CN116675690B — 一种肺癌治疗药物的制备方法
Assigned to Beijing Kang Lisheng Pharmaceutical Technology Development Co ltd · Expires 2026-03-27 · 0y expired
What this patent protects
本发明公开了一种肺癌治疗药物阿达格西布的制备方法：步骤1、1‑氯‑8‑碘萘与4‑氯‑2‑(甲硫基)‑5,6,7,8‑四氢吡啶并[3,4‑d]嘧啶经C‑N偶联反应，得到4‑氯‑7‑(8‑氯萘‑1‑基)‑2‑(甲硫基)‑5,6,7,8‑四氢吡啶并[3,4‑d]嘧啶；步骤2、步骤1产物经氧化反应得到4‑氯‑7‑(8‑氯萘‑1‑基)‑2‑(甲基亚磺酰基)‑5,6,7,8‑四氢吡啶并[3,4‑d]嘧啶；步骤3、步骤2产物与[(2S)‑1‑甲基吡咯烷‑2‑基]甲醇对接反应、再与(S)‑2‑(1‑(2‑氟丙烯酰基)哌嗪‑2‑基)乙腈经C‑N偶联反应得到阿达格西布。本发…
USPTO Abstract
本发明公开了一种肺癌治疗药物阿达格西布的制备方法：步骤1、1‑氯‑8‑碘萘与4‑氯‑2‑(甲硫基)‑5,6,7,8‑四氢吡啶并[3,4‑d]嘧啶经C‑N偶联反应，得到4‑氯‑7‑(8‑氯萘‑1‑基)‑2‑(甲硫基)‑5,6,7,8‑四氢吡啶并[3,4‑d]嘧啶；步骤2、步骤1产物经氧化反应得到4‑氯‑7‑(8‑氯萘‑1‑基)‑2‑(甲基亚磺酰基)‑5,6,7,8‑四氢吡啶并[3,4‑d]嘧啶；步骤3、步骤2产物与[(2S)‑1‑甲基吡咯烷‑2‑基]甲醇对接反应、再与(S)‑2‑(1‑(2‑氟丙烯酰基)哌嗪‑2‑基)乙腈经C‑N偶联反应得到阿达格西布。本发明所述阿达格西布的合成方法，相对现有技术具有路线短、起始原料易定制、操作安全简单、成本低和环境友好等优点。
Drugs covered by this patent
- Krazati (ADAGRASIB) · Bristol-Myers Squibb
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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