CN108017612B — 一种坎格列净中间体的制备方法
Assigned to Nantong Changyou Pharmaceutical Science & Technology Co ltd · Expires 2020-06-09 · 6y expired
What this patent protects
本发明公开了一种坎格列净中间体的制备方法,以取代溴苯为起始原料,首先与联硼酸频那醇酯制备成硼化物,再经Suzuki偶联反应、付克酰基化反应及还原反应制备得到。本发明的优点是:通过Suzuki偶联反应制备中间产物CZ‑2,条件温和,易于操作和控制,产品收率及纯度好,再经付克酰基化反应引入芳甲基,构建出主链,路线收率高,工艺条件易于控制,适合于大规模工业化生产。
USPTO Abstract
本发明公开了一种坎格列净中间体的制备方法,以取代溴苯为起始原料,首先与联硼酸频那醇酯制备成硼化物,再经Suzuki偶联反应、付克酰基化反应及还原反应制备得到。本发明的优点是:通过Suzuki偶联反应制备中间产物CZ‑2,条件温和,易于操作和控制,产品收率及纯度好,再经付克酰基化反应引入芳甲基,构建出主链,路线收率高,工艺条件易于控制,适合于大规模工业化生产。
Drugs covered by this patent
- Invokana (CANAGLIFLOZIN) · Johnson & Johnson
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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