CAS: 697300-68-8; 6-Bromo-5-Iodopyridin-3-Amine

该化合物是一种环环生物化合物,其特点是存在一个以溴和碘原子以及氨基组组成的环状,其特征为:分子结构特征为,一个环形6位置的溴原子和一个环形5位置的碘原子,一个氨基氨基环(-NH2)位于3位置;该化合物一般用于医药化学和研究,原因是其潜在的生物活动以及能够作为更复杂的分子的建筑块.其卤素替代成分可以增强回活动,影响化合物与生物目标的相互作用.氨基生物组的存在还有利于进一步实现功能化,使其成为药物合成的多功能中间体.此外,该化合物的特性,例如溶性与稳定性,可以受到卤素亚体和整个分子结构的电子影响.由于存在卤素,安全性和处理防范措施应当受到观察,因为存在可能对健康造成风险的卤素.

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1138444-06-0 13534-97-9 39856-57-0

上下游产品

CAS号25391-61-1 2-溴-3-碘-5-硝基吡啶 | CAS号25391-58-6 3-碘-2-羟基-5-硝基吡啶

合成工艺路线路线简述

  • 合成目标产物 6-Bromo-5-Iodopyridin-3-Amine 主要起始原料 2-Hydroxy-3-Iodo-5-Nitropyridine 97
  • (文献来源)合成步骤主要原料 2-Hydroxy-3-Iodo-5-Nitropyridine 97
📜3-碘-2-羟基-5-硝基吡啶置于铁粉,溶剂黄146,三溴氧磷体系中,用 喹啉,甲苯 作为反应溶剂,化学反应生成 6-溴-5-碘吡啶-3-胺
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

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✅ COA系统入驻 | 共享模式

合成参考文献

参考DOI号:10.1021/jm030432v
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