CN117430605A — 一种kras g12c抑制剂amg-510中间体的合成方法
Assigned to Guangxi Tianming Pharmaceutical Co ltd · Expires 2024-01-23 · 2y expired
What this patent protects
本发明公开了一种KRAS G12C抑制剂AMG‑510中间体的合成方法，首先2,6‑二氯‑5‑氟‑3‑吡啶甲酸经氯化氨解得到2,6‑二氯‑5‑氟烟酰胺；然后经草酰氯氯化后，通氨气氨解得到N‑氨基甲酰基‑2,6‑二氯‑5‑氟甲酰胺；再加入叔丁醇钠，经环化得到7‑氯‑6‑氟‑4‑羟基吡啶[2,3‑d]嘧啶‑2(1H)‑酮；最后在三苯基膦和偶氮试剂作用下，与2‑异丙基‑4‑甲基吡啶‑3‑醇反应得到AMG‑510中间体7‑氯‑6‑氟‑1‑(2‑异丙基‑4‑甲基吡啶‑3‑基)吡啶[2,3‑d]嘧啶‑2,4(1H,3H)‑二酮。本发明原料获取方便，操作简便，收率较高…
USPTO Abstract
本发明公开了一种KRAS G12C抑制剂AMG‑510中间体的合成方法，首先2,6‑二氯‑5‑氟‑3‑吡啶甲酸经氯化氨解得到2,6‑二氯‑5‑氟烟酰胺；然后经草酰氯氯化后，通氨气氨解得到N‑氨基甲酰基‑2,6‑二氯‑5‑氟甲酰胺；再加入叔丁醇钠，经环化得到7‑氯‑6‑氟‑4‑羟基吡啶[2,3‑d]嘧啶‑2(1H)‑酮；最后在三苯基膦和偶氮试剂作用下，与2‑异丙基‑4‑甲基吡啶‑3‑醇反应得到AMG‑510中间体7‑氯‑6‑氟‑1‑(2‑异丙基‑4‑甲基吡啶‑3‑基)吡啶[2,3‑d]嘧啶‑2,4(1H,3H)‑二酮。本发明原料获取方便，操作简便，收率较高，危险系数小，易于工业化生产。
Drugs covered by this patent
- Lumakras (SOTORASIB) · 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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