CN106967050A — 一种azd9291的制备方法
Assigned to Beijing University of Technology · Expires 2017-07-21 · 9y expired
What this patent protects
一种AZD9291的制备方法，属于药物制备技术领域。以3‑(2‑氯嘧啶‑4‑基)‑1‑甲基吲哚为原料，首先与4‑氟‑2‑甲氧基‑5‑硝基苯胺发生取代反应，生成3‑[2‑[(4‑氟‑2‑甲氧基‑5‑硝基)苯胺基]嘧啶‑4‑基]‑1‑甲基吲哚(3)；而后，化合物3在催化剂的作用下与N,N,N’‑三甲基乙二胺取代生成3‑[2‑[(4‑(N,N,N’‑三甲基乙二胺)‑2‑甲氧基‑5‑硝基)苯胺基]嘧啶‑4‑基]‑1‑甲基吲哚(5)；然后，化合物5经硝基的还原以及胺基的酰胺化，“一锅法”合成出AZD9291。该制备方法工艺简洁、环境友好、成本低廉且适合工业化生产。
USPTO Abstract
一种AZD9291的制备方法，属于药物制备技术领域。以3‑(2‑氯嘧啶‑4‑基)‑1‑甲基吲哚为原料，首先与4‑氟‑2‑甲氧基‑5‑硝基苯胺发生取代反应，生成3‑[2‑[(4‑氟‑2‑甲氧基‑5‑硝基)苯胺基]嘧啶‑4‑基]‑1‑甲基吲哚(3)；而后，化合物3在催化剂的作用下与N,N,N’‑三甲基乙二胺取代生成3‑[2‑[(4‑(N,N,N’‑三甲基乙二胺)‑2‑甲氧基‑5‑硝基)苯胺基]嘧啶‑4‑基]‑1‑甲基吲哚(5)；然后，化合物5经硝基的还原以及胺基的酰胺化，“一锅法”合成出AZD9291。该制备方法工艺简洁、环境友好、成本低廉且适合工业化生产。
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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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