Ethyl N-(o-Ethynyl)malonanilide as a Useful Building Block for the Preparation of 3,4-Disubstituted-2(1H)-quinolones, 3,4-Disubstituted- and 2,3,4-Trisubstituted Quinolines

Abstract
3,4-Disubstituted-2(1H)-quinolones have been prepared through a procedure based on the palladium-catalysed reaction of the readily available ethyl-N-(o-ethynyl)malonanilide with aryl, heteroaryl and vinyl halides or vinyl triflates followed by the cyclization of the resulting coupling derivatives under basic conditions. It is shown that 3,4-disubstituted-2(1H)-quinolones are useful synthetic intermediates for the preparation of 3,4-disubstituted- and 2,3,4-trisubstituted quinolines.

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