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

All articles of this category 3,4-Disubstituted-2(1 H )-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(1 H )-quinolones are useful synthetic intermediates for the preparation of 3,4-disubstituted- and 2,3,4-trisubstituted quinolines. quinolones - quinolines - palladium catalysis - coupling