CAS: 732245-99-7; 5-Isocyanato-2-Methylpyridine

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3430-14-6 29958-15-4 120739-89-1

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6-methyl-nicotinoyl azide 6-methyl-nicotinoyl chloride 6-methylnicotinic acid sodium is°Cyanate 4-{4-fluoro-3-[3-(6-methyl-pyridin-3-yl)-ureido]-benzyl}-piperazine-1-carboxylic acid tert-butyl ester methyl 4-[(2-fluoro-3-{[(6-methylpyridin-3-yl)carbamoyl]amino}phenyl)methyl]piperazine-1-carboxylate

6-甲基-3-吡啶羰基叠氮化物 以 甲苯 作为反应溶剂,化学反应 1.5H,反应生成 5-异氰基-2-甲基吡啶
参考文献:(+)-(2R,5S)-4-[4-Cyano-3-(Trifluoromethyl)Phenyl]-2,5-Dimethyl-N-[6-(Trifluoromethyl)Pyridin-3-Yl]Piperazine-1-Carboxamide (Ym580) As An Orally Potent And Peripherally Selective Nonsteroidal Androgen Receptor Antagonist
标题:(+)-(2R,5S)-4-[4-Cyano-3-(Trifluoromethyl)Phenyl]-2,5-Dimethyl-N-[6-(Trifluoromethyl)Pyridin-3-Yl]Piperazine-1-Carboxamide (Ym580) As An Orally Potent And Peripherally Selective Nonsteroidal Androgen Receptor Antagonist
摘要:A Novel Series Of Trans-N-Aryl-2,5-Dimethylpiperazine-1-Carboxamide Derivatives Was Synthesized And Their Androgen Receptor (Ar) Antagonist Activities And In Vivo Antiandrogenic Effects Were Evaluated. Pharmacological Assays Indicated That Compound 33 Was A Potent Ar Antagonist,And Subsequent Optical Resolution Provided (+)-(2R,5S)-4-[4-Cyano-3-(Trifluoromethyl)Phenyl]-2,5-Dimethyl-N-[6-(Trifluoromethyl)Pyridin-3-Yl]Piperazine-1-Carboxamide (33A,Ym580) Which Exhibited The Most Potent Antiandrogenic Activity. Unlike Bicalutamide,Compound 33A Decreased The Weight Of Rat Ventral Prostate In A Dose-Dependent Manner (Ed50 = 2.2 Mg/kg/day),And Induced The Maximum Antiandrogenic Effect,Comparable To That Of Surgical Castration,Without Significantly Affecting Serum Testosterone Levels. Compound 33A Is A Promising Clinical Candidate For Prostate Cancer Monotherapy.
DOI:10.1021/jm050293C