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发明公开
CN107759459A 一种2，5－二溴苯乙酸的合成方法 无效 - 驳回

  • 专利标题： 一种2，5－二溴苯乙酸的合成方法
  • 专利标题（英）： Synthetic method for 2,5-dibromophenylacetic acid
  • 申请号： CN201710269339.5
    申请日： 2017-04-18
  • 公开(公告)号： CN107759459A
    公开(公告)日： 2018-03-06
  • 发明人: 徐浩 , 郁斌 , 关建宁
  • 申请人： 南京工业大学
  • 申请人地址： 江苏省南京市浦口区浦珠南路30号
  • 专利权人： 南京工业大学
  • 当前专利权人： 南京工业大学
  • 当前专利权人地址： 江苏省南京市浦口区浦珠南路30号
  • 主分类号： C07C51/08
  • IPC分类号： C07C51/08 ;  C07C57/58
一种2，5－二溴苯乙酸的合成方法
摘要：
本发明公开了一种抗丙肝药物中间体2，5-二溴苯乙酸的合成。本发明以对二溴苯为原料，经氯甲基化，氰化，水解步骤得到2，5二溴苯乙酸。其中氯甲基化反应中以氯化钠为氯化试剂，多聚甲醛为原料，浓硫酸为溶剂和酸，和多聚甲醛反应生成2，5-二溴苄氯。再用2，5-二溴苄氯和氰化亚铜在DMF中回流反应得到2，5-二溴苯乙腈。最后用2，5-二溴苯乙腈在氢氧化钠水溶液中水解，再用盐酸酸化，得到产物2，5-二溴苯乙酸。该发明具有成品低廉，反应条件温和等特点。
摘要（英）：

The invention discloses a synthetic method for an intermediate 2,5-dibromophenylacetic acid of an anti-HCV drug. According to the invention, dibromobenzene is used as a raw material and is subjected to chloromethylation, cyanidation and hydrolysis successively to prepare 2,5-dibromophenylacetic acid. During a chloromethylation reaction, sodium chloride is used as a chlorination reagent; paraformaldehyde is used as a raw material; concentrated sulfuric acid is used as a solvent and an acid; and concentrated sulfuric acid is reacted with paraformaldehyde in the presence of sodium chloride to produce 2,5-dibromobenzyl chloride. Then 2,5-dibromobenzyl chloride and cuprous cyanide are subjected to a reflux reaction in DMF so as to obtain 2,5-dibromophenylacetonitrile. Finally, 2,5-dibromophenylacetonitrile is subjected to hydrolysis in an aqueous sodium hydroxide solution at first and then to acidification with hydrochloric acid so as to obtain the product 2,5-dibromophenylacetic acid. Thesynthetic method provided by the invention has the characteristics of low cost, mild reaction conditions and the like.

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