Finally, Levamisole, bearing an unusual sp 2 -sp 3 linkage between the benzene core and the directing group, was selectively difunctionalized to yield product 3k. A point worth noting is that even though the isolated yields for a number of presented examples were relatively low, in many cases these may still be comparable or exceeding expected overall yields from de novo synthesis of these analogues. The amount of material obtained from these reactions would suffice for the needs of biological studies, allowing for rapid access to SAR data in a fraction of time compared to de novo synthesis.