CN111057729B — 一种(r)-2-(2,5-二氟苯基)吡咯烷及其制备方法和应用
Assigned to Yikelai Biotechnology Group Co ltd · Expires 2023-08-29 · 3y expired
What this patent protects
本发明公开了一种(R)‑2‑(2,5‑二氟苯基)吡咯烷及其制备方法和应用。所述的制备方法包括：在亚胺还原酶和还原型辅酶NADPH的存在下，将5‑(2,5‑二氟苯基)‑3,4‑二氢‑2H‑吡咯进行加氢还原反应，即可。利用本发明的制备方法制备得到的R型的2‑(2,5‑二氟苯基)吡咯烷，ee值至少可达94％，通过HPLC检测转化率至少可达84％；满足了(R)‑2‑(2,5‑二氟苯基)吡咯烷和larotrectinib的工业化生产需求；且本发明制备方法比化学方法成本更低，环境更加友好。
USPTO Abstract
本发明公开了一种(R)‑2‑(2,5‑二氟苯基)吡咯烷及其制备方法和应用。所述的制备方法包括：在亚胺还原酶和还原型辅酶NADPH的存在下，将5‑(2,5‑二氟苯基)‑3,4‑二氢‑2H‑吡咯进行加氢还原反应，即可。利用本发明的制备方法制备得到的R型的2‑(2,5‑二氟苯基)吡咯烷，ee值至少可达94％，通过HPLC检测转化率至少可达84％；满足了(R)‑2‑(2,5‑二氟苯基)吡咯烷和larotrectinib的工业化生产需求；且本发明制备方法比化学方法成本更低，环境更加友好。
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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