|| Synthetic studies of ancistrocladinium A and B, antileishmanial compounds isolated from a Congolese Ancistrocladus sp., are described. Buchwald‒Hartwig coupling reaction between the dihydroisoquinoline and the naphthyl triflate failed. The main framework of ancistrocladinium A was constructed by 1,2‒addition of the amine to the naphthoquinone in the presence of celium trichloride as a catalyst. On the other hand, 1,4‒addition of the amine to the naphthoquinone proceeded without catalyst to form the framework of B. These products will be valuable leads for antileishmanial agents.