CAS: 142995-31-1; (S)-2-((Tert-Butoxycarbonyl)Amino)-3-(3-(Trifluoromethyl)Phenyl)Propanoic Acid

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tert-butyl dicarbonatedi-tert-butyl dicarbonate (2S)-2-amino-3-[3-(trifluoromethyl)phenyl]propanoic acid3)-NMeBzlB°C-Phe(3-CF3)-NMeBzl tert-butyl ester[1-(methoxy-methyl-carbamoyl)-2-(3-trifluoromethyl-phenyl)-ethyl]-carbamic acid tert-butyl ester tert-butyl ester[1-formyl-2-(3-trifluoromethyl-phenyl)-ethyl]-carbamic acid tert-butyl ester (S)-2-Amino-N-[(S)-2-ethylcarbamoyl-2-hydroxy-1-(3-trifluoromethyl-benzyl)-ethyl]-3-methyl-butyramide

📜二碳酸二叔丁酯,Phe(3-Cf3)置于三乙胺体系中,用 水,丙酮 用作溶剂,化学反应生成Boc-L-3-三氟甲基苯丙氨酸
参考文献:Studies On Neurokinin Antagonists. 4. Synthesis And Structure-Activity Relationships Of Novel Dipeptide Substance P Antagonists: N2-[(4R)-4-Hydroxy-1-[(1-Methyl-1H-Indol-3-yl)Carbonyl]-L-Prolyl]-N-Methyl-N-(Phenylmethyl)-3-(2-Naphthyl)-L-Alaninamide And Its Related Compounds
标题:Studies On Neurokinin Antagonists. 4. Synthesis And Structure-Activity Relationships Of Novel Dipeptide Substance P Antagonists: N2-[(4R)-4-Hydroxy-1-[(1-Methyl-1H-Indol-3-yl)Carbonyl]-L-Prolyl]-N-Methyl-N-(Phenylmethyl)-3-(2-Naphthyl)-L-Alaninamide And Its Related Compounds
摘要:As An Extension Of Our Studies On Discovering A Novel Substance P (Sp) Antagonist,We Modified The Previously Reported Dipeptide,N-2-[n-2-(1H-Indol-3-Ylcarbonyl)-L-Lysyl]-N-Methyl-N-(Phenylmethyl)-L-Phenylalaninamide (2B). The Lysine Part In 2B Was First Optimized To A (2S,4R)Hydroxyproline Derivative (3H),Which Is 2-Fold More Potent Than 2B In [h-3]Sp Binding Assay Using Guinea Pig Lung Membranes. Next We Modified The 1H-Indol-3-Ylcarbonyl Part In 3H. Introduction; Of A Methyl Group At The Indole Nitrogen Enhanced The Oral Activity,While Retaining The Binding Activity. Finally,We Modified The Phenylalanine Part To Culminate In The Most Potent Compound 7K (Fk888),Which Is A Potent Sp Antagonist With Nk1 Selectivity As Well As Oral Activity.
Doi:10.1021/jm00039A022