📜间三氟甲氧基苯腈置于lithium Hexamethyldisilazane体系中,化学反应生成 3-三氟甲氧基苯甲脒
参考文献:Pyrimidine Benzamide-Based Thrombopoietin Receptor Agonists
标题:Pyrimidine Benzamide-Based Thrombopoietin Receptor Agonists
摘要:A Series Of Pyrimidine Benzamide-Based Thrombopoietin Receptor Agonists Is Described. The Lead Molecule Contains A 2-Amino-5-Unsubstituted Thiazole,A Group That Has Been Associated With Idiosyncratic Toxicity. The Potential For Metabolic Oxidation At C-5 Of The Thiazole,The Likely Source Of Toxic Metabolites,Was Removed By Substitution At C-5 Or By Replacing The Thiazole With A Thiadiazole. Potency In The Series Was Improved By Modifying The Substituents On The Pyrimidine And/or On The Thiazole Or Thiadiazole Pendant Aryl Ring. In Vivo Examination Revealed That Compounds From The Series Are Not Highly Bioavailable. This Is Attributed To Low Solubility And Poor Permeability. (C) 2007 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2007.07.038