CN Patent

CN105884628A — 2,4-二叔丁基-5-氨基酚的制备方法

Assigned to Shanghai Famo Biotechnology Co ltd · Expires 2016-08-24 · 10y expired

What this patent protects

本发明涉及有机合成和原料药中间体的制备技术领域，具体涉及囊性纤维化治疗新药依伐卡托(ivacaftor)的关键中间体2,4‑二叔丁基‑5‑氨基酚的制备方法，包括如下步骤：(1)乙酰化：以(A)间氨基酚、(B)乙酸酐或乙酰氯为原料，反应制备得到N‑(3‑羟基苯基)乙酰胺；(2)叔丁基取代：N‑(3‑羟基苯基)乙酰胺与叔丁醇经浓硫酸催化，制备得到N‑(2,4‑二叔丁基‑5‑羟基苯基乙酰胺；(3)脱乙酰基：N‑(2,4‑二叔丁基‑5‑羟基苯基)乙酰胺用酸或碱水解得到2,4‑二叔丁基‑5‑氨基酚。该合成路线原料易得、反应条件温和、后处理简单方便，适合放大制备，而…

USPTO Abstract

本发明涉及有机合成和原料药中间体的制备技术领域，具体涉及囊性纤维化治疗新药依伐卡托(ivacaftor)的关键中间体2,4‑二叔丁基‑5‑氨基酚的制备方法，包括如下步骤：(1)乙酰化：以(A)间氨基酚、(B)乙酸酐或乙酰氯为原料，反应制备得到N‑(3‑羟基苯基)乙酰胺；(2)叔丁基取代：N‑(3‑羟基苯基)乙酰胺与叔丁醇经浓硫酸催化，制备得到N‑(2,4‑二叔丁基‑5‑羟基苯基乙酰胺；(3)脱乙酰基：N‑(2,4‑二叔丁基‑5‑羟基苯基)乙酰胺用酸或碱水解得到2,4‑二叔丁基‑5‑氨基酚。该合成路线原料易得、反应条件温和、后处理简单方便，适合放大制备，而且收率高。

Drugs covered by this patent

Patent Metadata

Patent number: CN105884628A
Jurisdiction: CN
Classification: —
Expires: 2016-08-24
Drug substance claim: No
Drug product claim: No
Assignee: Shanghai Famo Biotechnology 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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