📜3-碘-2-羟基-5-硝基吡啶置于氢氧化钾,Tetrafluoroboric Acid,铁粉,溶剂黄146,Sodium Nitrite,三溴氧磷体系中,用 喹啉,水,异丙醇,甲苯 作为反应溶剂,化学反应 2.33H,反应生成 2-溴-3-碘-5-羟基-吡啶
参考文献:5-Substituted Derivatives Of 6-Halogeno-3-((2-(S)-Azetidinyl)Methoxy)Pyridine And 6-Halogeno-3-((2-(S)-Pyrrolidinyl)Methoxy)Pyridine With Low Picomolar Affinity For α4β2 Nicotinic Acetylcholine Receptor And Wide Range Of Lipophilicity: Potential Probes For Imaging With Positron Emission Tomography
标题:5-Substituted Derivatives Of 6-Halogeno-3-((2-(S)-Azetidinyl)Methoxy)Pyridine And 6-Halogeno-3-((2-(S)-Pyrrolidinyl)Methoxy)Pyridine With Low Picomolar Affinity For α4β2 Nicotinic Acetylcholine Receptor And Wide Range Of Lipophilicity: Potential Probes For Imaging With Positron Emission Tomography
摘要:Potential Positron Emission Tomography (Pet) Ligands With Low Picomolar Affinity At The Nicotinic Acetylcholine Receptor (Nachr) And With Lipophilicity (Log D) Ranging From-1.6 To +1.5 Have Been Synthesized. Most Members Of The Series,Which Are Derivatives Of 5-Substituted-6-Halogeno-A-85380,Exhibited A Higher Binding Affinity At Alpha4Beta2-Nachrs Than Epibatidine. An Analysis,By Molecular Modeling,Revealed An Important Role Of The Orientation Of The Additional Heterocyclic Ring On The Binding Affinity Of The Ligands With Nachrs. The Existing Nicotinic Pharmacophore Models Do Not Accommodate This Finding. Two Compounds Of The Series,6-[f-18]-Fluoro-5-(Pyridin-3-yl)-A-85380 ([f-18]31) And 6-Chloro-3-((2-(S)-Azetidinyl)Methoxy)-5-(2-[f-18]-Fluoropyridin-5-yl)Pyridine) ([f-18]35),Were Radiolabeled With F-18. Comparison Of Pet Data For [f-18]31 And 2-[f-18]Fa Shows The Influence Of Lipophilicity On The Binding Potential. Our Recent Pet Studies With [f-18]35 Demonstrated That Its Binding Potential Values In Rhesus Monkey Brain Were Ca. 2.5 Times Those Of 2-[f-18]Fa. Therefore,[f-18]35 And Several Other Members Of The Series,When Radiolabeled,Will Be Suitable For Quantitative Imaging Of Extrathalamic Nachrs.
DOI:10.1021/jm030432V