CN Patent

CN103012265B — 一种7-氯-5-氧代-2,3,4,5-四氢-1h-1-苯并氮杂卓的制备方法

Assigned to Tianjin Institute of Pharmaceutical Research Co Ltd · Expires 2014-10-15 · 12y expired

What this patent protects

本发明涉及一种7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓的制备方法，7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓是制备精氨酸加压素V2受体拮抗剂托伐普坦的重要中间体。此制备方法以2-氨基-5-氯苯甲酸甲酯和4-溴丁酸乙酯为起始原料，在缚酸剂作用下生成仲胺，再经狄克曼缩合及水解反应，得到目标化合物7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓。此方法较已有方法反应步骤减少，操作简便，产物纯度良好，收率也大大提高，从而可降低生产成本，提高收益。

USPTO Abstract

本发明涉及一种7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓的制备方法，7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓是制备精氨酸加压素V2受体拮抗剂托伐普坦的重要中间体。此制备方法以2-氨基-5-氯苯甲酸甲酯和4-溴丁酸乙酯为起始原料，在缚酸剂作用下生成仲胺，再经狄克曼缩合及水解反应，得到目标化合物7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓。此方法较已有方法反应步骤减少，操作简便，产物纯度良好，收率也大大提高，从而可降低生产成本，提高收益。

Drugs covered by this patent

Patent Metadata

Patent number
CN103012265B
Jurisdiction
CN
Classification
—
Expires
2014-10-15
Drug substance claim
No
Drug product claim
No
Assignee
Tianjin Institute of Pharmaceutical Research 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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