CAS: 1061605-21-7; 2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-Dioxoisoindolin-4-yl)Oxy)Acetic Acid

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4-Hydroxythalidomide 3-hydroxyphthalic anhydride 3-nitrophthalic acid anhydride 3-aminophthalic anhydride dBET6

📜3-硝基邻苯二甲酸酐置于偶氮二甲酸二异丙酯,硫酸,Palladium 10% On Activated Carbon,Palladium On Activated Carbon,氢气,Magnesium Sulfate,三乙胺,三苯基膦体系中,用 四氢呋喃,二氯甲烷,乙酸乙酯 用作溶剂,140.0 °C,101.33 Kpa 条件下,反应 118.0H,反应生成2-[[[2-(2,6-二氧代-3-哌啶基)-2,3-二氢-1,3-二氧代-1H-异吲哚-4-基]氧基]乙酸
参考文献:Practical Synthesis Of A Phthalimide-Based Cereblon Ligand To Enable Protac Development
标题:Practical Synthesis Of A Phthalimide-Based Cereblon Ligand To Enable Protac Development
摘要:The Use Of Small Molecules To Regulate Cellular Levels Of Specific Proteins Is Poised To Become A Powerful Technique In The Coming Years. Critical To The Success Of Any Project Utilizing Such An Approach Will Be The Ability To Synthesize Libraries Of Candidate Small Molecules For Testing In Cellular Systems. Herein,We Describe A Practical Synthesis Of A Phthalimide-Based Scaffold,Which Can Be Easily Diversified To Make Cereblon-Targeting Protacs. We Demonstrate The Effectiveness Of This Approach By Synthesizing A 'Protac Toolbox' Of Four Amines Which Can Be Coupled To Inhibitors In A Straightforward Manner. (C) 2016 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2016.09.048