Copper-catalysed heteroannulation with alkynes: a general and highly regio-and stereoselective method for the synthesis of (E)-2-(2-arylvinyl) quinazolinones
A highly regio-and stereoselective procedure for the synthesis of 2-substituted-1, 2, 3, 4- tetrahydroquinazolinones through a two-step procedure, eg (i) palladium–copper catalysed C-arylation of terminal alkynes and (ii) copper-catalysed cyclisation of disubstituted alkynes, is described. 2-(N-Alkyl-N-prop-2′-ynyl) amino-N′-p-tolyl benzamides 5a and 5b reacted with aryl iodides 2 in the presence of (Ph3P) 2PdCl2 (2.5 mol%), CuI (5mol%), Et3N ( ...