CN105348172B — (s)‑1‑(4‑甲氧基‑3‑乙氧基)苯基‑2‑甲磺酰基乙胺的制备及阿普斯特的制备方法
Assigned to Xinfa Pharmaceutical Co Ltd · Expires 2017-11-14 · 9y expired
What this patent protects
本发明涉及一种(S)‑1‑(4‑甲氧基‑3‑乙氧基)苯基‑2‑甲磺酰基乙胺的制备及阿普斯特的制备方法。利用4‑甲氧基‑3‑乙氧基溴苯经格氏反应制备4‑甲氧基‑3‑乙氧基苯基溴化镁、与甲磺酰基乙腈加成、水解、还原得到(R,S)‑1‑(4‑甲氧基‑3‑乙氧基)苯基‑2‑甲磺酰基乙胺(Ⅲ)，再经拆分、过滤得到(S)‑1‑(4‑甲氧基‑3‑乙氧基)苯基‑2‑甲磺酰基乙胺N‑乙酰基‑L‑亮氨酸盐(Ⅳ),经中和后得到(S)‑1‑(4‑甲氧基‑3‑乙氧基)苯基‑2‑甲磺酰基乙胺(Ⅱ)；将化合物Ⅱ进行亚酰胺化制得阿普斯特(Ⅰ)。本发明拆分后的母液循环利用转化为化合物Ⅳ，…
USPTO Abstract
本发明涉及一种(S)‑1‑(4‑甲氧基‑3‑乙氧基)苯基‑2‑甲磺酰基乙胺的制备及阿普斯特的制备方法。利用4‑甲氧基‑3‑乙氧基溴苯经格氏反应制备4‑甲氧基‑3‑乙氧基苯基溴化镁、与甲磺酰基乙腈加成、水解、还原得到(R,S)‑1‑(4‑甲氧基‑3‑乙氧基)苯基‑2‑甲磺酰基乙胺(Ⅲ)，再经拆分、过滤得到(S)‑1‑(4‑甲氧基‑3‑乙氧基)苯基‑2‑甲磺酰基乙胺N‑乙酰基‑L‑亮氨酸盐(Ⅳ),经中和后得到(S)‑1‑(4‑甲氧基‑3‑乙氧基)苯基‑2‑甲磺酰基乙胺(Ⅱ)；将化合物Ⅱ进行亚酰胺化制得阿普斯特(Ⅰ)。本发明拆分后的母液循环利用转化为化合物Ⅳ，减少废液排放，绿色环保，降低成本。
Drugs covered by this patent
- Otezla (APREMILAST) · Amgen
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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