CAS: 21176-60-3; 2-Amino-4-Phenylbutanoic Acid Hydrochloride

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1012-05-1 100564-78-1 127862-89-9

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1-phenyl-2-bromoethane 2-acetylaminomalonic acid diethyl ester tert-butyl 1-hydroxy-3-phenylpropan-2-ylcarbamate methanesulfonyl chloride2-(RS)-amino-4-phenylbutyric acid ethyl ester hydr°Chloride 2-(RS)-(2-aminobenzoylamino)-4-phenylbutyric acid ethyl ester 2-(RS)-{2-[(1H-indole-2-carbonyl)amino]benzoylamino}-4-phenylbutyric acid ethyl ester (RS)-1H-indol-2-carboxylic acid 2-(1-hydroxycarbamoyl-3-phenylpropylcarbamoyl)phenylamide

📜2-乙酰氨基-2-苯乙基丙二醇二乙酯置于盐酸体系中,用 1,4-二氧六环,水 用作溶剂,以53%的收率获得l-苯基丁氨酸 盐酸盐
参考文献:New Anthranilic Acid Based Antagonists With High Affinity And Selectivity For The Human Cholecystokinin Receptor 1 (Hcck1-R)
标题:New Anthranilic Acid Based Antagonists With High Affinity And Selectivity For The Human Cholecystokinin Receptor 1 (Hcck1-R)
摘要:The Anthranilic Acid Diamides Represent The Most Recent Class Of Nonpeptide Cck1 Receptor (Cck1-R) Antagonists. Herein We Describe The Second Phase Of The Anthranilic Acid C-Terminal Optimization Using Nonproteinogenic Amino Acids Containing A Phenyl Ring In Their Side Chain. The Homo-Phe Derivative 2 (Vl-0797) Enhanced 12-Fold The Affinity For The Rat Cck1-R Affinity And 15-Fold For The Human Cck1-R Relative To The Reference Compound 12 (Vl-0395). The Eutomer Of 2 (6) Exhibited A Nanomolar Range Affinity Toward The Human Cck1-R And Was At Least 400-Fold Selective For The Cck1-R Over The Cck2-R. Molecular Docking In The Modeled Cck1-R And Its Validation By Site-Directed Mutagenesis Experiments Showed That The 6 Binding Site Overlaps That occupied By The C-Terminal Bioactive Region Of The Natural Agonist Cck. Owing To Their Interesting Properties,New Compounds Provided By This Study Represent A Solid Basis For Further Advances Aimed At Synthesis Of Clinically Valuable Cck1-R Antagonists.
Doi:10.1021/jm200438B