Reaktion #492
ord-ff0eb93bbb4b45cdb3807c4588dd206f
Reaktionsgleichung
COC(=O)c1cc(Br)cc(C(
C1COCCN1
→
COC(=O)c1cc(C(=O)OC)
Ausbeute 78.2%
Lösungsmittel
Reaktionsbedingungen
Temperatur
100°CELSIUS
Vorschrift
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 %)
Quelle
750 AstraZeneca ELN dataset