Synthesis method of a JAK inhibitor drug intermediate and application thereof
CN117924272BActive Publication Date: 2026-10-23ZHUHAI UNITED LAB
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Patent Information
- Application Number
- CN202211328486.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2022-10-26
- Publication Date
- 2026-10-23
- Estimated Expiration
- 2042-10-26
AI Technical Summary
Technical Problem
[0006]经过实际研究发现，该方法存在：(1)杂质多难去除，且原料、副产物与产物极性较接近，分离纯化困难，多步需要重复多次柱层析，溶剂用量大，成本高，周期长；(2)硼酸化和偶联反应均使用有机钯催化剂，有机钯催化剂易溶于有机溶剂，去除困难，存在重金属超标的风险
Benefits of technology
[0066](1)本发明提供的合成方法比现有技术合成路线更短；
✦ Generated by Eureka AI based on patent content.
Abstract
The application discloses a synthesis method of a JAK inhibitor drug intermediate and application thereof. The compound C with the structure as shown in formula (V) is prepared by treating compound A with the structure as shown in formula (III) and compound B with the structure as shown in formula (IV) by an organic lithium reagent; and the target compound, i.e. the compound with the structure as shown in formula (II), is prepared by dehydrating the compound C with the structure as shown in formula (V). The synthesis route of the application is short; no organic palladium catalyst is used, and there is no risk of residual heavy metal palladium, so the application is more green; the product obtained by the application has less impurities, no column chromatography is used for purification, the purification is simple, and the application is more suitable for industrial mass production; and the yield is high.
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