CN103288759B — 达克米替尼的制备方法
Assigned to Chongqing Yanchen Medical Technology Co.,Ltd. · Expires 2015-05-20 · 11y expired
What this patent protects
本发明揭示了一种达克米替尼(Dacomitinib,I)的制备方法,包括如下步骤:4-氯-6-氨基-7-羟基喹唑啉(II)和硫酸二甲酯或碘甲烷发生醚化反应生成4-氯-6-氨基-7-甲氧基喹唑啉(III),化合物(III)与4-(1-哌啶基)-2-丁烯酰氯进行酰化反应生成4-氯-6-[4-(1-哌啶基)-1-氧代-2-丁烯-1-基]氨基-7-甲氧基喹唑啉(IV),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
本发明揭示了一种达克米替尼(Dacomitinib,I)的制备方法,包括如下步骤:4-氯-6-氨基-7-羟基喹唑啉(II)和硫酸二甲酯或碘甲烷发生醚化反应生成4-氯-6-氨基-7-甲氧基喹唑啉(III),化合物(III)与4-(1-哌啶基)-2-丁烯酰氯进行酰化反应生成4-氯-6-[4-(1-哌啶基)-1-氧代-2-丁烯-1-基]氨基-7-甲氧基喹唑啉(IV),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
- Vizimpro (Dacomitinib) · Pfizer Inc.
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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