CAS: 174302-46-6; 7-Aminoisoquinolin-1(2H)-One

相似化合物

20141-83-7 93117-08-9 1909309-90-5

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7-硝基异喹啉-1(2H)-酮 7-Nitroisoquinolin-1(2H)-One 20141-83-7

📜2-甲基-5-硝基苯甲酰氯置于palladium 10% On Activated Carbon,氢气,三氟乙酸体系中,用 四氢呋喃,二氯甲烷,水,甲苯 用作溶剂,化学反应 7.33H,反应生成1(2H)-异喹啉-4,7-氨基(9Ci)
参考文献:Discovery Of Phenylglycine Lactams As Potent Neutral Factor Viia Inhibitors
标题:Discovery Of Phenylglycine Lactams As Potent Neutral Factor Viia Inhibitors
摘要:Inhibitors Of Factor Vila (Fviia),A Serine Protease In The Clotting Cascade,Have Shown Strong Antithrombotic Efficacy In Preclinical Thrombosis Models With Minimal Bleeding Liabilities. Discovery Of Potent,Orally Active Fviia Inhibitors Has Been Largely Unsuccessful Because Known Chemotypes Have Required A Highly Basic Group In The Si Binding Pocket For High Affinity. A Recently Reported Fragment Screening Effort Resulted In The Discovery Of A Neutral Heterocycle,7-Chloro-3,4-Dihydroisoquinolin-1(2H)-One,That Binds In The Si Pocket Of Fviia And Can Be Incorporated Into A Phenylglycine Fviia Inhibitor. Optimization Of This Pi Binding Group Led To The First Series Of Neutral,Permeable Fviia Inhibitors With Low Nanomolar Potency.
Doi:10.1021/acsmedchemlett.6B00282