CN Patent

CN103626774B — 伊鲁替尼的制备方法

Assigned to Tongling Wangyantang Biotechnology Co ltd · Expires 2015-11-04 · 11y expired

What this patent protects

本发明揭示了一种伊鲁替尼(Ibrutinib，I)的制备方法，其制备步骤包括：以4-苯氧基苯甲酰氯(II)为原料，与丙二腈和硫酸二甲酯发生缩合和甲氧化反应生成4-苯氧基苯基(甲氧基)亚乙烯基二氰甲烷(III)，该中间体(III)与1-(3R-肼基-1-哌啶基)-2-丙烯-1-酮(IV)发生吡唑环化反应得1-[(3R)-[3-(4-苯氧基苯基)-4-腈基-5-氨基-1H-吡唑基]-1-哌啶基]-2-丙烯-1-酮(V)，该中间体(V)与环合剂发生嘧啶环化反应制得伊鲁替尼(I)。该制备方法原料易得，工艺简洁，经济环保，适合工业化生产。

USPTO Abstract

本发明揭示了一种伊鲁替尼(Ibrutinib，I)的制备方法，其制备步骤包括：以4-苯氧基苯甲酰氯(II)为原料，与丙二腈和硫酸二甲酯发生缩合和甲氧化反应生成4-苯氧基苯基(甲氧基)亚乙烯基二氰甲烷(III)，该中间体(III)与1-(3R-肼基-1-哌啶基)-2-丙烯-1-酮(IV)发生吡唑环化反应得1-[(3R)-[3-(4-苯氧基苯基)-4-腈基-5-氨基-1H-吡唑基]-1-哌啶基]-2-丙烯-1-酮(V)，该中间体(V)与环合剂发生嘧啶环化反应制得伊鲁替尼(I)。该制备方法原料易得，工艺简洁，经济环保，适合工业化生产。

Drugs covered by this patent

Patent Metadata

Patent number
CN103626774B
Jurisdiction
CN
Classification
—
Expires
2015-11-04
Drug substance claim
No
Drug product claim
No
Assignee
Tongling Wangyantang 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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