For some reasons quite unknown even to Stephen L. Buchwald himself, coupling of an amine to chloroaryls is much more facile than that of their bromo-counterparts, and extremely torturous for iodoaryls. In agreement with this, the Buchwald coupling of 1 to 7 was found not to be feasible, thus compelled the synthesis of 11 in a manner similar to that for 7 (ESI S19 †). With 11 in hand, initially its Buchwald amination with 1 using BrettPhos Pd G3 and equimolar amounts of BrettPhos ligand in anhydrous THF and Cs 2 CO 3 gave poor yields of the desired NInC 10 i.e. ~ 20-25%. However, with some modification i.e. change of reagents and reaction conditions (ESI S18 †), the yields were almost doubled ~ 45-50% such that 10 was accomplished in excellent purity after flash column chromatography purification, as evidenced by H NMR (ESI S47 †). With NInC ethyl ester 10 in hand, numerous acid and base hydrolyses were attempted (ESI S1 †), but all failed to accomplish 12.