关键词: FONT-SIZE: 10.5pt, mso-bidi-font-size: 11.0pt, mso-bidi-font-family: 宋体, mso-font-kerning: 1.0pt, mso-ansi-language: EN-US, mso-fareast-language: ZH-CN, mso-bidi-language: AR-SA, mso-ascii-font-family: Calibri">甲苄氧喹啉hansi-font-family: 宋体" lang=EN-US>;3-FONT-SIZE: 10.5pt, mso-bidi-font-size: 11.0pt, mso-bidi-font-family: 宋体, mso-font-kerning: 1.0pt, mso-ansi-language: EN-US, mso-fareast-language: ZH-CN, mso-bidi-language: AR-SA, mso-ascii-font-family: Calibri">苄氧基hansi-font-family: 宋体" lang=EN-US>-4-FONT-SIZE: 10.5pt, mso-bidi-font-size: 11.0pt, mso-bidi-font-family: 宋体, mso-font-kerning: 1.0pt, mso-ansi-language: EN-US, mso-fareast-language: ZH-CN, mso-bidi-language: AR-SA, mso-ascii-font-family: Calibri">丁基苯胺hansi-font-family: 宋体" lang=EN-US>;FONT-SIZE: 10.5pt, mso-bidi-font-size: 11.0pt, mso-bidi-font-family: 宋体, mso-font-kerning: 1.0pt, mso-ansi-language: EN-US, mso-fareast-language: ZH-CN, mso-bidi-language: AR-SA, mso-ascii-font-family: Calibri">合成

Abstract:

An improved synthetic process for 3-benzyloxy-4-n-butylaniline hydrochloride the key intermediate of nequinate which is an anticoccidal drug to parasites of Eimeria,was described.The process was started with 3-aminophenol, via acylation, Fries rearrangement, benzylation, hydrolysis, and Huang-Minlon reduction, to give the title compound.The optimal reaction conditions and molar yield were as follows: acylation, 130—140℃ for 3 h; Fries rearrangement, 140℃ for 5 h, 77.9%(based on 3-aminophenol); benzylation, 70℃ for 2 h and 80℃ for 4 h, 81.3%; hydrolysis and Huang-Minlon reduction, reflux for 90 min, 78.2%.The structures of the main compounds were confirmed by ¹H NMR. The process is much of industrial value because of high yields, cheap and available materials, moderate reaction conditions and convenient operations.

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