1-Boc-4-哌啶甲酸置于正丁基锂,三乙胺,二异丙胺体系中,用 四氢呋喃,正己烷 用作溶剂,化学反应 13.0H,反应生成N-Boc-4-甲基-4-哌啶甲酸乙酯
参考文献:Pyrazolopyrimidines As Potent Stimulators For Transient Receptor Potential Canonical 3/6/7 Channels
标题:Pyrazolopyrimidines As Potent Stimulators For Transient Receptor Potential Canonical 3/6/7 Channels
摘要:Transient Receptor Potential Canonical 3/6/7 (Trpc3/6/7) Are Highly Homologous Receptor-Operated Nonselective Cation Channels. Despite Their Physiological Significance,Very Few Selective And Potent Agonists Are Available For Functional Examination Of These Channels. Using A Cell-Based High Throughput Screening Approach,A Lead Compound With The Pyrazolopyrimidine Skeleton Was Identified As A Trpc6 Agonist. Synthetic Schemes For The Lead And Its Analogues Were Established,And Structural Activity Relationship Studies Were Carried Out. A Series Of Potent And Direct Agonists Of Trpc3/6/7 Channels Were Identified,And Among Them,4M-4P Have A Potency Order Of Trpc3 > C7 > C6,With 4N Being The Most Potent With An Ec50 Of <20 Nm On Trpc3. Importantly,These Compounds Exhibited No Stimulatory Activity On Related Trp Channels. The Potent And Selective Compounds Described Here Should Be Suitable For Evaluation Of The Roles Of Trpc Channels In The Physiology And Pathogenesis Of Diseases,Including Glomerulosderosis And Cancer.
Doi:10.1021/acs.Jmedchem.7B00304