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

Marquise Nada; Tan Tai Nguyen; Chevallier Floris; Picot Laurent; Thiery Valerie<sup>*</sup>; Lozach Olivier; Bach Stephane; Ruchaud Sandrine; Mongin Florence

doi:10.1055/s-0035-1560496

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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

作者：Marquise Nada; Tan Tai Nguyen; Chevallier Floris; Picot Laurent; Thiery Valerie^*; Lozach Olivier; Bach Stephane; Ruchaud Sandrine; Mongin Florence

来源：Synlett, 2015, 26(20): 2811-2816.

DOI：10.1055/s-0035-1560496

摘要

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.