Efficient synthesis of 1-azakenpaullone, a selective inhibitor of glycogen synthase kinase-3β for cellular regeneration†

Abstract

1-Azakenpaullone, a selective inhibitor of glycogen synthase kinase-3β, was synthesized by carrying out a two-step protocol featuring an indium-trichloride-mediated intramolecular cyclization and mild reaction conditions. The concise synthesis showed significantly improved synthetic efficiency and reduced discharge of waste. We expect the present study to boost the applications of 1-azakenpaullone and its analogues in cellular regeneration and regenerative medicine.