1-(isoquinolin-1-yl)urea library generation via three-component reaction of 2-alkynylbenzaldoxime, carbodiimide, with electrophile.

A novel and highly efficient three-component reaction of 2-alkynylbenzaldoxime, carbodiimide, with electrophile (bromine or iodine monochloride) is disclosed, which generates 1-(4-haloisoquinolin-1-yl)ureas in good yields under mild conditions. Subsequent palladium-catalyzed Suzuki-Miyaura coupling reaction is introduced, leading to the diverse 1-(isoquinolin-1-yl)ureas.