CN Patent

CN109810065B — 一种恶拉戈利的合成方法

Assigned to Anhui Nature Pharmaceutical Co ltd · Expires 2022-07-15 · 4y expired

What this patent protects

本发明公开了一种恶拉戈利的合成方法，包括以下步骤：(1)将如式II所示的(R)‑(2‑(5‑(2‑氟‑3‑甲氧基苯基)‑3‑(2‑氟‑6‑(三氟甲基)苄基)‑4‑甲基‑2,6‑二氧代‑3,6‑二氢嘧啶‑1(2H)‑基)‑1‑苯乙基)氨基甲酸叔丁酯与如式IV所示的4‑溴丁酸乙酯经N‑烷基化得到如式VI所示中间体； (2)将如式VI所示的中间体经脱N‑BOC和O‑Et后得到如式(I)所示的Elagolix；本发明的优点在于，合成路线简单、副产物少、易于纯化。

USPTO Abstract

本发明公开了一种恶拉戈利的合成方法，包括以下步骤：(1)将如式II所示的(R)‑(2‑(5‑(2‑氟‑3‑甲氧基苯基)‑3‑(2‑氟‑6‑(三氟甲基)苄基)‑4‑甲基‑2,6‑二氧代‑3,6‑二氢嘧啶‑1(2H)‑基)‑1‑苯乙基)氨基甲酸叔丁酯与如式IV所示的4‑溴丁酸乙酯经N‑烷基化得到如式VI所示中间体； (2)将如式VI所示的中间体经脱N‑BOC和O‑Et后得到如式(I)所示的Elagolix；本发明的优点在于，合成路线简单、副产物少、易于纯化。

Drugs covered by this patent

Patent Metadata

Patent number: CN109810065B
Jurisdiction: CN
Classification: —
Expires: 2022-07-15
Drug substance claim: No
Drug product claim: No
Assignee: Anhui Nature Pharmaceutical Co ltd
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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