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Cyclocondensation reactions of 5-aminopyrazoles, pyruvic acids and aldehydes. Multicomponent approaches to pyrazolopyridines and related products by Biotage Initiator耐士科技

2015-02-09 10:22

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The reactions of 3-substituted 5-aminopyrazoles with arylidenepyruvic acids and their synthetic precursors, pyruvic acid and aromatic aldehydes, were studied. Several different reaction pathways for these cyclocondensation reactions were established depending on the reaction conditions and building block selection. The formation of pyrazolo[3,4-b]pyridine-6-carboxylic acids as major products and related compounds was discussed from the mechanistic point of view.
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We herein report several highly active catalyst systems with thiadiazolidine 1-oxides as ligands for palladium in the MizorokieHeck reaction. Excellent yields of stilbenes derived from aryl iodides and bromides have been achieved using as little as 0.00002 mol % catalyst. The ligand/palladiumsystem can be stored as a stock solution open to air at room temperature with no observable loss of activity for a period of several months.

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