CAS: 136888-20-5; 5-Fluoro-3-Nitropyridin-2(1H)-One

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5-氨基-2-甲氧基吡啶置于盐酸,Tetrafluoroboric Acid,硫酸,硝酸,Sodium Nitrite体系中,用 乙醇,水,甲苯 用作溶剂,化学反应 10.0H,反应生成2-羟基-3-硝基-5-氟吡啶
参考文献:Inhibitors Of Human Immunodeficiency Virus Type 1 (Hiv-1) Attachment. 12. Structure-activity Relationships Associated With 4-Fluoro-6-Azaindole Derivatives Leading To The Identification Of 1-(4-Benzoylpiperazin-1-yl)-2-(4-Fluoro-7-[1,2,3]Triazol-1-Yl-1H-Pyrrolo[2,3-C]Pyridin-3-yl)Ethane-1,2-Dione (Bms-585248)
标题:Inhibitors Of Human Immunodeficiency Virus Type 1 (Hiv-1) Attachment. 12. Structure-activity Relationships Associated With 4-Fluoro-6-Azaindole Derivatives Leading To The Identification Of 1-(4-Benzoylpiperazin-1-yl)-2-(4-Fluoro-7-[1,2,3]Triazol-1-Yl-1H-Pyrrolo[2,3-C]Pyridin-3-yl)Ethane-1,2-Dione (Bms-585248)
摘要:A Series Of Highly Potent Hiv-1 Attachment Inhibitors With 4-Fluoro-6-Azaindole Core Heterocycles That Target The Viral Envelope Protein Gp120 Has Been Prepared. Substitution In The 7-Position Of The Azaindole Core With Amides (12A,B),C-Linked Heterocycles (12C-I),And N-Linked Heterocycles (12M-U) Provided Compounds With Subnanomolar Potency In A Pseudotype Infectivity Assay And Good Pharmacokinetic Profiles In Vivo. A Predictive Model Was Developed From The Initial Sar In Which The Potency Of The Analogues Correlated With The Ability Of The Substituent In The 7-Position Of The Azaindole To Adopt A Coplanar Conformation By Either Forming Internal Hydrogen Bonds Or Avoiding Repulsive Substitution Patterns. 1-(4-Benzoylpiperazin-1-yl)-2-(4-Fluoro-7-[1,2,3]Triazol-1-Yl-1H-Pyrrolo[2,3-C]Pyridin-3-yl)Ethane-1,2-Dione (Bms-585248,12M) Exhibited Much Improved In Vitro Potency And Pharmacokinetic Properties Than The Previous Clinical Candidate Bms-488043 (1). The Predicted Low Clearance In Humans,Modest Protein Binding,And Good Potency In The Presence Of 40% Human Serum For 12M Led To Its Selection For Human Clinical Studies.
Doi:10.1021/jm3016377