📜2-(4-氟-苯氧基)-5-硝基-吡啶 反应生成6-(4-氟苯氧基)-3-氨基吡啶
参考文献:Potent,Selective Spiropyrrolidine Pyrimidinetrione Inhibitors Of Mmp-13
标题:Potent,Selective Spiropyrrolidine Pyrimidinetrione Inhibitors Of Mmp-13
摘要:Explorations In The Pyrimidinetrione Series Of Mmp-13 Inhibitors Led To The Discovery Of A Series Of Spiro-Fused Compounds That Are Potent And Selective Inhibitiors Of Mmp-13. While Other Spiro-Fused Motifs Are Hydrolytically Unstable,Presumably Due To Electronic Destabilization Of The Pyrimidinetrione Ring,The Spiropyrrolidine Series Does Not Share This Liability. Greater Than 100-Fold Selectivity Versus Other Mmp Family Members Was Achieved By Incorporation Of An Extended Aryl-Heteroaryl P1' Group. When Dosed As The Sodium Salt,These Compounds Displayed Excellent Oral Absorption And Pharmacokinetic Properties. Despite The Selectivity,A Representative Of This Series Produced Fibroplasia In A 14 Day Rat Study. (C) 2007 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2007.09.085