CAS: 315718-06-0; Tert-Butyl Ethyl(2-Oxoethyl)Carbamate

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149794-10-5 152192-95-5 123387-72-4

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乙基(2-羟基乙基)氨基甲酸叔丁酯 Tert-Butyl Ethyl(2-Hydroxyethyl)Carbamate 152192-95-5

📜乙基(2-羟基乙基)氨基甲酸叔丁酯置于2,2,6,6-四甲基哌啶氧化物,碘苯二乙酸体系中,化学反应生成 N-Boc-(乙基氨基)乙醛
参考文献:Rigorous Control Of Vesicle-Forming Lipid Pka By Fluorine-Conjugated Bioisosteres For Gene-Silencing With Sirna
标题:Rigorous Control Of Vesicle-Forming Lipid Pka By Fluorine-Conjugated Bioisosteres For Gene-Silencing With Sirna
摘要:While The Influence Of Pk(A) Provided By Amine-Containing Materials In Sirna Delivery Vectors For Use In Genesilencing Has Been Widely Studied,There Are Little Reports In Which Amine Pk(A) Is Controlled Rigorously By Using Bioisosteres And Its Effect On Gene-Silencing. Here,We Report That Amine Pk(A) Could Be Rigorously Controlled By Replacement Of Hydrogen Atom(S) With Fluorine Atom(S). A Series Of Mono-And Di-Amine Lipids With A Different Number Of Fluorine Atoms Were Synthesized. The Pk(A) Of The Polyamine Lipids Was Shifted To A Lower Value With An Increase In The Number Of Fluorine Atoms. The Optimal Pk(A) For High Gene-Silencing Efficiency Varied According To The Number Of Amine Residues In The Polyamine Lipid. Whereas The Endosomal Escape Ability Of Mono-Amine Lipid-Containing Lipid Vesicles (Lvs) Depended On The Pk(A),That Of All Tested Di-Amine Lipid-Containing Lvs Showed Equal Membrane-Destabilizing Activity. Lvs Showing Moderately Weak Interactions With Sirna Facilitated Cytoplasmic Release Of Sirna,Resulting In Strong Gene-Silencing. These Findings Indicate That Appropriate Amine Pk(A) Engineering Depending On The Number Of Amines Is Important For The Induction Of Effective Rna Interference.
DOI:10.1016/j.Jconrel.2018.12.044