4-acetoxyphenyl) butyrylamide; and in the step 2 photochemical Fries liquid phase rearrangement reaction is adopted, the product in the first step is dissolved in an organic solvent, then Fries rearrangement is carried out by irradiation of ultraviolet-visible light with a specific wavelength, the solvent is heated and evaporated after the reaction is completed, and the important intermediate 2-acetyl-4-n-butyryl aminophenol of Acebutolol is obtained after recrystallization. The method is simple and easy to implement, and low-toxicity, efficient and cheap green chemical reagents are used in the synthesis process.
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Paragraph 0025; 0027-0028; 0030-0031; 0033-0034; 0036...
(2021/10/27)
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- 2-aminopyridine derivatives and combinatorial libraries thereof
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The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1to R5have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
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