N-aryl heterocycles via coupling reactions with arylboronic acids

Add time:09/05/2019    Source:sciencedirect.com

Compounds having a partial 2-pyridone structure or 3-pyridazinones can be selectively N-arylated with phenylboronic acids according to the procedure described by Chan and Lam. This procedure leads to N5-arylated imidazo[4,5-c]pyridin-4-ones, precursors of potent factor Xa inhibitors. In addition, the synthesis of N-aryl substituted pyrrole- and indole-2-carboxylic acid esters is described. In the indole series this procedure offers a flexible entry in the synthesis of different 1,3-diaryl-2-carboxyindoles.

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