Preparation method of 2,4-ditertbutyl-5-aminophenol

The invention relates to the technical field of organic synthesis and bulk pharmaceutical chemical intermediate preparation, in particular to a preparation method of cystic fibrosis treatment new drug ivacaftor key intermediate 2,4-ditertbutyl-5-aminophenol. The method comprises the steps of 1, acet...

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Hauptverfasser: Wang Han, Zhu Chunping, Chen Tianyun, Jiang Luobin, Mao Yongjun, Zhu Guoqing
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to the technical field of organic synthesis and bulk pharmaceutical chemical intermediate preparation, in particular to a preparation method of cystic fibrosis treatment new drug ivacaftor key intermediate 2,4-ditertbutyl-5-aminophenol. The method comprises the steps of 1, acetylation, wherein (A) m-aminophenol or (B) acetic anhydride or acetyl chloride is used as a raw material, and a reaction is carried out to prepare N-(3-hydroxyphenyl)acetamide; 2, tertiary butyl substituting, wherein N-(3-hydroxyphenyl) acetamide and tert butyl alcohol are catalyzed by concentrated sulfuric acid to prepare N-(2,4-ditertbutyl-5-hydroxy phenyl)acetamide; 3, deacetylation, wherein the N-(2,4-ditertbutyl-5-hydroxy phenyl)acetamide is hydrolyzed by acid or alkali to obtain 2,4-ditertbutyl-5-aminophenol. According to the synthesis process, raw materials are easy to obtain, reaction conditions are mold, postprocessing is easy and convenient, amplified preparation is promoted, and the yield is high. 本发明涉及有机