反应 #492
ord-ff0eb93bbb4b45cdb3807c4588dd206f
反应方程式
COC(=O)c1cc(Br)cc(C(
C1COCCN1
→
COC(=O)c1cc(C(=O)OC)
收率 78.2%
反应条件
温度
100°CELSIUS
实验过程
To a solution of dimethyl 5-bromoisophthalate (10 g, 36.62 mmol) in toluene (100 mL) where BINAP (2.5 g, 4.01 mmol), morpholine (4.4 g, 50.50 mmol), CESIUM CARBONATE (18 g, 55.25 mmol) and PALLADIUM(II) ACETATE (0.9 g, 4.01 mmol) added. The solution was heated to reflux under inert atm for 14h. The silvent was filtered and the filtrate was concentrated. The residue was purified by column chropmatography (Hep:EA) 1:1 to give dimethyl 5-morpholinoisophthalate (8.00 g, 78 %)
来源
750 AstraZeneca ELN dataset