An oven-dried flask, charged with 7-bromo-3(R,S)-tert-butoxycarbonyl-1-ethyl-8-methoxy-2,3,4,5-tetrahydro-1H-1-benzazepine-2-one (48 mg, 0.121 mmol), piperazine (12.64 mg, 0.145 mmol), Pd(OAc)2 (2.72 mg, 0.0121 mmol, 10 mole), BINAP (11.65 mg, 0.0182 mmol) was purged with argon for 5 min. After addition of anhydrous toluene (1 mL) through a syringe followed by sodium tert-butoxide (16.78 mg, 0.169 mmol) in one portion, the flask was purged with argon, vigorously stirred and heated at 80° C. for 22 hrs. The course of the reaction was monitored by TLC. The reaction mixture was diluted with DCM (20 mL), percolated through a short column of Celite and evaporated to dryness. Purification of a crude product using preparative silica TLC developed with MeOH/DCM (1:4) provided the desired compound (8.0 mg, 16%) as a white crystalline product.
