Amination of Phosphorodiamidate-Substituted Pyridines and Related <i>N</i>-Heterocycles with Magnesium Amides
作者:Moritz Balkenhohl、Benjamin Heinz、Thomas Abegg、Paul Knochel
DOI:10.1021/acs.orglett.8b03698
日期:2018.12.21
The amination of various phosphorodiamidate-substituted pyridines, quinolines, and quinoxaline with magnesium amides R2NMgCl·LiCl proceeds at room temperature within 8 h. Several pharmaceutically active amines were suitable substrates for this amination procedure, and also the antihistaminic tripelennamine was prepared. Additionally, several heterocyclic phosphorodiamidates underwent directed ortho-metalation
各种二氨基磷酸酯基取代的吡啶,喹啉,并用镁酰胺喹喔啉的胺化- [R 2个8小时内于室温下NMgCl·LiCl前进。几种药物活性胺是用于该胺化程序的合适底物,并且还制备了抗组胺的三烯胺。另外,使用TMPMgCl·LiCl(TMP = 2,2,6,6-四甲基哌啶基)或TMP 2 Mg·2LiCl对几种杂环二氨基氨基磷酸酯进行定向邻位金属化(D o M),然后在胺化步骤之前进行亲电子官能化,导致邻官能化的胺化N-杂环。