CN Patent

CN114262291B — 一种阿伐可泮的合成方法

Assigned to Chongqing Medical University · Expires 2023-05-19 · 3y expired

What this patent protects

本发明提供一种阿伐可泮的合成方法，通过关环、手性还原、偶联环戊酮，再偶联4‑甲基‑3‑(三氟甲基)苯胺等步骤制得阿伐可泮，制备过程避免了手性拆分，提高了终产物收率。本发明使用二(1,5‑环辛二烯)四氟硼酸铑(I)(Rh(COD) 2 BF 4 为催化剂，(R)‑Ligand 1为催化剂的配体，并结合特定的工艺参数进行制备化合物4，产物收率高，且ee值高。本发明经过4步反应得到阿伐可泮，终产物收率可达42.55％，具有明显的工业实用性。

USPTO Abstract

本发明提供一种阿伐可泮的合成方法，通过关环、手性还原、偶联环戊酮，再偶联4‑甲基‑3‑(三氟甲基)苯胺等步骤制得阿伐可泮，制备过程避免了手性拆分，提高了终产物收率。本发明使用二(1,5‑环辛二烯)四氟硼酸铑(I)(Rh(COD) 2 BF 4 为催化剂，(R)‑Ligand 1为催化剂的配体，并结合特定的工艺参数进行制备化合物4，产物收率高，且ee值高。本发明经过4步反应得到阿伐可泮，终产物收率可达42.55％，具有明显的工业实用性。

Drugs covered by this patent

Patent Metadata

Patent number
CN114262291B
Jurisdiction
CN
Classification
—
Expires
2023-05-19
Drug substance claim
No
Drug product claim
No
Assignee
Chongqing Medical University
Source
FDA Orange Book + USPTO grounding via Google Patents

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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