CN106554363B — 一种Baricitinib中间体的制备方法
Assigned to Chia Tai Tianqing Pharmaceutical Group Co Ltd · Expires 2019-03-05 · 7y expired
What this patent protects
本发明属于医药化工领域,具体而言涉及一种Baricitinib中间体的制备方法,本发明的制备方法,通过4‑吡唑硼化物与2‑[1‑(乙基磺酰基)‑3‑氮杂环丁亚基]乙腈反应制备关键中间体2‑[1‑乙磺酰基‑3‑[4‑(4,4,5,5‑四甲基‑1,3,2‑二氧代硼戊环‑2‑基)‑1H‑吡唑‑1‑基]氮杂环丁‑3‑基]乙腈,无需对4‑吡唑硼化物吡唑环上的氮进行保护,从而后续也没有脱去该相应保护基步骤,因此整个反应路线短,原料更易获得,生产成本低,特别适合工业化生产。
USPTO Abstract
本发明属于医药化工领域,具体而言涉及一种Baricitinib中间体的制备方法,本发明的制备方法,通过4‑吡唑硼化物与2‑[1‑(乙基磺酰基)‑3‑氮杂环丁亚基]乙腈反应制备关键中间体2‑[1‑乙磺酰基‑3‑[4‑(4,4,5,5‑四甲基‑1,3,2‑二氧代硼戊环‑2‑基)‑1H‑吡唑‑1‑基]氮杂环丁‑3‑基]乙腈,无需对4‑吡唑硼化物吡唑环上的氮进行保护,从而后续也没有脱去该相应保护基步骤,因此整个反应路线短,原料更易获得,生产成本低,特别适合工业化生产。
Drugs covered by this patent
- Olumiant (baricitinib) · Eli Lilly
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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