19493-44-8

57260-71-6

205264-33-1

Example 14: Generalized arylation method E (as described in schemes 1 and 2) 1-Chloroisoquinoline (176 mg, 1.07 mmol), N-BOC-piperazine (420 mg, 2.26 mmol) and DBU (0.25 mL, 1.61 mmol) were dissolved in DMP (2 mL). The reaction mixture was heated to 105-110 °C and the reaction was stirred overnight. After completion of the reaction, the mixture was diluted with water and extracted with ether. The organic layers were combined, washed with saturated brine, dried over anhydrous sodium sulfate and concentrated under reduced pressure to remove the solvent. The resulting crude product was purified by column chromatography (eluent: 5% to 10% ethyl acetate/hexane) to give 222 mg of the title compound tert-butyl 4-(isoquinolin-1-yl)piperazine-1-carboxylate in 66% yield.