CN Patent

CN104119324B — 一种卡格列净的制备方法

Assigned to QILU PHARMACEUTICAL (HAINAN) Co.,Ltd. · Expires 2016-03-30 · 10y expired

What this patent protects

本发明公开了一种卡格列净的制备方法。该方法为：(1)以DMF为溶剂，采用苯甲酰氯对主原料SM1的羟基进行保护反应得到中间体I；(2)以乙腈为溶剂，中间体I在亚磷酸三甲酯作用下脱除甲氧基得到中间体II；(3)以四氢呋喃和无水乙醇或甲醇为溶剂，中间体II在甲醇钠作用下脱除苯甲酰基保护得到卡格列净，产品的纯度≥99.9％，收率≥81.6％。该方法的反应条件温和，经济环保，且收率高，产品质量好，易于工业生产。

USPTO Abstract

本发明公开了一种卡格列净的制备方法。该方法为：(1)以DMF为溶剂，采用苯甲酰氯对主原料SM1的羟基进行保护反应得到中间体I；(2)以乙腈为溶剂，中间体I在亚磷酸三甲酯作用下脱除甲氧基得到中间体II；(3)以四氢呋喃和无水乙醇或甲醇为溶剂，中间体II在甲醇钠作用下脱除苯甲酰基保护得到卡格列净，产品的纯度≥99.9％，收率≥81.6％。该方法的反应条件温和，经济环保，且收率高，产品质量好，易于工业生产。

Drugs covered by this patent

Patent Metadata

Patent number
CN104119324B
Jurisdiction
CN
Classification
—
Expires
2016-03-30
Drug substance claim
No
Drug product claim
No
Assignee
QILU PHARMACEUTICAL (HAINAN) 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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