CN Patent

CN106146512B — 依鲁替尼的制备方法

Assigned to Hangzhou Zhongmei Huadong Pharmaceutical Co Ltd · Expires 2018-07-17 · 8y expired

What this patent protects

本发明属于药物合成领域，涉及原料药与中间体的制备，特别涉及一种依鲁替尼1‑[(3R)‑3‑[4‑氨基‑3‑(4‑苯氧基苯基)‑1H吡唑并[3，4‑d]嘧啶‑1‑基]‑1‑哌啶基]‑2‑丙烯‑1‑酮的制备方法，所述方法的特征在于(1)以3‑(4‑苯氧基苯基)‑1H‑吡唑并[3，4‑d]嘧啶‑4‑胺(SM1)和(S)‑1‑叔丁氧羰基‑3‑羟基哌啶(SM2)为起始原料，经Mitsunobu反应，得到中间体‑1：(R)‑3‑(4‑苯氧基苯基)‑1‑(哌啶‑3‑基)‑1H‑吡唑并[3，4‑d]嘧啶‑4‑胺，与丙烯酸酐缩合进行酰胺化反应，经过重结晶制得成品依鲁替尼。

USPTO Abstract

本发明属于药物合成领域，涉及原料药与中间体的制备，特别涉及一种依鲁替尼1‑[(3R)‑3‑[4‑氨基‑3‑(4‑苯氧基苯基)‑1H吡唑并[3，4‑d]嘧啶‑1‑基]‑1‑哌啶基]‑2‑丙烯‑1‑酮的制备方法，所述方法的特征在于(1)以3‑(4‑苯氧基苯基)‑1H‑吡唑并[3，4‑d]嘧啶‑4‑胺(SM1)和(S)‑1‑叔丁氧羰基‑3‑羟基哌啶(SM2)为起始原料，经Mitsunobu反应，得到中间体‑1：(R)‑3‑(4‑苯氧基苯基)‑1‑(哌啶‑3‑基)‑1H‑吡唑并[3，4‑d]嘧啶‑4‑胺，与丙烯酸酐缩合进行酰胺化反应，经过重结晶制得成品依鲁替尼。

Drugs covered by this patent

Patent Metadata

Patent number
CN106146512B
Jurisdiction
CN
Classification
—
Expires
2018-07-17
Drug substance claim
No
Drug product claim
No
Assignee
Hangzhou Zhongmei Huadong 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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