1026504-57-3Relevant articles and documents
Amination of Phosphorodiamidate-Substituted Pyridines and Related N-Heterocycles with Magnesium Amides
Balkenhohl, Moritz,Heinz, Benjamin,Abegg, Thomas,Knochel, Paul
supporting information, p. 8057 - 8060 (2019/01/14)
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 (DoM) using TMPMgCl·LiCl (TMP = 2,2,6,6-tetramethylpiperidyl) or TMP2Mg·2LiCl, followed by electrophilic functionalization prior to the amination step, which led to ortho-functionalized aminated N-heterocycles.