CN105646452B — 一种蛋白激酶抑制剂的合成方法
Assigned to BEIJING KANG LISHENG PHARMACEUTICAL TECHNOLOGY DEVELOPMENT Co Ltd · Expires 2018-05-01 · 8y expired
What this patent protects
本发明涉及一种蛋白激酶抑制剂的合成方法,以2‑(异丙基磺酰基)苯胺、2,4,5‑三氯嘧啶及5‑甲基‑2‑异丙氧基‑4‑(4‑吡啶基)苯胺(4)为起始原料,一锅法发生反应,制备得到5‑氯‑N4‑[2‑[(1‑甲基乙基)磺酰基]苯基]‑N2‑[5‑甲基‑2‑(1‑甲基乙氧基)‑4‑(4‑吡啶基)苯基]‑2,4‑嘧啶二胺;在二氧化铂的催化下加氢还原,得到最终化合物色瑞替尼。此制备方法简便易行、收率高,质量好,便于工业化生产。
USPTO Abstract
本发明涉及一种蛋白激酶抑制剂的合成方法,以2‑(异丙基磺酰基)苯胺、2,4,5‑三氯嘧啶及5‑甲基‑2‑异丙氧基‑4‑(4‑吡啶基)苯胺(4)为起始原料,一锅法发生反应,制备得到5‑氯‑N4‑[2‑[(1‑甲基乙基)磺酰基]苯基]‑N2‑[5‑甲基‑2‑(1‑甲基乙氧基)‑4‑(4‑吡啶基)苯基]‑2,4‑嘧啶二胺;在二氧化铂的催化下加氢还原,得到最终化合物色瑞替尼。此制备方法简便易行、收率高,质量好,便于工业化生产。
Drugs covered by this patent
- Zykadia (ceritinib) · Novartis
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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