CAS: 69872-15-7; 3-Bromo-4-Methyl-5-Nitropyridine

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CAS号31872-63-6 3-溴-4-氯-5-硝基吡啶 | CAS号105-53-3 丙二酸二乙酯 | CAS号69872-14-6 (3-bromo-5-nitr... | CAS号31872-65-8 3-溴-4-羟基-5-硝基吡啶 | CAS号5435-54-1 4-羟基-3-硝基吡啶 | CAS号69872-17-9 4-溴-1H-吡咯并[2,3-c]吡啶

📜4-羟基-3-硝基吡啶置于溴,Sodium Hydride,二乙胺,三氯氧磷体系中,用 水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 22.5H,反应生成 3-溴-4-甲基-5-硝基吡啶
参考文献:1-(2-Hydroxy-2-Methyl-3-Phenoxypropanoyl)Indoline-4-Carbonitrile Derivatives As Potent And Tissue Selective Androgen Receptor Modulators
标题:1-(2-Hydroxy-2-Methyl-3-Phenoxypropanoyl)Indoline-4-Carbonitrile Derivatives As Potent And Tissue Selective Androgen Receptor Modulators
摘要:We Present A Novel Series Of Selective Androgen Receptor Modulators (Sarms) Which Shows Excellent Biological Activity And Physical Properties. 1-(2-Hydroxy-2-Methyl-3-Phenoxypropanoyl)-Indoline-4-Carbonitriles Showed Potent Binding To The Androgen Receptor (Ar) And Activated Ar-Mediated Transcription In Vitro. Representative Compounds Demonstrated Diminished Activity In Promoting The Intramolecular Interaction Between The Ar Carboxyl (C) And Amino (N) Termini. This N/c-Termini Interaction Is A Biomarker Assay For The Undesired Androgenic Responses In Vivo. In Orchidectomized Rats,Daily Administration Of A Lead Compound From This Series Showed Anabolic Activity By Increasing Levator Ani Muscle Weight. Importantly,Minimal Androgenic Effects (Increased Tissue Weights) Were Observed In The Prostate And Seminal Vesicles,Along With Minimal Repression Of Circulating Luteinizing Hormone (Lh) Levels And No Change In The Lipid And Triglyceride Levels. This Lead Compound Completed A Two Week Rat Toxicology Study,And Was Well Tolerated At Doses Up To 100 Mg/kg/day,The Highest Dose Tested,For 14 Consecutive Days.
DOI:10.1021/jm401625B