반응 #492
ord-ff0eb93bbb4b45cdb3807c4588dd206f
반응 방정식
COC(=O)c1cc(Br)cc(C(
C1COCCN1
→
COC(=O)c1cc(C(=O)OC)
수율 78.2%
반응 조건
온도
100°CELSIUS
실험 절차
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 %)
출처
750 AstraZeneca ELN dataset