CN Patent

CN103288758B — 一种达克米替尼的制备方法

Assigned to Jiangsu Qianyuan Construction Co ltd · Expires 2015-01-21 · 11y expired

What this patent protects

本发明揭示了达克米替尼(dacomitinib，I)的制备方法，包括如下步骤：6-氨基-7-羟基-3,4-二氢喹唑啉-4-酮(II)和硫酸二甲酯或碘甲烷发生醚化反应生成6-氨基-7-甲氧基-3,4-二氢喹唑啉-4-酮(III)，化合物(III)与4-(1-哌啶基)-2-丁烯酰氯进行酰化反应生成6-[4-(1-哌啶基)-1-氧代-2-丁烯-1-基]氨基-7-甲氧基-3,4-喹唑啉-4-酮(IV)，该化合物(IV)与4-氟-3-氯苯胺缩合制得达克米替尼(I)。该制备方法工艺简洁、经济和环保，适合工业化放大的要求。

USPTO Abstract

本发明揭示了达克米替尼(dacomitinib，I)的制备方法，包括如下步骤：6-氨基-7-羟基-3,4-二氢喹唑啉-4-酮(II)和硫酸二甲酯或碘甲烷发生醚化反应生成6-氨基-7-甲氧基-3,4-二氢喹唑啉-4-酮(III)，化合物(III)与4-(1-哌啶基)-2-丁烯酰氯进行酰化反应生成6-[4-(1-哌啶基)-1-氧代-2-丁烯-1-基]氨基-7-甲氧基-3,4-喹唑啉-4-酮(IV)，该化合物(IV)与4-氟-3-氯苯胺缩合制得达克米替尼(I)。该制备方法工艺简洁、经济和环保，适合工业化放大的要求。

Drugs covered by this patent

Patent Metadata

Patent number
CN103288758B
Jurisdiction
CN
Classification
—
Expires
2015-01-21
Drug substance claim
No
Drug product claim
No
Assignee
Jiangsu Qianyuan Construction 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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