CN Patent

CN101973997B — 一种磷酸西他列汀侧链的制备方法

Assigned to Zhejiang University ZJU · Expires 2012-06-06 · 14y expired

What this patent protects

本发明公开了一种结构如式1所示的磷酸西他列汀侧链的制备方法，包括如下步骤：a)用硫化试剂使结构如式2所示的2-哌嗪酮硫化得到结构如式4所示的2-哌嗪硫酮；所述的硫代试剂为五硫化二磷或者结构如式3所示的Lawesson试剂；b)使式5所示的三氟乙酸肼和2-哌嗪硫酮通过Pellizzari反应环合、加入盐酸成盐，即得到目标产物3-三氟甲基-[1，2，4]三唑[4，3-a]哌嗪盐酸盐。本发明方法不仅路线较短，原料便宜易得，同时操作简单，各步收率较高，成本相对较低。

USPTO Abstract

本发明公开了一种结构如式1所示的磷酸西他列汀侧链的制备方法，包括如下步骤：a)用硫化试剂使结构如式2所示的2-哌嗪酮硫化得到结构如式4所示的2-哌嗪硫酮；所述的硫代试剂为五硫化二磷或者结构如式3所示的Lawesson试剂；b)使式5所示的三氟乙酸肼和2-哌嗪硫酮通过Pellizzari反应环合、加入盐酸成盐，即得到目标产物3-三氟甲基-[1，2，4]三唑[4，3-a]哌嗪盐酸盐。本发明方法不仅路线较短，原料便宜易得，同时操作简单，各步收率较高，成本相对较低。

Drugs covered by this patent

Patent Metadata

Patent number
CN101973997B
Jurisdiction
CN
Classification
—
Expires
2012-06-06
Drug substance claim
No
Drug product claim
No
Assignee
Zhejiang University ZJU
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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