反応 #731

反応方程式

CC(C)(C)OC(=O)Nc1cc(

C1CNCCN1

→

CC(C)(C)OC(=O)Nc1cc(

収率 57.1%

溶媒

Cc1ccccc1

反応条件

実験手順

palladium(II) acetate (0.110 g, 0.49 mmol), BINAP (0.244 g, 0.39 mmol) and CS2CO3 (1.594 g, 4.89 mmol) were added to a mixture of [Reactants] and piperazine (2.76 g, 32.10 mmol) in toluene (10 mL), The suspension were heated to 110 °C for 16 hours, LCMS showed product mass [M+1]:312.0 at retention time RT=1.69 min (polar short purity method). Workup reaction by additional of water (10mL), extracted with EtOAc (3x20 mL), washed with brine, dried with Na2SO4, evaporated off solvent to give a residue, which was purified by isco chromatographer, eluting with 0-10% MeOH in DCM to give as a yellow solid. LCMS confirmed the target compound.

出典