Реакция #727

ord-088bd21d086a43258b728521904f368d

Уравнение реакции

COc1cc(Br)cc([N+](=O)[O-])c1
COc1cc(Br)cc([N+](=O
CN1CCNCC1
CN1CCNCC1
COc1cc(N2CCN(C)CC2)cc([N+](=O)[O-])c1
COc1cc(N2CCN(C)CC2)c
Выход 71.2%

Растворители

Условия реакции

Температура
150°CELSIUS

Методика

1-bromo-3-methoxy-5-nitrobenzene (116 mg, 0.5 mmol), 1-methylpiperazine (167 µl, 1.50 mmol), Palladium(II) acetate (11.23 mg, 0.05 mmol), BINAP (31.1 mg, 0.05 mmol), Cs2CO3 (326 mg, 1.00 mmol) and PhCH3 (10 mL) were added to a 100ml rb flask and heated at 150 °C for 1h. LCMS showed rxn done with desired product formed. Rxn was filtered and concentrated. The residue was purified by Gilson (CH3CN/Water 0-50% + 0.1%TFA) to get the desired product 1-(3-methoxy-5-nitrophenyl)-4-methylpiperazine (130 mg, 71.2 %).

Источник

750 AstraZeneca ELN dataset