Title of article :
Convenient synthesis of 2-alkylamino-6-carboxy-5,7-diarylcyclopenteno[1,2-b]pyridines via direct acylamination with imidoyl chlorides
Author/Authors :
Hirobumi Takahashi، نويسنده , , Takehiro Fukami، نويسنده , , Hisaki Kojima، نويسنده , , Takeru Yamakawa، نويسنده , , Hiroyuki Takahashi، نويسنده , , Toshihiro Sakamoto، نويسنده , , Teruyuki Nishimura، نويسنده , , Masayuki Nakamura، نويسنده , , Takashi Yosizumi، نويسنده , , Kenji Niiyama، نويسنده , , Norikazu Ohtake، نويسنده , , Takashi Hayama، نويسنده ,
Abstract :
A robust synthetic method for 2-alkylamino-6-carboxy-5,7-diarylcyclopenteno[1,2-b]pyridines via acylamination at the alpha position of the functionalized pyridine system has been developed. The key step in this method was achieved by treatment of the corresponding pyridine N-oxides with 2.5 equiv of imidoyl chlorides in the presence of triethylamine, thus producing the desired 2-acylaminopyridines in good yields (74–96%).
Keywords :
Imidoyl chloride , 2-b]pyridines , Acylamination , ETA antagonist
