A chemoselective synthesis of novel indolizine derivatives were reported via three-component reactions of aminopyridines, acetylenic diesters and alpha-halo ketones. In these reactions, the zwitterion generated from aminopyridines and acetylenic diesters reacted with alpha-halo ketones to produce indolizine skeleton in good to high yields under mild reaction conditions. (C) 2015 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.