CN114907315B — Selitrectinib中间体的合成方法
Assigned to Chongqing Medical University · Expires 2023-09-12 · 3y expired
What this patent protects
本发明提供Selitrectinib中间体2‑氯‑5‑氟‑3‑(吡咯烷‑2‑基)吡啶和中间体5‑氯吡唑[1,5‑a]嘧啶‑3‑羧酸乙酯的合成方法。2‑氯‑5‑氟‑3‑(吡咯烷‑2‑基)吡啶以对2‑氯‑5‑氟烟酸为起始原料，与氯化亚砜酯化形成2‑氯‑5‑氟烟酸乙酯，然后与与1‑乙烯基吡咯烷酮缩合得到3‑(2‑氯‑5‑氟烟碱酰基)‑1‑乙烯基吡咯烷‑2‑酮，之后重排得到2‑氯‑5‑氟‑3‑(吡咯烷‑2‑基)吡啶，然后与还原试剂反应制得。5‑氯吡唑[1,5‑a]嘧啶‑3‑羧酸乙酯以1,3‑二甲基嘧啶‑2,4(1H，3H)‑二酮为原料，与3‑氨基‑1H‑吡唑‑4…
USPTO Abstract
本发明提供Selitrectinib中间体2‑氯‑5‑氟‑3‑(吡咯烷‑2‑基)吡啶和中间体5‑氯吡唑[1,5‑a]嘧啶‑3‑羧酸乙酯的合成方法。2‑氯‑5‑氟‑3‑(吡咯烷‑2‑基)吡啶以对2‑氯‑5‑氟烟酸为起始原料，与氯化亚砜酯化形成2‑氯‑5‑氟烟酸乙酯，然后与与1‑乙烯基吡咯烷酮缩合得到3‑(2‑氯‑5‑氟烟碱酰基)‑1‑乙烯基吡咯烷‑2‑酮，之后重排得到2‑氯‑5‑氟‑3‑(吡咯烷‑2‑基)吡啶，然后与还原试剂反应制得。5‑氯吡唑[1,5‑a]嘧啶‑3‑羧酸乙酯以1,3‑二甲基嘧啶‑2,4(1H，3H)‑二酮为原料，与3‑氨基‑1H‑吡唑‑4‑羧酸乙酯反应得到5‑氧代‑4,5‑二氢吡唑[1,5‑a]嘧啶‑2‑羧酸乙酯，然后取代得到。
Drugs covered by this patent
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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