CAS: 132740-43-3; 4-Fluorobenzylisocyanate

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CAS号32315-10-9 三光气 | CAS号140-75-0 对氟苄胺 | CAS号405-50-5 对氟苯乙酸 | CAS号75-44-5 光气 | CAS号459-04-1 4-氟苯乙酰氯 | CAS号503-38-8 氯甲酸三氯甲酯

对氟苯乙酰氯置于sodium Azide体系中,用 氯仿,水,丙酮 用作溶剂,化学反应 1.0H,反应生成4-氟代苯异氰酸盐
参考文献:Orally Active .Beta.-Lactam Inhibitors Of Human Leukocyte Elastase-1. Activity Of 3,3-Diethyl-2-Azetidinones
标题:Orally Active .Beta.-Lactam Inhibitors Of Human Leukocyte Elastase-1. Activity Of 3,3-Diethyl-2-Azetidinones
摘要:A Thorough Analysis Of The Mechanism Of Inhibition Of Human Leukocyte Elastase (Hle) By A Monocyclic Beta-Lactam And The Mechanism Of Beta-Lactam Hydrolysis Led To The Preparation Of Potent And Highly Stable Inhibitors Of Hle. This Work Led To The Identification Of 4-[(4-Carboxyphenyl)-Oxy]-3,3-Diethyl-1-[[(Phenylmethyl)Amino]Carbonyl]-2-Azetidinone (2) As The First Orally Active Inhibitor Of Human Leukocyte Elastase (Hle). Analogs Of 2 With Different Substituents On The Urea N Were Synthesized And Evaluated For Their Activity In Vitro Against Hle As Well As In Vivo In A Hamster Lung Hemorrhage Model. Compounds With A Methyl Or A Methoxy Group In The Para Position Of The Benzene Ring Were Very Potent In Both Assays. The Results Are Discussed On The Basis Of The Proposed Model For The Binding Of This Class Of Inhibitors To Hle And A Possible Mechanism Of Inhibition Is Presented.
Doi:10.1021/jm00099A003