CN105440026A — 依匹哌唑的制备方法
Assigned to Shanghai Xunhe Pharmaceutical Technology Co Ltd · Expires 2016-03-30 · 10y expired
What this patent protects
本发明提供了一种依匹哌唑的制备方法,包括如下步骤:以7-(4-氯丁氧基)-1H-喹啉-2-酮(6)为起始原料,与哌嗪单盐酸盐发生单取代反应,生成中间体7-(4-哌嗪丁氧基)-1H-喹啉-2-酮盐酸盐(13),13再与4-氯苯并[b]噻吩(14)经催化偶联反应制得终产物依匹哌唑(1)。本发明所述的依匹哌唑制备方法,具有原料易得、工艺简单、操作方便、总收率高(总收率达75%)和易于工业化生产的优点。反应通式如下: 。
USPTO Abstract
本发明提供了一种依匹哌唑的制备方法,包括如下步骤:以7-(4-氯丁氧基)-1H-喹啉-2-酮(6)为起始原料,与哌嗪单盐酸盐发生单取代反应,生成中间体7-(4-哌嗪丁氧基)-1H-喹啉-2-酮盐酸盐(13),13再与4-氯苯并[b]噻吩(14)经催化偶联反应制得终产物依匹哌唑(1)。本发明所述的依匹哌唑制备方法,具有原料易得、工艺简单、操作方便、总收率高(总收率达75%)和易于工业化生产的优点。反应通式如下: 。
Drugs covered by this patent
- Rexulti (BREXPIPRAZOLE) · Otsuka
Bibliographic data sourced from FDA Orange Book + USPTO public records. Plain-English summary generated by AI grounded in source text. Patent term extensions (PTR, SPC, pediatric) may shift the effective expiry. Not legal advice.
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