Azine and Diazine Functionalization Using 2,2,6,6-Tetramethylpiperidino-Based Lithium–Metal Combinations: Application to the Synthesis of 5,9-Disubstituted Pyrido[3′,2′:4,5]pyrrolo[1,2-c] pyrimidines

Abstract : The synthesis of triaryl methanols was investigated by reacting different 4-metalated 2-substituted pyrimidines with diaryl ketones, the latter being generated by deprotocupration-aroylation of azine and diazine substrates. Cyclization of the triaryl methanols thus obtained afforded pyrido[3’,2’:4,5]pyrrolo[1,2-c]pyrimidines, which were evaluated for kinase inhibition and antiproliferative activities in melanoma cells.
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Nada Marquise, Tan Tai Nguyen, Floris Chevallier, Laurent Picot, Valérie Thiéry, et al.. Azine and Diazine Functionalization Using 2,2,6,6-Tetramethylpiperidino-Based Lithium–Metal Combinations: Application to the Synthesis of 5,9-Disubstituted Pyrido[3′,2′:4,5]pyrrolo[1,2-c] pyrimidines. SYNLETT, Georg Thieme Verlag, 2015, 26 (20), pp.2811-2816. ⟨10.1055/s-0035-1560496⟩. ⟨hal-01248092⟩

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