Huperzine A C12-site arylated series derivatives as well as preparation method and application of huperzine A C12-site arylated series derivatives
Through palladium-catalyzed heck coupling reaction, aryl groups were introduced at C12 of titanium aryl derivatives were prepared, which solved the problems of large side effects and complex preparation of existing Alzheimer's disease drugs, and achieved high-efficiency and low-toxic acetylcholinesterase inhibitory activity and neuroprotective activity.
Patent Information
- Application Number
- CN202510570468.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-05-06
- Publication Date
- 2025-08-08
AI Technical Summary
The existing Alzheimer's disease treatment drugs have problems such as large side effects, complex preparation methods and inefficient preparation. In particular, long-term use of (-)-Halconazole A may cause dizziness, nausea and digestive disorders, and the existing methods lack fast and efficient chemical modification methods.
Using tetrakisylamine a as the lead compound, aryl groups were introduced at C12 position through a palladium-catalyzed heck coupling reaction to prepare a series of aryl derivatives of aryl derivatives at C12 position. The reaction conditions were 90°C to 110°C for a time of 24 to 48 hours. A catalytic system such as tetrakis(triphenylphosphine)palladium, tris(2-thienyl)phosphine, sodium tert-butoxide were used, and the solvent was toluene.
The rapid, simple and highly chemically selective preparation of titanium methyl derivatives is achieved, providing new structural modification sites, and the derivatives exhibit efficient acetylcholinesterase inhibitory activity and neuroprotective activity, with potential anti-Alzheimer's disease effect.